lenacapavir sodium: clinical use

Prescribing considerations

• Prescribing and administration should be led by clinicians experienced in HIV management.
• Confirm that a suppressive regimen cannot otherwise be constructed.
• Assess the ability to attend injection visits; poor adherence risks viral rebound and capsid-inhibitor resistance.
• Review all medicines for CYP3A, P-gp and UGT1A1 interactions, including interactions that may persist after stopping the injection.
• Safety and efficacy are not established in people under 18 years.

Contraindications and cautions

• Hypersensitivity to lenacapavir or a formulation excipient.
• Co-administration with strong CYP3A, P-gp and UGT1A1 inducers, including rifampicin, carbamazepine, phenytoin and St John's wort.
• Use caution where evidence is absent in end-stage renal disease or severe hepatic impairment.

Monitoring

• HIV-1 RNA response, adherence and evidence of virological failure or resistance.
• Injection sites, particularly persistent nodules, induration, ulceration or necrosis.
• Symptoms of immune reconstitution inflammatory syndrome and opportunistic infection.
• New or changed medicines for clinically significant interactions.

Clinical pharmacology

Lenacapavir is a multistage HIV-1 capsid inhibitor and a substrate of CYP3A, P-gp and UGT1A1. It moderately inhibits CYP3A and inhibits P-gp. Slow release from the subcutaneous depot produces prolonged exposure, with residual concentrations remaining after treatment stops.

Formulation and product differences

• Film-coated tablets may be taken with or without food and must be swallowed whole.
• The injection is a clear yellow-to-brown solution administered subcutaneously into separate abdominal sites by a healthcare professional.
• Injection-site nodules and induration may persist because the formulation creates a subcutaneous depot.

Tablet

Route: Oral

Strengths: 300 mg

Injection

Route: Parenteral

Strengths: 464 mg