Effectiveness and Safety of Direct-Acting Antiviral Agents for the Treatment of Chronic Hepatitis C: Multi-center, Prospective, Observational Real-world Study in EASTERN China

Clinical trials evaluating DAA have shown excellent rates of SVR and good safety profiles in patients with CHC infection. Real world data from TARGET, TRIO, IFI, DHCR, DALTON-C, as well as those cohorts from Japan, Taiwan and Korea further confirmed clinical trial findings of DAA in routine practice where populations are more complex. However, these populations are different from Chinese for different host and virus characteristics which limit the applicability of results to local practice.
As DAA launched in China since 2017, the availability of INF free DAA treatment will likely lead to better treatment outcome in routine practice, but there are currently no data available to test the hypothesis.
In clinical practice, the uptake of DAA regimen will depend on a combination of physician preference, patient's characteristics and drug access. This study will also identify how these three variables affect DAA regimen uptake.
This study to 1) characterize pts receiving IFN free DAA regimens, 2) represent common practice in China, 3) describe outcome of various INF free DAA therapy, and 4) confirm registration study results.

Start Date06 Mar 2019

Sponsor / Collaborator

Ruijin Hospital

[+2]

NCT03037151

/ Unknown statusPhase 4

Safety and Fibrosis Improvement of Grazoprevir and Elbasvir for HCV GT1 and GT6 With or Without HIV

This study will evaluate the safety and efficacy of combination treatment with grazoprevir + elbasvir for compensated cirrhotic participants with chronic genotype 1 (GT1) and genotype 6 (GT6) hepatitis C virus (HCV) infection with or without human immunodeficiency virus (HIV) infection.

Start Date01 Aug 2018

Sponsor / Collaborator

The HIV Netherlands Australia Thailand Research Collaboration

[+2]

100 Clinical Results associated with Grazoprevir Hydrate

100 Translational Medicine associated with Grazoprevir Hydrate

100 Patents (Medical) associated with Grazoprevir Hydrate

591

Literatures (Medical) associated with Grazoprevir Hydrate

23 Feb 2026·CHEMISTRY-A EUROPEAN JOURNAL

Conformational Trajectory of the Molecular Chameleon Grazoprevir From Formulation to Target‐Bound

Article

Author: Gonen, Tamir ; Danelius, Emma Rova ; Erdélyi, Máté ; Wieske, Lianne H. E. ; Kihlberg, Jan ; Bu, Guanhong

ABSTRACT:

Macrocycles represent a promising class of beyond‐rule‐of‐5 (bRo5) therapeutics, capable of targeting proteins traditionally considered undruggable by conventional small molecules. Macrocycles exhibit intrinsic flexibility and often display a “chameleon‐like” ability to adapt to their environment, thereby enhancing their oral bioavailability. Describing their structures and conformational changes is essential for advancing their development in the bRo5 space. In this study, we present the novel solid‐ and solution‐state structures of the macrocycle grazoprevir, determined using microcrystal electron diffraction (MicroED) and nuclear magnetic resonance (NMR) spectroscopy. A low‐energy core conformation was consistently identified throughout the conformational journey, from solid formulation to solvated states and upon complexation with the biological target, while the vinyl cyclopropyl sulfonamide side chain reoriented. The presence of a common core conformation (RMSD up to 0.273 Å) suggests that grazoprevir adopts a partial pre‐organized state, optimizing its suitability for target binding. In apolar environment, mimicking the cell membrane, intramolecular hydrogen bonding promoted the formation of compact conformations with reduced radii of gyration and solvent accessible 3D polar surface area, likely facilitating cell permeability. This work presents a comprehensive conformational trajectory of a macrocyclic chameleon and provides potential insights into understanding and characterizing cell permeability and chameleonicity of similar bRo5 therapeutics.

01 Nov 2025·JOURNAL OF CLINICAL PHARMACOLOGY

Evaluation of Characteristics and Ethnic Sensitivity for FDA‐Approved Drugs with Racial and Ethnic Differences in Pharmacokinetics, Safety, and Efficacy

Article

Author: Muto, Chieko ; Kawai, Norisuke ; Fukuhara, Kei ; Tanetsugu, Yusuke ; Wada, Shinsuke

Abstract:

Racial and ethnic differences in drug disposition and response may have a significant impact on its risk‐benefit balance. Therefore, it is important to examine whether an investigational drug has characteristics that make the pharmacokinetics (PK), safety, and efficacy likely to be affected by intrinsic and extrinsic ethnic factors based on ethnic sensitivity assessment. This assessment is recommended by the latest Japanese guideline (issued in December 2023) for Japanese phase 1 studies before participation in multi‐regional clinical trials (MRCTs). To comprehensively understand characteristics and ethnic sensitivity of drugs that seem to have racial/ethnic differences in its disposition and response, we investigated 620 new molecular entities (NMEs) approved by the United States Food and Drug Administration (FDA) between 2008 and 2023. Of those, only 6.5% (40 NMEs) reported racial/ethnic differences in the PK (5.0%), safety (1.6%), and/or efficacy (0.6%) in the FDA drug labeling, with only one NME (0.16%) having a clinically significant PK difference which requires a reduced starting dose in East Asian patients. Additionally, 4.4% of 620 NMEs reported differences in the pharmacogenetics for drug‐metabolizing enzymes. The comprehensive evaluation of characteristics and ethnic sensitivity of 40 NMEs with racial/ethnic differences in the PK, safety, and/or efficacy indicated two key findings. First, participation in MRCTs from various regions as early as possible is much more important than conduct of an additional phase 1 study in a specific region/country. Second, more attention and deeper evaluation of Asian PK would be needed for drugs with low bioavailability in the overall drug development.

01 Sep 2025·Klinicka mikrobiologie a infekcni lekarstvi

[Antiviral treatment for chronic viral hepatitis B and C in children in Ostrava].

Article

Author: Mrázek, Jakub ; Orságová, Irena ; Kabieszová, Libuše ; Kloudová, Alena ; Rožnovský, Luděk ; Konečná, Martina ; Petroušová, Lenka

BACKGROUND:

Retrospective evaluation of the frequency, efficacy, and tolerance of antiviral treatment for chronic viral hepatitis B and C (VHB, VHC) in children in Ostrava.

MATERIAL AND METHODS:

The sample included 17 children with chronic VHB, aged 3-15 years, treated with conventional interferon alpha in 1993-2008, and 11 children with chronic VHC, aged 5-17 years, of whom six were treated with interferon regimens in 1995-2016 and five used direct-acting antivirals since 2020.

RESULTS:

In the 1990s, children with chronic VHB prevailed; 12 of them were infected vertically. In the last decade, children with chronic VHC dominated, with vertical transmission found in seven children. All 17 children with chronic VHB, 15 of whom were HBeAg (hepatitis B virus e-antigen-positive), were treated with interferon alpha (IFN). HBeAg positivity disappeared in seven children during treatment or within a year after treatment and in another six patients within 15 years after treatment. Treatment tolerance was good, except for psychological problems in two children. Thirteen patients continued to be observed into adulthood, six of whom were treated with interferons or oral antivirals. HBsAg (hepatitis B virus s-antigen) disappeared in four patients aged 7-38 years. Six children with chronic VHC were treated with IFN or pegylated IFN; four received ribavirin. The virus was permanently cleared in five children, the last of whom after treatment with elbasvir and grazoprevir at the age of 18. The tolerance of IFN treatment was good, except for a 5-year-old boy who developed hypothyroidism. Direct-acting antivirals were administered to five children; the first received glecaprevir with pibrentasvir, and the other four received sofosbuvir with velpatasvir. All treatments were successful. Long-term follow-up after treatment was recommended for only three patients.

CONCLUSIONS:

Antiviral treatment for chronic VHB in children has become a thing of the past thanks to VHB vaccination. However, chronic VHB persists into adulthood after infection in childhood. Currently, chronic VHC dominates in children. After successful treatment with direct-acting antivirals, further follow-up in adulthood is usually unnecessary.

News (Medical) associated with Grazoprevir Hydrate

21 Jun 2024

·www.biospace.com

Aprea Therapeutics to Host Virtual KOL Event on APR-1051, a Highly Selective and Potentially Best-in-Class Oral WEE1 Inhibitor, on Monday, June 24, 2024

DOYLESTOWN, Pa., June 21, 2024 (GLOBE NEWSWIRE) -- Aprea Therapeutics, Inc. (Nasdaq: APRE) (“Aprea”, or the “Company”), a clinical-stage biopharmaceutical company focused on precision oncology through synthetic lethality, today announced that it will host a virtual KOL event to discuss APR-1051, a highly selective and potentially best-in-class oral WEE1 inhibitor, on Monday, June 24, 2024 at 9:00 AM ET. To register, click here. The webinar will feature Joseph Vacca, PhD, Medicinal Chemistry Expert and Consultant to Aprea, who will discuss the medicinal chemistry history, highly selective drug design, and preclinical findings of APR-1051. It will also feature Eric J. Brown, PhD (University of Pennsylvania) who will discuss preclinical findings across the WEE1 inhibitor class. WEE1 is an enzyme involved in the DNA damage response pathway and is a validated oncology target. APR-1051 is a potent and selective small molecule that has been designed to limit off-target toxicity. Aprea recently initiated the Phase 1 ACESOT-1051 trial evaluating APR-1051 as monotherapy treatment in patients with significant unmet medical need, including patients with Cyclin E over expression. A live question and answer session will follow the formal presentations. Joseph Vacca, PhD is a medicinal chemist who spent 30 years at Merck Research Laboratories (1981 to 2011). He and his teams made major contributions to several approved drugs including the HIV protease inhibitor CRIXIVAN™ (indinavir sulfate), the HIV integrase inhibitor Isentress™ (raltegravir); the HCV protease Inhibitor (Vanihep™, vaniprevir), the combination product Zepatier™ which is a combination of the second generation HCV protease Inhibitor grazoprevir and the NS5A protein Inhibitor elbasvir and the recently approved second generation HIV NNRTI inhibitor doravirine. Upon his retirement from Merck in 2011, Dr. Vacca took a role as Senior Vice President of Early Success Sharing Partnerships at WuXi AppTec Limited. He left WuXi in September 2015 to be a consultant and now acts as an interim head of chemistry for several small startup companies. Dr. Vacca has over 100 publications and patents and is the holder of many awards including a Merck Directors Award (1998); PhRMA Discoverers Award (1999); Intellectual Property Owners “National Inventor of the year Award” (1997); European Inventor of the Year (non-EU nation) (2007); ACS “Award for Creative Invention” (1999); and was a named a Merck Research Laboratories Presidential Fellow in 2008. He was named to the American Chemical Society Medicinal Chemistry Hall of Fame (Aug. 2012) and was also named a “Hero of Chemistry” (along with the research team) for his role in the discovery and development of the HIV integrase inhibitorIsentress™. Dr. Vacca earned a BS in chemistry in 1977 from St. John Fisher College, Rochester, New York, and obtained a PhD degree in Organic Chemistry under Professor Peter T. Lansbury Sr. at the State University of New York at Buffalo (New York). Eric J. Brown, PhD is Associate Professor of Cancer Biology at the University of Pennsylvania and a Scientific Consultant to Aprea Therapeutics. Dr. Brown’s laboratory at Penn focuses on the role of the replication stress response on genome stability. His research seeks to identify the cancer-associated genetic changes that increase the efficacy of therapeutics that abrogate replication stress responses, such as ATR and WEE1 inhibitors. The genetic changes that impact sensitivity to these therapies are identified through various orthogonal approaches, including proteomics, genome-wide breakpoint mapping, and computational methods. Overall, the goal of this research is both to better understand the mechanism by which these cancer therapeutics operate and to improve responses to these treatments in patients. About Aprea Aprea Therapeutics, Inc. is a clinical-stage biopharmaceutical company headquartered in Doylestown, Pennsylvania, focused on precision oncology through synthetic lethality. The Company’s lead program is ATRN-119, a clinical-stage small molecule ATR inhibitor in development for solid tumor indications. APR-1051, an oral, small molecule WEE1 inhibitor, recently entered the clinic. For more information, please visit the company website at . The Company may use, and intends to use, its investor relations website at as a means of disclosing material nonpublic information and for complying with its disclosure obligations under Regulation FD. Forward-Looking Statement Certain information contained in this press release includes “forward-looking statements”, within the meaning of Section 27A of the Securities Act of 1933, as amended, and Section 21E of the Securities Exchange Act of 1934, as amended related to our study analyses, clinical trials, regulatory submissions, and projected cash position. We may, in some cases use terms such as “future,” “predicts,” “believes,” “potential,” “continue,” “anticipates,” “estimates,” “expects,” “plans,” “intends,” “targeting,” “confidence,” “may,” “could,” “might,” “likely,” “will,” “should” or other words that convey uncertainty of the future events or outcomes to identify these forward-looking statements. Our forward-looking statements are based on current beliefs and expectations of our management team and on information currently available to management that involve risks, potential changes in circumstances, assumptions, and uncertainties. All statements contained in this press release other than statements of historical fact are forward-looking statements, including statements regarding our ability to develop, commercialize, and achieve market acceptance of our current and planned products and services, our research and development efforts, including timing considerations and other matters regarding our business strategies, use of capital, results of operations and financial position, and plans and objectives for future operations. Any or all of the forward-looking statements may turn out to be wrong or be affected by inaccurate assumptions we might make or by known or unknown risks and uncertainties. These forward-looking statements are subject to risks and uncertainties including, without limitation, risks related to the success, timing, and cost of our ongoing clinical trials and anticipated clinical trials for our current product candidates, including statements regarding the timing of initiation, pace of enrollment and completion of the trials (including our ability to fully fund our disclosed clinical trials, which assumes no material changes to our currently projected expenses), futility analyses, presentations at conferences and data reported in an abstract, and receipt of interim or preliminary results (including, without limitation, any preclinical results or data), which are not necessarily indicative of the final results of our ongoing clinical trials, our understanding of product candidates mechanisms of action and interpretation of preclinical and early clinical results from its clinical development programs, and the other risks, uncertainties, and other factors described under “Risk Factors,” “Management’s Discussion and Analysis of Financial Condition and Results of Operations” and elsewhere in the documents we the U.S. Securities and Exchange Commission. For all these reasons, actual results and developments could be materially different from those expressed in or implied by our forward-looking statements. You are cautioned not to place undue reliance on these forward-looking statements, which are made only as of the date of this press release. We undertake no obligation to update such forward-looking statements for any reason, except as required by law. Investor Contact: Mike Moyer LifeSci Advisors mmoyer@lifesciadvisors.com

Phase 1Executive Change

28 Feb 2024

·www.biospace.com

ViiV Healthcare to present data for its next generation of ultra long-acting treatments for HIV

Other key data to be presented from ViiV Healthcare’s innovative pipeline and portfolio include the exploration of different mechanisms of action through broadly neutralising antibodies as well as real-world insights from established long-acting and 2-drug regimens LONDON--(BUSINESS WIRE)-- ViiV Healthcare, the global specialist HIV company majority owned by GSK, with Pfizer and Shionogi as shareholders, today announced the presentation of 64 abstracts that includes highlights of the company’s next-generation pipeline advancements, alongside data from its diverse portfolio of marketed HIV treatment and prevention options at the Conference on Retroviruses and Opportunistic Infections (CROI 2024) being held in Denver, Colorado, from 3 – 6 March 2024. Kimberly Smith, M.D., MPH, Head of Research & Development at ViiV Healthcare, said: “As leaders in developing long-acting injectables for the treatment of HIV, we’re excited to present new data setting the stage for ViiV’s next generation of medicines and demonstrating how key pipeline assets will target HIV in different ways. These findings, as well as the breadth of data we’ll present on our marketed products, including new interim results from the LATITUDE study, reflect a portfolio and future-looking pipeline focused on ending the HIV epidemic. We look forward to sharing them with the scientific and HIV communities at CROI 2024.” Key abstracts to be presented at CROI 2024 by ViiV Healthcare and its study partners will include: Data introducing our next generation of potential ultra long-acting medicines for HIV: ViiV Healthcare will share findings from a phase I study evaluating different formulations of cabotegravir and their potential for dosing every four months. The ongoing, open-label, single-dose, dose-escalation phase I study in 70 healthy adults assessed both the 200 mg/mL formulation of cabotegravir in combination with recombinant human hyaluronidase PH20 (rHuPH20), as well as a new formulation of cabotegravir (CAB ULA) administered by itself.1 Researchers will share safety and pharmacokinetic findings from both ultra long-acting approaches and their potential for future clinical development. Findings advancing different mechanisms of action in HIV research: New phase IIa findings from the BANNER study of VH3810109 (N6LS), an investigational, broadly neutralising antibody (bNAb), will be presented. Researchers will share findings of the bNAb administered intravenously and the first efficacy findings of its subcutaneous administration.2 Findings from the SPAN study of N6LS, examining the safety and tolerability of the highest subcutaneous and intravenous N6LS doses administered to date, with and without PH20, will also be presented.3 Additionally, efficacy and safety data from a non-ViiV owned bNAb asset, VRC07-523LS, in a phase II, open-label clinical trial used in combination with long-acting CAB for maintenance antiretroviral therapy (ART) will be presented.4 New data on long-acting therapy vs daily oral standard of care, in traditionally non-adherent populations: Interim analysis of the LATITUDE phase III trial will be presented showing that, the injectable antiretroviral treatment for HIV, Cabenuva (cabotegravir and rilpivirine [CAB+RPV LA]), demonstrates superior efficacy compared to daily oral standard of care (SOC) in individuals with a history of antiretroviral adherence challenges. The NIAID/ACTG also announced a modification to the study, where further randomisation has been stopped and participants in the SOC arm are being given the option to switch to the long-acting therapy arm.5 Real-world evidence from across our treatment and prevention portfolios: New findings from SEARCH, a randomised study evaluating the real-world impact of the inclusion of long-acting cabotegravir for PrEP in an HIV prevention coverage package compared to the standard-of-care of oral PrEP and PEP alone in rural Uganda and Kenya, will also be presented.6 Real-world evidence findings for the complete long-acting HIV treatment regimen Cabenuva will be presented from the OPERA cohort examining ART-experienced, virally suppressed adults living with HIV who switched to CAB+RPV LA or to an oral regimen.7 Findings for the 2-drug regimen, Dovato (dolutegravir, lamivudine [DTG/3TC]), will include the InfCare HIV study, which presents three-year switch data, from 3-drug regimen to Dovato, in a long-term real-world Swedish cohort.8 This study adds to the body of real-world evidence to date that includes more than 40,000 people living with HIV.9 Here is a list of ViiV Healthcare-sponsored or supported studies to be presented at CROI 2024: Title First Author Presentation Number Presentation Dolutegravir A single once-daily ABC/DTG/3TC tablet predicts safe and effective exposures in children 3 to <6kg H. Chandasana 02770 Poster Tuesday, March 5 2:30-4:00pm MST Population pharmacokinetics of ABC/DTG/3TC FDC to support dosing in peds with HIV-1 (IMPAACT 2019) H. Chandasana 03110 Poster Tuesday, March 5:30-4:00pm MST Dolutegravir and growth in pediatric populations with HIV-1: IMPAACT P1093 and IMPAACT 2019 M. McKenna 01783 Poster Tuesday, March 5 2:30-4:00pm MST Switching to DTG+3TC vs 3-drug regimens in routine clinical care: long-term Swedish data E. Sörstedt 01838 Poster Tuesday, March 5 2:30-4:00pm MST Temporal trends of cardiovascular disease incidence in people with HIV from 2001-2021 N. Jaschinski 02263 Poster Tuesday, March 5 2:30-4:00pm MST Increased cancer risk with low CD4 counts persists despite over 2 years of virological suppression J. Hoy 01462 Poster Wednesday, March 6 2:30-4:00pm MST Cabotegravir for Treatment Long-acting Injectable CAB/RPV is Superior to Oral ART in PWH with adherence challenges: ACTG A5359 A. Rana 03579 Oral Wednesday, March 6 12:51-1:00pm MST Real-world utilization of cabotegravir + rilpivirine in the US: data from Trio Health cohort J. J. Eron 01374 Poster Monday, March 4 2:30-4:00pm MST Real-world effectiveness of cabotegravir + rilpivirine vs. standard of care oral regimens in the US R. K. Hsu 01952 Poster Monday, March 4 2:30-4:00pm MST HIV-1 RNA blips and low-level viral replication: SOLAR (CAB+RPV LA vs. BIC/FTC/TAF) C. Latham 00138 Poster Monday, March 4 2:30-4:00pm MST Model based comparison of cabotegravir pharmacokinetics following thigh and gluteal injections K. Han 03157 Poster Wednesday, March 6 2:30-4:00pm MST Cabotegravir for PrEP SEARCH Randomized trial of Dynamic Choice HIV Prevention including injectable cabotegravir (CAB-LA) J. Kabami 03405 Late-Breaker Oral Tuesday, March 5 10:00-12:00pm MST Pre-exposure prophylaxis with cabotegravir long-acting injectable in the OPERA cohort A. Mills 01400 Poster Monday, March 4 2:30-4:00pm MST Real-world use of cabotegravir long acting for pre-exposure prophylaxis: TRIO cohort K. Mayer 01907 Poster Monday, March 4 2:30-4:00pm MST Cabotegravir PopPK analysis of adults and adolescents living with HIV or at risk for HIV receiving PrEP Y. Lin 03038 Poster Tuesday, March 5 2:30-4:00pm MST Interest in long-acting injectable PrEP among transgender women in the United States E. E. Cooney 00621 Poster Wednesday, March 6 2:30-4:00pm MST Healthcare staff acceptability and feasibility of telehealth delivery of cabotegravir for PrEP A. Liu 03080 Poster Wednesday, March 6 2:30-4:00pm MST Fostemsavir Temsavir treatment enhances bNAb recognition and subsequent clearance of HIV-1 infected cells R. Ferris 02971 Poster Monday, March 4 2:30-4:00pm MST Pipeline: Ultra Long-Acting Cabotegravir Phase I study of cabotegravir long-acting injectable formulations supports ≥4-monthly dose interval K. Han 00251 Oral Monday, March 4 10:00-12:00pm MST Pipeline: Broadly Neutralising Antibodies VH3810109 (N6LS) in antiretroviral therapy–naive adults with HIV-1: phase IIa BANNER efficacy data P. Leone 01911 Oral Monday, March 4 10:00-12:00pm MST Safety and efficacy of VRC07-523LS plus long-acting cabotegravir in the phase 2 ACTG A5357 Trial B. Taiwo 02254 Oral Monday, March 4 10:00-12:00pm MST High-dose VH3810109 (N6LS) ± recombinant human hyaluronidase PH20: phase I SPAN study safety results B. Win 01988 Poster Wednesday, March 6 2:30-4:00pm MST Pipeline: Maturation Inhibitors Next-generation maturation inhibitor GSK3640254 showed broad spectrum potency without MI resistance B. McAuliffe 03095 Poster Wednesday, March 6 2:30-4:00pm MST The preclinical pro maturation inhibitor VH3739937 J. Jeffrey 02819 Poster Wednesday, March 6 2:30-4:00pm MST General HIV Resistance in young children newly diagnosed with HIV in Western Cape, South Africa K. Anderson 01012 Poster Tuesday, March 5 2:30-4:00pm MST DOVATO (dolutegravir and lamivudine) tablets INDICATION Dovato is indicated as a complete regimen to treat HIV-1 infection in adults with no antiretroviral (ARV) treatment history or to replace the current ARV regimen in those who are virologically suppressed (HIV-1 RNA <50 copies/mL) on a stable ARV regimen with no history of treatment failure and no known resistance to any component of Dovato. IMPORTANT SAFETY INFORMATION BOXED WARNING: PATIENTS CO-INFECTED WITH HEPATITIS B VIRUS (HBV) AND HIV-1: EMERGENCE OF LAMIVUDINE-RESISTANT HBV AND EXACERBATIONS OF HBV All patients with HIV-1 should be tested for the presence of HBV prior to or when initiating Dovato. Emergence of lamivudine-resistant HBV variants associated with lamivudine-containing antiretroviral regimens has been reported. If Dovato is used in patients co-infected with HIV-1 and HBV, additional treatment should be considered for appropriate treatment of chronic HBV; otherwise, consider an alternative regimen. Severe acute exacerbations of HBV have been reported in patients who are co-infected with HIV-1 and HBV and have discontinued lamivudine, a component of Dovato. Closely monitor hepatic function in these patients and, if appropriate, initiate anti-HBV treatment. CONTRAINDICATIONS Do not use Dovato in patients with previous hypersensitivity reaction to dolutegravir or lamivudine Do not use Dovato in patients receiving dofetilide WARNINGS AND PRECAUTIONS Hypersensitivity Reactions: Hypersensitivity reactions have been reported with dolutegravir and were characterized by rash, constitutional findings, and sometimes organ dysfunction, including liver injury Discontinue Dovato immediately if signs or symptoms of severe skin or hypersensitivity reactions develop, as a delay in stopping treatment may result in a life-threatening reaction. Clinical status, including liver aminotransferases, should be monitored and appropriate therapy initiated Hepatotoxicity: Hepatic adverse events have been reported, including cases of hepatic toxicity (elevated serum liver biochemistries, hepatitis, and acute liver failure), in patients receiving a dolutegravir-containing regimen without pre-existing hepatic disease or other identifiable risk factors Patients with underlying hepatitis B or C or marked elevations in transaminases prior to treatment may be at increased risk for worsening or development of transaminase elevations with use of Dovato. In some cases, the elevations in transaminases were consistent with immune reconstitution syndrome or hepatitis B reactivation, particularly in the setting where anti-hepatitis therapy was withdrawn Monitoring for hepatotoxicity is recommended Embryo Fetal Toxicity: Assess the risks and benefits of Dovato and discuss with the patient to determine if an alternative treatment should be considered at the time of conception through the first trimester of pregnancy due to the risk of neural tube defects Pregnancy testing is recommended before initiation of Dovato. Individuals of childbearing potential should be counseled on the consistent use of effective contraception Lactic Acidosis and Severe Hepatomegaly With Steatosis: Fatal cases have been reported with the use of nucleoside analogs, including lamivudine. Discontinue Dovato if clinical or laboratory findings suggestive of lactic acidosis or pronounced hepatotoxicity develop, including hepatomegaly and steatosis in the absence of marked transaminase elevations. Adverse Reactions or Loss of Virologic Response Due to Drug Interactions with concomitant use of Dovato and other drugs may occur (see Contraindications and Drug interactions). Immune Reconstitution Syndrome, including the occurrence of autoimmune disorders with variable time to onset, has been reported with the use of Dovato. Adverse reactions The most common adverse reactions (incidence ≥2%, all grades) with Dovato were headache (3%), nausea (2%), diarrhea (2%), insomnia (2%), fatigue (2%), and anxiety (2%). Drug interactions Consult full Prescribing Information for Dovato for more information on potentially significant drug interactions Dovato is a complete regimen. Coadministration with other antiretroviral medications for the treatment of HIV-1 infection is not recommended Drugs that induce or inhibit CYP3A or UGT1A1 may affect the plasma concentrations of dolutegravir Administer Dovato 2 hours before or 6 hours after taking polyvalent cation-containing antacids or laxatives, sucralfate, oral supplements containing iron or calcium, or buffered medications. Alternatively, Dovato and supplements containing calcium or iron can be taken with food Use in specific populations Pregnancy: There are insufficient human data on the use of Dovato during pregnancy to definitively assess a drug-associated risk for birth defects and miscarriage. An Antiretroviral Pregnancy Registry has been established. Advise individuals of childbearing potential of the potential risk of neural tube defects. Assess the risks and benefits of Dovato and discuss with the patient to determine if an alternative treatment should be considered at the time of conception through the first trimester of pregnancy or if pregnancy is confirmed in the first trimester Lactation: Breastfeeding is not recommended due to the potential for HIV-1 transmission, developing viral resistance in HIV-positive infants, and adverse reactions in a breastfed infant Females and Males of Reproductive Potential: Pregnancy testing is recommended before initiation of Dovato. Counsel individuals of childbearing potential taking Dovato on the consistent use of effective contraception Renal Impairment: Dovato is not recommended for patients with creatinine clearance <30 mL/min. Patients with a sustained creatinine clearance between 30 and 49 mL/min should be monitored for hematologic toxicities, which may require a dosage adjustment of lamivudine as an individual component Hepatic Impairment: Dovato is not recommended in patients with severe hepatic impairment (Child-Pugh Score C) For more information, please see full US Prescribing Information for Dovato: https://gskpro.com/content/dam/global/hcpportal/en_US/Prescribing_Information/Dovato/pdf/DOVATO-PI-PIL.PDF CABENUVA (cabotegravir; rilpivirine) extended-release injectable suspensions INDICATION CABENUVA is indicated as a complete regimen for the treatment of HIV-1 infection in adults and adolescents 12 years of age and older and weighing at least 35 kg to replace the current antiretroviral regimen in those who are virologically suppressed (HIV-1 RNA <50 copies/mL) on a stable antiretroviral regimen with no history of treatment failure and with no known or suspected resistance to either cabotegravir or rilpivirine. IMPORTANT SAFETY INFORMATION CONTRAINDICATIONS Do not use CABENUVA in patients with previous hypersensitivity reaction to cabotegravir or rilpivirine Do not use CABENUVA in patients receiving carbamazepine, oxcarbazepine, phenobarbital, phenytoin, rifabutin, rifampin, rifapentine, systemic dexamethasone (>1 dose), and St John’s wort WARNINGS AND PRECAUTIONS Hypersensitivity Reactions: Serious or severe hypersensitivity reactions have been reported in association with other integrase inhibitors and could occur with CABENUVA Hypersensitivity reactions, including cases of drug reaction with eosinophilia and systemic symptoms (DRESS), have been reported during postmarketing experience with rilpivirine-containing regimens. While some skin reactions were accompanied by constitutional symptoms such as fever, other skin reactions were associated with organ dysfunctions, including elevations in hepatic serum biochemistries Discontinue CABENUVA immediately if signs or symptoms of hypersensitivity reactions develop. Clinical status, including liver transaminases, should be monitored and appropriate therapy initiated. Cabotegravir and rilpivirine oral lead-in may be used to help identify patients who may be at risk of a hypersensitivity reaction Post-Injection Reactions: Serious post-injection reactions (reported in less than 1% of subjects) were reported within minutes after the injection of rilpivirine, including dyspnea, bronchospasm, agitation, abdominal cramping, rash/urticaria, dizziness, flushing, sweating, oral numbness, changes in blood pressure, and pain (e.g., back and chest). These events may have been associated with accidental intravenous administration and began to resolve within a few minutes after the injection Carefully follow the Instructions for Use when preparing and administering CABENUVA. The suspensions should be injected slowly via intramuscular injection and avoid accidental intravenous administration. Observe patients briefly (approximately 10 minutes) after the injection. If a post-injection reaction occurs, monitor and treat as clinically indicated Hepatotoxicity: Hepatotoxicity has been reported in patients receiving cabotegravir or rilpivirine with or without known pre-existing hepatic disease or identifiable risk factors Patients with underlying liver disease or marked elevations in transaminases prior to treatment may be at increased risk for worsening or development of transaminase elevations Monitoring of liver chemistries is recommended and treatment with CABENUVA should be discontinued if hepatotoxicity is suspected Depressive Disorders: Depressive disorders (including depressed mood, depression, major depression, mood altered, mood swings, dysphoria, negative thoughts, suicidal ideation, suicide attempt) have been reported with CABENUVA or the individual products Promptly evaluate patients with depressive symptoms Risk of Adverse Reactions or Loss of Virologic Response Due to Drug Interactions: The concomitant use of CABENUVA and other drugs may result in known or potentially significant drug interactions (see Contraindications and Drug Interactions) Rilpivirine doses 3 and 12 times higher than the recommended oral dosage can prolong the QTc interval CABENUVA should be used with caution in combination with drugs with a known risk of Torsade de Pointes Long-Acting Properties and Potential Associated Risks with CABENUVA: Residual concentrations of cabotegravir and rilpivirine may remain in the systemic circulation of patients for prolonged periods (up to 12 months or longer). Select appropriate patients who agree to the required monthly or every-2-month injection dosing schedule because non-adherence could lead to loss of virologic response and development of resistance To minimize the potential risk of developing viral resistance, it is essential to initiate an alternative, fully suppressive antiretroviral regimen no later than 1 month after the final injection doses of CABENUVA when dosed monthly and no later than 2 months after the final injections of CABENUVA when dosed every 2 months. If virologic failure is suspected, switch the patient to an alternative regimen as soon as possible ADVERSE REACTIONS The most common adverse reactions in adults (incidence ≥2%, all grades) treated with CABENUVA were injection site reactions, pyrexia, fatigue, headache, musculoskeletal pain, nausea, sleep disorders, dizziness, and rash The safety of CABENUVA in adolescents is expected to be similar to adults DRUG INTERACTIONS Refer to the applicable full Prescribing Information for important drug interactions with CABENUVA, VOCABRIA (cabotegravir), or EDURANT (rilpivirine) Because CABENUVA is a complete regimen, coadministration with other antiretroviral medications for the treatment of HIV-1 infection is not recommended Drugs that are strong inducers of UGT1A1 or UGT1A9 are expected to decrease the plasma concentrations of cabotegravir. Drugs that induce or inhibit CYP3A may affect the plasma concentrations of rilpivirine CABENUVA should be used with caution in combination with drugs with a known risk of Torsade de Pointes USE IN SPECIFIC POPULATIONS Pregnancy: There are insufficient human data on the use of CABENUVA during pregnancy to adequately assess a drug-associated risk for birth defects and miscarriage. Discuss the benefit-risk of using CABENUVA during pregnancy and conception and consider that cabotegravir and rilpivirine are detected in systemic circulation for up to 12 months or longer after discontinuing injections of CABENUVA. An Antiretroviral Pregnancy Registry has been established Lactation: Potential risks of breastfeeding include HIV-1 transmission, developing viral resistance in HIV-positive infants, and adverse reactions in a breastfed infant For more information, please see full US Prescribing Information for Cabenuva: APRETUDE (cabotegravir) extended-release injectable suspensions INDICATION APRETUDE is indicated in at-risk adults and adolescents weighing at least 35 kg for pre-exposure prophylaxis (PrEP) to reduce the risk of sexually acquired HIV-1 infection. Individuals must have a negative HIV-1 test prior to initiating APRETUDE (with or without an oral lead-in with oral cabotegravir) for HIV-1 PrEP. IMPORTANT SAFETY INFORMATION BOXED WARNING: RISK OF DRUG RESISTANCE WITH USE OF APRETUDE FOR HIV-1 PRE-EXPOSURE PROPHYLAXIS (PrEP) IN UNDIAGNOSED HIV-1 INFECTION Individuals must be tested for HIV-1 infection prior to initiating APRETUDE or oral cabotegravir, and with each subsequent injection of APRETUDE, using a test approved or cleared by the FDA for the diagnosis of acute or primary HIV-1 infection. Drug-resistant HIV-1 variants have been identified with use of APRETUDE by individuals with undiagnosed HIV-1 infection. Do not initiate APRETUDE for HIV-1 PrEP unless negative infection status is confirmed. Individuals who become infected with HIV-1 while receiving APRETUDE for PrEP must transition to a complete HIV-1 treatment regimen. CONTRAINDICATIONS Do not use APRETUDE in individuals: with unknown or positive HIV-1 status with previous hypersensitivity reaction to cabotegravir receiving carbamazepine, oxcarbazepine, phenobarbital, phenytoin, rifampin, and rifapentine WARNINGS AND PRECAUTIONS Comprehensive Management to Reduce the Risk of HIV-1 Infection: Use APRETUDE as part of a comprehensive prevention strategy, including adherence to the administration schedule and safer sex practices, including condoms, to reduce the risk of sexually transmitted infections (STIs). APRETUDE is not always effective in preventing HIV-1 acquisition. Risk for HIV-1 acquisition includes, but is not limited to, condomless sex, past or current STIs, self-identified HIV risk, having sexual partners of unknown HIV-1 viremic status, or sexual activity in a high prevalence area or network. Inform, counsel, and support individuals on the use of other prevention measures (e.g., consistent and correct condom use; knowledge of partner[s] HIV-1 status, including viral suppression status; regular testing for STIs) Use APRETUDE only in individuals confirmed to be HIV-1 negative. HIV-1 resistance substitutions may emerge in individuals with undiagnosed HIV-1 infection who are taking only APRETUDE, because APRETUDE alone does not constitute a complete regimen for HIV-1 treatment. Prior to initiating APRETUDE, ask seronegative individuals about recent (in past month) potential exposure events and evaluate for current or recent signs or symptoms consistent with acute HIV-1 infection (e.g., fever, fatigue, myalgia, skin rash). If recent (<1 month) exposures to HIV-1 are suspected or clinical symptoms consistent with acute HIV-1 infection are present, use a test approved or cleared by the FDA as an aid in the diagnosis of acute HIV-1 infection When using APRETUDE, HIV-1 testing should be repeated prior to each injection and upon diagnosis of any other STIs Additional HIV testing to determine HIV status is needed if an HIV-1 test indicates possible HIV-1 infection or if symptoms consistent with acute HIV-1 infection develop following an exposure event. If HIV-1 infection is confirmed, then transition the individual to a complete HIV-1 treatment Counsel HIV-1 uninfected individuals to strictly adhere to the recommended dosing and testing schedule for APRETUDE Potential Risk of Resistance with APRETUDE: There is a potential risk of developing resistance to APRETUDE if an individual acquires HIV-1 either before, while taking, or following discontinuation of APRETUDE. To minimize this risk, it is essential to clinically reassess individuals for risk of HIV-1 acquisition and to test before each injection to confirm HIV-1–negative status. Individuals who are confirmed to have HIV-1 infection must transition to a complete HIV-1 treatment. If individuals at continuing risk of HIV-1 acquisition discontinue APRETUDE, alternative forms of PrEP should be considered and initiated within 2 months of the final injection of APRETUDE Long-Acting Properties and Potential Associated Risks with APRETUDE: Residual concentrations of cabotegravir may remain in the systemic circulation of individuals for prolonged periods (up to 12 months or longer). Take the prolonged-release characteristics of cabotegravir into consideration and carefully select individuals who agree to the required every-2-month injection dosing schedule because non-adherence or missed doses could lead to HIV-1 acquisition and development of resistance Hypersensitivity Reactions: Serious or severe hypersensitivity reactions have been reported in association with other integrase inhibitors and could occur with APRETUDE Discontinue APRETUDE immediately if signs or symptoms of hypersensitivity reactions develop. Clinical status, including liver transaminases, should be monitored and appropriate therapy initiated Hepatotoxicity: Hepatotoxicity has been reported in a limited number of individuals receiving cabotegravir with or without known pre-existing hepatic disease or identifiable risk factors Clinical and laboratory monitoring should be considered and APRETUDE should be discontinued if hepatotoxicity is suspected and individuals managed as clinically indicated Depressive Disorders: Depressive disorders (including depression, depressed mood, major depression, persistent depressive disorder, suicidal ideation or attempt) have been reported with APRETUDE Promptly evaluate patients with depressive symptoms Risk of Reduced Drug Concentration of APRETUDE Due to Drug Interactions: The concomitant use of APRETUDE and other drugs may result in reduced drug concentration of APRETUDE Refer to the full Prescribing Information for steps to prevent or manage these possible and known significant drug interactions, including dosing recommendations. Consider the potential for drug interactions prior to and during use of, and after discontinuation of APRETUDE; review concomitant medications during use of APRETUDE ADVERSE REACTIONS The most common adverse reactions (incidence ≥1%, all grades) with APRETUDE were injection site reactions, diarrhea, headache, pyrexia, fatigue, sleep disorders, nausea, dizziness, flatulence, abdominal pain, vomiting, myalgia, rash, decreased appetite, somnolence, back pain, and upper respiratory tract infection. DRUG INTERACTIONS Refer to the full Prescribing Information for important drug interactions with APRETUDE Drugs that induce UGT1A1 may significantly decrease the plasma concentrations of cabotegravir USE IN SPECIFIC POPULATIONS Lactation: Assess the benefit-risk of using APRETUDE to the infant while breastfeeding due to the potential for adverse reactions and residual concentrations in the systemic circulation for up to 12 months or longer after discontinuation Pediatrics: Not recommended in individuals weighing less than 35 kg For more information, please see full US Prescribing Information for APRETUDE: RUKOBIA (fostemsavir) extended-release tablets INDICATION RUKOBIA, in combination with other antiretrovirals (ARVs), is indicated to treat HIV-1 infection in heavily treatment-experienced adults with multidrug-resistant HIV-1 infection failing their current ARV regimen due to resistance, intolerance, or safety considerations. IMPORTANT SAFETY INFORMATION CONTRAINDICATIONS Do not use in patients with previous hypersensitivity to fostemsavir or any of the components of RUKOBIA. Do not use RUKOBIA in patients receiving strong cytochrome P450 (CYP)3A inducers, including but not limited to enzalutamide, carbamazepine, phenytoin, rifampin, mitotane, and St John’s wort (Hypericum perforatum). WARNINGS AND PRECAUTIONS Immune Reconstitution Syndrome, including the occurrence of autoimmune disorders with variable time to onset, has been reported with the use of RUKOBIA. QTc Prolongation with Higher than Recommended Dosages: RUKOBIA at 2,400 mg twice daily has been shown to significantly prolong the QTc interval of the electrocardiogram. Use RUKOBIA with caution in patients with a history of QTc interval prolongation or in patients with relevant pre-existing cardiac disease or who are taking drugs with a known risk of Torsade de Pointes. Elderly patients may be more susceptible to drug-induced QT interval prolongation. Elevations in Hepatic Transaminases in Patients with Hepatitis B or C Virus Co-infection: Monitoring of liver chemistries is recommended in patients with hepatitis B and/or C co-infection. Diligence should be applied in initiating or maintaining effective hepatitis B therapy when starting RUKOBIA in patients co-infected with hepatitis B. Adverse Reactions or Loss of Virologic Response Due to Drug Interactions with concomitant use of RUKOBIA and other drugs may occur (see Contraindications and Drug Interactions). Adverse reactions The most common adverse reaction (all grades, randomized cohort) observed in ≥5% of subjects was nausea (10%). 81% of adverse reactions reported with RUKOBIA were mild or moderate in severity. Drug interactions See the full Prescribing Information for RUKOBIA for a complete list of significant drug interactions. Temsavir may increase plasma concentrations of grazoprevir and voxilaprevir. Use an alternative hepatitis C virus regimen if possible. Use the lowest possible starting dose for statins and monitor for statin-associated adverse events. Patients receiving RUKOBIA should not take doses of estrogen-based therapies, including oral contraceptives, that contain more than 30 mcg/day of ethinyl estradiol. Caution is advised particularly in patients with additional risk factors for thromboembolic events. Use in specific populations Pregnancy: There are insufficient human data on the use of RUKOBIA during pregnancy to definitively assess a drug-associated risk for birth defects and miscarriage. An Antiretroviral Pregnancy Registry has been established. Lactation: Breastfeeding is not recommended due to the potential for HIV-1 transmission, developing viral resistance, and adverse reactions in a breastfed infant. For more information, please see full US Prescribing Information for RUKOBIA: About ViiV Healthcare ViiV Healthcare is a global specialist HIV company established in November 2009 by GSK (LSE: GSK) and Pfizer (NYSE: PFE) dedicated to delivering advances in treatment and care for people living with HIV and for people who are at risk of acquiring HIV. Shionogi became a ViiV shareholder in October 2012. The company’s aims are to take a deeper and broader interest in HIV and AIDS than any company has done before and take a new approach to deliver effective and innovative medicines for HIV treatment and prevention, as well as support communities affected by HIV. For more information on the company, its management, portfolio, pipeline, and commitment, please visit viivhealthcare.com. About GSK GSK is a global biopharma company with a purpose to unite science, technology, and talent to get ahead of disease together. Find out more at gsk.com. Cautionary statement regarding forward-looking statements GSK cautions investors that any forward-looking statements or projections made by GSK, including those made in this announcement, are subject to risks and uncertainties that may cause actual results to differ materially from those projected. Such factors include, but are not limited to, those described under Item 3.D “Risk factors” in the company's Annual Report on Form 20-F for 2022, and Q4 Results for 2023. Registered in England & Wales: GSK plc ViiV No. 3888792 Healthcare Limited No. 06876960 Registered Office: GSK plc 980 Great West Road Brentford, Middlesex United Kingdom TW8 9GS ViiV Healthcare Limited GSK Medicines Research Centre Gunnels Wood Road, Stevenage United Kingdom SG1 2NY References 1 Han, et al. Phase I Study of Cabotegravir Long-Acting Injectable Formulations Supports ≥4-Monthly Dose Interval. Presented at 31st Conference on Retroviruses and Opportunistic Infections (CROI). March 2024. 2 Leone, et al. VH3810109 (N6LS) in Antiretroviral Therapy–Naive Adults With HIV-1: Phase IIa BANNER Efficacy Data. Presented at 31st Conference on Retroviruses and Opportunistic Infections (CROI). March 2024. 3 Win, et al. High-Dose VH3810109 (N6LS) ± Recombinant Human Hyaluronidase PH20: Phase I SPAN Study Safety Results. Presented at 31st Conference on Retroviruses and Opportunistic Infections (CROI). March 2024. 4 Taiwo, et al. Safety and Efficacy of VRC07-523LS plus Long-Acting Cabotegravir in the Phase 2 ACTG A5357 Trial. Presented at 31st Conference on Retroviruses and Opportunistic Infections (CROI). March 2024. 5 Rana, et al. Long-acting Injectable CAB/RPV is Superior to Oral ART in PWH with adherence challenges: ACTG A5359. Presented at 31st Conference on Retroviruses and Opportunistic Infections (CROI). March 2024. 6 Kamya, et al. SEARCH Randomized trial of Dynamic Choice HIV Prevention including injectable cabotegravir (CAB-LA). Presented at 31st Conference on Retroviruses and Opportunistic Infections (CROI). March 2024. 7 Hsu, et al. Real-World Effectiveness of Cabotegravir + Rilpivirine vs. Standard of Care Oral Regimens in the US. Presented at 31 Conference on Retroviruses and Opportunistic Infections (CROI). March 2024. 8 Sörstedt, et al. Switching to DTG+3TC vs 3-drug regimens in routine clinical care: long-term Swedish data. Presented at 31st Conference on Retroviruses and Opportunistic Infections (CROI). March 2024. 9 Data on File

Phase 2Phase 1Clinical ResultPhase 3

12 Dec 2023

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What are NS5A inhibitors and how do you quickly get the latest development progress?

NS5A is a crucial protein found in the human body that plays a significant role in the life cycle of the hepatitis C virus (HCV). It is involved in viral replication, assembly, and release, making it an attractive target for antiviral therapies. NS5A interacts with various host proteins and cellular pathways, modulating the immune response and promoting viral persistence. Inhibiting NS5A can disrupt HCV replication, leading to reduced viral load and improved clinical outcomes. Understanding the function of NS5A is essential for developing effective treatments against HCV and combating the global burden of this infectious disease. The analysis of the current competitive landscape of target NS5A reveals that Gilead Sciences, Inc., AbbVie, Inc., and Merck & Co., Inc. are the leading companies in terms of R&D progress. These companies have drugs in multiple phases of development, including the approved phase. The indication analysis shows that drugs under the target NS5A have been approved for various indications related to Hepatitis C, Fibrosis, Cirrhosis, and other diseases. The drug types progressing most rapidly are small molecule drugs and synthetic peptides, indicating intense competition in the market. China is a significant player in the development of drugs targeting NS5A, with the highest number of drugs in the approved phase. Other countries such as Japan, European Union, and the United States also have a considerable presence in the development of NS5A drugs. The future development of target NS5A is promising, with ongoing research and development by various companies and institutions. The competition in the market is expected to intensify, especially for small molecule drugs and synthetic peptides. Further advancements in the treatment of Hepatitis C and other related indications can be expected with the continued efforts of the pharmaceutical industry. How do they work?NS5A inhibitors are a type of antiviral medication that target the NS5A protein in the hepatitis C virus (HCV). From a biomedical perspective, these inhibitors work by blocking the function of the NS5A protein, which is essential for viral replication and assembly. By inhibiting NS5A, these drugs help to prevent the spread and multiplication of the hepatitis C virus in the body. NS5A inhibitors are commonly used in combination with other direct-acting antiviral drugs to treat chronic hepatitis C infection. They have shown high efficacy in achieving sustained virologic response (SVR), which means that the virus is undetectable in the blood six months after completing treatment. These inhibitors have revolutionized the treatment of hepatitis C, offering shorter treatment durations, improved tolerability, and higher cure rates compared to older therapies. It's important to note that NS5A inhibitors are specific to the treatment of hepatitis C and are not used for other viral infections or diseases. They are typically prescribed by healthcare professionals and should be taken as directed to ensure optimal treatment outcomes. Common examples of NS5A inhibitors include ledipasvir, daclatasvir, and ombitasvir. List of NS5A InhibitorsThe currently marketed NS5A inhibitors include: Emitasvir PhosphateRavidasvir HydrochlorideCoblopasvir hydrochlorideGlecaprevir/PibrentasvirGlecaprevir/PibrentasvirElbasvirSofosbuvir/VelpatasvirElbasvir/GrazoprevirOmbitasvir/Paritaprevir/RitonavirLedipasvir/SofosbuvirFor more information, please click on the image below. What are NS5A inhibitors used for?NS5A inhibitors are commonly used in combination with other direct-acting antiviral drugs to treat chronic hepatitis C infection. For more information, please click on the image below to log in and search. How to obtain the latest development progress of NS5A inhibitors?In the Synapse database, you can keep abreast of the latest research and development advances of NS5A inhibitors anywhere and anytime, daily or weekly, through the "Set Alert" function. Click on the image below to embark on a brand new journey of drug discovery!

100 Deals associated with Grazoprevir Hydrate

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KEGG	Wiki	ATC	Drug Bank
-	Grazoprevir Hydrate	J05AP11	DB11575

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Hepatitis C	Japan	Merck Sharp & Dohme Corp.	28 Sep 2016

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Chronic hepatitis C genotype 3	Phase 3	Denmark	-	14 Jul 2017
HIV Infections	Phase 3	Belgium	Merck & Co., Inc.	07 Jan 2016
Hepatitis C, Chronic	Phase 3	-	Merck Sharp & Dohme Corp.	17 Mar 2014
Chronic hepatitis C genotype 2	Phase 2	-	Merck Sharp & Dohme Corp.	28 Nov 2011
Chronic hepatitis C genotype 1	Phase 2	-	Merck Sharp & Dohme Corp.	27 Jun 2011

Clinical Result

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Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT02902120 (CTgov)	Phase 4	Hepatitis C, Chronic \| Chronic Kidney Diseases	21	Post-transplant Grazoprevir and Elbasvir	zymcbpxgib(woigzuktyj) = xycipavglw lkcgyovsvx (zcugprmazr, 15.21) View more	-	18 Nov 2022
NCT02251990 (C-CORAL, Pubmed)	Phase 3	Hepatitis C	152	Elbasvir/Grazoprevir 50mg/100mg	gcgspalynk(rblwjiqdjm) = iuhvrjjwog zxswmoipfz (eneyqceswb )	Positive	01 Dec 2020
NCT03379506 (5172-079 \| MK-5172-079, CTgov)	Phase 2	Hepatitis C, Chronic	57	GZR (Age Cohort 1: 12 to <18 Years: Mini and Expanded)	xnlzcidtmt(nnbplgwdkl) = mdjrqaoeya siueydeomc (fqutowrqqx, sklpbhmaak - nqypnhpvrf) View more	-	17 Aug 2020
				GZR (Age Cohort 2: 7 to <12 Years: Mini and Expanded)	xnlzcidtmt(nnbplgwdkl) = dbsuebhuug siueydeomc (fqutowrqqx, inwugwtdgx - kidoflqgfq) View more
ZEPHYR (EASL2019)	Not Applicable	Hepatitis C, Chronic	183	Elbasvir/Grazoprevir (EBR/GZR)	tricozzleu(tbcjqotedu) = ipbbllukdb inbnwbkvvd (cntkthcymh )	-	11 Apr 2019
NCT03111966 (Pubmed \| J Viral Hepat)	Not Applicable	Hepatitis C, Chronic	804	Elbasvir/Grazoprevir	agxprmaemh(dcjsvkqphw) = Eighty patients experienced an AE, resulting in treatment discontinuation in three. xeyaookwrr (hryenkmkwb )	Positive	01 Jan 2019
NCT01932762 (C-SCAPE, Pubmed \| J Viral Hepat)	Phase 2	Hepatitis C	-	EBR/GZR + RBV	hhpdudhghe(mrpdsrxcsb) = nhhqrluznv yfoqplpstn (kglbezmwcz )	-	01 May 2018
				GZR + RBV	hhpdudhghe(mrpdsrxcsb) = kppmbbfnzw yfoqplpstn (kglbezmwcz )
NCT00998985 \| NCT01532973 (Pubmed \| Clin Ther)	Phase 1	Hepatitis C	-	Elbasvir	cknveqjreq(gjmcdlsqeg) = toucblrvpj kdsthceeux (elqypphkwp )	-	01 May 2018
				Grazoprevir	cknveqjreq(gjmcdlsqeg) = vcgoqtyvul kdsthceeux (elqypphkwp )
NCT02601573 (MK-5172-083 \| 5172-083 \| C-ISLE, CTgov)	Phase 2	Chronic hepatitis C genotype 3	101	Elbasvir+Grazoprevir+Sofosbuvir+Ribavirin (Arm 1: HCV GT3 TN EBG/GZR+SOF+RBV 8 Weeks)	zmfbadndcu = lvlhyurmwr hkuzgzvwvi (vegrnjaiwe, jppwwvwtzo - azjxmiuxza) View more	-	13 Nov 2017
				Elbasvir+Grazoprevir+Sofosbuvir (Arm 2: HCV GT3 TN EBG/GZR+SOF 12 Weeks)	zmfbadndcu = cxsaxgvqnc hkuzgzvwvi (vegrnjaiwe, qzwdhprxzw - tyxbxlvtbg) View more
NCT02332707 \| NCT02332720 (C-CREST-1 and C-CREST-2, Pubmed \| Lancet Gastroenterol Hepatol)	Phase 2	Liver Cirrhosis \| Hepatitis C, Chronic	676	Grazoprevir, ruzasvir, and uprifosbuvir with ribavirin	bjlttkyinp(kndwtlkpft) = jfsetzzwkc azodrzjdro (kbjyajioeh, 81 - 99)	-	01 Nov 2017
				Grazoprevir, ruzasvir, and uprifosbuvir without ribavirin	bjlttkyinp(kndwtlkpft) = hvpmsptdpp azodrzjdro (kbjyajioeh, 88 - 100)
NCT02105701 \| NCT02105467 \| NCT02105688 \| NCT02092350 \| NCT02105662 \| NCT02358044 (Pubmed \| Hepatol Commun)	Phase 3	Hepatitis C	-	Elbasvir/grazoprevir	skrtqwuohl(pdojhtvwux) = mmvbfxrnju rmzuchtmsp (lscfhoiksj )	-	01 Oct 2017
				Proton pump inhibitor	skrtqwuohl(pdojhtvwux) = wypavckzkx rmzuchtmsp (lscfhoiksj )

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