fosamprenavir / Generic mfg. - LARVOL DELTA

Advances in Laryngopharyngeal Reflux Disease: The Future of Diagnosis and Management (AAO-HNSF 2025) - "Audience response system will be utilized for audience participation. In addition, panelist Q&A will be included to encourage discussion of challenging cases.Learning Objectives: Understand the availability of current diagnostic testing for LPR including hypopharyngeal esophageal pH impedance, salivary pepsin testing, high resolution manometry, esophageal fluoroscopy, and future directions for laryngeal biopsy and salivary biomarkers.Review the data supporting the role of fosamprenavir as an anti-pepsin treatment and its role in management of LPRDemonstrate the benefits of providing an individualized and holistic approach to treating the extra-esophageal symptoms of reflux with the current understanding of LPRD reflux vs reflex pathophysiology"

Chronic Cough • Cough • Dysphonia • Gastroesophageal Reflux Disease • Otorhinolaryngology • Respiratory Diseases • Sinusitis

Oral Fosamprenavir + Sodium Alginate for GERD (clinicaltrials.gov) - P2 | N=60 | Not yet recruiting | Sponsor: Medical College of Wisconsin | Trial completion date: Sep 2027 ➔ Jun 2028 | Initiation date: May 2025 ➔ Mar 2026 | Trial primary completion date: May 2027 ➔ Feb 2028

Trial completion date • Trial initiation date • Trial primary completion date • Gastroenterology • Gastroesophageal Reflux Disease

Bioanalytical method development of nevirapine, fosamprenavir calcium and its metabolite amprenavir by RP-HPLC in rat plasma. (PubMed, J Chromatogr B Analyt Technol Biomed Life Sci) - "The method is reliable and does not show any kind of interference due to the plasma sample. Thus, the results support that a reliable, reproducible, and efficient method was developed, and validation was carried out for the estimation of the drug nevirapine, fosamprenavir, and its metabolite amprenavir in rat plasma samples."

Journal • Preclinical • Human Immunodeficiency Virus • Infectious Disease

Oral Fosamprenavir-Sodium Alginate for LPR (clinicaltrials.gov) - P2 | N=104 | Not yet recruiting | Sponsor: Medical College of Wisconsin | Trial completion date: Apr 2026 ➔ Oct 2027 | Trial primary completion date: Feb 2026 ➔ Jun 2027

Trial completion date • Trial primary completion date

A new RP-HPLC approach for estimation of potential impurities of Fosamprenavir - method development and validation. (PubMed, BMC Pharmacol Toxicol) - "The optimized approach excelled existing methods in lower retention time, run time, sensitivity, and linearity for all potential impurities, making it a novel and trustworthy method for monitoring Fosamprenavir drug quality and assessing stated impurities. The established method allows precise measurement of Fosamprenavir and related substances, supporting drug safety and regulatory compliance."

Journal

Darunavir inhibits dengue virus replication by targeting the hydrophobic pocket of the envelope protein. (PubMed, Biochem Pharmacol) - "This study screened FDA-approved drugs for their antiviral ability against DENV and identified three promising candidates: darunavir (DRV), domperidone, and tetracycline...Among DRV's structurally related drugs, fosamprenavir (FPV) significantly reduced DENV infectivity and virus yield, with EC50 values below 0.5 µM...Chimeric DENV-2 single-round infectious particle tests confirmed DRV's effective targeting of this pocket, though mutations at K128, L198, Q200, I270, and T280 reduced its efficacy. These findings highlight DRV as a potent antiviral agent against DENV, targeting the E protein's βOG hydrophobic pocket, with the potential for rapid deployment in treating and preventing infections."

Journal • Dengue Fever • Infectious Disease

Fosamprenavir and Tirofiban to combat COPD and cancer: A drug repurposing strategy integrating virtual screening, MD simulation, and DFT studies. (PubMed, J Mol Graph Model) - "This study identified fosamprenavir and tirofiban as promising hits that can exhibit potent macrophage metalloelastase inhibition which was also validated by the MD simulation and DFT-based calculations. Therefore, this study not only revealed these repurposed drugs as effective macrophage metalloelastase inhibitors but also opened up a horizon in developing novel potent macrophage metalloelastase inhibitors for the management of cancer and COPD in the future."

Journal • Asthma • Chronic Obstructive Pulmonary Disease • Immunology • Oncology • Pulmonary Disease • Respiratory Diseases

Oral Fosamprenavir + Sodium Alginate for GERD (clinicaltrials.gov) - P2 | N=60 | Not yet recruiting | Sponsor: Medical College of Wisconsin

New P2 trial • Gastroenterology • Gastroesophageal Reflux Disease

Pharmacokinetics of Antiretroviral Drugs in Older People Living with HIV, Part II: Drugs Licensed Before 2005. (PubMed, Clin Pharmacokinet) - "Exposure to 3TC, TDF, FTC, ATV, LPV, and RTV increases with age, while exposure to ABC and EFV appears to be unaffected. Despite the large quantity of data on PK in young adults, there is still a gap in knowledge about the effects of aging on the PK of these ARVs."

Journal • PK/PD data • Review • Human Immunodeficiency Virus • Infectious Disease

Advances in laryngopharyngeal reflux: Etiology, diagnosis, and management. (PubMed, Ann N Y Acad Sci) - "Laryngeal hypersensitivity should be considered as part of a comprehensive therapeutic approach. Promising medical and scientific research continues to yield new insights into the complex etiology of LPR and novel strategies for its diagnosis and management."

Journal • Review • Gastroenterology • Gastroesophageal Reflux Disease • Immunology • Otorhinolaryngology

Pretreatment drug resistance among people living with HIV from 2018 to 2022 in Guangzhou, China. (PubMed, J Med Virol) - "Abacavir (0.8%) resistance was the most common in NRTI, followed by resistance to emtricitabine (0.6%), lamivudine (0.6%), and tenofovir disoproxil fumarate (0.3%). In NNRTI, nevirapine (3.7%) resistance was the most common, followed by efavirenz (3.5%) and rilpivirine (3.4%). Among PI, resistance to tipranavir (0.8%), nelfinavir (0.6%), fosamprenavir (0.2%) and lopinavir (0.1%) was most frequent...The overall prevalence of PDR in Guangzhou was moderate, with relatively severe NNRTI resistance. Therefore, it remains crucial to continue monitoring PDR among newly diagnosed HIV-infected individuals."

Journal • Hepatitis B • Hepatology • Human Immunodeficiency Virus • Infectious Disease • Inflammation

Oral Fosamprenavir-Sodium Alginate for LPR (clinicaltrials.gov) - P2 | N=104 | Not yet recruiting | Sponsor: Medical College of Wisconsin | Phase classification: P3 ➔ P2 | Trial completion date: Oct 2025 ➔ Apr 2026 | Trial primary completion date: Oct 2025 ➔ Feb 2026

Phase classification • Trial completion date • Trial primary completion date

Study APV20002: Safety and Efficacy Results Through Week 684 for Pediatric Participants Living With HIV-1 Treated With Ritonavir-Boosted Fosamprenavir Oral Solution-Based Antiretroviral Therapy. (PubMed, AIDS Res Hum Retroviruses) - "HIV from 1/9 VFs through 48W developed treatment-emergent reduced susceptibility to FPV and 1/9 to lamivudine/emtricitabine. Post-48W, 4/5 participants with VF had phenotype results; all were still susceptible to all study drugs at VF. In conclusion, FPV OS-based ART was efficacious and generally well tolerated in this long-running pediatric study through 684 weeks of treatment, with a safety profile consistent with experience in adults and older children."

Journal • Human Immunodeficiency Virus • Infectious Disease • Pediatrics • CD4

Lexiva for the Treatment of LPR (clinicaltrials.gov) - P3 | N=104 | Not yet recruiting | Sponsor: Medical College of Wisconsin | Trial completion date: Oct 2024 ➔ Oct 2025 | Trial primary completion date: Oct 2024 ➔ Oct 2025

Trial completion date • Trial primary completion date

Inhaled fosamprenavir for laryngopharyngeal reflux: Toxicology and fluid dynamics modeling. (PubMed, Laryngoscope Investig Otolaryngol) - "A formal GLP assessment is underway to support a phase I clinical trial of an FOS DPI for LPR. NA."

Journal • Cardiovascular

Developing an adult stem cell derived microphysiological intestinal system for predicting oral prodrug bioconversion and permeability in humans. (PubMed, Lab Chip) - "Fosamprenavir underwent phosphatase mediated hydrolysis to amprenavir while dabigatran etexilate (DABE) exhibited proper CES2- and, as anticipated, not CES1-mediated de-esterification, followed by permeation of amprenavir to the vascular channel. When comparing organoids from MPS and transwells, expression of intestinal alkaline phosphatase (ALPI), carboxylesterase (CES)2, cytochrome P450 3A4 (CYP3A4) and sucrase isomaltase (SI) was 2.97-, 1.2-, 11.3-, and 27.7-fold higher for duodenum and 7.7-, 4.6-, 18.1-, and 112.2-fold higher for jejunum organoids in MPS, respectively. The MPS approach can provide a more physiological system than enzymes, organoids, and organoids on transwells for pharmacokinetic analysis of prodrugs that account for 10% of all commercial medicines."

Journal • CYP3A4

Development and Evaluation of a Protease Inhibitor Antiretroviral Drug-Loaded Carbon Nanotube Delivery System for Enhanced Efficacy in HIV Treatment. (PubMed, Int J Pharm) - "To achieve this, Fosamprenavir calcium (FPV), a prodrug of amprenavir known for inhibiting the proteolytic cleavage of immature virions, was selected as the protease inhibitor antiretroviral drug, and loaded onto COOH-MWCNTs using a direct loading method...The successful encapsulation, sustained drug release, and reduced toxicity make FPV-MWCNT a compelling candidate for enhancing the therapeutic efficacy of protease inhibitor antiretroviral drugs in the treatment of HIV. The developed delivery system holds great promise for future advancements in HIV treatment and paves the way for further research and development in the field of drug delivery utilizing carbon nanotube-based systems."

Journal • Hematological Disorders • Human Immunodeficiency Virus • Infectious Disease • Musculoskeletal Diseases • Orthopedics

Study Of An Investigational Regimen Including FDA Approved HIV Drugs In HIV-Infected Pediatric Subjects (clinicaltrials.gov) - P2 | N=59 | Completed | Sponsor: ViiV Healthcare | Unknown status ➔ Completed

Trial completion • Human Immunodeficiency Virus • Infectious Disease • Pediatrics • CD4

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

Drug repurposing of FDA-approved anti-viral drugs via computational screening against novel 6M03 SARS-COVID-19. (PubMed, Ir J Med Sci) - "In our study, we also observed the nucleotide sequence of protease protein consisting of 316 amino acid residues and the influence of these pronouncing drugs over these sequences. The outcome of this research work provides researchers with a track record for carrying out further investigational procedures by applying docking simulations and in vitro and in vivo experimentation with these reprofile drugs so that a better drug can be formulated against coronavirus."

FDA event • Journal • Infectious Disease • Novel Coronavirus Disease • Respiratory Diseases

Lexiva for the Treatment of LPR (clinicaltrials.gov) - P3 | N=104 | Not yet recruiting | Sponsor: Medical College of Wisconsin | Trial primary completion date: Jun 2024 ➔ Oct 2024

Trial primary completion date

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

Lexiva for the Treatment of LPR (clinicaltrials.gov) - P3 | N=104 | Not yet recruiting | Sponsor: Medical College of Wisconsin | Trial completion date: Mar 2024 ➔ Aug 2024 | Trial primary completion date: Jan 2024 ➔ Jun 2024

Trial completion date • Trial primary completion date

Validation of an LC-MS/MS method for quantitation of fostemsavir in plasma. (PubMed, J Pharmacol Toxicol Methods) - "In summary, the developed method has been successfully validated and pharmacokinetic parameters were demonstrated after oral administration of Fostemsavir to healthy rabbits."

Journal • Human Immunodeficiency Virus • Infectious Disease

In-vitro Dynamic Dissolution/Bioconversion/Permeation of Fosamprenavir using a Novel Tool with an Artificial Biomimetic Permeation Barrier and Microdialysis-Sampling. (PubMed, Eur J Pharm Sci) - "At conditions with an almost 10-fold higher dose than the usual human dose, some replicates showed premature precipitation and collapse of supersaturation, while others did not. In conclusion, the proposed novel tool appears very promising in gaining an in-depth mechanistic understanding of the bioconversion/permeation interplay, including transient supersaturation of phosphate-ester prodrugs like fosamprenavir."

Journal • Preclinical