Drug intelligence / Profile preview

Lersivirine + methadone

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral, Intravenous, Intramuscular, Subcutaneous
01

Overview

Lersivirine + methadone is a combination of two drugs. Lersivirine (UK-453,061) is a next-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) developed for the treatment of HIV-1 infection. Methadone is a synthetic opioid used primarily for the management of severe pain and as maintenance therapy or detoxification in opioid use disorder. Lersivirine acts by inhibiting HIV-1 reverse transcriptase and thereby blocking viral replication. Methadone works as a full agonist at the µ-opioid receptor and also antagonizes N-methyl-D-aspartate (NMDA) receptors to relieve pain and prevent withdrawal symptoms in opioid-dependent individuals. Clinical studies have shown that co-administration of lersivirine with methadone does not result in clinically relevant changes in methadone concentrations or withdrawal symptoms; no dose adjustment is required when these drugs are used together.

Other names
DisketsMethadose Sugar-Free
02

Targets

NMDAR (Glutamate receptor ionotropic, NMDA)Human immunodeficiency virus type 1 reverse transcriptaseMOR (Mu opioid receptor)

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