Cabotegravir, sold under the brand name Vocabria.
Introducing the genome into DNA is a necessary step for the virus to replicate, and therefore it’s further spread is hampered.
It is a antiretroviral medication used for the treatment of HIV/AIDS.
It is available in the form of tablets and as an intramuscular injection, as well as in an injectable combination with rilpivirine.
Pregnancy category AU: B1.
Protein binding>99%
Metabolites glucuronide
Elimination half-life tablets: 41 hours
injection: 5.6–11.5 weeks
Excretion 47% via feces, 27% via urine
Approved cabotegravir for pre-exposure prophylaxis (PrEP) in at-risk people.
Cabotegravir in combination with rilpivirine is indicated for the treatment of human immunodeficiency virus type-1 (HIV-1) in adults.
The combination injection is intended for maintenance treatment of adults who have undetectable HIV levels in the blood (viral load less than 50 copies/mL) with their current antiretroviral treatment, and when the virus has not developed resistance to non-nucleoside reverse transcriptase inhibitors (NNRTIs) and integrase strand transfer inhibitors.
The tablets are used to check whether a person tolerates the treatment before the injection therapy is started.
Cabotegravir is indicated for use in at-risk people weighing at least 35 kilograms (77 lb) for pre-exposure prophylaxis (PrEP) to reduce the risk of sexually acquired HIV.
It must not be combined with the drugs rifampicin, rifapentine, carbamazepine, oxcarbazepine, phenytoin or phenobarbital, which induce the enzyme UGT1A1, and will significantly decrease cabotegravir concentrations in the body.
These drugs induce the enzyme CYP3A4, which leads to reduced rilpivirine concentrations in the body.
The most common adverse side effects of the injectable combination therapy with rilpivirine are reactions at the injection site in up to 84% of patients.
Pain and swelling at the injection site, as well as headache in up to 12% of patients and fever in 10%.
Tablet associated headache and fever are slightly less frequent.
Less common side effects of under 10% for both formulations are depressive disorders, insomnia, and rashes.
Cabotegravir glucuronide is the main metabolite in human bile and urine.
Orally, it reaches highest blood plasma levels after three hours.
Intramuscularly, cabotegravir is slowly absorbed into the bloodstream, reaching its highest blood plasma levels after about seven days.
Over 99% bound to plasma proteins.
The drug is inactivated in the body by glucuronidation, mainly by the enzyme UGT1A1.
More than 90% of the circulating substance is unchanged.
Its biological half-life is 41 hours for the tablets and 5.6 to 11.5 weeks for the injection.
The oral drug is eliminated via the feces in unchanged form (47%).
To a lesser extent it is excreted via the urine (27%), almost exclusively as the glucuronide.
Randomized, double-blind trials that compared cabotegravir to emtricitabine/tenofovir, a once daily oral medication for HIV PrEP:
The first trial showed participants who took cabotegravir had 69% less risk of getting infected with HIV when compared to participants who took emtricitabine/tenofovir.
In Trial 2, participants who took cabotegravir had 90% less risk of getting infected with HIV when compared to participants who took emtricitabine/tenofovir.
Long acting cabotegravir is the first injectable medication to prevent HIV.
The long acting drug is more likely to prevent HIV acquisition than daily oral medication for people at risk of sexually acquiring HIV.