ReviewClinical pharmacokinetics2007
Clinical pharmacokinetics of darunavir.
Review in Clinical pharmacokinetics, 2007. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 54 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.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
54 citing papers in PubMed, 121 citations in OpenAlex.
- Pharmacokinetics of once-daily darunavir/ritonavir in second-line treatment in African children with HIV.The Journal of antimicrobial chemotherapy · 2024Trial
- Fosamprenavir with Ritonavir Pharmacokinetics during Pregnancy.Antimicrobial agents and chemotherapy · 2020Trial
- Simultaneous pharmacogenetics-based population pharmacokinetic analysis of darunavir and ritonavir in HIV-infected patients.Clinical pharmacokinetics · 2013Trial
- Pharmacokinetic interaction of vicriviroc with other antiretroviral agents: results from a series of fixed-sequence and parallel-group clinical trials.Clinical pharmacokinetics · 2011Trial
- Herb-drug interaction between Echinacea purpurea and darunavir-ritonavir in HIV-infected patients.Antimicrobial agents and chemotherapy · 2011Trial
- Cruzain Inhibitors for Chagas Disease: Anticorrelated Optimisation Landscapes and the Multiparametric Path to Clinical Candidates.Chemical biology & drug design · 2026Review
- In Vitro Pharmacokinetic Properties of MK-2048, a Potent Drug Candidate for HIV Prevention.Viruses · 2026Article
- Nanoparticle delivery systems for HIV pre-exposure prophylaxis (PrEP): advances and challenges.Beilstein journal of nanotechnology · 2026Review
- Drug interactions in people with HIV treated with antivirals for other viral illnesses.Expert opinion on drug metabolism & toxicology · 2025Review
- Antiretroviral Therapy during Long-term Surgical Care: 'Exploring Difficult Cases in HIV Clinics' of the Korean Society for AIDS Conference in 2023.Infection & chemotherapy · 2024Review
- Preclinical characterization of a non-peptidomimetic HIV protease inhibitor with improved metabolic stability.Antimicrobial agents and chemotherapy · 2024Article
- Comparative efficacy of repurposed drugs lopinavir-ritonavir and darunavir-ritonavir in hospitalised COVID-19 patients: insights from a tertiary centre cohort.Frontiers in cellular and infection microbiology · 2024Article
- Predicting disruptions to drug pharmacokinetics and the risk of adverse drug reactions in non-alcoholic steatohepatitis patients.Acta pharmaceutica Sinica. B · 2023Review
- Viral proteases as therapeutic targets.Molecular aspects of medicine · 2022Review
- Pharmacodynamic model of slow reversible binding and its applications in pharmacokinetic/pharmacodynamic modeling: review and tutorial.Journal of pharmacokinetics and pharmacodynamics · 2022Review
- The Effect of Rifampicin on Darunavir, Ritonavir, and Dolutegravir Exposure within Peripheral Blood Mononuclear Cells: a Dose Escalation Study.Antimicrobial agents and chemotherapy · 2022Article
- Intranasal Delivery of Darunavir-Loaded Mucoadhesive In Situ Gel: Experimental Design, In Vitro Evaluation, and Pharmacokinetic Studies.Gels (Basel, Switzerland) · 2022Article
- Acquired bedaquiline resistance during the treatment of drug-resistant tuberculosis: a systematic review.JAC-antimicrobial resistance · 2022Review
- Inflammation Induces Changes in the Functional Expression of P-gp, BCRP, and MRP2: An Overview of Different Models and Consequences for Drug Disposition.Pharmaceutics · 2021Review
- Management of Antiretroviral Therapy with Boosted Protease Inhibitors-Darunavir/Ritonavir or Darunavir/Cobicistat.Biomedicines · 2021Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
2 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Darunavir (TMC114) is a newly developed HIV-1 protease inhibitor with potent antiviral activity against both wild-type and multidrug resistant HIV-1 strains. The drug is currently approved by the US FDA for antiretroviral treatment-experienced patients with limited therapeutic options. The approved dosage of darunavir is 600 mg in combination with ritonavir 100mg twice daily. Darunavir is rapidly absorbed after oral administration, reaching peak plasma concentrations after 2.5-4 hours. Absorption is followed by a fast distribution/elimination phase and a subsequent slower elimination phase with a terminal elimination half-life of 15 hours in the presence of low-dose ritonavir. Darunavir is approximately 95% plasma protein bound, mainly to alpha(1)-acid glycoprotein. Systemic exposure is increased by 30% when darunavir is taken with a meal. Darunavir is extensively and almost exclusively metabolised by cytochrome P450 (CYP) 3A4. Coadministration with small doses of the strong CYP3A4 inhibitor ritonavir results in an increase in darunavir bioavailability from 37% to 82%. Darunavir and its metabolites are mainly excreted in faeces (79.5%) and, to a lesser extent, in urine (13.9%). With regard to the necessary coadministration with low-dose ritonavir as a potent CYP3A4 inhibitor, coadministration of other substrates of CYP3A4 with darunavir/ritonavir requires caution or is even contraindicated. Guidance is derived from drug-drug interaction trials and experience from comparable ritonavir-boosted protease inhibitor regimens.
Indexed as
Identifiers
What OpenQuestion holds
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.