Drug intelligence / Profile preview

cabotegravir stearate

Development stage
Phase 1
Lead developer
University of Nebraska Medical Center
Modality
Small Molecules
Administration
Intramuscular, Subcutaneous
01

Overview

VH4367310 (also known as VH-310 or XVIR-110) is an investigational, ultra-long-acting prodrug of the integrase strand transfer inhibitor (INSTI) cabotegravir. Originally developed by researchers at the University of Nebraska Medical Center (UNMC) and licensed to Exavir Therapeutics, the compound was subsequently out-licensed to ViiV Healthcare for clinical development. VH4367310 is formulated as an aqueous nanocrystalline suspension of cabotegravir stearate (M2CAB), a lipophilic 18-carbon ester prodrug. Following intramuscular or subcutaneous injection, the nanocrystals slowly dissolve and undergo esterase-catalyzed hydrolysis to release active cabotegravir, creating a sustained drug depot. This mechanism provides an exceptionally long half-life, supporting a dosing interval of every six months or longer. VH4367310 is currently in Phase 1 clinical development for the treatment and prevention (pre-exposure prophylaxis, or PrEP) of HIV-1 infection.

Other names
M2CABM-2CABM 2CABcabotegravir stearoylatecabotegravir stearoylate prodrug
02

Targets

Integrase allosteric pocket (HIV)

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