Drug intelligence / Profile preview

XVIR-110

Development stage
Preclinical
Lead developer
Exavir Therapeutics
Modality
Nanoparticles → Drug Delivery Systems, Small Molecules
Administration
Intramuscular
01

Overview

XVIR-110 is an investigational ultra-long-acting **nanocrystalline prodrug formulation of cabotegravir stearate (NM2CAB)**, designed as an injectable HIV integrase strand transfer inhibitor (INSTI) for **once-every-six-months to once-yearly** dosing in HIV treatment and pre-exposure prophylaxis (PrEP).[1][2][4][15][17] Developed using Exavir Therapeutics’ nanocrystalline prodrug technology, XVIR-110 consists of a highly lipophilic cabotegravir 18‑carbon ester prodrug formulated as aqueous nanocrystals; after intramuscular injection, slow **nanocrystal dissolution** is followed by pH‑dependent and esterase‑mediated hydrolysis to release active cabotegravir, yielding markedly prolonged plasma cabotegravir exposures versus conventional cabotegravir long-acting (CAB-LA).[1][4][15][17][19] Preclinical studies in rodents and dogs demonstrate cabotegravir half-lives of approximately 120–150 days and maintenance of plasma concentrations above protein-binding–adjusted inhibitory thresholds for many months, with fewer and less severe acute injection-site reactions than CAB-LA at equivalent cabotegravir doses, supporting its development as a potential best-in-class ultra-long-acting INSTI backbone for next-generation HIV regimens and PrEP.[1][2][4][5][18]

Other names
cabotegravir 18 carbon ester prodrugcabotegravir18 carbon ester prodrugcabotegravir-18 carbon ester prodrugultra-long-acting cabotegravir prodrugultra-long-acting HIV integrase inhibitor XVIR-110
02

Targets

Integrase allosteric pocket (HIV)

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