Cabotegravir is an HIV-1 integrase strand transfer inhibitor (INSTI) indicated for the treatment of HIV-1 infection and pre-exposure prophylaxis (PrEP) against HIV-1.

How to Use Cabotegravir

For the Treatment of HIV-1 Infection

Oral Lead-In Phase: To assess the patient’s tolerance to cabotegravir. The recommended dosage is 30 mg cabotegravir combined with 25 mg rilpivirine, administered once daily for approximately 1 month (at least 28 days). The last oral dose should be taken on the same day as the injectable formulation (CABENUVA).

Alternative for Missed Injections: If a patient is scheduled to miss a monthly CABENUVA injection by more than 7 days, oral alternative therapy (30 mg cabotegravir + 25 mg rilpivirine daily) may be used, for a maximum of 2 months.

For HIV-1 Pre-Exposure Prophylaxis (PrEP)

Oral Lead-In Phase: 30 mg cabotegravir is administered as a single agent once daily for 1 month (at least 28 days), followed by the initiation of the long-acting injectable formulation APRETUDE.

Alternative for Missed Injections: If an APRETUDE injection is missed by more than 7 days, switch to 30 mg oral cabotegravir daily, for a maximum of 2 months.

Key Precautions

The medication should be taken with meals to improve bioavailability.

A negative HIV-1 status must be confirmed before starting the medication, and re-testing should be performed regularly every 3 months.

Dosage Adjustment of Cabotegravir

Drug Interactions and Dosage Adjustment

Absolute Contraindications: Carbamazepine, oxcarbazepine, phenobarbital, phenytoin, rifampicin, and rifapentine (as these drugs significantly reduce the plasma concentration of cabotegravir).

Antacids: Antacids containing aluminum/magnesium/calcium must be taken with an interval of 2 hours before or 4 hours after cabotegravir administration.

Medication for Special Populations of Cabotegravir

Children and Adolescents

Aged ≥ 12 years and weighing ≥ 35 kg: The dosage is the same as that for adults, but additional adherence support is required.

Safety: The adverse reaction profile in adolescents is consistent with that in adults, with common reactions including headache, diarrhea, and dizziness.

Elderly Patients and Those with Hepatic or Renal Impairment

Elderly patients: No dosage adjustment is needed, but attention should be paid to concurrent medications and hepatic/renal function.

Renal impairment: No dosage adjustment is needed.

Hepatic impairment: No dosage adjustment is needed for mild to moderate impairment; caution is required for severe impairment.