Summary: A diarylpyrimidine derivative and REVERSE TRANSCRIPTASE INHIBITOR with antiviral activity against HIV-1 that is used in the treatment of HIV INFECTIONS. It is also used in combination with other ANTI-HIV AGENTS, since ANTIVIRAL DRUG RESISTANCE emerges rapidly when it is used alone.

Top Publications

  1. Crauwels H, van Heeswijk R, Buelens A, Stevens M, Hoetelmans R. Lack of an effect of rilpivirine on the pharmacokinetics of ethinylestradiol and norethindrone in healthy volunteers. Int J Clin Pharmacol Ther. 2014;52:118-28 pubmed publisher
    b>Rilpivirine is a human immunodeficiency virus Type 1 (HIV-1) non-nucleoside reverse transcriptase inhibitor. Rilpivirine metabolism involves cytochrome P450 3A4 (CYP3A4). This trial (ClinicalTrials...
  2. Wei L, Wang H, Huang L, Chen C, Morris Natschke S, Lee K, et al. Drug-like property-driven optimization of 4-substituted 1,5-diarylanilines as potent HIV-1 non-nucleoside reverse transcriptase inhibitors against rilpivirine-resistant mutant virus. Bioorg Med Chem Lett. 2017;27:2788-2792 pubmed publisher
    ..p-cyanoethyl-DAANs (4a-4c) were evaluated not only for anti-HIV potency against both wild-type HIV virus and rilpivirine-resistant (E138K, E138K+M184I) viral replication, but also for multiple drug-like properties, including aqueous ..
  3. Capetti A, Astuti N, Cattaneo D, Rizzardini G. Pharmacokinetic drug evaluation of dolutegravir plus rilpivirine for the treatment of HIV. Expert Opin Drug Metab Toxicol. 2017;13:1183-1192 pubmed publisher
    ..Among these the association of rilpivirine and dolutegravir is emerging as a twin randomized clinical trial (SWORD1&2) and at least three ..
  4. Dolgin E. Long-acting HIV drugs advanced to overcome adherence challenge. Nat Med. 2014;20:323-4 pubmed publisher
  5. Todesco E, Surgers L, Marcelin A, Calvez V, Meynard J, Morand Joubert L. Presence of Minority Resistant Variants After Failure of a Tenofovir, Emtricitabine, and Rilpivirine Regimen. J Acquir Immune Defic Syndr. 2016;72:e43-5 pubmed publisher
  6. DeJesus E, Ramgopal M, Crofoot G, Ruane P, Lamarca A, Mills A, et al. Switching from efavirenz, emtricitabine, and tenofovir disoproxil fumarate to tenofovir alafenamide coformulated with rilpivirine and emtricitabine in virally suppressed adults with HIV-1 infection: a randomised, double-blind, multicentre, phase 3b, . Lancet HIV. 2017;4:e205-e213 pubmed publisher
    ..The coformulation of rilpivirine, emtricitabine, and tenofovir alafenamide has recently been approved, and we aimed to investigate the efficacy, ..
  7. Kiertiburanakul S, Boettiger D, Ng O, Van Kinh N, Merati T, Avihingsanon A, et al. Factors associated with pre-treatment HIV RNA: application for the use of abacavir and rilpivirine as the first-line regimen for HIV-infected patients in resource-limited settings. AIDS Res Ther. 2017;14:27 pubmed publisher
    Abacavir and rilpivirine are alternative antiretroviral drugs for treatment-naïve HIV-infected patients. However, both drugs are only recommended for the patients who have pre-treatment HIV RNA <100,000 copies/mL...
  8. Sculier D, Gayet Ageron A, Battegay M, Cavassini M, Fehr J, Hirzel C, et al. Rilpivirine use in the Swiss HIV cohort study: a prospective cohort study. BMC Infect Dis. 2017;17:476 pubmed publisher
    b>Rilpivirine is safe and effective in HIV-naïve patients with low baseline HIV-RNA or in switch strategy. It offers the advantages of few drug-drug interactions and a favourable toxicity profile...
  9. Zainuddin R, Zaheer Z, Sangshetti J, Momin M. Enhancement of oral bioavailability of anti-HIV drug rilpivirine HCl through nanosponge formulation. Drug Dev Ind Pharm. 2017;43:2076-2084 pubmed publisher
    ..cyclodextrin nanosponges using a novel and efficient microwave mediated method for enhancing bioavailability of Rilpivirine HCl (RLP). Belonging to BCS class II RLP has pH dependent solubility and poor oral bioavailability...