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Cabotegravir

Apretude, Vocabria

Small molecule

integrase strand transfer inhibitor; INSTI)

Cabotegravir (CAB), also known as GSK1265744, is a HIV-1 integrase strand transfer inhibitor (INSTI). Long-acting versions of CAB (CAB-LA) are currently administered once monthly or every-2-months as a intramuscular (IM) injection containing an extended-release drug particle nanosuspension, with an optional ~30 day oral-lead in period. CAB-LA administered by IM injection requires approximately one week to achieve maximal plasma drug concentration. CAB is metabolised in the body by the enzyme UGT1A1; with the average half-life of IM CAB-LA ranging from 5.6 to 11.5 weeks.

An injectable formulation of cabotegravir is approved for use for HIV PrEP and as part of a regimen, for HIV treatment

Cabotegravir LA, both as suspension for intramuscular injection 600mg/3ml (200mg/ml) and as 30 mg tablet is included in WHO PQ: https://extranet.who.int/prequal/sites/default/files/document_files/EOI_23rd%20HIV_9July_2025_clean_PQ.pdf Cabotegravir for PrEP is included in WHO guidelines. CAB+RPV LA injectable for treatment, is also recommended by WHO to be used as an alternative switching option for adults and adolescents with undetectable HIV viral load on oral ART and without active hepatitis B infection : https://www.who.int/teams/global-hiv-hepatitis-and-stis-programmes/guidelines ViiV Healthcare and Medicines Patent Pool have signed a voluntary licensing agreement to enable access to long-acting injectable cabotegravir for HIV PrEP and HIV treatment