Cabotegravir is an HIV-1 integrase strand transfer inhibitor (INSTI). As the active ingredient in VOCABRIA, it must be used in combination with EDURANT (Rilpivirine) and is indicated for the short-term treatment of virologically suppressed adult patients with HIV-1 infection.

Cabotegravir: Precautions and Monitoring for Medication Use

Contraindications

Patients with a previous history of hypersensitivity to cabotegravir.

Concomitant use with the following drugs: Carbamazepine, Oxcarbazepine, Phenobarbital, Phenytoin, Rifampicin, and Rifapentine. These drugs can reduce the blood concentration of cabotegravir, leading to loss of efficacy.

Medication Use in Special Populations

Pregnancy: Current data are insufficient to assess the risk of birth defects, but dolutegravir—another integrase inhibitor in the same class—is associated with neural tube defects. Individuals of childbearing potential are advised to fully evaluate the benefits and risks before using the medication.

Hepatic or Renal Impairment: No dosage adjustment is required for patients with mild to moderate hepatic or renal impairment; data on patients with severe hepatic impairment (Child-Pugh Class C) are limited.

Elderly Patients: Caution is needed when administering the medication, as this population may have concurrent hepatic/renal function decline and polypharmacy (concomitant use of multiple drugs).

Drug Interactions

Antacids: Antacids containing aluminum/magnesium hydroxide or calcium carbonate should be taken either 2 hours before or 4 hours after cabotegravir administration.

Enzyme Inducers: Concomitant use with strong UGT1A1 inducers significantly reduces cabotegravir blood concentration and is absolutely contraindicated.

Other Antiretroviral Drugs: Cabotegravir plus Rilpivirine is already a complete treatment regimen; concurrent use with other anti-HIV drugs is not recommended.

Hypersensitivity Reactions

Severe rash, or rash accompanied by fever, general malaise, and musculoskeletal pain.

Mucosal lesions (oral blisters/ulcers), conjunctivitis, and facial edema.

Symptoms such as dyspnea (difficulty breathing) and angioedema.

If relevant symptoms occur, discontinue the drug immediately and seek medical attention; liver function indicators must be monitored.

Hepatic Dysfunction

Hepatotoxicity may occur during treatment, independent of underlying liver disease.

Regular monitoring of liver enzyme levels is recommended.

If symptoms of liver injury (such as nausea, vomiting, abdominal pain, jaundice, or tea-colored urine) appear, discontinue the drug immediately.

Medication Monitoring for Cabotegravir

Routine Monitoring Items

Viral Load: Ensure HIV-1 RNA remains < 50 copies/mL.

Liver Function: Conduct regular ALT/AST tests at baseline and during treatment.

Mental State Assessment: Especially for patients with a history of depression.

Special Genotype Monitoring

Enhanced monitoring is required for patients with HIV-1 subtype A1 and the integrase L74I substitution, as this population has a higher rate of treatment failure.

When virological failure occurs, drug resistance testing should be performed promptly.