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Fosamprenavir
Published in M. Lindsay Grayson, Sara E. Cosgrove, Suzanne M. Crowe, M. Lindsay Grayson, William Hope, James S. McCarthy, John Mills, Johan W. Mouton, David L. Paterson, Kucers’ The Use of Antibiotics, 2017
Suzanne M. Crowe, Christine Katlama, Robert Murphy
Fosamprenavir is a sulfa-containing calcium phosphate ester prodrug of amprenavir. Like other HIV-1 protease inhibitors, amprenavir binds to the active site of the HIV-1 protease. This prevents the processing of viral Gag and Gag–Pol polyprotein precursors, resulting in the formation of immature noninfectious viral particles.
Cutaneous Manifestations of Highly Active Antiretroviral Therapy
Published in Clay J. Cockerell, Antoanella Calame, Cutaneous Manifestations of HIV Disease, 2012
Deborah B. Henderson, Clay J. Cockerell
While neither amprenavir nor its prodrug, fosamprenavir, cause the metabolic disturbances seen with indinavir, cutaneous hypersensitivity reactions are a common side-effect of both. Approximately 20% of patients taking amprenavir are reported to develop an eruption soon after starting treatment. Generally, the eruption is mild and fewer than 5% of patients discontinue their therapy because of it. In rare cases, it may be more severe.42 An isolated cutaneous eruption occurs in 7% of patients receiving fosamprenavir. Most of these eruptions are mild although SJS has been reported.43 Atazanavir, an azapeptide PI with convenient single day dosing, may cause hyperbilirubinemia and a mild eruption comparable to that of fosamprenavir; as with amprenavir and fosamprenavir, it does not alter lipid levels.44
Safety analysis of Lexiva tablets 700 (fosamprenavir calcium hydrate) in post-marketing surveillance in Japan
Published in Current Medical Research and Opinion, 2020
Akiko Fukuda, Takako Nagao, Tomomi Kitaichi, Ichiro Koga, Akihiro Kobayashi, Toshiyuki Miura
Fosamprenavir (Lexiva® Tablets 700, ViiV Healthcare, Tokyo), a prodrug of amprenavir (GlaxoSmithKline, United Kingdom), is one of the drugs available for treatment of HIV infection. The approved dosage of fosamprenavir is 1400 mg daily with ritonavir or 2800 mg daily without ritonavir.5 The conditions for approval by the Japanese Ministry of Health, Labor and Welfare required that post-marketing surveillance of all patients who received fosamprenavir in Japan should be conducted to assess the actual use of the product at its initial approval. Post-marketing data were collected from 365 patients at 26 sites in Japan between January 2005 and December 2014 and analyzed for safety and effectiveness of fosamprenavir. When fosamprenavir was used as a component of ART, the incidence of adverse events whose causal relationship could not be completely ruled out (adverse drug reactions; ADRs) and serious adverse events were 43.7% and 21.7%, respectively.
Aspartic peptidase of Phialophora verrucosa as target of HIV peptidase inhibitors: blockage of its enzymatic activity and interference with fungal growth and macrophage interaction
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2020
Marcela Q. Granato, Ingrid S. Sousa, Thabatta L. S. A. Rosa, Diego S. Gonçalves, Sergio H. Seabra, Daniela S. Alviano, Maria C. V. Pessolani, André L. S. Santos, Lucimar F. Kneipp
Peptidase activity was determined using 7-methoxycoumarin-4-acetyl (MCA)-Gly-Lys-Pro-Ile-Leu-Phe-Phe-Arg-Leu-Lys(DNP)-D-Arg-amide (cathepsin D fluorogenic substrate, Sigma-Aldrich Chemical Co) as described by Santos et al.29. The assay was performed in triplicate using a 96-well microtiter plate. Briefly, the reaction was started by the addition of substrate (12 µM) to fungal concentrated supernatant (1 µg of protein) in a buffer containing 100 mM sodium acetate, pH 4.7, 1 M sodium chloride, 1 mM ethylenediamine tetraacetic acid (EDTA), 1 mM dithiothreitol (DTT), 10% DMSO and 1 mg/mL bovine serum albumin (BSA). The system was treated with pepstatin A (10 µM) or 100 µM of HIV-PIs (amprenavir, atazanavir, indinavir, lopinavir, nelfinavir, ritonavir or saquinavir) and a non-treated system was used as control. After 30 min, the cleavage of the cathepsin D substrate was detected in a spectrofluorimeter (FlexStation 3, Molecular Devices, CA, USA) with 328 nm excitation and 393 nm emission wavelengths. The proteolytic activity was calculated based on a standard curve of MCA fluorophore. Protein concentration was measured using the method described by Lowry et al.28. All HIV-PIs were purchased from National Institutes of Health (NIH, MA, USA) and dissolved in DMSO. All buffer reagents were obtained from Sigma-Aldrich Chemical Co (St Louis, MO, USA).
Nanocarriers for brain specific delivery of anti-retro viral drugs: challenges and achievements
Published in Journal of Drug Targeting, 2018
Nila Mary Varghese, Venkatachalam Senthil, Shailendra K. Saxena
Various influx and efflux transporters belonging to specific families are present at the endothelial cells of BBB and BCSFB that reduces the penetration of drug to the brain by their specific mechanism of action [35–37]. Edwards et al. [38], reported that the inhibition of P-gp by Pgp inhibitor, GF120918, partially increased the brain concentration of Amprenavir. Furthermore, the concentration of saquinavir was substantially increased in P-gp deficient mice [39]. Hence, the anti-retroviral nanomedicines have to combat the physical, chemical and metabolic barriers of BBB and BCSFB, for the effective pharmacotherapy against neuroAIDS.