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.

开始日期2013-12-01

申办/合作机构

中南大学湘雅三医院

[+1]

NCT01638650

/ Completed临床1期

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.

开始日期2012-01-01

申办/合作机构

Hoffmann-La Roche, Inc.

JPRN-UMIN000004621

/ CompletedN/A

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

开始日期2010-11-01

申办/合作机构-

100 项与甲磺酸沙奎那韦相关的临床结果

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100 项与甲磺酸沙奎那韦相关的转化医学

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100 项与甲磺酸沙奎那韦相关的专利（医药）

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项与甲磺酸沙奎那韦相关的文献（医药）

2025-06-01·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

作者: 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.

2025-04-01·BIOORGANIC CHEMISTRY

Molecular simulations guided drugs repurposing to inhibit human GPx1 enzyme for cancer therapy

Article

作者: Irfan, Muhammad ; Al-Ghanim, Khalid A ; Nawaz, Muhammad Zohaib ; Yuan, Qipeng ; Haider, Syed Zeeshan ; Iqbal, Muhammad Waleed ; Sun, Xinxiao

Overexpression of the antioxidant enzyme glutathione peroxidase-1 (GPx1) is associated with different cancer types. Inhibitors of GPx1, including mercaptosuccinic acid and pentathiepins derivatives, have been proposed previously and investigated as potent drugs to combat cancer. However, these compounds often lack specificity and demonstrate off-target effects, which necessitates the need for more targeted, non-toxic, and effective GPx1 inhibitors. This study utilized molecular docking and dynamic simulations based computational pipeline to repurpose drugs, approved by The Food and Drug Administration [1], as potent GPx1 inhibitors from a library containing 1615 synthetic compounds. The drug suitability and stability of the selected compounds were further investigated using ADMET, bioactivity probability, Molecular Mechanics-Generalized Born Surface Area (MM-GBSA), and Molecular Mechanics-Poisson-Boltzmann Surface Area (MM-PBSA) analyses. Initially, 13 compounds were virtually screened based on the Triangle Matcher algorithm, docking modules, and GBVI/WSA dG scoring function. Of these 13 screened compounds, three compounds, including dronedarone, nilotinib, and thonzonium, were rigorously selected based on their ADMET profiles, physicochemical properties, drug suitability, and stability and were subjected to Molecular Dynamic (MD) simulations. MD simulations further validated the stability of the dronedarone, nilotinib, and thonzonium complexes with GPx1 and provided further insights into the mechanism of their interaction. The in-silico approaches used herein revealed thonzonium, dronedarone, and nilotinib as potent GPx1 inhibitors.

2025-03-01·Chemical Biology & Drug Design

The Nature of Nanodisc Lipids Influences Fragment‐Based Drug Discovery Results

Article

作者: Kobayashi, Masakazu ; Ubbink, Marcellus ; van Son, Henri ; Knetsch, Tim G. J.

ABSTRACT:

Membrane proteins (MPs) are important yet challenging targets for drug discovery. MPs can be reconstituted in protein‐lipid Nanodiscs (NDs), which resemble the native membrane environment. Drug‐membrane interactions can affect the apparent binding stoichiometry and affinity, as well as the kinetics of ligands for a particular target, which is important for the extrapolation to pharmacokinetic studies. To investigate the role of the membrane, we have applied fragment‐based drug discovery (FBDD) methods to cytochrome P450 3A4 (CYP3A4), reconstituted in NDs composed of different phosphocholine lipids: 1‐palmitoyl‐2‐oleoyl‐sn‐glycero‐3‐phosphocholine (POPC), 1,2‐dimyristoyl‐sn‐glycero‐3‐phosphocholine (DMPC), dipalmitoylphosphatidylcholine (DPPC), or 1,2‐diphytanoyl‐sn‐glycero‐3‐phosphocholine (DPhPC). Surface plasmon resonance screening of fragments and marketed drugs revealed extensive binding to the empty ND, correlating with analyte hydrophobicity, and the binding was critically dependent on ND lipid composition. POPC NDs showed much higher binding of fragments than DMPC and DPhPC NDs, resulting in a lower hit rate for CYP3A4 in POPC NDs, which demonstrated that the choice of the ND lipid is crucial to the outcome of a screen. The number of binders that were rejected based on atypical binding kinetics was lower for monomeric CYP3A4 in NDs than for non‐native oligomeric CYP3A4 without the ND. Several fragments were exclusively identified as hits for CYP3A4 in the presence of the ND membrane. It is concluded that the nature of the ND is a critical factor for fragment screening of membrane proteins.

项与甲磺酸沙奎那韦相关的新闻（医药）

2025-05-15

·GlobeNewswire-Health Care

Amneal Receives U.S. FDA Approval for Brekiya® (dihydroergotamine mesylate) injection for the Acute Treatment of Migraine and Cluster Headaches in Adults

Brekiya® becomes the first and only DHE autoinjector that allows patients to self-administer the same medication used in hospitals in a ready-to-use form Product will be available for appropriate patients in the second half of 2025 BRIDGEWATER, N.J., May 15, 2025 (GLOBE NEWSWIRE) -- Amneal Pharmaceuticals, Inc. (Nasdaq: AMRX) (“Amneal” or the “Company”) today announced that the U.S. Food and Drug Administration (FDA) has approved Brekiya® (dihydroergotamine mesylate) injection, the first and only dihydroergotamine (DHE) autoinjector for the acute treatment of migraine with or without aura and the acute treatment of cluster headaches in adults.1,2 Brekiya autoinjector provides patients with the potential for sustained* pain relief† in a convenient, self-administered form.1,3,4 It contains the same medication (DHE) used in hospitals, now in a ready-to-use device.1,5 Brekiya autoinjector does not require refrigeration, assembly, or priming of the device.1 Patients can deliver one dose subcutaneously into the middle of the thigh.1 This may be beneficial for patients who respond inadequately to oral therapies due to lack of efficacy, experience nausea or vomiting during attacks, have gastroparesis, or delay dosing until too late into the attack.1,5,6 “We are thrilled to offer the first and only ready-to-use autoinjector for patients suffering from acute migraine and cluster headaches. Physicians are familiar with DHE, which is an effective and well-established therapy that provides sustained relief for headaches. Our single-dose autoinjector represents an innovative therapeutic option for patients that allows for quick self-administration of the medication during these painful attacks without visiting the emergency room,” said Joe Renda, Senior Vice President, Chief Commercial Officer – Specialty. DHE is commonly administered in emergency rooms, urgent care facilities, and headache clinics intravenously. DHE can be used at any point during a migraine attack, and may protect patients from headache recurrence.1,3,4 Approximately 39 million Americans are living with migraine7, and up to one million with cluster headache.8 Also, headache is the fourth most common reason for emergency department visits, and accounts for 3% of all emergency room visits in the United States.9 There are limited treatment options available for cluster headache, and Brekiya autoinjector represents a new treatment option for this underserved population.2 Do not take Brekiya autoinjector with strong CYP3A4 inhibitors including protease inhibitors and macrolide antibiotics. See additional Important Safety Information below. IndicationBrekiya autoinjector is a prescription medicine used for the acute treatment of migraine with or without aura and acute cluster headaches in adults. Brekiya autoinjector 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 autoinjector is safe and effective in children. IMPORTANT SAFETY INFORMATIONSerious or potentially life-threatening reductions in blood flow to the brain or extremities due to interactions between dihydroergotamine (the active ingredient in Brekiya autoinjector) 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 autoinjector 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 autoinjector.have taken any of the following medicines in the last 24 hours: sumatriptan, frovatriptan, ergotamine or ergotamine-type medicines, almotriptan, naratriptan, zolmitriptan, eletriptan, or rizatriptanhave taken any medicines that constrict your blood vessels or raise your blood pressure. Before you take Brekiya autoinjector, 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 autoinjector may cause preterm labor. Brekiya autoinjector 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 autoinjector may reduce breast milk supply and pass into your breast milk. Brekiya autoinjector may be harmful to your baby. Do not breastfeed your baby while taking Brekiya autoinjector and for 3 days after you use Brekiya autoinjector. Talk with your healthcare provider about the best way to feed your baby if you take Brekiya autoinjector. 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 autoinjector works. Your healthcare provider can tell you if it is safe to take Brekiya autoinjector 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 autoinjector is for injection under the skin (subcutaneous) only.Use Brekiya autoinjector 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. What are the possible side effects of Brekiya autoinjector?Brekiya autoinjector can cause serious side effects, including: Heart attack and other heart problems. Heart problems may lead to death. Stop taking Brekiya autoinjector 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 autoinjector 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.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 autoinjector may make their headaches worse. If your headaches get worse, your healthcare provider may decide to stop your treatment with Brekiya autoinjector.Preterm labor.Tissue changes (fibrotic complications). Inflammation and fiber-like tissue that is not normal (fibrosis) can occur around the lungs and stomach. 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 autoinjector. Call your healthcare provider for medical advice about side effects. How should I store Brekiya autoinjector? Store at room temperature between 68°F to 77°F (20°C to 25°C). Do not refrigerate or freeze.Protect Brekiya autoinjector from light.Keep Brekiya autoinjector 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. *Sustained represents a duration of approximately 24-72 hours2,3†Cluster headache results reported using IV administration.4 References: Brekiya [package insert]. Bridgewater, NJ: Amneal Pharmaceuticals LLC; 2025.Data on File. Amneal Pharmaceuticals LLC.Winner P, Ricalde O, Le Force B, Saper J, Margul B. Arch Neurol. 1996;53(2):180-184.Mather PJ, Silberstein SD, Schulman EA, Hopkins MM. Headache. 1991;31(8):525-532.Silberstein SD, Shrewsbury SB, Hoekman J. Headache. 2020;60(1):40-57. doi:10.1111/head.13700Aurora SK, Papapetropoulos S, Kori SH, Kedar A, Abell TL. Cephalalgia. 2013;33(6):408-415.https://migraineresearchfoundation.org/about-migraine/migraine-facts/https://americanmigrainefoundation.org/resource-library/cluster-headache-2/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. 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 Contact Anthony DiMeoVP, Investor Relations anthony.dimeo@amneal.comMedia ContactBrandon SkopSr. Director, Corporate CommunicationsBrandon.skop@amneal.com PP-PRS-DHE-US-0001 05/2025

上市批准

2024-10-16

·GlobeNewswire-Health Care

Calliditas Therapeutics to Present Four Abstracts at American Society of Nephrology (ASN) Kidney Week 2024

STOCKHOLM, Sweden, Oct. 16, 2024 (GLOBE NEWSWIRE) -- Calliditas Therapeutics AB (Nasdaq Stockholm: CALTX) (“Calliditas”), today announced upcoming presence and data presentations at the American Society of Nephrology Kidney Week 2024 in San Diego, California on October 23 – 27, 2024. Presentations will highlight an open-label extension study of the efficacy and safety of Nefecon (TARPEYO® (budesonide) delayed release capsules)) in patients with primary immunoglobulin A nephropathy (IgAN), results from a real-world case series of IgAN patients, and additional insights from biomarker analysis. “We look forward to attending ASN Kidney Week and sharing additional data that reinforce Nefecon as a cornerstone treatment in IgAN,” said Richard Philipson, Chief Medical Officer at Calliditas. "This conference offers a great opportunity to exchange scientific knowledge with leading experts in nephrology and contribute to discussions around innovative treatments, including our potentially disease-modifying option." The oral presentation and poster presentation details are below. Following the meeting, they will be available on the Presentations and Publications page on Calliditas’ corporate website. Oral Presentation Details: Title: “NeflgArd Open-Label Extension: Efficacy and Safety of Nefecon in Patients with IgAN Who Completed the 2-Year Phase 3 Trial”Date and Time: October 25, 2024 from 4:40 PM to 4:50 PM PTLocation: Room 6D, Convention Center Poster Presentation Details: Title: “Results from a real-world case series of IgAN patients who received at least 9 months of Tarpeyo”Date and Time:Location: October 25, 2024 from 10:00 AM to 12:00 PM PT Title: Specificity of Nefecon in Targeting Pathogenic IgA in IgA Nephropathy While Preserving Systemic Humoral ImmunityDate and Time: October 25, 2024 from 10:00 AM to 12:00 PM PT Title: Impact of Nefecon on Complement Pathways in IgA Nephropathy: An Analysis of Lectin, Alternative, and Terminal PathwaysDate and Time: October 25, 2024 from 10:00 AM to 12:00 PM PT For more information, visit booth 1920 or visit the ASN Kidney Week 2024 website here. 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 PRECAUTIONSHypercorticism 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 POPULATIONSPregnancy: 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 TARPEYOTARPEYO is an oral 4mg delayed release formulation of budesonide, designed to remain intact until it reaches the 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 NephropathyPrimary immunoglobulin A nephropathy (IgA nephropathy or IgAN or Berger’s Disease) is a rare, progressive, chronic autoimmune disease that attacks the kidneys and occurs when galactose deficient IgA1 is recognized by autoantibodies, creating IgA1 immune complexes that become deposited in the glomerular mesangium of the kidney. This deposition in the kidney can lead to progressive kidney damage and potentially a clinical course resulting in end- stage renal disease. IgAN most often develops between late teens and late 30s. 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. For further information, please contact:Emma Santosegsantos@lifescicomms.com The information was sent for publication, through the agency of the contact persons set out above, on October 16, 2024, at 14.00 p.m. CET.

临床3期

2024-05-29

·BioSpace

Petros Pharmaceuticals Successfully Completes AI-Integrated Formative Human Factors Study Demonstrating Positive Interaction with Web App Designed for STENDRA(R) (avanafil) OTC Switch

Study paves the way toward a first-ever innovation program to include AI-optimization for FDA-guided Rx-to-OTC switch NEW YORK, NY / ACCESSWIRE / May 29, 2024 / Petros Pharmaceuticals, Inc. (NASDAQ:PTPI) ("Petros" or the "Company"), a company focused on expanding consumer access to medication through over-the-counter ("OTC") drug development programs, announces the successful completion of a Formative Human Factors study of its AI-integrated Web App, designed to facilitate OTC access of STENDRA® (avanafil) for consumers. This important development follows the Company's recent execution of an AI licensing agreement with a leading multi-billion dollar software provider announced earlier this year. The Web App (previously referred to as the "technology component") is an integral part of the Company's efforts to complete an Rx-to-OTC switch for STENDRA® (avanafil) under the guidance of the U.S. Food and Drug Administration. The study demonstrated a 90% or better error-free completion rate for nearly all 5,820 tasks assessed. The successful completion of the study paves the way for the Company to initiate the next stage of the evolving program, while continuing to optimize the AI component of the Web App. "The successful completion of the Human Factors Study and the positive outcomes we've seen to date continue to be encouraging signs of our progress in navigating the Rx-to-OTC switch for STENDRA® (avanafil). As we've previously indicated, we believe we have the potential to be first-in-class for the category with regards to OTC access," stated Fady Boctor, Petros' President and Chief Commercial Officer. "We continue to refine our program based on our regular interactions with the FDA, and the learnings from this study will allow us to continue to optimize the AI component of the Web App. Combined, we strongly believe in our approach and look forward to continuing development into the next indicated step for STENDRA® (avanafil) in a non-prescription setting." The Formative Human Factors study was conducted in a population of 30 consumers, including a cohort with limited literacy. The consumers were provided with five different use scenarios requiring correct demonstration of 194 different tasks using the Web App with no training or guidance. The study also included a proprietary AI interface that confirmed the identity of the consumer, a first-ever innovation for an Rx-to-OTC switch program. About Petros Pharmaceuticals Petros Pharmaceuticals, Inc. is committed to the goal of becoming a leading innovator in the emerging self-care market driving expanded access to key prescription pharmaceuticals as OTC treatment options. Currently, Petros is pursuing increased access for its flagship prescription ED therapy, STENDRA® (avanafil), via potential OTC designation. If ultimately approved by the FDA for OTC access, STENDRA® (avanafil) may be the first in its class to achieve this marketing status, also establishing company know how as a proven platform for other prospective prescription therapeutics. About the OTC Pathway The process of switching a prescription medication to OTC first involves the design of a Drug Facts Label ("DFL") that is well understood by potential consumers. Then, data must show that consumers can make an appropriate informed decision to use or not to use the product based only upon the information on the DFL and their personal medical history. Then consumers must demonstrate that they can properly use the product based upon the information on the DFL. To accomplish this, the FDA ordinarily requires a consumer tested OTC DFL. Such testing includes conduct of iterative Label Comprehension Studies (LCS) in the general population, Self-Selection Studies (SSS) in a population interested in using the product and in specific populations who may be harmed if they use the product, and usually one Actual Use Trial (AUT) demonstrating safe and appropriate use by consumers in a simulated OTC setting. The regulations that FDA is currently finalizing introduced Additional Conditions for Nonprescription Use (ACNU) criteria that enable correct self-selection by consumers and may expand OTC access to medications that formerly could only be available by prescription. An ACNU may be an innovative computerized tool, or the additional conditions may use other approaches that support the switch process. Important Safety Information about STENDRA® (avanafil) STENDRA® (avanafil), originally launched by Auxilium Pharmaceuticals prior to its sale to Endo Pharmaceuticals, is an oral phosphodiesterase 5 (PDE5) inhibitor for the treatment of erectile dysfunction. STENDRA® (avanafil) is not for use in women or children. It is not known if STENDRA® (avanafil) is safe and effective in women or children under 18 years of age. A 100-mg and 200-mg tablet can be taken as early as ~15 minutes before sexual activity. STENDRA® (avanafil) only works with sexual stimulation and should not be taken more than once a day. STENDRA can be taken with or without food; do not drink too much alcohol when taking STENDRA® (avanafil) (for example, more than three glasses of wine or three shots of whiskey) as it can increase chances of side effects. Of people enrolled in clinical trials, 1.4%, 2.0%, and 2.0%, respectively, stopped taking STENDRA® (avanafil) (50 mg, 100 mg, or 200 mg) due to side effects compared to 1.7% taking a placebo. STENDRA® (avanafil) was designed and developed expressly for erectile dysfunction. STENDRA is contraindicated for any form of organic nitrates, in patients with known hypersensitivity to any component of the tablet, and in patients who are using a guanylate cyclase stimulator. Patients should not use STENDRA if sexual activity is inadvisable due to cardiovascular status or any other reason. Before taking STENDRA, tell your doctor if you have had any kind of heart issues including heart attack, heart failure, angina and irregular heartbeat or have elevated or low blood pressure. Use of STENDRA with alpha-blockers, other antihypertensives, or substantial amounts of alcohol (greater than three units) may lead to hypotension. Patients should seek emergency treatment if an erection lasts greater than 4 hours. Patients should stop STENDRA and seek medical care if a sudden loss of vision occurs in one or both eyes, which could be a sign of Non-Arteritic Ischemic Optic Neuropathy ("NAION"). Doctors should discuss with patients the increased risk of NAION in patients with a history of NAION. Patients should stop taking STENDRA and seek prompt medical attention in the event of sudden decrease or loss of hearing. STENDRA can potentiate the hypotensive effect of nitrates, alpha blockers, antihypertensives, and alcohol. CYP3A4 inhibitors (e.g., ketoconazole, ritonavir, erythromycin) increase STENDRA exposure. For patients taking concomitant strong CYP3A4 inhibitors (including ketoconazole, ritonavir, atazanavir, clarithromycin, indinavir, itraconazole, nefazodone, nelfinavir, saquinavir and telithromycin), do not use STENDRA. Combination with Other PDE5 Inhibitors or Erectile Dysfunction Therapies is not recommended. The safety of STENDRA is unknown in patients with bleeding disorders and patients with active peptic ulceration. The use of STENDRA offers no protection against sexually transmitted diseases including HIV. Consider counseling patients on protective measures for sexually transmitted diseases. The most common adverse reactions reported with use of STENDRA include headache, flushing, nasal congestion, nasopharyngitis, and back pain. For more information about STENDRA, call 844-458-4887. If you would like to report an adverse event or product complaint, please contact us at 844-458-4887. You are encouraged to report negative side eﬀects of prescription drugs to the FDA by calling 1-800-FDA-1088, or at . Please see the full Prescribing Information and Patient Information. Cautionary Note Regarding Forward-Looking Statements This press release includes forward-looking statements within the meaning of Section 27A of the Securities Act of 1933, as amended, and Section 21E of the Securities Exchange Act of 1934, as amended. These forward-looking statements are based upon Petros Pharmaceuticals, Inc.'s ("Petros," "we," "our," "us" or the "Company") management's assumptions, expectations, projections, intentions, and beliefs about future events. In some cases, predictive, future-tense or forward-looking words such as "intend," "develop," "goal," "plan," "predict", "may," "will," "project," "estimate," "anticipate," "believe," "expect," "continue," "potential," "opportunity," "forecast," "should," "target," "strategy" and similar expressions, whether in the negative or affirmative, that reflect our current views with respect to future events and operational, economic and financial performance are intended to identify forward-looking statements, but are not the exclusive means of identifying such statements. Such forward-looking statements are only predictions, and actual results and the timing of certain events and circumstances may differ materially from those described by the forward-looking statements as a result of risks and uncertainties, Petros' ability to execute on its business strategy, including its plans to develop and commercialize its product candidates; Petros' ability to comply with obligations as a public reporting company; Petros' ability to maintain compliance with the Nasdaq Stock Market's listing standards; risks related to Petros' ability to continue as a going concern; risks related to Petros' history of incurring significant losses; risks related to Petros' dependence on the commercialization of a single product, STENDRA®; and risks related to Petros' ability to obtain regulatory approvals for, or market acceptance of, any of its products or product candidates. Additional factors that could cause actual results to differ materially from the results anticipated in these forward-looking statements are contained in the Company's periodic reports and in other filings that the Company has or may file, with the U.S. Securities and Exchange Commission (the "SEC") under the headings "Risk Factors" and "Management's Discussion and Analysis of Financial Condition and Results of Operations" and elsewhere. The Company cautions readers that the forward-looking statements included in this press release represent our beliefs, expectations, estimates and assumptions only as of the date of hereof and are not intended to give any assurance as to future results. New factors emerge from time to time, and it is not possible for us to predict all these factors. Further, the Company cannot assess the effect of each such factor on our business or the extent to which any factor, or combination of factors, may cause actual results to be materially different from those contained in any forward-looking statement. Accordingly, you should not unduly rely on any forward-looking statements. The Company undertakes no obligation to update or revise any forward-looking statements contained in this press release, whether as a result of new information, future events, a change in our views or expectations or otherwise, except as required by federal securities laws. Contacts Investors: CORE IR ir@petrospharma.com Media: Jules Abraham CORE IR 917-885-7378 pr@coreir.com SOURCE: Petros Pharmaceuticals, Inc. View the original press release on accesswire.com

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100 项与甲磺酸沙奎那韦相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D01160	甲磺酸沙奎那韦	J05AE01	DB01232

研发状态

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适应症	国家/地区	公司	日期
HIV感染	美国	Hoffmann-La Roche, Inc.	1995-12-06

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适应症	最高研发状态	国家/地区	公司	日期
艾滋病相关性肾病	临床3期	美国	Hoffmann-La Roche, Inc.	2001-08-31
肾脏毒性	临床2期	泰国	Roche Pharma AG	2004-05-01
艾滋病相关机会致病菌感染	临床2期	美国	Abbott Laboratories	2002-08-01
艾滋病相关机会致病菌感染	临床2期	加拿大	Abbott Laboratories	2002-08-01

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT00623597 (CTgov)	临床2期	HIV感染	18	NNRTI+saquinavir+ritonavir (Group A)	築網獵築鹹壓網餘繭窪(網壓壓廠鑰鬱觸鑰壓鏇) = 鹽鑰鹹壓淵簾衊襯壓鏇衊遞鏇夢夢製觸獵鏇蓋 (壓餘鹹觸願蓋鬱餘製構, 536) 更多	-	2016-01-14
				NNRTI+saquinavir+ritonavir (Group B)	築網獵築鹹壓網餘繭窪(網壓壓廠鑰鬱觸鑰壓鏇) = 繭壓鹹範範艱憲願網積衊遞鏇夢夢製觸獵鏇蓋 (壓餘鹹觸願蓋鬱餘製構, 1060) 更多
NCT00435929 (CTgov)	临床1期	HIV感染	16	saquinavir (SQV)+ritonavir (RTV) (Normal Liver Function)	齋壓餘願醖鬱網簾廠觸(簾夢簾範獵遞鏇夢簾膚) = 選壓選廠構繭簾鑰廠顧鏇淵鬱鹹製襯憲夢鏇鏇 (壓糧鏇獵鹽衊蓋壓齋膚, 20157) 更多	-	2016-01-08
				SQV+RTV (Moderate Hepatic Impairment)	齋壓餘願醖鬱網簾廠觸(簾夢簾範獵遞鏇夢簾膚) = 願糧積衊願築鏇願艱觸鏇淵鬱鹹製襯憲夢鏇鏇 (壓糧鏇獵鹽衊蓋壓齋膚, 24700) 更多
AACR2015	N/A	铂耐药性卵巢癌	-	Saquinavir	願鏇鑰選鏇糧範鑰網簾(壓艱鹹淵積廠築獵窪觸) = 鏇構鏇顧壓淵夢夢築鏇鑰遞築糧製衊遞淵遞遞 (遞鏇選鏇衊醖範觸構餘 )	-	2015-08-01
IAS2012	N/A	-	-	Sustained-release saquinavir	壓簾蓋鹽艱餘餘膚鑰鏇(築鑰廠艱艱選鬱製製繭) = 壓鑰鏇醖網襯齋鏇淵鏇鑰鏇製夢簾廠構夢積網 (選構廠鏇餘壓膚構選淵 )	-	2012-01-01
NCT00105079 (CTgov)	临床3期	HIV感染	337	saquinavir [Invirase]+Emtricitabine/tenofovir disoproxil fumarate+Ritonavir (Saquinavir/Ritonavir)	遞鏇蓋製艱觸積艱製糧 = 願鹹鏇築遞襯夢製築餘壓顧顧襯鹽願鬱淵餘顧 (鏇構醖鹽餘簾艱糧廠餘, 夢淵鹽膚糧艱築齋壓鹹 ~ 淵艱膚廠鏇醖遞鏇構鬱) 更多	-	2011-11-02
				Emtricitabine/tenofovir disoproxil fumarate+Lopinavir/ritonavir (Lopinavir/Ritonavir)	遞鏇蓋製艱觸積艱製糧 = 築簾鏇範糧獵築網衊築壓顧顧襯鹽願鬱淵餘顧 (鏇構醖鹽餘簾艱糧廠餘, 鹹淵襯襯夢顧選顧蓋醖 ~ 顧齋願獵齋艱艱繭鬱網) 更多
IAS2010	N/A	HIV感染	-	ritonavir-boosted saquinavir (Group 1)	蓋窪遞繭膚鏇選鬱窪簾(醖餘築顧簾夢窪築遞簾) = 壓觸構鏇鏇簾夢膚鬱壓廠網繭製構鹹廠鬱壓繭 (繭淵齋積鏇淵選齋選願, 70.7) 更多	-	2010-01-01
				ritonavir-boosted saquinavir (Group 2)	蓋窪遞繭膚鏇選鬱窪簾(醖餘築顧簾夢窪築遞簾) = 遞觸壓壓鏇遞窪夢憲餘廠網繭製構鹹廠鬱壓繭 (繭淵齋積鏇淵選齋選願, 101.5) 更多
NCT00476359 (Pubmed \| Antivir Ther)	临床4期	-	50	Saquinavir and lopinavir/ritonavir	願鹹鏇範簾廠餘憲獵衊(餘顧顧糧淵衊獵遞遞醖) = 顧願壓繭範窪窪鏇鏇範艱製淵餘醖襯齋願艱窪 (艱餘選餘範鹹餘鬱齋糧 ) 更多	-	2009-01-01
NCT00084058 (Pubmed \| Antimicrob Agents Chemother)	临床1/2期	HIV感染	26	High-dose lopinavir-ritonavir without saquinavir or nonnucleoside reverse transcriptase inhibitors	選獵廠醖構夢襯夢獵衊(淵艱繭繭顧範鏇築襯製) = 糧鏇醖膚顧製窪鹽衊衊選壓構鹽夢窪窪顧窪獵 (糧簾範襯簾製鬱衊艱衊 ) 更多	-	2008-09-01
				High-dose lopinavir-ritonavir with saquinavir or nonnucleoside reverse transcriptase inhibitors	構艱蓋鬱獵鹽網觸鏇艱(蓋窪憲範構蓋鬱憲鏇築) = 觸壓艱製簾積鬱鹽觸網廠夢壓繭廠鬱鹽繭鏇餘 (窪衊鹹鏇鬱鬱遞夢遞憲 )
NCT00476359 (Pubmed \| Pediatr Infect Dis J)	临床4期	-	50	Double boosted protease inhibitors (saquinavir and lopinavir/ritonavir)	鹽蓋廠簾觸艱襯選淵觸(窪範廠築醖網糧壓鹹壓) = 夢夢壓壓醖積憲膚蓋襯餘觸齋鑰憲鬱選積蓋觸 (鏇衊壓顧鹹襯築構鹽餘 ) 更多	-	2008-07-01
IAS2008	N/A	HIV感染	13	Saquinavir-hgc plus low-dose ritonavir (1000/100 mg BID)	餘夢獵襯膚鹽壓網構範(醖網衊蓋積衊齋餘蓋鹹) = 艱膚築膚製醖簾鹹積淵構鹽顧獵遞醖顧製製顧 (糧範遞廠醖淵醖衊願淵 ) 更多	-	2008-01-01