Lenacapavir

SUNLENCA, a human immunodeficiency virus type 1 (HIV-1) capsid inhibitor, is indicated: in combination with other antiretroviral(s), for the treatment of HIV-1 infection in heavily treatment-experienced adults with multidrug resistant HIV-1 whose current antiretroviral regimen is failing due to resistance, intolerance, or safety considerations. for oral loading as a component of the initiation regimen for BIXLENVO (bictegravir [BIC]/lenacapavir [LEN]), a complete regimen for the treatment of HIV-1 infection, in adults to replace the current antiretroviral regimen in those who are virologically suppressed (HIV-1 RNA less than 50 copies per mL) on a stable antiretroviral regimen with no known or suspected resistance to the individual components of BIXLENVO.

SUNLENCA is an HIV-1 antiretroviral agent.

Recommended dosage in heavily treatment-experienced adults: Initiation with one of two options followed by once every 6 months maintenance injection dosing. Tablets may be taken without regard to food. Initiation Option 1 Day 1 927 mg by subcutaneous injection (2 × 1.5 mL injections) 600 mg orally (2 × 300 mg tablets) Day 2 600 mg orally (2 × 300 mg tablets) Initiation Option 2 Day 1 600 mg orally (2 × 300 mg tablets) Day 2 600 mg orally (2 × 300 mg tablets) Day 8 300 mg orally (1 × 300 mg tablet) Day 15 927 mg by subcutaneous injection (2 × 1.5 mL injections) Maintenance 927 mg by subcutaneous injection (2 × 1.5 mL injections) every 6 months (26 weeks) from the date of the last injection +/-2 weeks. Recommended dosage for oral loading for initiation of BIXLENVO: Refer to Table 3 of the full prescribing information for dosing schedule.

Concomitant administration of SUNLENCA with strong CYP3A inducers is contraindicated due to decreased lenacapavir plasma concentrations, which may result in the loss of therapeutic effect and development of resistance to SUNLENCA. Concomitant administration of SUNLENCA is contraindicated with strong CYP3A inducers.

Immune reconstitution syndrome: May necessitate further evaluation and treatment. Residual concentrations of lenacapavir may remain in systemic circulation for up to 12 months or longer. Counsel patients regarding the dosing schedule, non-adherence could lead to loss of virologic response and development of resistance. May increase exposure and risk of adverse reactions to drugs primarily metabolized by CYP3A initiated within 9 months after the last subcutaneous dose of SUNLENCA. If discontinued, initiate an alternative, fully suppressive antiretroviral regimen where possible no later than 28 weeks after the final injection of SUNLENCA. If virologic failure occurs, switch to an alternative regimen if possible. Injection site reactions may occur, and nodules and indurations may be persistent.

The following adverse reactions are discussed in other sections of the labeling: Immune Reconstitution Syndrome Injection Site Reactions. Most common adverse reactions (incidence greater than or equal to 3%, all grades) are nausea and injection site reactions.

Consult the Full Prescribing Information prior to and during treatment for important drug interactions. Effect of Other Drugs on SUNLENCA Lenacapavir is a substrate of P-gp, UGT1A1, and CYP3A. Strong or Moderate CYP3A Inducers Drugs that are strong or moderate inducers of CYP3A may significantly decrease plasma concentrations of lenacapavir, which may result in loss of therapeutic effect of SUNLENCA and development of resistance. Concomitant administration of SUNLENCA with strong CYP3A inducers during SUNLENCA treatment is contraindicated. Concomitant administration of SUNLENCA with moderate CYP3A inducers during SUNLENCA treatment is not recommended. Combined P-gp, UGT1A1, and Strong CYP3A Inhibitors Combined P-gp, UGT1A1, and strong CYP3A inhibitors may significantly increase plasma concentrations of SUNLENCA.

Store bottle and blister packs at 20 °C – 25 °C (68 °F – 77 °F), excursions permitted to 15 °C – 30 °C (59 °F – 86 °F). Store at 20 °C to 25 °C (68 °F to 77 °F), excursions permitted between 15 °C to 30 °C (59 °F to 86 °F). Dispense and store only in original bottle or blister pack. Keep the vials in the original carton until just prior to preparation of the injections in order to protect from light.