A Phase IIa, Open-label, Randomized Trial in Treatment-naive HIV-1-infected Subjects to Determine the Antiviral Activity of 14 Days of Monotherapy With 4 Different Dose Regimens of TMC310911 Coadministered With Ritonavir

The purpose of this study is to evaluate the antiviral activity as measured by the change in viral load from baseline in the 14 days following initiation of treatment with 4 different dose regimens of TMC310911 co-administered with ritonavir.

Start Date01 Jun 2009

Sponsor / Collaborator

Janssen R&D Ireland Ltd.

NCT00908414

/ WithdrawnPhase 1

Phase I, Double-blind, Randomized, Placebo-controlled Trial in Healthy Volunteers to Examine Safety, Tolerability, Plasma Pharmacokinetics of TMC589337&TMC589354 After Increasing Single Oral Doses & in an Open-label Part After Different Repeated Doses in Combination With Single Oral Dose of TMC310911

The purpose of the study is to determine the safety, tolerability, and plasma pharmacokinetics (i.e., the levels of TMC589337 and TMC589354 circulating in your blood over time) of increasing single oral doses of TMC589337 and TMC589354 and of multiple increasing oral doses followed by a single dose of TMC310911 to assess the potential boosting effect on the latter compound. In this study 3 investigational new drugs are involved. These new investigational drugs called TMC589337 and TMC589354 (from the PEPI family) and TMC310911 are in process of development for the treatment of Human Immunodeficiency Virus-Type 1 (HIV-1). TMC589337 and TMC589354 are novel molecules with no antiviral activity to be used to enhance the pharmacokinetics profile of a drug. TMC310911 is a novel and potent compound and belongs to a medication class called protease inhibitors (PI).

Start Date01 May 2009

Sponsor / Collaborator

Tibotec Pharmaceuticals

NCT00838760

/ CompletedPhase 1

Phase I, Double-blind, Randomized, Placebo-controlled Trial to Examine the Safety, Tolerability and Plasma Pharmacokinetics of Increasing Single Oral Doses of TMC558445 With and Without Food, and Increasing Repeated Oral Doses in Combination With a Single Dose of TMC310911

The purpose of the study is to determine the safety, tolerability and plasma pharmacokinetics (pk) (i.e., the levels of TMC558445 circulating in your blood over time) of increasing single oral doses of TMC558445 and of multiple increasing oral doses followed by a single dose of TMC310911 to assess the potential boosting effect on the latter compound. In this study, two investigational new drugs are involved, TMC558445 and TMC310911.
The study has been amended as follows:
TMC558445 will be administered either twice a day (b.i.d.) or once daily (q.d.). A single 300 mg or 600 mg dose of TMC310911 will be administered under fasted or fed conditions. The boosting effect on Darunavir will be investigated.

Start Date01 Feb 2009

Sponsor / Collaborator

Tibotec Pharmaceuticals

100 Clinical Results associated with TMC-310911

100 Translational Medicine associated with TMC-310911

100 Patents (Medical) associated with TMC-310911

Literatures (Medical) associated with TMC-310911

19 Dec 2022·Journal of Biomolecular Structure and Dynamics

Anti-HIV and anti-HCV small molecule protease inhibitors in-silico repurposing against SARS-CoV-2 M^pro for the treatment of COVID-19

Article

Author: Ishrat, Romana ; Ali, Rafat ; Ali, Sher ; Sultan, Armiya

The COVID-19 pandemic is caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). It is a global health emergency warranting development and implementation of targeted treatment. The enzyme main protease (M^pro; also known as 3C-like protease) is emerging as an attractive drug target. This enzyme plays an indispensable role in processing the translated polyproteins of viral RNA. Inhibiting the activity of M^pro would wedge viral replication. To facilitate the discovery of targeted therapy for COVID-19, we carried out the structure-assisted repurposing of existing protease inhibiting small molecules to target SARS-CoV-2 M^pro. Based on the structure of SARS-CoV-2 M^pro, here we report the small drug molecule namely saquinavir as its potent inhibitor. Findings support the premise that this promising antiviral protease inhibiting small drug molecule can be validated and implemented for the treatment and clinical management of COVID-19 pandemic disease.Communicated by Ramaswamy H. Sarma.

22 Sep 2022·Journal of Biomolecular Structure and Dynamics

Anti-HIV-drug and phyto-flavonoid combination against SARS-CoV-2: a molecular docking-simulation base assessment

Article

Author: Swain, Shasank S. ; Sahoo, Alaka ; Hussain, Tahziba ; Pati, Sanghamitra ; Singh, Satya R.

At the health emergence, no such potent prophylactic therapy is available to control the deadly emerged Severe Acute Respiratory Syndrome Coronavirus-2 (SARS-CoV-2). However, existing antiviral, anti-inflammatory, antimalarial drugs is the only option against SARS-CoV-2, but it may be harmful to patients without more clinical evidence. As an alternative solution, we proposed a newer hypothesis using the selective 10 potent anti-HIV drugs and flavonoid class of phytochemicals from previous reports to use in combination against SARS-CoV-2. Primarily, 10 anti-HIV protease inhibitor drugs and 10 phyto-flavonoids as ligands in molecular docking study against the putative target, the SARS-CoV-2-main protease (M^pro) ID: 6Y2E), as an essential enzyme in viral genome replication. According to molecular docking and drug-ability scores of each ligand, the anti-HIV drug, the darunavir (with a docking score, -10.25 kcal/mol and drug-likeness rating, 0.60) and the quercetin-3-rhamnoside (with a docking score, -10.90 kcal/mol and drug-likeness rating, 0.82) were selected for further analysis in combined effect. Perceptibly, the combined 'anti-HIV drug and phyto-flavonoid' docking complex has actively interacted with eight strong H-bonds with stability, briefly elucidated through RMRD-, RMSF- Rg-plots and MM/PBSA-binding energy calculation during 100 ns than the individual against SARS-CoV-2-M^pro. Thus, the 'anti-HIV-drug-phyto-flavonoid' combination therapy could be used against SARS-CoV-2 after some experimental validation.Communicated by Ramaswamy H. Sarma.

22 Sep 2022·Journal of Biomolecular Structure and Dynamics

Targeting allosteric pockets of SARS-CoV-2 main protease M^pro

Article

Author: Bhat, Zahoor Ahmad ; Chitara, Dheeraj ; Madhumalar, Arumugam ; Iqbal, Jawed ; Sanjeev, B. S.

Repurposing of antivirals is an attractive therapeutic option for the treatment of COVID-19. Main protease (M^pro⁾, also called 3 C-like protease (3CL^pro) is a key protease of SARS-CoV-2 involved in viral replication, and is a promising drug target for antivirals. A major challenge to test the efficacy of antivirals is the conformational plasticity of M^pro and its future mutation prone flexibility. Suitable choice of drugs in catalytic and allosteric pockets appear to be essential for combination therapy. Current study, based on docking and extensive set of MD simulations, finds the combination of Elbasvir, Glecaprevir and Ritonavir to be a viable candidate for further experimental drug testing/pharmacophore design for M^pro.Communicated by Ramaswamy H. Sarma.

News (Medical) associated with TMC-310911

08 May 2018

·www.biospace.com

Two Chinese Pharma Companies, WuXi AppTec and Ascletis Pharma, List IPOs on Asian Exchanges

Shares of Chinese pharmaceutical and medical device company WuXi AppTec were a hot commodity Tuesday as the company made its debut on the Shanghai Stock Exchange. Another Chinese company, Ascletis Pharma, also chose a new stock listing. Shares of Chinese pharmaceutical and medical device company WuXi AppTec were a hot commodity Tuesday as the company made its debut on the Shanghai Stock Exchange . WuXi AppTec, which is headquartered in Shanghai, listed 104,198,600 shares of common stock at a public offering price of RMB21.60 per share. Chinese news service Xinhua reported that share prices surged nearly 44 percent Tuesday to reach 31.1 yuan, about $4.98. In announcing its IPO WuXi AppTec said the proceeds will be used to expand its R&D facilities in China and strengthen its “capabilities and capacities to better serve global customers and partners.” Ge Li, chairman and chief executive officer of WuXi AppTec, said he was grateful for the confidence investors are showing in the company. That confidence, he said, will allow the company to focus on its mission and accelerate the growth of its platform. “Our commitment has always remained the same -- we want to empower and enable anyone and any company to advance medicines for patients faster. This commitment will underpin everything we do as we build a strong, valuable and socially responsible public company,” Li said in a statement. This is the second time the Chinese company has been listed on a stock exchange. The company had been listed on the New York Stock Exchange from 2007 to 2015 when the company opted to become privately held. When WuXi AppTec sought to list itself on the Shanghai exchange, Xinhua reported the request was quickly greenlit by the China Securities Regulatory Commission (CSRC). That move was part of a CSRC effort fast-track new listings from unicorn companies in order to “to invigorate the country’s capital market and foster the new economy,” Xinhua said. Another Chinese company, Ascletis Pharma, also chose a new stock listing. The Hangzhou-based company filed for an IPO on the Hong Kong exchange as it prepares to launch its hepatitis C treatment Danoprevir by September. Danoprevir, which was licensed from Roche, is aimed at the treatment of chronic hepatitis C. Clinical study results show that with 12-week treatment, the cure rate of treatment with Danoprevir exceeded 95 percent in genotype 1 CHC patients. The South China Morning P ost reported that hepatitis C affects about 350,000 people in China annually. Unlike the United States, where there are numerous near-cure treatments for the disease, in China there has been a lack of breakthrough therapies, the Post said. In addition to Danoprevir Ascletis also has Ravidasvir, which licensed from Presidio Pharmaceuticals. Like Danoprevir, Ravidasvir is also aimed at treating hepatitis C. Ascletis also has two other drug candidates in its pipeline: ASC06, a clinical stage, first-in-class, RNAi therapeutic for the treatment of liver cancers, which was licensed from Alnylam Pharmaceuticals; and ASC09, a phase 2a completed HIV protease inhibitor, licensed from Janssen, a division of Johnson & Johnson. The actions of WuXi AppTec and Ascletis highlights the growing importance of China in the pharmaceutical industry. The country has a pharmaceutical market value that is expected to reach $175 billion by 2022, according to data from health-care information company IQVIA (formerly QuintilesIMS). Not only does there appear to be a strong market for liver disease treatments, such as hepatitis, China is also a key market for new oncology treatments. WuXi AppTec is certainly working on strengthening its presence in oncology treatments. Last year WuXi formed a partnership with Seattle-based Juno Therapeutics to develop treatments for cancer with the formation of a new Chinese company called JW Biotechnology Co., Ltd . The new company’s mission will be to build a cell therapy company in China through using Juno’s chimeric antigen receptor (CAR) and T cell receptor (TCR) technologies in combination with WuXi AppTec’s R&D and manufacturing platform.

Phase 2IPO

100 Deals associated with TMC-310911

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Indication	Highest Phase	Country/Location	Organization	Date
HIV Infections	Phase 2	-	Ascletis Pharma, Inc.	-
HIV Infections	Phase 2	-	Ascletis Pharma, Inc.	-

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT00838162 (CTgov)	Phase 2	HIV Infections	33	Ritonavir 100 mg twice daily+TMC310911 75 mg twice daily (TMC310911/Rtv 75/100 mg Twice Daily)	urartvnpvj(qpincfhoej) = mehajzmedt aeuolefrjn (vpjjygcaci, cqstgcfdif - fhiuyrjtgl) View more	-	07 Mar 2013
				Ritonavir 100 mg twice daily+TMC310911 150 mg twice daily (TMC310911/Rtv 150/100 mg Twice Daily)	urartvnpvj(qpincfhoej) = tayvhwcczj aeuolefrjn (vpjjygcaci, mzcocfszyh - benwbjgccu) View more

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