Drug intelligence / Profile preview

cabotegravir prodrug

Development stage
Preclinical
Lead developer
University of Nebraska Medical Center
Modality
Nanoparticles → Drug Delivery Systems, Small Molecules
Administration
Intramuscular
01

Overview

Cabotegravir prodrug is a modified form of cabotegravir designed to extend the drug's release profile beyond the current monthly administration. The prodrug consists of fatty acid ester modifications of cabotegravir with added carbon chains (14, 18, or 22 carbons) encased in biocompatible surfactants (poloxamer coating). These modifications create hydrophobic and lipophilic versions with controlled hydrolysis and tissue penetrance properties. The lead formulation, NM2CAB (18-carbon ester chain), has demonstrated plasma cabotegravir levels above the protein-adjusted 90% inhibitory concentration for up to a year in pharmacokinetic studies performed in mice and rhesus macaques.

Other names
fatty acid ester CAB nanocrystal prodrugs
02

Targets

Integrase allosteric pocket (HIV)

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