bictegravir sodium + emtricitabine + tenofovir alafenamide fumarate: clinical use

Prescribing considerations

• Confirm HIV-1 treatment and resistance history.
• Review renal and hepatic function, HIV/HBV coinfection, pregnancy status and interacting products.
• Significant renal impairment, end-stage renal disease, severe hepatic impairment and paediatric renal impairment require product-specific assessment.
• Consider mental-health history because suicidal ideation and attempts have been reported, particularly with pre-existing psychiatric illness.

Contraindications and cautions

• Hypersensitivity to an active substance or excipient.
• Concurrent rifampicin.
• Concurrent St John’s wort.

Monitoring

• HIV viral load and clinical response; assess resistance if virological failure is suspected.
• Renal function before or at initiation and during treatment as clinically appropriate.
• Liver function and HBV status, with prolonged follow-up after stopping in HIV/HBV coinfection.
• Weight, blood lipids and glucose as clinically appropriate.
• Closer viral-load monitoring during pregnancy.
• Bone health when clinically indicated in children.

Clinical pharmacology

Bictegravir inhibits integrase and is metabolised through CYP3A and UGT1A1 pathways. Emtricitabine and intracellular tenofovir diphosphate inhibit reverse transcriptase and terminate viral DNA chains. Tenofovir alafenamide is a P-gp/BCRP substrate designed for intracellular tenofovir delivery.

Formulation and product differences

• The selected product is a lower-strength, pink, capsule-shaped film-coated tablet with a score line to aid swallowing, not to divide it into equal portions.
• The appropriate marketed tablet strength is selected according to age and weight.
• Do not chew or crush the tablet. If split, take both halves immediately and do not store them.
• Keep the moisture-protecting desiccant in the bottle and do not swallow it.

Tablet

Route: Oral

Strengths: 30 mg + 120 mg + 15 mg, 50 mg + 200 mg + 25 mg