amprenavir / Generic mfg. - LARVOL DELTA

Amprenavir Protects Lung Epithelial Cells From Pepsin Induced Inflammation and Fibrotic Changes. (PubMed, Laryngoscope) - "Pepsin elicited dose- and time-dependent proinflammatory and fibrotic effects in airway epithelial cells in vitro, which were prevented by amprenavir. This supports the capacity of amprenavir to mitigate airway damage caused by chronic reflux-related microaspiration and highlights its potential therapeutic utility for progressive fibrotic lung diseases."

Journal • Fibrosis • Gastroenterology • Gastroesophageal Reflux Disease • Human Immunodeficiency Virus • Idiopathic Pulmonary Fibrosis • Immunology • Infectious Disease • Inflammation • Interstitial Lung Disease • Pulmonary Disease • Respiratory Diseases • CDH1 • CTNNB1 • CXCL8 • VIM

Amprenavir Protects Human Airway Cells from Pepsin Induced Inflammation and Early Epithelial Mesenchymal Transition (COSM 2026) - "Pepsin elicits dose and time dependent effects in airway epithelial cells. Low-dose pepsin rapidly induces IL-8 mediated inflammation, whereas high-dose exposure does not increase IL-8 but may trigger alternative stress pathways, such as apoptosis, leading to epithelial injury and early EMT. Amprenavir prevents both inflammatory and epithelial-disruptive responses, highlighting its potential as a therapeutic agent to mitigate aspiration-related airway damage."

Human Immunodeficiency Virus • Infectious Disease • Inflammation • Pulmonary Disease • Respiratory Diseases • CDH1 • CXCL8 • VIM

Modulation of Pepsin-Mediated Inflammatory Responses in Vocal Cord Epithelial Cells by Amprenavir. (PubMed, Laryngoscope) - "Pepsin exposure increased HIF-2α and upregulated key inflammatory genes. While amprenavir significantly reduced cytokine expression, HIF-2α inhibition alone had only a modest effect, suggesting additional pathways contribute to pepsin-induced inflammation. Amprenavir's ability to attenuate this response supports its therapeutic potential in LPR."

Journal • Inflammation • CXCL8 • EPAS1 • ICAM1 • IL1B

Drug Repurposing: Conversion of the Peripherally Restricted HIV Protease Inhibitor Amprenavir to Potent, Selective, and CNS-Penetrant Agonists for the Cannabinoid Receptor 2. (PubMed, J Med Chem) - "Selected compounds were profiled in rat i.v. dosing cassettes; several novel amprenavir analogues displayed good t1/2 (>2 h), moderate plasma clearance, and appreciable brain exposure. Additionally, fully flexible protein-ligand docking studies with molecular dynamics (MD) simulations were used to predict the most likely mode of interaction of highly potent analogue VU6077967 with CB2 and to provide a rationale for the observed selectivity of this series relative to CB1."

Journal • Human Immunodeficiency Virus • Infectious Disease

Insights into Transport Function of the Murine Organic Anion-Transporting Polypeptide OATP1B2 by Comparison with Its Rat and Human Orthologues. (PubMed, Toxics) - "Cyclosporine A, ritonavir, odevixibat, rosuvastatin, and rifampicin markedly inhibited uptake...A comparison of the rodent data with the human orthologues revealed similar inhibition patterns but distinct substrate selectivity: hOATP1B1 showed high affinity for E1S but negligible TCA uptake, while hOATP1B3 transported TCA weakly but not E1S. This study provides insights into species-specific differences in OATP-mediated hepatic uptake and is therefore valuable for the interpretation of preclinical studies and their transfer to human pharmacology."

Journal • Preclinical

Classifying Effluxable Versus Non-Effluxable Compounds Using a Permeability Threshold Based on Fundamental Energy Constraints. (PubMed, Pharmaceutics) - "Concentration-dependent measurements for Amprenavir, Eletriptan, Loperamide, and Quinidine-chosen because these borderline compounds exhibited the highest Pm×Cext while still being actively effluxed-enabled the most accurate determination of the threshold. In contrast, more than 60% of the compounds analyzed without significant ER values (123 compounds) fell above the threshold, in strong agreement with our theory of an energy limitation to active transport. This permeability threshold thus provides a simple and broadly applicable criterion to identify compounds for which active efflux is energetically not feasible and may serve as a practical tool for early drug discovery and optimization, pending further validation in practical applications."

Journal • ABCB1

Structure-based drug design; Computational strategies in drug discovery; Antihypertensive agents; Antiviral drugs; Molecular docking; QSAR; Pharmacological insights. (PubMed, Comput Biol Chem) - "This review meticulously examines the development, design, and pharmacological assessment of both well known antiviral and antihypertensive medications all time employing new chemical techniques and structure-based drug design to design and synthesize vital therapeutic entities such as aliskiren (renin inhibitor), captopril (a2-ACE-Inhibitor), dorzolamide (inhibitor of carbonic anhydrase) the review demonstrates initial steps regarding the significance of stereoselective synthesis, metal chelating pharmacophores, and rational molecular properties. More importantly, protease inhibitors (i.e., saquinavir, ritonavir, indinavir, amprenavir, etc.) and more contemporary agents (i.e., oseltamivir, nirmatrelvir/ritonavir (Paxlovid), etc.) were identified in the review and form a basis of advancement in antiviral therapy...In conclusion, this review highlights the transformative power of interdisciplinary approaches, including structure-based design, computational modeling, and..."

Journal • Review • Cardiovascular • Infectious Disease

Herbal formulations, Product Nkabinde and Gnidia sericocephala, exhibit potent in vitro activity against HIV-1 infection. (PubMed, Front Pharmacol) - "TZM-bl cells were treated with PN and G. sericocephala extracts, alone or combined with antiretrovirals (AZT, raltegravir, maraviroc, amprenavir), then infected with the viruses. Fractional inhibitory concentration index (FICI) analysis indicated no synergistic or antagonistic interactions. Thus, this current data suggests that PN and G. sericocephala possess anti-HIV-1 activity."

Journal • Preclinical • Human Immunodeficiency Virus • Infectious Disease

Amprenavir Mitigates Pepsin-Induced Transcriptomic Changes in Normal and Precancerous Esophageal Cells. (PubMed, Int J Mol Sci) - "Pepsin drives transcriptomic dysregulation in esophageal epithelial cells under non-acidic conditions, and amprenavir shows potential to counteract peptic injury. Further studies are needed to validate these findings and explore amprenavir's therapeutic utility in GERD management and EAC prevention."

Journal • Barrett Esophagus • Esophageal Adenocarcinoma • Esophageal Cancer • Gastric Cancer • Gastroenterology • Gastroesophageal Cancer • Gastroesophageal Reflux Disease • Gastrointestinal Disorder • Oncology • Solid Tumor

Engineered Virus-like Particles with Minimal Viral Components for Improved Base Editing Efficiency in vivo (ASGCT 2025) - "The introduction of Amprenavir, an HIV protease inhibitor, during Gag-Pro particle production resulted in up to a 5-fold increase in particle Cas9 content relative to untreated Gag-Pro controls and a dramatic increase in editing efficiency of HEK293T cells...The increased production efficiency and cargo loading/release resulting from the design and process changes described above, in addition to the improved safety profile, enable exploration of the full potential of DLVR-X as a therapeutic protein delivery platform. Disease Focus of Abstract:None"

Preclinical • Hematological Malignancies • Human Immunodeficiency Virus • Infectious Disease • Leukemia • Oncology

Insights into the interaction mechanism of first-generation HIV-1 protease inhibitors with wild-type and mutant (D30N and L76V) enzymes through in-silico based approach. (PubMed, J Biomol Struct Dyn) - "The present study focuses on to understand the alterations in wild-type and mutants (D30N and L76V) PR structure by interaction of first-generation PR inhibitors amprenavir, indinavir, nelfinavir, ritonavir and saquinavir. L76V mutant does not form any direct interaction with the first line drugs; hence the drugs forming strong interactions with the active site, flap domain and substrate binding region residues are quite enough to manage the resistance provided by L76V mutant. The results provided the insight into the drug-resistant or drug-susceptibility mechanism of L76V and D30N mutation against first-generation PR inhibitors."

Journal • Human Immunodeficiency Virus • Infectious Disease

Ritonavir enhances the efficacy of amprenavir: a promising combination therapy by targeting Leishmania DNA Topoisomerase I for treatment of visceral leishmaniasis HIV-VL co-infection. (PubMed, Exp Parasitol) - "From the in vitro, ex vivo and in vivo studies, it was indicated that lower dose of APV in lower dose in combination with RTV elevated the effective killing of the parasites as compared to the single higher dose of APV. Thus, the current study highlights repurposing of available protease inhibitors in combination, which might be exploited further for the therapeutic development against VL as well as HIV-VL co-infection."

Journal • Human Immunodeficiency Virus • Infectious Disease • TOP1

PRIMARY HUMAN ORAL EPITHELIUM TREATED WITH ANTI-HIV PROTEASE INHIBITOR IDENTIFIES HOST GENES AND SIGNALING PATHWAYS THAT FAVOR HPV16 INFECTION AND DE NOVO VIRION BIOSYNTHESIS (IPVC 2024) - " In the current study, we performed microarray analysis to determine expression of host genes and pathways that are differentially modulated by Amprenavir treatment that potentially support HPV16 infection and viral life cycle. Amprenavir treatment of primary gingiva rafts showed upregulated gene expression profiles associated with mitochondrial metabolism and oxidative stress that link with pathways known to regulate HPV functions... Changes in subsequent viral load could promote new infections, increase virus persistence, and the risk of developing oral cancers in HIV-positive patients undergoing long-term HAART treatment."

Head and Neck Cancer • Human Immunodeficiency Virus • Human Papillomavirus Infection • Infectious Disease • Oncology • Oral Cancer • Solid Tumor • CDK1 • CDK2 • CDKN1A

Regulatory Role of IL6 in Immune-Related Adverse Events during Checkpoint Inhibitor Treatment in Melanoma. (PubMed, Int J Mol Sci) - "Furthermore, we conducted an integrative network and molecular-level analysis, including virtual screening, of drug libraries, such as the Collection of Open Natural Products (COCONUT) and the Zinc15 FDA-approved library, to identify potential IL6 inhibitors. Subsequently, the compound amprenavir was identified as the best molecule that may disrupt essential interactions between IL6 and IL6R, which are responsible for initiating the signaling cascades underlying irAEs in ICI therapies."

Adverse events • Checkpoint inhibition • Journal • Crohn's disease • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammatory Arthritis • Inflammatory Bowel Disease • Melanoma • Oncology • Rheumatoid Arthritis • Rheumatology • Solid Tumor • Ulcerative Colitis • IL6 • IL6R • PD-1 • PD-L1

Identification of steroidal cardenolides from Calotropis procera as novel HIV-1 PR inhibitors: A molecular docking & molecular dynamics simulation study. (PubMed, Indian J Med Res) - "Results We found that all tested cardenolides had higher binding affinities than Amprenavir, indicating their potential as potent HIV-1 PR inhibitors...Interpretation & conclusions These findings suggest that Calotropis procera could potentially be a source of compounds for developing novel HIV-1 PR inhibitors, contributing to the efforts to combat HIV. Further studies and clinical trials are needed to evaluate the safety and efficacy of these compounds as potential drug candidates for the treatment of HIV-1 infection."

Journal • Human Immunodeficiency Virus • Infectious Disease

In Silico Drug Repurposing Endorse Amprenavir, Darunavir and Saquinavir to Target Enzymes of Multidrug Resistant Uropathogenic E. Coli. (PubMed, Indian J Microbiol) - "Combination or sole application of Amprenavir, Darunavir and Saquinavir to MDR-UPEC infections may leads to cure and inhibition of mortality. The online version contains supplementary material available at 10.1007/s12088-024-01282-x."

Journal • Human Immunodeficiency Virus • Infectious Disease

Development and validation of an LC-MSMS method for the quantitation of pacritinib; application of kinetics in rabbits. (PubMed, J Pharmacol Toxicol Methods) - "After oral administration of Pacritinib to healthy rabbits, pharmacokinetic characteristics were presented, and the established technique was effectively verified."

Journal • Preclinical • Myelofibrosis

Anti-HIV Activity and Immunomodulatory Properties of Fractionated Crude Extracts of Alternaria alternata. (PubMed, Microorganisms) - "These included maraviroc, azidothymidine, raltegravir, and amprenavir. A. alternata could be a key source of innovative anti-HIV drugs with immunomodulatory characteristics."

Immunomodulating • IO biomarker • Journal • Human Immunodeficiency Virus • Infectious Disease • Targeted Protein Degradation • CD4 • PD-1

Molecular modeling of some commercially available antiviral drugs and their derivatives against SARS-CoV-2 infection. (PubMed, Narra J) - "In parallel, antiviral compounds like abacavir, acyclovir, adefovir, amantadine, amprenavir, darunavir, didanosine, oseltamivir, penciclovir, and tenofovir are under investigation for their potential in drug repurposing to address this infection. Moreover, NCH3 derivative of abacavir (-6.506 kJ/mol), NO2 derivative of didanosine (-6.877 kJ/mol), NCH3 derivative of darunavir (-7.618 kJ/mol) exerted promising affinity to Mpro. In conclusion, the results of the in silico screenings can serve as a useful information for future experimental works."

Journal • Infectious Disease • Novel Coronavirus Disease • Respiratory Diseases

Molecular Docking Improved With Human Spatial Perception Using Virtual Reality. (PubMed, IEEE Trans Vis Comput Graph) - "We also explain the benefits of using VR as a tool for expediting the process of ligand binding, outlining an experimental protocol that enables iMD-VR users to guide Amprenavir into and out of the binding pockets of HIV-1 protease and recreate their respective crystallographic binding poses within 5 minutes...Finally, we describe the novelty of the research and discuss results showcasing a faster and more effective convergence of the ligand to the protein's binding site as compared to a standard molecular dynamics simulation, proving the effectiveness of VR in the field of drug discovery. Future work includes the development of an artificial intelligence algorithm capable of predicting optimal binding trajectories for many protein-ligand pairs, as well as the required force needed to steer the ligand to follow the said trajectory."

Journal • Human Immunodeficiency Virus • Infectious Disease

Amprenavir inhibits pepsin-mediated laryngeal epithelial disruption and E-cadherin cleavage in vitro. (PubMed, Laryngoscope Investig Otolaryngol) - "Amprenavir, at serum concentrations achievable provided the manufacturer's recommended dose of fosamprenavir for HIV, protects against pepsin-mediated cell dissociation, E-cadherin cleavage, and MMP dysregulation thought to contribute to barrier dysfunction and related symptoms during LPR. Fosamprenavir to amprenavir conversion by laryngeal epithelia, serum and saliva, and relative drug efficacies in an LPR mouse model are under investigation to inform development of inhaled formulations for LPR."

Journal • Preclinical • Chronic Cough • Cough • Gastroesophageal Reflux Disease • Gastrointestinal Disorder • Human Immunodeficiency Virus • Infectious Disease • Oncology • Otorhinolaryngology • Pulmonary Disease • Respiratory Diseases • Targeted Protein Degradation • CDH1 • MMP1

Development of a novel fluorogenic assay method for screening inhibitors of bovine leukemia virus (BLV) protease and identification of mitorubrinic acid as an anti-BLV compound. (PubMed, Biosci Biotechnol Biochem) - "The developed assay method was used to screen a chemical library, and mitorubrinic acid was identified as a BLV protease inhibitor that exhibited stronger inhibitory activity than amprenavir...This study presents the first report of a natural inhibitor of BLV protease-mitorubrinic acid-a potential candidate for the development of anti-BLV drugs. The developed method can be used for high-throughput screening of large-scale chemical libraries."

Journal • Hematological Malignancies • Leukemia • Oncology

The Protease Inhibitor Amprenavir Protects against Pepsin-Induced Esophageal Epithelial Barrier Disruption and Cancer-Associated Changes. (PubMed, Int J Mol Sci) - "Amprenavir, at serum concentrations achievable given the manufacturer-recommended dose of fosamprenavir, protected against pepsin-induced cell dissociation, E-cadherin cleavage, and MMP induction. These results support a potential therapeutic role for amprenavir in GERD recalcitrant to PPI therapy and for preventing GERD-associated neoplastic changes."

Journal • Barrett Esophagus • Esophageal Adenocarcinoma • Esophageal Cancer • Gastroenterology • Gastroesophageal Reflux Disease • Gastrointestinal Cancer • Gastrointestinal Disorder • Human Immunodeficiency Virus • Infectious Disease • Oncology • Solid Tumor • Targeted Protein Degradation • CDH1

Vitamin E TPGS-Based Nanomedicine, Nanotheranostics, and Targeted Drug Delivery: Past, Present, and Future. (PubMed, Pharmaceutics) - "Since then, four drugs with TPGS in their formulation have been approved for sale in the United States and Europe including ibuprofen, tipranavir, amprenavir, and tocophersolan...Docetaxel, paclitaxel, and doxorubicin are examples of poorly bioavailable therapeutic agents; hence, much effort is applied for developing TPGS-based nanomedicine, nanotheranostics, and targeted drug delivery systems to increase circulation time and promote the reticular endothelial escape of these drug delivery systems...However, various randomized or human clinical trials have been underway for TPGS-based drug delivery systems for multiple diseases such as pneumonia, malaria, ocular disease, keratoconus, etc. In this review, we have emphasized in detail the review of the nanotheranostics and targeted drug delivery approaches premised on TPGS. In addition, we have covered various therapeutic systems involving TPGS and its analogs with special references to its patent and clinical trials."

Journal • Review • Infectious Disease • Malaria • Oncology • Ophthalmology • Pneumonia • Respiratory Diseases

Understanding the impact of halogen functional group (Br, Cl, F, OH) in amprenavir ligand of the HIV protease. (PubMed, J Biomol Struct Dyn) - "The present work will reveal an understandable picture about the halogen and hydrogen bond interaction that grip the contact of ligand and amino acids in the hinge region. Overall the Halogen atom (Br, Cl, F) functional groups improved the binding strength of APV in HIV protease; which provide a new novel path for the functional group preference on the ligand that enclose perfectly with the amino acid in the hinge region.Communicated by Ramaswamy H. Sarma."

Journal • Human Immunodeficiency Virus • Immunology • Infectious Disease