Drug intelligence / Profile preview

cabotegravir

Development stage
Approved
Lead developer
ViiV Healthcare
Modality
Small Molecules
Administration
Intramuscular, Oral
01

Overview

Cabotegravir is a small molecule antiretroviral drug classified as an integrase strand transfer inhibitor (INSTI). It is used for both the treatment and pre-exposure prophylaxis (PrEP) of HIV type 1 infection. Its mechanism of action involves binding to the active site of HIV integrase, thereby preventing the integration of viral DNA into the host genome, which is essential for viral replication. Cabotegravir is available as an oral tablet and as a long-acting intramuscular injection. For HIV treatment, it is always used in combination with rilpivirine; for PrEP, it can be used alone. The drug was developed by ViiV Healthcare and has been approved by regulatory agencies including the FDA for use in adults and adolescents at risk of or living with HIV[1][2][3][5][8].

Brand names
ApretudeVocabria
Other names
Cabotegravir sodiumCabotegravir (JAN/USAN/INN)Cabotegravir(GSK744)SCHEMBL82803SCHEMBL-82803SCHEMBL 82803CHEMBL2403238CHEMBL-2403238CHEMBL 2403238
02

Targets

SLC22A8 (Organic anion transporter 3)Integrase allosteric pocket (HIV)OAT1 (Organic anion transporter 1)HTLV-1 IN (HTLV-1 integrase)

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