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

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

3,138

Literatures (Medical) associated with Saquinavir Mesylate

12 Jun 2026·ACS Pharmacology & Translational Science

Repurposing FDA-Approved Drugs as Potential Inhibitors of Feline Infectious Peritonitis Virus 3CL ^pro : An Integrated In Silico and In Vitro Study with Synergistic Combination Analysis

Article

Author: Lueangaramkul, Varanya ; Lekcharoensuk, Porntippa ; Semkum, Ploypailin ; Mana, Natjira ; Thangthamniyom, Nattarat ; Theerawatanasirikul, Sirin ; Limprasutr, Vudhiporn

Feline infectious peritonitis (FIP), caused by feline coronavirus (FCoV) remains a critical therapeutic challenge with no universally approved treatments. We employed a drug repurposing strategy targeting the viral main protease (3CL^pro), essential for FCoV replication. Virtual screening of FDA-approved drugs identified 15 candidates, with threesaquinavir (antiretroviral), lumacaftor (CFTR corrector), and gliquidone (antidiabetic)demonstrating notable antiviral activity. Postentry antiviral assays (cytopathic effect reduction, immunoperoxidase staining, RT-qPCR) yielded EC₅₀ values of 0.25-0.48 μM (saquinavir), 30.32-58.49 μM (lumacaftor), and 48.85-51.28 μM (gliquidone). We validated 3CL^pro inhibition using an intracellular dual-luciferase reporter assay designed to simultaneously account for compound cell penetration and metabolic stability. This confirmed specific protease inhibition with IC₅₀ values of 23.70 ± 1.38 μM (saquinavir) and 38.68 ± 1.59 μM (lumacaftor), and 82.52 ± 1.50 μM (gliquidone). Synergy analysis with established anti-FIP agents (GC376, remdesivir, GS-441524, and molnupiravir) using SynergyFinder 3.0 revealed strong synergistic interactions: saquinavir + GC376 (mean ZIP score: 54.59), lumacaftor + GC376 (mean ZIP: 21.44), and gliquidone + remdesivir (mean ZIP: 24.13). Notably, optimal synergistic doses achieved 0.97-2.03 log₁₀ viral suppression using only 20-50% of individual drug EC₅₀ values, concurrently modulating viral-induced cytokine expression (TNF-α, IFN-β, and IL-6) in CRFK cells (p < 0.05). These rational combinations enable substantial dose reduction, offering practical strategies to improve treatment accessibility, reduce costs, and minimize adverse effects. This study establishes a framework for repurposing FDA-approved drugs in FIP therapy and supports translational evaluation of these combination regimens.

01 Jun 2026·BIOORGANIC CHEMISTRY

Repurposing amide-based drugs unveils inhibition mechanisms of plasmodium falciparum Plasmepsin V enzymatic activity for antimalarial therapy

Article

Author: Choudhary, Sinjan ; Singh, Garima ; Lopus, Manu ; Prajapati, Anitadevi K

Understanding how enzymes are inhibited at the molecular level is essential for rational drug design against malaria parasites. Plasmodium falciparum Plasmepsin V (PfPlmV), an aspartic protease essential for exporting parasite proteins into host red blood cells has emerged as potent target for anti-malarial therapy. In this work, we investigated whether three approved amide-based drugs favipiravir, 5-fluorouracil (5-FU), and saquinavir could inhibit catalytic activity of PfPlmV. All three compounds bound to PfPlmV with affinities of ∼10⁴ M^-1, but with distinct binding behaviours. Binding by isothermal titration calorimetry (ITC) showed involvement of both hydrogen bonds and hydrophobic interactions, which stabilized the enzyme-drug complexes. Enzyme kinetics and docking studies demonstrated that the inhibitory effect depends on the degree of catalytic cleft coverage. The results showed that saquinavir interacts with key active-site residues, including the catalytic dyad Asp118 and Asp365, consistent with competitive inhibition having IC₅₀ value of 0.35 ± 0.01 μM and a low Ki value of (0.14 ± 0.02) μM. 5-FU interacts only near Asp118, resulting in mixed-type inhibition with higher IC₅₀ and Ki values. Favipiravir binds at the periphery of the cleft without engaging the catalytic dyad and therefore behaves as a weak, non-inhibitory binder. The insights of interaction-structure-inhibitory activity obtained from this study may guide repurposing strategies to develop selective potent inhibitors/antimalarial agents targeting PfPlmV.

06 May 2026·CNS & Neurological Disorders-Drug Targets

Re-Profiling and Re-purposing of FDA-Approved AntiViral Agents Against Neurological Targets of Memory and Cognition: Molecular Docking and Simulation Approach

Article

Author: Faheem, Muhammad ; Khan, Yousaf ; Costa, Renato Araújo da ; Khan, Salma Saeed ; Naeem, Mujeeb Ul

Background::

Dementia is a prevalent symptom of Alzheimer’s Disease (AD), associated with either low levels of acetylcholine or destruction by enzymes. Such enzymes are acetylcholinesterase (AChE) and butyryl-cholinesterase (BuChE). The current research worked on re-purposing of 69 Food and Drug Administration Authority (FDA) approved antiviral agents against targets of AD, including AChE (PDB ID: 4BDT) and BuChE (PDB ID: 5LKT).

Methods::

Targets proteins like AChE (PDB ID: 4BDT) and BuChE (PDB ID: 5LKT), and their PDB IDs were retrieved from the Protein Data Bank (PDB), purified through Discovery Studio Visualizer 2016 (DSV-2016), and saved in PDB format. Data of 69 FDA-approved antiviral agents and standard donepezil were obtained from different published literature, and structures were downloaded from the PubChem structure search tool. DSV-2016 was used for the purification of the targets. PyRx was utilized for the docking of 69 test agents and the standard drug donepezil. DSV-2016 was used for post-docking analysis. In addition, Physio-chemical properties, pharmacokinetics, drug-likeness, and medicinal chemistry analysis of three potential compounds (based on binding affinity) and molecular dynamic simulation (MDS) were performed using SWISSADME and AMBER24 software, respectively.

Results::

Docking revealed the binding affinities of Saquinavir (-9.1 kcal.mol-1 ), paritaprevir (-10.8 kcal.mol-1 ), and simeprevir (-10.1 kcal.mol-1 ) with AChE. The recorded binding affinities against BuChE were Saquinavir (-11.7 kcal.mol-1 ), paritaprevir -11.2 kcal.mol-1 ), and simeprevir (-11.4 kcal.mol-1 ). Saquinavir and paritaprevir constructed one hydrogen bond with Threonine (THR38) and Glycine (GLN291), respectively. Simeprevir with Asparagine (ASN283), Valine (VAL282), and Tyrosine (TYR72), granting three hydrogen bonds. The data on lipophilicity was determined in terms of Log Po/w (ILOGP). Water solubility of Saquinavir, Paritaprevir, and Simeprevir demonstrated that the Log S (ESOL) value is much higher, and hence the mentioned three compounds are water insoluble. Saquinavir, paritaprevir, and simeprevir were subjected to molecular dynamics simulations, which showed good interactions of the test agents with BuChE compared to AChE.

Discussion::

The study revealed that already approved 69 FDA anti-viral agents showed potential interaction with the selected targets (AChE and BuChE). Three compounds, saquinavir, paritaprevir, and simeprevir, were found with high binding affinities. As they are utilized in human life for various viral infections with known pharmacology and pharmacokinetics data, we can repurpose such a drug to be active against memory loss or cognitive problems.

Conclusion::

Based on the applied computational techniques on 69 FDA-approved agents, including molecular docking, SWISS-ADME, and MDS, we identified saquinavir, simeprevir, and paritaprevir as potential molecules modulating the action of AChE and BuChE to restore memory and cognition. Hence, it is supposed that these agents may serve as anti-Alzheimer agents

News (Medical) associated with Saquinavir Mesylate

19 May 2026

·www.prnewswire.com

DataXight Launches protoXell to Unlock Mechanistic Insight from Large-Scale Perturbation Data

New scientific software enables researchers to explore chemical and genetic perturbations, accelerating target discovery and drug repurposing MOUNTAIN VIEW, Calif., May 19, 2026 /PRNewswire/ -- Addressing the persistent challenge scientists face in transforming complex biological perturbation data into actionable mechanistic insight, DataXight today announced protoXell, a new scientific software designed to streamline discovery. To learn more about protoXell and explore access options, visit . protoXell enables scientists to move beyond data processing toward biological understanding—allowing them to compare perturbation effects across experiments through an intuitive, point-and-click environment, uncover pathway-level responses, and generate hypotheses for target discovery and drug repurposing. The system supports analyses that are often impractical, even for well-resourced computational teams, due to the scale and complexity of modern perturbation datasets. DataXight will formally introduce protoXell at the Bio-IT World Conference & Expo 2026, May 19–21, 2026, where attendees can experience how the software supports mechanism discovery at scale. "At DataXight, we've spent years helping scientists navigate the complexity of biological data," said Tuan Nguyen, CEO of DataXight. "With protoXell, we are enabling researchers not just to simplify analysis, but to perform analyses that were previously out of reach—helping them move from perturbation data to mechanistic understanding and better therapeutic decisions." Addressing a Critical Bottleneck Advances in single-cell perturbation technologies have generated massive datasets spanning hundreds of millions of cells across thousands of perturbations, but translating these into actionable insight remains challenging. Current approaches require complex pipelines, integration work, and specialized expertise, slowing analysis and limiting exploration. protoXell addresses this gap with an integrated environment for exploring perturbation data. Researchers can compare perturbation effects, understand pathway responses, and generate hypotheses in real time— without pipelines or code. Built-in AI assistance interprets results in biological context, connecting molecular signals to mechanisms and scientific literature. By removing technical barriers, protoXell makes previously difficult analyses accessible, so scientists can focus on discovery, not infrastructure. Key Capabilities Curated Perturbation Catalog – Access analysis-ready datasets spanning 150+ million cells across cell lines, tissues, compounds, and CRISPRi perturbations. Comparative Analytics – Identify shared and distinct biological responses across genes, compounds, and cell types. AI-Powered Interpretation – inXighter translates results into biological meaning, connecting signals to mechanisms and literature. Enterprise Data Integration – Integrate proprietary and public datasets across cloud and on-premise environments. Example Insight protoXell can reveal shared transcriptional responses between compounds with distinct pharmacology—such as similarities observed between the HIV protease inhibitor Saquinavir and β-adrenoceptor agonists—highlighting biological connections that may inform mechanism-of-action studies and drug repurposing. Availability protoXell is available with a free access option, flexible licensing, and enterprise deploymen t across cloud and on-premise environments. Availability on DNAnexus is planned for June 2026. For further details on features and deployment options, please visit . To request access, contact [email protected]. About DataXight DataXight () is an engineering and software company dedicated to transforming biological data into actionable insight, supporting the journey from data generation to discovery. Product Announcement SOURCE DataXight 21% more press release views with Request a Demo

30 Mar 2026

·www.prnewswire.com

Calliditas Therapeutics AB to Present Exploratory Biomarker and Post-Hoc NefIgArd Analyses at the World Congress of Nephrology

Calliditas will present new secondary, biomarker, and mechanistic analyses from the Phase 3 NefIgArd study at the 2026 World Congress of Nephrology. Data further support Nefecon's gut–targeted, disease–modifying mechanism of action in IgA nephropathy. Calliditas to present seven posters and sponsor a scientific symposium highlighting the evolving IgAN treatment paradigm. STOCKHOLM, March 30, 2026 /PRNewswire/ -- Calliditas Therapeutics AB, an Asahi Kasei company, announced today that new data from the Phase 3 NefIgArd study in patients with primary immunoglobulin A nephropathy (IgAN) will be presented at the 2026 World Congress of Nephrology (WCN), taking place from March 28 to 31 in Yokohama, Japan. 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. It is available in Europe where it is marketed as Kinpeygo® by STADA Arzneimittel AG and in select countries in Asia, including Mainland China, Hong Kong, Macau, Taiwan, Singapore, and South Korea by Everest Medicines. It is also the subject of clinical trials in Japan by Viatris Pharamaceticals Japan Inc. The presentations will highlight secondary analyses from the Phase 3 NefIgArd study evaluating Nefecon, its effects on serum biomarkers associated with gut-associated lymphoid tissue (GALT) activity and the immunological impact of orally administered budesonide on B- and T-cell subsets in murine Peyer's patches following in vivo stimulation. These findings reinforce observations from earlier exploratory biomarker analyses and demonstrate the immunomodulatory effects in the Peyer's patches that underlie Nefecon's mechanism of action in modulating the mucosal immune system in the gut. Collectively, these data support a disease-modifying role for Nefecon in reducing levels of pathogenic galactose-deficient IgA1 in patients with IgAN. In total, 7 abstracts, of which 3 are based on secondary clinical efficacy and safety analyses from the Phase 3 NefIgArd study and 2 on mechanistic/biomarker analyses, will be presented. In addition, the initial demographics of the real-world PERFORM registry will be presented. Calliditas will also sponsor a symposium for educational scientific exchange, highlighting the evolving treatment paradigm in IgA nephropathy. Symposium and Presentation details as follows: Company Sponsored Symposium: Title: "The Evolving IgAN Treatment Paradigm: Why Target the Gut?" Date and time: March 30, 12:50 pm to 13:50 pm JST Presenters: Dr. Yusuke Suzuki, Juntendo University, Tokyo, Japan Dr. Sayna Norouzi, Loma Linda University Medical Center, Loma Linda, California, USA Dr. Chee Kay Cheung, University of Leicester, Leicester, UK Poster Presentations: Abstract No. WCN26-AB-8040 Title: "Impact of treatment with Nefecon on serum biomarkers of gut-associated lymphoid tissue function in patients with immunoglobulin A nephropathy from the Phase 3 NefIgArd trial" Date and time: March 30, 17:00 pm – 18:00 pm JST Presenter: Nadia Nawaz, College of Life Sciences, University of Leicester, Leicester, United Kingdom Abstract No. WCN26-AB-8197 Title: "Budesonide Modulates B- and T-Cell Immunity in Peyer's Patches: Implications for IgA Nephropathy" Date and time: March 28, 17:30 pm – 18:30 pm JST Presenter: Roza Ghotbi, Calliditas Therapeutics AB, Stockholm, Sweden Encore Poster Presentations: Title: "Urine protein–creatinine ratio response at 12 months in patients with immunoglobulin A nephropathy receiving Nefecon vs placebo: Analysis of NefIgArd trial data" Date and time: March 28, 17:30 pm – 18:30 pm JST Presenter: Richard Lafayette, Stanford University, CA Title: "Duration of absolute proteinuria response with Nefecon in patients with primary immunoglobulin A nephropathy: Results from the 2-year NefIgArd trial" Date and time: March 30, 17:00 pm – 18:00 pm JST Presenter: Brad Rovin , The Ohio State University Wexner Medical Center Title: "Absolute proteinuria over time with Nefecon vs placebo in patients with immunoglobulin A nephropathy: Results from the Phase 3 NefIgArd trial" Date and time: March 30, 17:00 pm – 18:00 pm JST Presenter: Heather Reich, University of Toronto Title: "The creation and initial demographics of the PERFORM™ Patient Registry: A novel real-world registry of patients treated for IgA nephropathy in the United States" Date and time: March 29, 17:00 pm – 18:00 pm JST Presenter: Russell Jones, Calliditas Therapeutics AB, Stockholm, Sweden 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: March 28, 17:30 pm – 18:30 pm JST Presenter: Daniel Gale , University College London The World Congress of Nephrology (WCN) is the flagship scientific, educational, and networking event of the International Society of Nephrology (ISN). Each year, WCN brings together kidney care professionals from around the world to exchange knowledge, showcase groundbreaking research, and participate in regionally-relevant symposia, training programs, and courses. 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-IgA1), 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-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 late teens and late 30s. 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 Calliditas Therapeutics Calliditas Therapeutics is a biopharma company with offices 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 Kase i Asahi Kasei is a diversified global company that contributes to life and living for people around the world. Since its foundation in 1922, with businesses in ammonia and cellulose fiber, Asahi Kasei has consistently grown through proactive portfolio transformation to meet the evolving needs of every age. With 50,000 employees worldwide, the company contributes to sustainability by providing solutions to the world's challenges across its three business sectors: Healthcare, Homes, and Material. For more information, visit . SOURCE Calliditas Therapeutics 21% more press release views with Request a Demo

Phase 3Drug ApprovalClinical ResultPhase 2

05 Feb 2026

·www.biospace.com

IBSA USA Announces FDA Approval of VYBRIQUE™, the First and Only Oral Film to Treat Men with Erectile Dysfunction

Developed with IBSA’s innovative FilmTec ® technology that dissolves in the mouth without the need for food or water Approved in four dosage strengths (25, 50, 75, 100mg) for a tailored therapy to support the patient’s needs Direct home delivery will be available in all states, providing patients a convenient fulfillment option U.S. Commercial availability anticipated in March 2026 Erectile dysfunction affects 30-50 million men in the US and is becoming more prevalent among men under 40 PARSIPPANY, N.J.--(BUSINESS WIRE)--IBSA USA, the U.S. subsidiary of the Swiss pharmaceutical company IBSA, announced today that the Food and Drug Administration (FDA) has approved VYBRIQUE™, the first sildenafil oral film available to treat men aged 18 years and older with erectile dysfunction. Erectile dysfunction (ED) impacts an estimated 30 to 50 million men in the U.S. and becomes more prevalent with age. However, ED is not limited to older populations; cases among younger men are on the rise 1 . This trend highlights the importance of proactive measures, including healthy lifestyle choices and regular physical activity, to help reduce the risk of developing ED 1 . VYBRIQUE is a discreet, easy-to-use, single-dose film that dissolves on the tongue without the need for water or other liquids, providing an on-the-go use option that may be taken anywhere from 30 minutes to 4 hours before sexual activity. VYBRIQUE can be taken with or without food. “While awareness and open discussion around ED have grown, it’s still a sensitive topic where many men value discretion,” said Nicholas Hart, IBSA USA CEO. “The FDA approval of VYBRIQUE provides men experiencing ED with a novel treatment option that helps meet the evolving needs of patients today.” VYBRIQUE was evaluated in a randomized, double-blind, placebo-controlled, flexible-dose study of 475 adult men with ED. Over the 12-week study, participants received VYBRIQUE at doses of 25 mg, 50 mg, 75 mg and 100 mg. The study’s co-primary efficacy endpoints, assessed at Week 4, demonstrated that VYBRIQUE provided superior improvements in sexual function compared to placebo. Additionally, pharmacokinetic analyses showed that peak plasma concentrations were reached between 30 and 300 minutes (median 80 minutes) under fasting conditions. “Beyond age-related factors, research 2 shows that anxiety, depression, and stress can contribute to ED,” said Dr. Ralph Zagha, MD, Principal Investigator, Precision Clinical Research. “Providing a treatment option that is discreet and easy to administer supports men in managing ED in a way that feels approachable and respectful of their sexual health.” IBSA USA is committed to supporting the millions of men affected by ED through filling the treatment gap. For more information on VYBRIQUE, click here. About VYBRIQUE ™ VYBRIQUE (sildenafil) is the first and only FDA-approved oral film for the treatment of erectile dysfunction in adult men in the US. What is VYBRIQUE? VYBRIQUE (sildenafil) oral film is a prescription medicine used to treat erectile dysfunction (ED). VYBRIQUE is not for use in women or children. It is not known if VYBRIQUE is safe and effective in women or children under 18 years of age. IMPORTANT SAFETY INFORMATION VYBRIQUE can cause your blood pressure to drop suddenly to an unsafe level if it is taken with certain other medicines. Do not take VYBRIQUE if you take medicines called nitrates. A sudden drop in blood pressure can cause you to feel dizzy, faint, or have a heart attack or stroke. Do not take VYBRIQUE if you take medicines called guanylate cyclase stimulators, which include riociguat, a medicine that treats pulmonary arterial hypertension and chronic thromboembolic pulmonary hypertension. Do not take VYBRIQUE if you are allergic to sildenafil or any of the ingredients in VYBRIQUE. Tell all your healthcare providers that you take VYBRIQUE. If you need emergency medical care for a heart problem, it will be important for your healthcare provider to know when you last took VYBRIQUE. Stop sexual activity and get medical help right away if you get symptoms such as chest pain, dizziness, or nausea during sex. Sexual activity can put an extra strain on your heart, especially if your heart is already weak from a heart attack or heart disease. VYBRIQUE does not protect you or your partner from getting sexually transmitted diseases, including Human Immunodeficiency Virus (HIV). VYBRIQUE can cause serious side effects including: an erection that will not go away (priapism). If you have an erection that lasts more than 4 hours, get medical help right away because priapism can permanently damage your penis. sudden vision loss in one or both eyes. Sudden vision loss in one or both eyes can be a sign of a serious eye problem called non-arteritic anterior ischemic optic neuropathy (NAION). Stop taking VYBRIQUE and call your healthcare provider right away if you have sudden vision loss in one or both eyes. sudden hearing decrease or hearing loss. Some people may also have ringing in their ears (tinnitus) or dizziness. If you have these symptoms, stop taking VYBRIQUE and contact a healthcare provider right away. Before you take VYBRIQUE, tell your healthcare provider if you: have or have had heart problems such as a heart attack, irregular heartbeat, angina, chest pain, narrowing of the aortic valve or heart failure have had heart surgery within the last 6 months have pulmonary hypertension have had a stroke have low blood pressure, or high blood pressure that is not controlled have a deformed penis shape have had an erection that lasted for more than 4 hours have problems with your blood cells such as sickle cell anemia, multiple myeloma, or leukemia have retinitis pigmentosa, a rare genetic (runs in families) eye disease have ever had severe vision loss, including NAION have bleeding problems have or have had stomach ulcers have liver problems have kidney problems or are having kidney dialysis Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements. Tell your doctor especially if you take any of the following: nitrates guanylate cyclase stimulators, such as riociguat alpha-blockers, such as doxazosin. The use with VYBRIQUE can lead to a drop in blood pressure or to fainting. HIV protease inhibitors, such as ritonavir and saquinavir oral antifungal medicines, such as ketoconazole and itraconazole antibiotics, such as erythromycin medicines that treat high blood pressure other medicines or treatments for ED The most common side effects of VYBRIQUE are: headache; flushing; upset stomach; stuffy or runny nose; and dizziness. Other side effects include: abnormal vision, such as changes in color vision and blurred vision; back pain; muscle pain; nausea; and rash. These are not all of the possible side effects of VYBRIQUE. Call your doctor for medical advice about side effects. You are encouraged to report negative side effects of prescription drugs to the FDA. Visit , or call 1-800-FDA-1088, or contact IBSA Pharma Inc. at 1-800-587-3513. Please see accompanying Full Prescribing Information and Patient Information. About IBSA IBSA ( Institut Biochimique SA ) is a Swiss pharmaceutical multinational with 20 subsidiaries across Europe, China, and the United States. Its products are available in over 90 countries, and its R&D activities focus on 10 therapeutic areas. In 2025, IBSA celebrated the 40 th anniversary of its acquisition by current President and CEO, Arturo Licenziati, who has transformed the company into a multinational corporation employing over 2,300 personnel worldwide. IBSA’s growth and development can be attributed to its ability to innovate by refining well-known molecules, as well as to its commitment to looking to the future responsibly and transparently, thanks to the dedication and dynamism of its people. References 1 Safa A, Waked C. Erectile Dysfunction in Young Adults: A Narrative Review. Cureus. 2025 Aug 12;17(8):e89918. doi: 10.7759/cureus.89918. PMID: 40809937; PMCID: PMC12349891. 2 National Institute of Diabetes and Digestive and Kidney Diseases. (2024, Last Reviewed October 2024 ). Symptoms & Causes of Erectile Dysfunction . U.S. Department of Health and Human Services, National Institutes of Health. Retrieved from PM-1436-EN-v2 Contacts Andrea Cohen, Sam Brown Healthcare Communications andreacohen@sambrown.com , 917-209-7163

Clinical ResultDrug ApprovalAcquisitionPhase 3

100 Deals associated with Saquinavir Mesylate

External Link

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
Acquired Immunodeficiency Syndrome	Phase 3	Italy	Roche Holding AG	15 Feb 2005
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)	hpfpkrxndu(wdckwyctce) = tqcpprqtmo ogedgwswdu (nimavcjahm, 536) View more	-	14 Jan 2016
NCT00623597 (CTgov)	Phase 2	HIV Infections	18	NNRTI+saquinavir+ritonavir (Group B)	hpfpkrxndu(wdckwyctce) = smeqrvythd ogedgwswdu (nimavcjahm, 1060) View more	-	14 Jan 2016
NCT00435929 (CTgov)	Phase 1	HIV Infections	16	saquinavir (SQV)+ritonavir (RTV) (Normal Liver Function)	lqikhcliix(mdhkmxqhag) = qxmmavwrhh cgovmvwldf (xvigtenhar, 20157) View more	-	08 Jan 2016
NCT00435929 (CTgov)	Phase 1	HIV Infections	16	SQV+RTV (Moderate Hepatic Impairment)	lqikhcliix(mdhkmxqhag) = krpmevdses cgovmvwldf (xvigtenhar, 24700) View more	-	08 Jan 2016
NCT00105079 (CTgov)	Phase 3	HIV Infections	337	saquinavir [Invirase]+Emtricitabine/tenofovir disoproxil fumarate+Ritonavir (Saquinavir/Ritonavir)	cuglmaxgzk = qlakxthqul aegqyaeeqt (nvqrukoqod, nqsvgxqzdb - xotnfsuxzz) View more	-	02 Nov 2011
NCT00105079 (CTgov)	Phase 3	HIV Infections	337	Emtricitabine/tenofovir disoproxil fumarate+Lopinavir/ritonavir (Lopinavir/Ritonavir)	cuglmaxgzk = smaufximms aegqyaeeqt (nvqrukoqod, vlcdccaroe - dyeymntsrz) View more	-	02 Nov 2011
Pubmed \| Antivir Ther	Phase 4	-	50	Saquinavir and lopinavir/ritonavir	khgdvfspaz(vbsyrntwax) = kmrkkygxkh canstvxplr (kmpqlbamzo ) 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	ixuspeamaw(vtwmbgbeml) = memxwvehnc qhymzmppwy (baljmkagmo ) 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	kpdipjmfhl(xmqcbjogwy) = ufrkdnrlaz fbhkztkxfy (ypzfsokygg )	-	01 Sep 2008
Pubmed \| Pediatr Infect Dis J	Phase 4	-	50	Double boosted protease inhibitors (saquinavir and lopinavir/ritonavir)	cmxroihivv(moczholejj) = tzvqzdynfn olnaboabtl (aprcinxjxr ) View more	-	01 Jul 2008
IAS2007	Not Applicable	-	24	Atazanavir/Saquinavir/Ritonavir	hvlnzyeqxt(mvilnjmwwu) = ykmohbpnjl qcecmswcxu (pafyslcsjt )	-	01 Jan 2007
IAS2006	Not Applicable	-	50	Double boosted SQV/LPV/r	qshlvtmzji(iklkdwxftv) = bvrzlvkxud xyqofneyjr (mggfkkpgme ) View more	-	01 Jan 2006
IAS2006	Not Applicable	-	66	Boosted saquinavir (SQV/r) 200mg capsules	xvryguiaoa(qmvpwsjgyw) = cfixznclfv fwvmlnrtcn (yorarjitbn ) View more	-	01 Jan 2006
IAS2004	Not Applicable	-	12	Switching from non PI-containing regimen to saquinavir (SQV) and lopinavir (LPV)	kztasnkewt(seczrzuwmr) = gztpfzdign ecnhenyudx (nttextyfex ) View more	-	01 Jan 2004

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