Sunlenca

Generic name: lenacapavir

Drug class: HIV capsid inhibitor

Dosage form: 300 mg oral tablet; 463.5 mg/1.5 mL subcutaneous injection

Route of administration: Oral; subcutaneous injection

Dose:

• Initiation Option 1: Day 1: 600 mg orally (2 x 300 mg tablets) and 927 mg by subcutaneous injection; Day 2: 600 mg orally (2 x 300 mg tablets); Maintenance: 927 mg by subcutaneous injection every 26 weeks ± 2 weeks from the date of the last injection.
• Initiation Option 2: Day 1: 600 mg orally (2 x 300 mg tablets); Day 2: 600 mg orally (2 x 300 mg tablets); Day 8: 300 mg orally (1 x 300 mg tablet); Day 15: 927 mg by subcutaneous injection; Maintenance: 927 mg by subcutaneous injection every 26 weeks ± 2 weeks from the date of the last injection.

Mechanism of action: Lenacapavir inhibits HIV-1 replication by binding to the capsid protein, disrupting multiple stages of the viral lifecycle, including uncoating, reverse transcription, and nuclear import, thereby preventing the virus from replicating effectively.

Drug usage cases:

• Treatment of HIV-1 infection in heavily treatment-experienced adults with multi-drug resistant HIV-1 infection failing their current antiretroviral regimen due to resistance, intolerance, or safety considerations.

Drug contraindications:

• Concomitant administration with strong CYP3A inducers.

Side effects:

• Injection site reactions (65% incidence): swelling, pain, redness, skin hardening, small mass or lump, and itching.
• Nausea (4% incidence).

Warnings:

• Immune reconstitution syndrome, including the occurrence of autoimmune disorders with variable time to onset, has been reported in patients treated with combination antiretroviral therapy.
• Residual concentrations of lenacapavir may remain in the systemic circulation of patients for up to 12 months or longer. Lenacapavir may increase exposure, and potential risk of adverse reactions, to drugs primarily metabolized by CYP3A initiated within 9 months after the last injection. Counsel patients regarding the dosing schedule because nonadherence could lead to loss of virologic response and development of resistance. If virologic failure occurs, switch to an alternative regimen if possible. If discontinuing lenacapavir, begin alternate suppressive antiretroviral regimen within 28 weeks from the last injection.

Use during pregnancy or breastfeeding: The safety and efficacy of lenacapavir during pregnancy and breastfeeding have not been established. It is recommended that pregnant women and breastfeeding mothers consult their healthcare provider to discuss potential risks and benefits before initiating treatment with lenacapavir.