emtricitabine + rilpivirine hydrochloride + tenofovir alafenamide fumarate: clinical use

Prescribing considerations

• Confirm HIV-1 viral load and review current or historical resistance results.
• Assess adherence carefully, particularly in adolescents.
• Review renal and hepatic function, hepatitis B status, pregnancy and interacting products.
• Consider lactose content in relevant rare hereditary disorders.

Contraindications and cautions

• Hypersensitivity to an active substance or excipient.
• Concomitant proton-pump inhibitors, specified inducing anticonvulsants, rifamycins, repeated systemic dexamethasone or St John’s wort.
• Avoid in specified severe renal impairment populations; do not use in severe hepatic impairment.
• Not licensed where relevant resistance mutations are known or HIV-1 viral load exceeds the licensed threshold.

Monitoring

• HIV-1 viral load and adherence, particularly during pregnancy.
• Renal function before and during treatment where clinically appropriate.
• Liver function in pre-existing liver disease or viral hepatitis.
• Clinical and laboratory follow-up after discontinuation in HIV/HBV co-infection because hepatitis may flare.
• Weight, blood lipids and glucose as part of routine antiretroviral care.

Clinical pharmacology

Emtricitabine is an NRTI; rilpivirine is a CYP3A-metabolised NNRTI; tenofovir alafenamide is a P-gp/BCRP substrate and intracellular prodrug of tenofovir. Their active metabolites inhibit HIV reverse transcriptase through complementary non-competitive inhibition and DNA-chain termination.

Formulation and product differences

• The fixed-combination product is a grey, capsule-shaped film-coated tablet containing lactose.
• The tablet should not be chewed, crushed or split because of its bitter taste.
• It is essentially sodium-free.

Tablet

Route: Oral

Strengths: 200 mg + 25 mg + 25 mg