Testing of HIV Protease Inhibitors to Suppress Inflammation and Improve Cardio Pulmonary Hemodynamics in Subjects With Pulmonary Arterial Hypertension

Study Rationale:There is recent evidence that HIV protease inhibitors (HIV-PI) can improve pulmonary hemodynamics in experimental models of pulmonary arterial hypertension (PAH). There is also experimental evidence that both TLR4 and high mobility group box 1 (HMGB1) participate in the pathogenesis of experimental pulmonary hypertension. A recent high throughput screen for inhibitors of HMGB1 induced macrophage activation yielded HIV-protease inhibitors (PIs) as potent inhibitors of HMGB1 induced cytokine production. Based on the experimental evidence we propose a trial to determine whether HIV-PIs will alter the pathobiology of PAH.
Study Objectives:The main objective of this study is to determine whether saquinavir and ritonavir (SQV+RIT) which have a well-characterized safety profile in humans will reduce bio markers of inflammation and pulmonary artery pressures in patients with PAH.
Study Hypothesis:We hypothesize that the HIV-PI, SQV+RIT, will reduce circulating parameters of inflammation including HMGB1, IL1-beta, IL-6, IL-8, IL-10, TNF-alpha and CRP. Our end points will be changes in these parameters from baseline over the duration of the study.We hypothesize that treatment with SQV+RIT will reduce pulmonary artery(PA) pressure of patients with PAH as measured by echocardiography.
Study Design:This is a single center open label phase 0 study to evaluate the effect of SQV +RIT in patients with IPAH. Subjects with IPAH(N=20) will be enrolled into a study, which will be divided into 3 cohorts and entail the administration of HIV protease inhibitors in three doses. The first cohort (n=3) will receive a starting dose of SQV 0.3 mg/kg twice daily in combination with RIT 0.03 mg/kg twice daily. If the first dose is well-tolerated, the second cohort (n= 3 ) with IPAH will be given doses of SQV 3 mg/kg and RIT 0.3 mg/kg twice daily. If the second dose is well-tolerated, the last cohort (n= 14 ) with IPAH will be given doses of SQV 15 mg/kg and RIT 1.5 mg/kg twice daily.

Start Date01 Dec 2013

Sponsor / Collaborator

The Third Xiangya Hospital of Central South University

[+1]

NCT01638650

/ CompletedPhase 1

To Determine the Effect of the Modified SQV/r (Saquinavir-boosted by Ritonavir) Regimen (500/100 mg for the 1st Week Followed by 1000/100 mg for the 2nd Week) on the QTc Interval, Pharmacokinetics, and Antiviral Activity in Treatment-naive HIV-1 Infected Patients

This open-label study will evaluate the safety, pharmacokinetics and antiviral activity of a modified Invirase (saquinavir)/ritonavir regimen in treatment-naïve HIV-1 infected patients. Patients will receive Invirase 500 mg plus ritonavir 100 mg twice daily orally for the first week, followed by Invirase 1000 mg plus ritonavir 100 mg twice daily orally for the second week. The study treatment will be given in combination with two Nucleoside Reverse Transcriptase Inhibitors (NRTIs), in accordance with the current clinical HIV treatment guidelines. Anticipated time on study treatment is 14 days.

Start Date01 Jan 2012

Sponsor / Collaborator

Hoffmann-La Roche, Inc.

JPRN-UMIN000004621

/ CompletedNot Applicable

Effect of a pharmaceutical excipient, cremophol EL on the plasma concentration-time profile of saquinavir and fexofenadine after their oral administrations at doses used in the exploratory investigational new drug clinical studies - Effect of cremophol EL on pharmacokinetics of saquinavir and fexofenadine at doses used in the exploratory investigational new drug clinical studies

Start Date01 Nov 2010

Sponsor / Collaborator-

100 Clinical Results associated with Saquinavir Mesylate

100 Translational Medicine associated with Saquinavir Mesylate

100 Patents (Medical) associated with Saquinavir Mesylate

3,723

Literatures (Medical) associated with Saquinavir Mesylate

24 Sep 2025·ACS physical chemistry Au

Insights into Antiviral Candidates against Oropouche Virus: A Molecular Dynamics Study

Article

Author: Cardoso, Wesley B. ; Colherinhas, Guilherme

The Oropouche virus (OROV), an emerging arbovirus from the Peribunyaviridae family, represents a growing public health concern in Latin America, particularly due to its rapid urban spread and lack of specific treatments. In this study, we employed an integrated computational strategy combining molecular docking and molecular dynamics (MD) simulations to evaluate the potential of HIV protease inhibitors as candidates for repurposing against the Gc glycoprotein of OROV, a critical component in viral fusion and host cell entry. While docking initially ranked Saquinavir as the top binder, subsequent MD simulations revealed that nelfinavir and indinavir exhibited superior performance across multiple criteria, including binding energy, structural stability, center-of-mass distance maintenance, and consistent hydrogen bonding. These findings emphasize the limitations of docking-only approaches and highlight the importance of dynamic and energetic analyses for accurate inhibitor selection. The proposed computational pipeline demonstrates its value in identifying stable, high-affinity ligands and offers a promising route for accelerating drug discovery against neglected viral diseases such as OROV.

01 Jul 2025·BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Repurposing HIV protease inhibitors as senotherapeutic agents in cervical cancer: Dual targeting of CDK1/6-cell cycle arrest and p53/p21/p16 signaling axis

Article

Author: Sun, Shiguo ; Li, Hongjuan ; Han, Weiqiang ; Yu, Lan ; Liu, Guoxin ; Liu, Fengyu ; Zhang, Jing ; Xu, Yongqian

The clinical management of cervical cancer remains constrained by limited therapeutic options and a paucity of targeted pharmacological interventions. Drug repurposing emerges as a promising strategy to expedite oncological therapeutics development. This study systematically investigates the antineoplastic potential of HIV protease inhibitors saquinavir (SQV) and tipranavir (TPV) through multimodal mechanistic validation. In vitro analyses demonstrated dose-dependent inhibition of cervical cancer cell proliferation accompanied by significant upregulation of senescence-associated β-galactosidase (SA-β-Gal) activity. Molecular characterization revealed concomitant activation of senescence-regulatory proteins p53, p21, and p16, suggesting induction of tumor-suppressive senescence pathways. Transcriptomic profiling of inhibitor-treated SiHa cells identified critical cell cycle regulators CDK1 and CDK6, findings corroborated by molecular docking simulations revealing high-affinity binding to cyclin-dependent kinases (-32.0607 to -47.6820 kJ/mol). In vivo validation using xenograft models demonstrated comparable tumor growth inhibition to doxorubicin with preserved host viability and negligible systemic toxicity. Mechanistic integration revealed dual pathway modulation: G1-phase cell cycle arrest mediated through CDK1/6 suppression and coordinated activation of the p53/p21/p16 senescence signaling axis. These findings establish SQV and TPV as multi-targeted senotherapeutic agents, providing preclinical rationale for repurposing HIV antivirals as novel therapeutic strategy against cervical malignancies.

01 Jun 2025·MOLECULAR DIVERSITY

A deep drug prediction framework for viral infectious diseases using an optimizer-based ensemble of convolutional neural network: COVID-19 as a case study

Article

Author: Babu, K R Remesh ; Deepthi, K ; Aruna, A S ; Babu, K. R. Remesh ; Aruna, A. S. ; Deepthi, K.

The SARS-CoV-2 outbreak highlights the persistent vulnerability of humanity to epidemics and emerging microbial threats, emphasizing the lack of time to develop disease-specific treatments. Therefore, it appears beneficial to utilize existing resources and therapies. Computational drug repositioning is an effective strategy that redirects authorized drugs to new therapeutic purposes. This strategy holds significant promise for newly emerging diseases, as drug discovery is a lengthy and expensive process. Through this study, we present an ensemble method based on the convolutional neural network integrated with genetic algorithm and deep forest classifier for virus-drug association prediction (CGDVDA). We generated feature vectors by combining drug chemical structure and virus genomic sequence-based similarities, and extracted prominent deep features by applying the convolutional neural network. The convoluted features are optimized using the genetic algorithm and classified using the ensemble deep forest classifier to predict novel virus-drug associations. The proposed method predicts drugs for COVID-19 and other viral diseases in the dataset. The model could achieve ROC-AUC scores of 0.9159 on fivefold cross-validation. We compared the performance of the model with state-of-the-art approaches and classifiers. The experimental results and case studies illustrate the efficacy of CGDVDA in predicting drugs against viral infectious diseases.

News (Medical) associated with Saquinavir Mesylate

04 Nov 2025

·www.prnewswire.com

Calliditas Therapeutics to Present at the American Society of Nephrology Kidney Week

STOCKHOLM, Nov. 4, 2025 /PRNewswire/ -- Calliditas Therapeutics (Calliditas), an Asahi Kasei company, announced today that new data will be presented at the 2025 American Society of Nephrology Kidney Week, taking place from November 6 to 9 in Houston, Texas. The presentations will include new secondary analyses from the Phase 3 NefIgArd study of Nefecon (marketed as TARPEYO® [budesonide] delayed-release capsules in the United States in patients with primary immunoglobulin A nephropathy [IgAN] who are at risk for disease progression) as well as initial demographics of the PERFORM registry of IgAN patients that have received TARPEYO. Additional real-world treatment and management evidence, derived from the Veterans Health Administration and the Cure Glomerulopathy Network (CureGN) registry, will also be presented. Data from a Phase 2a, randomized, double-blind, placebo-controlled trial studying setanaxib for the treatment of Alport Syndrome, will be presented in a High-Impact Clinical Trials session on November 8. Alport Syndrome is a rare genetic kidney disease resulting from mutations in collagen type IV genes that can lead to progressive loss of kidney function and end-stage kidney disease. A total of eight abstracts were accepted for presentation, including one selected as a High-Impact Clinical Trial, one oral presentation, five poster presentations, and one informational poster. High-impact Clinical Trial: Abstract No. 3345 Title: "Safety and preliminary efficacy findings from a Phase 2a randomized, double-blind, placebo-controlled trial of setanaxib in patients with Alport syndrome" Date and time: November 8, 10 am to 12 pm CT (presentation scheduled for 10:30-10:45 am) Location: Hall A Presenter: Daniel Gale, University College London Oral Presentation: Abstract No. SA-OR047 Title: "Duration of Absolute Proteinuria Response with Nefecon in Patients with Primary IgAN: Results from the Two-Year NefIgArd Trial" Date and time: November 8, 4:30 to 6 pm CT (presentation scheduled for 4:40-4:50 pm) Location: Room 310A Presenter: Brad Rovin, The Ohio State University Wexner Medical Center Poster Presentations: Abstract No. FR-PO0804 Title: "Absolute Proteinuria over Time with Nefecon vs. Placebo in Patients with IgAN: Results from the Phase 3 NefIgArd Trial" Date and time: November 7, 10 am to 12 pm CT Presenter: Heather Reich, University of Toronto Abstract No. FR-PO0849 Title: "Real-World Treatment for IgA Nephropathy in the Veterans Health Administration" Date and time: November 7, 10 am to 12 pm CT Presenter: Lucile Gregg, Baylor College of Medicine Abstract No. SA-PO0789 Title: "Creation and Initial Demographics of the PERFORM Patient Registry: Novel Real-World Registry of Patients Treated for IgAN in the United States" Date and time: November 8, 10 am to 12 pm CT Presenter: Russell Jones, Calliditas Therapeutics Abstract No. SA-PO0804 Title: "Kidney outcomes in immunoglobulin A nephropathy (IgAN) across the age spectrum in the Cure Glomerulopathy Network (CureGN)" Date and time: November 8, 10 am to 12 pm CT Presenter: Myda Khalid, Indiana University School of Medicine Abstract No. SA-PO0840 Title: "Therapies for Immunoglobulin A Nephropathy (IgAN) in Cure Glomerulopathy Network (CureGN)" Date and time: November 8, 10 am to 12 pm CT Presenter: Terri Madison, Madison Epi Solutions LLC Abstract No. INFO14-TH Title: "Investigating Extended Nefecon Treatment Beyond Nine Months in Patients with IgAN: The Phase 4 NefXtend Trial" Date and time: November 6, 10 am to 12 pm CT (display only) Kidney Week is the world's premier nephrology meeting, hosted by the American Society of Nephrology (ASN), that brings together thousands of kidney health professionals to share the latest advances in kidney science, research, and treatments. About TARPEYO® /Kinpeygo® TARPEYO is an oral 4mg delayed-release formulation of budesonide, designed to dissolve in the pH of the distal ileum. Each capsule contains coated beads of budesonide that target mucosal B-cells present in the ileum, including the Peyer's patches, which are responsible for the production of galactose-deficient IgA1 antibodies (Gd-Ag1), causing IgA nephropathy. About Primary Immunoglobulin A Nephropathy Primary immunoglobulin A nephropathy (IgA nephropathy or IgAN or Berger's Disease) is a rare, progressive, chronic immune-mediate disease that attacks the kidneys and occurs when galactose-deficient IgA1 is recognized by autoantibodies, creating IgA1 containing immune complexes that become deposited in the glomerular mesangium of the kidney. This deposition in the kidney can lead to progressive kidney damage, potentially resulting in end-stage kidney disease. IgAN most often develops between late teens and late 30s. IMPORTANT SAFETY INFORMATION INDICATION TARPEYO is indicated to reduce the loss of kidney function in adults with primary immunoglobulin A nephropathy (IgAN) who are at risk for disease progression. IMPORTANT SAFETY INFORMATION CONTRAINDICATIONS TARPEYO is contraindicated in patients with hypersensitivity to budesonide or any of the ingredients of TARPEYO. Serious hypersensitivity reactions, including anaphylaxis, have occurred with other budesonide formulations. WARNINGS AND PRECAUTIONS Hypercorticism and adrenal axis suppression: When corticosteroids are used chronically, systemic effects such as hypercorticism and adrenal suppression may occur. Corticosteroids can reduce the response of the hypothalamus-pituitary-adrenal (HPA) axis to stress. In situations where patients are subject to surgery or other stress situations, supplementation with a systemic corticosteroid is recommended. When discontinuing therapy or switching between corticosteroids, monitor for signs of adrenal axis suppression. Patients with moderate to severe hepatic impairment (Child-Pugh Class B and C respectively) could be at an increased risk of hypercorticism and adrenal axis suppression due to an increased systemic exposure to oral budesonide. Avoid use in patients with severe hepatic impairment (Child-Pugh Class C). Monitor for increased signs and/or symptoms of hypercorticism in patients with moderate hepatic impairment (Child-Pugh Class B). Immunosuppression and Increased Risk of Infection: Corticosteroids, including TARPEYO, suppress the immune system and increase the risk of infection with any pathogen, including viral, bacterial, fungal, protozoan, or helminthic pathogens. Corticosteroids can: reduce resistance to new infections, exacerbate existing infections, increase the risk of disseminated infections, increase the risk of reactivation or exacerbation of latent infections, and mask some signs of infection. Corticosteroid-associated infections can sometimes be serious. Monitor for infection and consider TARPEYO withdrawal as needed. Avoid corticosteroid therapy, including TARPEYO, in patients with active or quiescent tuberculosis or hepatitis B infection; untreated fungal, bacterial, systemic viral, or parasitic infections; ocular herpes simplex; or Kaposi's sarcoma. Avoid exposure to active, easily-transmitted infections (e.g., chickenpox, measles). Corticosteroid therapy may decrease the immune response to some vaccines. Other corticosteroid effects: TARPEYO is a systemically available corticosteroid and is expected to cause related adverse reactions. Monitor patients with hypertension, prediabetes, diabetes mellitus, osteoporosis, peptic ulcer, glaucoma or cataracts, or with a family history of diabetes or glaucoma, or with any other condition where corticosteroids may have unwanted effects. ADVERSE REACTIONS In clinical studies, the most common adverse reactions with TARPEYO (occurring in ≥5% of TARPEYO treated patients, and ≥2% higher than placebo) were peripheral edema (17%), hypertension (12%), muscle spasms (12%), acne (11%), headache (10%), upper respiratory tract infection (8%), face edema (8%), weight increased (7%), dyspepsia (7%), dermatitis (6%), arthralgia (6%), and white blood cell count increased (6%). DRUG INTERACTIONS Budesonide is a substrate for CYP3A4. Avoid use with potent CYP3A4 inhibitors, such as ketoconazole, itraconazole, ritonavir, indinavir, saquinavir, erythromycin, and cyclosporine. Avoid ingestion of grapefruit juice with TARPEYO. Intake of grapefruit juice, which inhibits CYP3A4 activity, can increase the systemic exposure to budesonide. USE IN SPECIFIC POPULATIONS Pregnancy: The available data from published case series, epidemiological studies, and reviews with oral budesonide use in pregnant women have not identified a drug-associated risk of major birth defects, miscarriage, or other adverse maternal or fetal outcomes. There are risks to the mother and fetus associated with IgAN. Infants exposed to in-utero corticosteroids, including budesonide, are at risk for hypoadrenalism. Please see Full Prescribing Information About Setanaxib Setanaxib is a novel enzyme-dependent hydrogen peroxide depleting agent with anti-fibrotic and anti-inflammation properties. Setanaxib is in development for fibrotic rare diseases, such as Alport Syndrome, where targeting inflammation and fibrosis may potentially slow disease progression. About Calliditas Calliditas Therapeutics is a biopharma company headquartered in Stockholm, Sweden, focused on identifying, developing, and commercializing novel treatments in orphan indications with significant unmet medical needs. Visit Calliditas.com for further information. About Asahi Kasei The Asahi Kasei Group contributes to life and living for people around the world. Since its foundation in 1922 with ammonia and cellulose fiber business, Asahi Kasei has consistently grown through the proactive transformation of its business portfolio to meet the evolving needs of every age. With more than 50,000 employees worldwide, the company contributes to a sustainable society by providing solutions to the world's challenges through its three business sectors of Healthcare, Homes, and Material. Its Healthcare operations include devices and systems for acute critical care, and manufacture of biotherapeutics, as well as pharmaceuticals. For further information, please visit asahi-kasei.com. SOURCE Asahi Kasei Corporation 21% more press release views with Request a Demo

Phase 3Phase 2Clinical Result

04 Nov 2025

·www.businesswire.com

Nefecon Included in the Updated KDIGO Clinical Practice Guideline, Strengthening Asahi Kasei’s Position in IgA Nephropathy Treatment

CHELMSFORD, Mass. & TOKYO--(BUSINESS WIRE)--Asahi Kasei, a global provider of healthcare and pharmaceutical solutions, announced that Nefecon (marketed in the United States as TARPEYO® (budesonide) delayed release capsules), has been included in the Kidney Disease: Improving Global Outcomes (KDIGO) 2025 Clinical Practice Guideline for the Management of IgA Nephropathy (IgAN) and Immunoglobulin A Vasculitis (IgAV). TARPEYO is a key product in Asahi Kasei’s pharmaceutical business, which the company has identified as a strategic growth area in its medium-term management plan. The inclusion of Nefecon in the KDIGO guidelines underscores its place in therapy and is expected to further support sustainable, long-term growth within Asahi Kasei’s healthcare portfolio. The updated KDIGO 2025 guideline aims to standardize care and improve outcomes by providing evidence-based recommendations related to IgAN diagnosis, prognosis and treatment.1 It is considered the global standard for nephrology practice and plays a central role in shaping treatment decisions for patients with IgAN. The KDIGO 2025 guideline suggests treatment with a 9-month course of Nefecon for patients at risk of progressive loss of kidney function, recognizing the treatment benefit of Nefecon in reducing the loss of kidney function and reducing proteinuria as demonstrated in the NefIgArd phase 3 randomized placebo-controlled trial.2,3 The effect of Nefecon on proteinuria and kidney function was assessed in adults with biopsy-proven IgAN who were on a stable dose of maximally tolerated RAS inhibitor therapy. Adverse events were mild or moderate and generally resolved after treatment cessation. KDIGO also notes that Nefecon is the only treatment approved for IgAN to date that has been proven to reduce the levels of pathogenic forms of IgA, which is an underlying cause of the disease.1,4* “The inclusion of Nefecon in the KDIGO 2025 Guideline provides important external validation of its place in therapy. It also reinforces its role as the first and only approved therapy for IgAN shown to reduce the levels of pathogenic IgA and as an essential part of the comprehensive treatment approach now suggested by KDIGO,” said Ken Shinomiya, Leader of the Healthcare sector of Asahi Kasei. About Nefecon Nefecon is an oral 4 mg targeted-release formulation of budesonide, designed to dissolve in the pH of the distal ileum. Each capsule contains coated beads of budesonide that target mucosal B-cells present in the ileum, including the Peyer's patches, which are responsible for the production of galactose-deficient IgA1 antibodies (Gd-IgAg1), causing IgA nephropathy. It has not been established to what extent the efficacy of Nefecon is mediated via local effects in the ileum vs. systemic effects. Nefecon’s approval status, labeled indication, and availability vary globally. It is approved in the United States where it is marketed as TARPEYO® (budesonide) delayed-release capsules by Calliditas Therapeutics. It is available in the European Economic Area (EEA) where it is marketed by STADA Arzneimittel AG and in select countries in Asia, including Mainland China, Hong Kong, Macau, Taiwan, and Singapore where it is marketed by Everest Medicines. It is also in development in Japan by Viatris. About the NeflgArd Study NefIgArd was a global, Phase 3, randomized, double-blind, placebo-controlled, multicenter study to evaluate the efficacy and safety of Nefecon 16 mg once daily vs placebo in adult patients with primary IgAN (N=364) in addition to optimized RASi therapy. Patients were randomized 1:1 to receive 16 mg/day oral capsules of Nefecon or matching placebo for 9 months, followed by a 15-month observational follow-up period without the study drug. The primary efficacy endpoint was time-weighted average of eGFR over 2 years. The time-weighted average of eGFR over 2 years showed a statistically significant treatment benefit with Nefecon versus placebo (difference 5.05 mL/min per 1.73 m² [95% CI 3.24 to 7.38], p<0.0001). The mean reduction in UPCR from baseline was 35% at the end of treatment (month 9), with a 52% reduction achieved at 12 months, and a 34% reduction at month 24 (15 months off treatment). The most common adverse reactions with Nefecon (occurring in ≥5% of Nefecon treated patients and ≥2% higher than placebo) were peripheral edema (17%), hypertension (12%), muscle spasms (12%), acne (11%), headache (10%), upper respiratory tract infection (8%), face edema (8%), weight increase (7%), dyspepsia (7%), dermatitis (6%), arthralgia (6%), and white blood cell count increase (6%). About Primary Immunoglobulin A Nephropathy Primary immunoglobulin A nephropathy (IgA nephropathy or IgAN or Berger's Disease) is a rare, progressive, chronic immune-mediated disease that attacks the kidneys and occurs when galactose-deficient IgA1 is recognized by autoantibodies, creating IgA1 containing immune complexes that become deposited in the glomerular mesangium of the kidney. This deposition in the kidney can lead to progressive kidney damage, potentially resulting in end-stage kidney disease. IgAN most often develops between the late teens and late 30s. * Data are exploratory. Clinical significance has not been established. IMPORTANT SAFETY INFORMATION FOR US AUDIENCE INDICATION TARPEYO is indicated to reduce the loss of kidney function in adults with primary immunoglobulin A nephropathy (IgAN) who are at risk for disease progression. IMPORTANT SAFETY INFORMATION CONTRAINDICATIONS TARPEYO is contraindicated in patients with hypersensitivity to budesonide or any of the ingredients of TARPEYO. Serious hypersensitivity reactions, including anaphylaxis, have occurred with other budesonide formulations. WARNINGS AND PRECAUTIONS Hypercorticism and adrenal axis suppression: When corticosteroids are used chronically, systemic effects such as hypercorticism and adrenal suppression may occur. Corticosteroids can reduce the response of the hypothalamus-pituitary-adrenal (HPA) axis to stress. In situations where patients are subject to surgery or other stress situations, supplementation with a systemic corticosteroid is recommended. When discontinuing therapy or switching between corticosteroids, monitor for signs of adrenal axis suppression. Patients with moderate to severe hepatic impairment (Child-Pugh Class B and C respectively) could be at an increased risk of hypercorticism and adrenal axis suppression due to an increased systemic exposure to oral budesonide. Avoid use in patients with severe hepatic impairment (Child-Pugh Class C). Monitor for increased signs and/or symptoms of hypercorticism in patients with moderate hepatic impairment (Child-Pugh Class B). Immunosuppression and Increased Risk of Infection: Corticosteroids, including TARPEYO, suppress the immune system and increase the risk of infection with any pathogen, including viral, bacterial, fungal, protozoan, or helminthic pathogens. Corticosteroids can: reduce resistance to new infections, exacerbate existing infections, increase the risk of disseminated infections, increase the risk of reactivation or exacerbation of latent infections, and mask some signs of infection. Corticosteroid-associated infections can sometimes be serious. Monitor for infection and consider TARPEYO withdrawal as needed. Avoid corticosteroid therapy, including TARPEYO, in patients with active or quiescent tuberculosis or hepatitis B infection; untreated fungal, bacterial, systemic viral, or parasitic infections; ocular herpes simplex; or Kaposi’s sarcoma. Avoid exposure to active, easily-transmitted infections (e.g., chickenpox, measles). Corticosteroid therapy may decrease the immune response to some vaccines. Other corticosteroid effects: TARPEYO is a systemically available corticosteroid and is expected to cause related adverse reactions. Monitor patients with hypertension, prediabetes, diabetes mellitus, osteoporosis, peptic ulcer, glaucoma or cataracts, or with a family history of diabetes or glaucoma, or with any other condition where corticosteroids may have unwanted effects. ADVERSE REACTIONS In clinical studies, the most common adverse reactions with TARPEYO (occurring in ≥5% of TARPEYO treated patients, and ≥2% higher than placebo) were peripheral edema (17%), hypertension (12%), muscle spasms (12%), acne (11%), headache (10%), upper respiratory tract infection (8%), face edema (8%), weight increased (7%), dyspepsia (7%), dermatitis (6%), arthralgia (6%), and white blood cell count increased (6%). DRUG INTERACTIONS Budesonide is a substrate for CYP3A4. Avoid use with potent CYP3A4 inhibitors, such as ketoconazole, itraconazole, ritonavir, indinavir, saquinavir, erythromycin, and cyclosporine. Avoid ingestion of grapefruit juice with TARPEYO. Intake of grapefruit juice, which inhibits CYP3A4 activity, can increase the systemic exposure to budesonide. USE IN SPECIFIC POPULATIONS Pregnancy: The available data from published case series, epidemiological studies, and reviews with oral budesonide use in pregnant women have not identified a drug-associated risk of major birth defects, miscarriage, or other adverse maternal or fetal outcomes. There are risks to the mother and fetus associated with IgAN. Infants exposed to in-utero corticosteroids, including budesonide, are at risk for hypoadrenalism. Please see Full Prescribing Information About Asahi Kasei The Asahi Kasei Group contributes to life and living for people around the world. Since its foundation in 1922 with ammonia and cellulose fiber business, Asahi Kasei has consistently grown through the proactive transformation of its business portfolio to meet the evolving needs of every age. With more than 50,000 employees worldwide, the company contributes to sustainable society by providing solutions to the world’s challenges through its three business sectors of Healthcare, Homes, and Material. For more information, visit www.asahi-kasei.com. Asahi Kasei is also dedicated to sustainability initiatives and is contributing to reaching a carbon neutral society by 2050. To learn more, visit https://www.asahi-kasei.com/sustainability/. References Kidney Disease: Improving Global Outcomes (KDIGO). KDIGO 2025 Clinical Practice Guideline for the Management of Immunoglobulin A Nephropathy (IgAN) and Immunoglobulin A Vasculitis (IgAV). Kidney Int. 2025 Oct;108(4S):S1-S71. Lafayette R, et al. Lancet . 2023;402(10405):859-870. TARPEYO. Prescribing information. Calliditas Therapeutics AB; 2024. Khan, I, et al. #2642 Effects of Nefecon on hits 1, 2, and 3 of the pathogenic cascade of IgA nephropathy: a full NefIgArd analysis. Nephrol Dial Tranplant . 2025 Oct 21; 40 (Supplement 3): Presented at ERA 2025, Vienna, Austria.

Phase 3Clinical ResultDrug Approval

27 Oct 2025

·www.globenewswire.com

Amneal Launches Brekiya® – the First and Only DHE Autoinjector for Adults with Migraine With or Without Aura and Cluster Headaches

Brekiya® autoinjector, a new specialty therapy from Amneal, is now available for prescription exclusively through Walgreens Specialty Pharmacy and Sterling Specialty Pharmacy BRIDGEWATER, N.J., Oct. 27, 2025 (GLOBE NEWSWIRE) -- Amneal Pharmaceuticals, Inc. (Nasdaq: AMRX) (“Amneal” or the “Company”) today announced the U.S. commercial launch of Brekiya® (dihydroergotamine mesylate) injection, the first and only ready-to-use dihydroergotamine (DHE) autoinjector approved for the acute treatment of migraine with or without aura and the acute treatment of cluster headaches in adults.1,2 The Brekiya autoinjector is now available by prescription exclusively through Walgreens Specialty Pharmacy and Sterling Specialty Pharmacy. “We are excited to introduce Brekiya autoinjector, making this innovative therapy broadly available to healthcare providers and patients. As the first and only self-administered, ready-to-use DHE autoinjector, Brekiya offers patients the ability to treat debilitating attacks in a convenient way and avoid visits to the emergency room. With our expanding neurology portfolio, Amneal is committed to supporting providers through comprehensive education and ensuring strong patient access as we bring Brekiya autoinjector to market,” said Joe Renda, Senior Vice President, Chief Commercial Officer – Specialty. Migraine affects approximately 43 million Americans3, and about 300,000 live with cluster headache.4 Headache disorders are also the fourth most common reason for U.S. emergency department visits, accounting nearly for 3% of cases.5 There are limited treatment options available for cluster headache, and Brekiya autoinjector represents a new treatment option for this underserved population.2 Information for Physicians and Patients: Brekiya is available only through prescription.Eligible commercially insured patients may pay as little as $40 per carton (4 single-dose autoinjectors per carton), applied automatically through the specialty pharmacy.To support healthcare providers, field reimbursement specialists will be available to assist with patient access, coverage and reimbursement questions. Do not take Brekiya with strong CYP3A4 inhibitors including protease inhibitors and macrolide antibiotics. See additional Important Safety Information below. IndicationBrekiya is a prescription medicine used for the acute treatment of migraine with or without aura and acute cluster headaches in adults. Brekiya is not used to prevent migraine or used to treat other types of headaches such as hemiplegic migraines (that make you unable to move on one side of your body) or basilar migraines (rare form of migraine with aura). It is not known if Brekiya is safe and effective in children. IMPORTANT SAFETY INFORMATIONBOXED WARNING: WARNING: PERIPHERAL ISCHEMIA FOLLOWING COADMINISTRATION WITH STRONG CYP3A4 INHIBITORSSerious or potentially life-threatening reductions in blood flow to the brain or extremities due to interactions between dihydroergotamine (the active ingredient in Brekiya) with strong CYP3A4 inhibitors (such as protease inhibitors and macrolide antibiotics) have been reported rarely. As a result, these medications should not be taken together. Do not use Brekiya if you: are taking medicines known as strong CYP3A4 inhibitors, such as: ritonavir, nelfinavir, indinavir, erythromycin, clarithromycin, ketoconazole, or itraconazole.have heart problems or a history of heart problems, or uncontrolled high blood pressure.have narrowing of blood vessels in your legs, arms, stomach, or kidneys (peripheral vascular disease).have sepsis, had vascular surgery, severe liver or kidney problems.are allergic to dihydroergotamine, ergot alkaloids, latex, or any of the ingredients in Brekiya.have taken any of the following medicines in the last 24 hours, before intended administration: sumatriptan, frovatriptan, ergotamine or ergotamine-type medicines, almotriptan, naratriptan, zolmitriptan, eletriptan, or rizatriptan.have taken any medicines that constrict your blood vessels or raise your blood pressure. Before you take Brekiya, tell your healthcare provider about all your medical conditions, including if you: have high blood pressure, liver problems, or kidney problems.have risk factors for heart disease, such as: high blood pressure, high cholesterol levels, smoke, are overweight, diabetes, family history of heart disease.are pregnant or plan to become pregnant. Brekiya may cause preterm labor. Brekiya should be avoided during pregnancy. Talk to your healthcare provider right away if you are pregnant or want to become pregnant.are breastfeeding or plan to breastfeed. Brekiya may reduce breast milk supply and pass into your breast milk. Brekiya may be harmful to your baby. Do not breastfeed your baby while taking Brekiya and for 3 days after you use Brekiya. Talk with your healthcare provider about the best way to feed your baby if you take Brekiya. Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements. Especially tell your healthcare provider if you take: sumatriptan, ergot-type medicine, saquinavir, nefazodone, fluconazole, grapefruit juice, zileuton, nicotine, propranolol or other medicines that can lower your heart rate, any medicines that can increase your blood pressure, selective serotonin reuptake inhibitors. These are not all of the medicines that could affect how Brekiya works. Your healthcare provider can tell you if it is safe to take Brekiya with other medicines. How should I use Brekiya autoinjector? Certain people should take their first dose of Brekiya autoinjector in their healthcare provider’s office or in another medical setting.Brekiya is for injection under the skin (subcutaneous) only.Use Brekiya exactly as your healthcare provider tells you to use it.Each autoinjector contains one dose (1 mg).If your headache comes back after the first complete dose, you may give yourself up to 2 more doses as needed. Wait at least one hour between doses.Do not inject more than 3 doses (3 mg) of Brekiya autoinjector in a 24-hour period or 6 doses (6 mg) in a 1-week (7 day) period.Using BREKIYA for 10 or more days in 1 month may make your headache worse. What are the possible side effects of Brekiya?Brekiya can cause serious side effects, including: Heart attack and other heart problems. Heart problems may lead to death. Stop taking Brekiya and get emergency medical help right away if you have any symptoms of a heart attack, such as: numbness or tingling in your fingers and toes, muscle pain or cramps in your arms and legs, weakness in your legs, temporary speeding or slowing of your heart rate, or swelling or itching. Brekiya is not for people with risk factors for heart disease unless a heart exam is done and shows no problem.Stroke. Stop using Brekiya autoinjector and get emergency medical help right away if you have any of the symptoms of a stroke, such as face drooping, slurred speech and unusual weakness.Changes in color or sensation in your fingers and toes (Raynaud’s syndrome).Stomach and intestinal problems.Increased blood pressure.Medicine overuse headache. Some people who use too much Brekiya may make their headaches worse. If your headaches get worse, your healthcare provider may decide to stop your treatment with Brekiya.Preterm labor.Tissue changes (fibrotic complications). Inflammation and fiber-like tissue that is not normal (fibrosis) can occur around the lungs and stomach.The most common but serious side effects of Brekiya are heart problems that happen but may lead to death. These heart problems include: temporary squeezing of arteries that supply the heart (coronary artery vasospasm)temporary decrease of blood flow to the heart (transient myocardial ischemia)heart rhythm problems (ventricular tachycardia and ventricular fibrillation). Tell your healthcare provider if you have any side effect that bothers you or that does not go away. These are not all of the possible side effects of Brekiya. Call your healthcare provider for medical advice about side effects. How should I store Brekiya? Store at room temperature between 68°F to 77°F (20°C to 25°C). Do not refrigerate or freeze.Protect Brekiya from light.Keep Brekiya in the original pack until ready to use. To report SUSPECTED ADVERSE REACTIONS, contact Amneal Specialty, a division of Amneal Pharmaceuticals LLC at 1-877-835-5472, or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. Please see full Prescribing Information, including Boxed Warning, Medication Guide, and Instructions for Use at Brekiya.com. References: Brekiya package insert. Bridgewater, NJ: Amneal Pharmaceuticals LLC; 2025.Data on File. Amneal Pharmaceuticals LLC.Cohen F, et al. Headache. 2024;64(5):516-532.Fischera M et al. Cephalalgia. 2008;28(6)614-618.Phelan, M, Thompson NR, Zubair A et al. Emergency department utilization among patients who receive outpatient specialty care for headache: A retrospective cohort study analysis. Headache. 2023;63:472–483. Note: Brekiya is a registered trademark of Amneal Pharmaceuticals LLC. About AmnealAmneal Pharmaceuticals, Inc. (Nasdaq: AMRX), headquartered in Bridgewater, NJ, is a global biopharmaceutical company. We make healthy possible through the development, manufacturing, and distribution of a diverse portfolio of over 280 pharmaceuticals, primarily within the United States. In its Affordable Medicines segment, the Company is expanding across a broad range of complex product categories and therapeutic areas, including injectables and biosimilars. In its Specialty segment, Amneal has a growing portfolio of branded pharmaceuticals focused primarily on central nervous system and endocrine disorders. Through its AvKARE segment, the Company is a distributor of pharmaceuticals and other products for the U.S. federal government, retail, and institutional markets. For more information, please visit www.amneal.com and follow us on LinkedIn. Cautionary Statement on Forward-Looking StatementsCertain statements contained herein, regarding matters that are not historical facts, may be forward-looking statements (as defined in the U.S. Private Securities Litigation Reform Act of 1995). Such forward-looking statements include statements regarding management’s intentions, plans, beliefs, expectations, financial results, or forecasts for the future, including among other things: discussions of future operations; expected or estimated operating results and financial performance; and statements regarding our positioning, including our ability to drive sustainable long-term growth, and other non-historical statements. Words such as “plans,” “expects,” “will,” “anticipates,” “estimates,” and similar words, or the negatives thereof, are intended to identify estimates and forward-looking statements. The forward-looking statements contained herein are also subject generally to other risks and uncertainties that are described from time to time in the Company’s filings with the Securities and Exchange Commission, including under Item 1A, “Risk Factors” in the Company’s most recent Annual Report on Form 10-K and in its subsequent reports on Forms 10-Q and 8-K. Forward-looking statements included herein speak only as of the date hereof and we undertake no obligation to revise or update such statements to reflect the occurrence of events or circumstances after the date hereof. Investor ContactAnthony DiMeoVP, Investor Relationsanthony.dimeo@amneal.comMedia ContactBrandon SkopSr. Director, Corporate Communicationsbrandon.skop@amneal.com

Drug Approval

100 Deals associated with Saquinavir Mesylate

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KEGG	Wiki	ATC	Drug Bank
D01160	Saquinavir Mesylate	J05AE01	DB01232

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
HIV Infections	United States	Hoffmann-La Roche, Inc.	06 Dec 1995

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
AIDS-Associated Nephropathy	Phase 3	United States	Hoffmann-La Roche, Inc.	31 Aug 2001
Nephrotoxicity	Phase 2	Thailand	Roche Pharma AG	01 May 2004
AIDS-Related Opportunistic Infections	Phase 2	United States	Abbott Laboratories	01 Aug 2002
AIDS-Related Opportunistic Infections	Phase 2	Canada	Abbott Laboratories	01 Aug 2002

Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT00623597 (CTgov)	Phase 2	HIV Infections	18	NNRTI+saquinavir+ritonavir (Group A)	fsbkjkuokk(frszsepshu) = xquuokgaws soqjlvbrxh (auajakxrvv, 536) View more	-	14 Jan 2016
NCT00623597 (CTgov)	Phase 2	HIV Infections	18	NNRTI+saquinavir+ritonavir (Group B)	fsbkjkuokk(frszsepshu) = ctiwcyzahp soqjlvbrxh (auajakxrvv, 1060) View more	-	14 Jan 2016
NCT00435929 (CTgov)	Phase 1	HIV Infections	16	saquinavir (SQV)+ritonavir (RTV) (Normal Liver Function)	blqppxmzjw(hlczydxfvw) = pfiitraeol jhymdelyly (goodtcauvd, 20157) View more	-	08 Jan 2016
NCT00435929 (CTgov)	Phase 1	HIV Infections	16	SQV+RTV (Moderate Hepatic Impairment)	blqppxmzjw(hlczydxfvw) = isrrdxfsdq jhymdelyly (goodtcauvd, 24700) View more	-	08 Jan 2016
NCT00105079 (CTgov)	Phase 3	HIV Infections	337	saquinavir [Invirase]+Emtricitabine/tenofovir disoproxil fumarate+Ritonavir (Saquinavir/Ritonavir)	iebjtxlmll = qsswsqpmuj gvzwnrtmux (mucsuqrmpd, speuqnurdb - knwlrfeqif) View more	-	02 Nov 2011
NCT00105079 (CTgov)	Phase 3	HIV Infections	337	Emtricitabine/tenofovir disoproxil fumarate+Lopinavir/ritonavir (Lopinavir/Ritonavir)	iebjtxlmll = midbjgxarm gvzwnrtmux (mucsuqrmpd, nxvechzmmr - nmynikhuip) View more	-	02 Nov 2011
NCT00476359 (Pubmed \| Antivir Ther)	Phase 4	-	50	Saquinavir and lopinavir/ritonavir	hijhsoxcac(vfmuurkhnf) = alrjeznbit thonszxebl (qkqapsakqf ) View more	-	01 Jan 2009
NCT00084058 (Pubmed \| Antimicrob Agents Chemother)	Phase 1/2	HIV Infections	26	High-dose lopinavir-ritonavir without saquinavir or nonnucleoside reverse transcriptase inhibitors	ylfcafvdab(cnqqzrnrmd) = sydnjjyjyu cmwbdethmc (xgzubmzxpf ) View more	-	01 Sep 2008
NCT00084058 (Pubmed \| Antimicrob Agents Chemother)	Phase 1/2	HIV Infections	26	High-dose lopinavir-ritonavir with saquinavir or nonnucleoside reverse transcriptase inhibitors	nxwigmyaug(ovolkpysns) = dvsagdscif gjxrwloyzc (wrfmuazfac )	-	01 Sep 2008
Pubmed \| Pediatr Infect Dis J	Phase 4	-	50	Double boosted protease inhibitors (saquinavir and lopinavir/ritonavir)	hkuoklrisa(xqdbqfyrhe) = bfytmzksbp obpqdpvmio (gbhuuggmdy ) View more	-	01 Jul 2008
IAS2007	Not Applicable	-	24	Atazanavir/Saquinavir/Ritonavir	zgqufnfnud(ghwymemubp) = wbkrbvhztn heteilufvm (ipseikngbn )	-	01 Jan 2007
IAS2006	Not Applicable	-	66	Boosted saquinavir (SQV/r) 200mg capsules	mvliwspfsg(ukaiwmsmps) = stenmvyotp nfhbiyfhsz (owputmawdb ) View more	-	01 Jan 2006
IAS2006	Not Applicable	-	50	Double boosted SQV/LPV/r	xzfleoabgu(gsihgherxq) = kbhslzwhrf ucdlgyhjdn (gzksawzlmu ) View more	-	01 Jan 2006
IAS2004	Not Applicable	-	12	Switching from non PI-containing regimen to saquinavir (SQV) and lopinavir (LPV)	gkujtbjwya(bhvfhtktus) = uybnnlxjmq ufahhrvenc (jkwouhvsui ) View more	-	01 Jan 2004

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