Trial reportAntimicrobial agents and chemotherapy1999
Safety and pharmacokinetics of amprenavir (141W94), a human immunodeficiency virus (HIV) type 1 protease inhibitor, following oral administration of single doses to HIV-infected adults.
Trial report in Antimicrobial agents and chemotherapy, 1999. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 28 papers, 1 of them a synthesis that pooled it.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
28 citing papers in PubMed, 1 synthesis or guideline pooled it, 66 citations in OpenAlex.
- Interactions of Antiretroviral Drugs with Food, Beverages, Dietary Supplements, and Alcohol: A Systematic Review and Meta-analyses.AIDS and behavior · 2023Pooled it
- Low frequency of intermittent HIV-1 semen excretion in patients treated with darunavir-ritonavir at 600/100 milligrams twice a day plus two nucleoside reverse transcriptase inhibitors or monotherapy.Antimicrobial agents and chemotherapy · 2010Trial
- Amprenavir and efavirenz pharmacokinetics before and after the addition of nelfinavir, indinavir, ritonavir, or saquinavir in seronegative individuals.Antimicrobial agents and chemotherapy · 2005Trial
- Single-dose safety and pharmacokinetics of amprenavir (141W94), a human immunodeficiency virus type 1 (HIV-1) protease inhibitor, in HIV-infected children.Antimicrobial agents and chemotherapy · 2005Trial
- Genotypic inhibitory quotient as predictor of virological response to ritonavir-amprenavir in human immunodeficiency virus type 1 protease inhibitor-experienced patients.Antimicrobial agents and chemotherapy · 2003Trial
- Pharmacokinetic interaction between amprenavir and delavirdine after multiple-dose administration in healthy volunteers.British journal of clinical pharmacology · 2003Trial
- Single-dose pharmacokinetics of amprenavir coadministered with grapefruit juice.Antimicrobial agents and chemotherapy · 2002Trial
- Pharmacokinetic study of human immunodeficiency virus protease inhibitors used in combination with amprenavir.Antimicrobial agents and chemotherapy · 2001Trial
- In vivo effect of alpha(1)-acid glycoprotein on pharmacokinetics of amprenavir, a human immunodeficiency virus protease inhibitor.Antimicrobial agents and chemotherapy · 2001Trial
- Pharmacokinetic and pharmacodynamic study of the human immunodeficiency virus protease inhibitor amprenavir after multiple oral dosing.Antimicrobial agents and chemotherapy · 2001Trial
- Pharmacokinetic interaction between amprenavir and clarithromycin in healthy male volunteers.Antimicrobial agents and chemotherapy · 2000Trial
- Single-dose pharmacokinetics of amprenavir, a human immunodeficiency virus type 1 protease inhibitor, in subjects with normal or impaired hepatic function.Antimicrobial agents and chemotherapy · 2000Trial
- Mpox Knowledge Graph: a comprehensive representation embedding chemical entities and associated biology of Mpox.Bioinformatics advances · 2023Article
- Chemogenetic ON and OFF switches for RNA virus replication.Nature communications · 2021Article
- Identification of potential antivirals against SARS-CoV-2 using virtual screening method.Informatics in medicine unlocked · 2021Article
- Repurposing Approved Drugs for Guiding COVID-19 Prophylaxis: A Systematic Review.Frontiers in pharmacology · 2020Review
- Organic carbamates in drug design and medicinal chemistry.Journal of medicinal chemistry · 2015Review
- Relevance of Liver Failure for Anti-Infective Agents: From Pharmacokinetic Alterations to Dosage Adjustments.Therapeutic advances in infectious disease · 2014Article
- Pregnane X receptor mediates dyslipidemia induced by the HIV protease inhibitor amprenavir in mice.Molecular pharmacology · 2013Article
- Multiple peaking phenomena in pharmacokinetic disposition.Clinical pharmacokinetics · 2010Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
5 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
We conducted a double-blind, placebo-controlled, parallel, dose-escalation trial to evaluate the pharmacokinetics and safety of single, oral doses of amprenavir (141W94; formerly VX-478), a potent inhibitor of human immunodeficiency virus (HIV) type 1 protease, administered as hard gelatin capsules in 12 HIV-infected subjects. The doses of amprenavir evaluated were 150, 300, 600, 900, and 1,200 mg. Amprenavir was rapidly absorbed, with the time to maximum concentration occurring within 1 to 2 h after dosing. On the basis of power model analysis, the increase in the maximum concentration of amprenavir in plasma (Cmax) was less than dose proportional, and the increase in the area under the concentration-time curve from time zero to infinity (AUC0-infinity) was greater than dose proportional; mean slopes (with 90% confidence intervals) were 1.25 (1.16 to 1.35) and 0.78 (0.78 to 0.86) for AUC0-infinity and Cmax, respectively. Amprenavir was eliminated slowly, with a terminal-phase half-life of 8 h. A second study was conducted to determine the bioavailability of the hard gelatin capsule relative to that of a subsequently developed soft gelatin capsule. The capsules were bioequivalent in terms of AUC0-infinity but not in terms of Cmax; geometric-least-squares means ratios (with 90% confidence intervals) were 1.03 (0.92 to 1.14) and 1.25 (1.03 to 1. 53) for AUC0-infinity and Cmax, respectively. Administration of soft gelatin capsules of amprenavir with a high-fat breakfast resulted in a 14% decrease in the mean AUC0-infinity (from 9.58 to 8.26 microg. h/ml), which is not likely to be clinically significant. The most common adverse events related to amprenavir were headache, nausea, and hypesthesia. Amprenavir appears to be safe and well tolerated over the dose range of 150 to 1200 mg. On the basis of the present single-dose studies, amprenavir is an HIV protease inhibitor with favorable absorption and clearance pharmacokinetics that are only minimally affected by administration with food.
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