Trial reportAntimicrobial agents and chemotherapy2001
Pharmacokinetic and pharmacodynamic study of the human immunodeficiency virus protease inhibitor amprenavir after multiple oral dosing.
Trial report in Antimicrobial agents and chemotherapy, 2001. The graph could read no effect estimate from its abstract, so it casts no vote on the map. It is linked to trial NCT00002183 (A Phase I Trial to Evaluate the Safety, Pharmacokinetics and Antiviral Activity of 141W94 After Multiple Dosing in Patients With HIV Infection), which is not on this map. Cited by 33 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
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.
The trial behind it
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.
A Phase I Trial to Evaluate the Safety, Pharmacokinetics and Antiviral Activity of 141W94 After Multiple Dosing in Patients With HIV Infection
Who cites it
33 citing papers in PubMed, 98 citations in OpenAlex.
- Fosamprenavir with Ritonavir Pharmacokinetics during Pregnancy.Antimicrobial agents and chemotherapy · 2020Trial
- Predictive values of the human immunodeficiency virus phenotype and genotype and of amprenavir and lopinavir inhibitory quotients in heavily pretreated patients on a ritonavir-boosted dual-protease-inhibitor regimen.Antimicrobial agents and chemotherapy · 2008Trial
- Effect of antacids and ranitidine on the single-dose pharmacokinetics of fosamprenavir.Antimicrobial agents and chemotherapy · 2005Trial
- Six-week randomized controlled trial to compare the tolerabilities, pharmacokinetics, and antiviral activities of GW433908 and amprenavir in human immunodeficiency virus type 1-infected patients.Antimicrobial agents and chemotherapy · 2004Trial
- Twice-daily amprenavir 1200 mg versus amprenavir 600 mg/ritonavir 100 mg, in combination with at least 2 other antiretroviral drugs, in HIV-1-infected patients.BMC infectious diseases · 2003Trial
- Indinavir, efavirenz, and abacavir pharmacokinetics in human immunodeficiency virus-infected subjects.Antimicrobial agents and chemotherapy · 2003Trial
- 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
- 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
- Doravirine Suppresses Common Nonnucleoside Reverse Transcriptase Inhibitor-Associated Mutants at Clinically Relevant Concentrations.Antimicrobial agents and chemotherapy · 2016Article
- Relevance of Liver Failure for Anti-Infective Agents: From Pharmacokinetic Alterations to Dosage Adjustments.Therapeutic advances in infectious disease · 2014Article
- Pharmacokinetics and pharmacodynamics of ASP2151, a helicase-primase inhibitor, in a murine model of herpes simplex virus infection.Antimicrobial agents and chemotherapy · 2013Article
- Novel method to assess antiretroviral target trough concentrations using in vitro susceptibility data.Antimicrobial agents and chemotherapy · 2012Article
- Article
- Antiretroviral therapeutic drug monitoring in Canada: current status and recommendations for clinical practice.The Canadian journal of hospital pharmacy · 2009Article
- Regional adipose tissue and lipid and lipoprotein levels in HIV-infected women.Journal of acquired immune deficiency syndromes (1999) · 2008Article
- A review of the pharmacokinetics of abacavir.Clinical pharmacokinetics · 2008Review
- Variability in non-nucleoside reverse transcriptase and protease inhibitors concentrations among HIV-infected adults in routine clinical practice.British journal of clinical pharmacology · 2007Article
- Compartmental pharmacokinetic analysis of oral amprenavir with secondary peaks.Antimicrobial agents and chemotherapy · 2007Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
4 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
In a dose-ranging study of amprenavir (formerly 141W94), an inhibitor of the protease enzyme of human immunodeficiency virus (HIV) type 1, single-dose and steady-state pharmacokinetic parameters were estimated from plasma samples collected on day 1 and during week 3, respectively. Amprenavir was administered on either a twice-daily (b.i.d.) or three-times-daily dosage schedule to 62 HIV-infected adults, 59 of whom had pharmacokinetic data. Log-log regression analysis (the power model) revealed that the steady-state area under the curve (AUC(ss)) and the maximum, minimum, and average concentrations at steady state (C(max,ss), C(min,ss), and C(avg,ss), respectively) increased in a dose-proportional manner over the 300- to 1,200-mg dose range. Steady-state clearance was dose independent. AUC(ss)/AUC(0-->infinity) decreased linearly with dose and correlated significantly with treatment-associated decreases in alpha(1)-acid glycoprotein. After 3 weeks, the dose of 1,200 mg b.i. d. provided a median amprenavir C(min,ss) (0.280 microg/ml) that was higher than the median in vitro 50% inhibitory concentration for clinical HIV isolates (0.023 microg/ml), even after adjustment for protein binding. The median amprenavir C(min,ss) was also greater than the estimated in vivo trough concentration calculated to yield 90% of the maximum antiviral effect (0.228 microg/ml) over 4 weeks. A pharmacodynamic analysis of the relationship between steady-state pharmacokinetic parameters and safety revealed headache and oral numbness to be the only side effects significantly associated with C(max). The pharmacodynamic relationship defined in this study supports the use of 1,200 mg b.i.d. as the approved dose of amprenavir.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.