Drug intelligence / Profile preview

daridorexant + efavirenz

Development stage
Unknown
Lead developer
Idorsia
Modality
Small Molecules
Administration
Oral
01

Overview

This is a combination of **daridorexant**, a dual orexin receptor antagonist used for the treatment of insomnia, and **efavirenz**, a non-nucleoside reverse transcriptase inhibitor (NNRTI) used in the management of HIV infection. Daridorexant acts by selectively and competitively antagonizing the orexin 1 (OX1R) and orexin 2 (OX2R) receptors, inhibiting wake-promoting neuropeptides. Efavirenz blocks HIV-1 reverse transcriptase, an enzyme required for viral replication. There is no established medical use for the combination of these two drugs, but they are sometimes co-administered, leading to significant drug interactions due to efavirenz's modulation of liver enzymes. Efavirenz is a moderate inducer of CYP3A4, reducing plasma concentrations and efficacy of daridorexant when used concomitantly.

02

Targets

HTR6 (5-hydroxytryptamine receptor 6)HCRTR2 (Orexin/hypocretin receptor type 2)HTR2A (Serotonin receptor 5-HT2A)HTR2C (5-hydroxytryptamine 2C receptor)HCRTR1 (Orexin/hypocretin receptor type 1)HTR3A (5-hydroxytryptamine receptor 3A)Human immunodeficiency virus type 1 reverse transcriptase

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