Rilpivirine is non-nucleoside reverse transcriptase inhibitor (NNRTI) which is used for the treatment of HIV-1 infections in treatment-naive patients.[A31328] It is a diarylpyrimidine derivative.[A31329] The internal conformational flexibility of rilpivirine and the plasticity of it interacting binding site gives it a very high potency and reduces the chance of resistance compared to other NNRTI's.[A31331] Rilpivirine was developed by Tilbotec, Inc. and FDA approved on May 20, 2011.[L1030] On November 21, 2017, Rilpivirine, in combination with [dolutegravir], was approved as part of the first complete treatment regimen with only two drugs for the treatment of adults with HIV-1 named Juluca.[L1031] Rilpivirine in combination with [cabotegravir] was granted FDA approval on 21 January 2021.[L31193] While previously administered once-monthly only, this combination product was granted FDA approval for dosing every two months on February 01, 2022 [L40084] and without the need for an oral lead-in period prior.[L31193]
Rilpivirine, in combination with other agents, is indicated for the treatment of HIV-1 infections in antiretroviral treatment-naive patients with HIV-1 RNA ≤100,000 copies/mL and CD4+ cell count >200 cells/mm<sup>3</sup>.[L1030] The FDA combination therapy approval of rilpivirine and [dolutegravir] is indicated for adults and adolescents 12 years of age and older weighing at least 35 kg with HIV-1 infections whose virus is currently suppressed (< 50 copies/ml) on a stable regimen for at least six months, without a history of treatment failure and no known substitutions associated to resistance to any of the two components of the therapy.[L1031] Rilpivirine in combination with [cabotegravir] is indicated as a complete regimen for the treatment of HIV-1 infection in adults and adolescents - ≥12 years old and weighing at least 35kg - to replace the current antiretroviral regimen in those who are virologically suppressed (HIV-1 RNA <50 copies/mL) on a stable antiretroviral regimen with no history of treatment failure and with no known or suspected resistance to either cabotegravir or rilpivirine.[L31193]
Categories
Anti-HIV Agents
Anti-Infective Agents
Anti-Retroviral Agents
Antiinfectives for Systemic Use
Antiviral Agents
Antivirals for Systemic Use
Antivirals used in combination for the treatment of HIV infections
Drug Info/Drug Targets: DrugBank 3.0: a comprehensive resource for 'omics' research on drugs. Knox C, Law V, Jewison
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