Drug intelligence / Profile preview

etravirine + buprenorphine + naloxone

Development stage
Unknown
Lead developer
Indivior
Modality
Small Molecules
Administration
Oral, Sublingual
01

Overview

Etravirine + buprenorphine + naloxone is a combination of three active pharmaceutical ingredients: etravirine (a non-nucleoside reverse transcriptase inhibitor used in antiretroviral therapy for HIV-1), buprenorphine (a partial agonist at the mu-opioid receptor and antagonist at kappa- and delta-opioid receptors, used to treat opioid dependence), and naloxone (an opioid receptor antagonist added primarily to deter misuse of buprenorphine by causing withdrawal if injected rather than taken orally). There is no evidence of a commercially available fixed-dose combination product containing all three components; rather, this listing most likely reflects co-administration in patients with opioid use disorder and HIV infection. Etravirine inhibits the replication of HIV-1 by binding to and inhibiting reverse transcriptase, while buprenorphine attenuates opioid withdrawal and cravings, and naloxone reduces abuse potential.

02

Targets

Human immunodeficiency virus type 1 reverse transcriptaseCYP3A4 (Cytochrome P450 3A4)KOR (Kappa opioid receptor)MOR (Mu opioid receptor)

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