【INDICATIONS AND USAGE 】
LuciLena, a human immunodeficiency virus type 1 (HIV-1) capsid inhibitor, is indicated for the following two conditions:
1. HIV-1 Treatment: In combination with other antiretroviral(s), for the treatment of HIV-1 infection in adults who: have multidrug-resistant HIV-1; are heavily treatment-experienced; and whose current antiretroviral regimen is failing due to resistance, intolerance, or safety considerations.
2. HIV-1 Pre-Exposure Prophylaxis (PrEP): To reduce the risk of sexually acquired HIV-1 in adults and adolescents weighing at least 35 kg who are at risk for HIV-1 acquisition. Note: Individuals must have a negative HIV-1 test prior to initiating LuciLena.
【DOSAGE AND ADMINISTRATION】
Pre-Screening: For PrEP, screen all individuals for HIV-1 infection and confirm negative status prior to initiation and prior to each injection. The recommended dosage regimen consists of an initiation period and a maintenance period:
· Initiation Period (Indication Specific):
o Option 1 (For Treatment & PrEP): On Day 1, 927 mg by subcutaneous injection (2 x 1.5 mL) and 600 mg orally (2 x 300 mg tablets); On Day 2, 600 mg orally (2 x 300 mg tablets).
o Option 2 (For Treatment ONLY): On Day 1 and Day 2, 600 mg orally each day; On Day 8, 300 mg orally; On Day 15, 927 mg by subcutaneous injection (2 x 1.5 mL).
· Maintenance Period: 927 mg by subcutaneous injection (2 x 1.5 mL) every 6 months (26 weeks) from the date of the last injection +/- 2 weeks.
· Planned Missed Injections (Oral Bridging): If a scheduled injection is delayed by > 2 weeks, oral tablets may be used for bridging for up to 6 months. (For PrEP: The delayed injection dosage is 300 mg orally once every 7 days ).
· Unplanned Missed Injections: If > 28 weeks have elapsed since the last injection without oral bridging, restart initiation from Day 1 if clinically appropriate.
· Administration Limitations: Tablets may be taken with or without food. The injection is ONLY for subcutaneous administration (abdomen or thigh) by a healthcare provider; do NOT administer intradermally to avoid serious injection site reactions
【DOSAGE FORMS AND STRENGTHS】
Injection: Single-dose pre-filled syringe (PFS), 463.5 mg/1.5 mL (309 mg/mL).
【CONTRAINDICATIONS】
For Treatment & PrEP: Concomitant administration is contraindicated with strong CYP3A inducers.
For PrEP ONLY: Unknown or positive HIV-1 status.
【WARNINGS AND PRECAUTIONS】
Risk of Resistance (PrEP): Drug-resistant HIV-1 variants have been identified with the use of lenacapavir in individuals with undiagnosed HIV-1 infection. Individuals who acquire HIV-1 while receiving PrEP must immediately transition to a complete treatment regimen.
Immune Reconstitution Syndrome: May necessitate further evaluation and treatment in HIV-1 infected patients.
Long-Acting Properties: Residual concentrations may remain in the systemic circulation for up to 12 months or longer. May increase exposure and risk of adverse reactions to drugs primarily metabolized by CYP3A initiated within 9 months after the last subcutaneous dose.
Injection Site Reactions: Local reactions may occur, and nodules and indurations may be persistent. Improper administration (intradermal) has been associated with severe reactions (necrosis/ulcer).
【ADVERSE REACTIONS】
The most common adverse reactions (incidence >= 5%) are injection site reactions, headache, and nausea.
【DRUG INTERACTIONS】
CYP3A Inducers: Strong or moderate CYP3A inducers may significantly decrease the plasma concentration. Contraindicated with strong inducers; not recommended with moderate inducers. (Dosage modifications are required if co-administration is necessary ).
Combined Inhibitors: Combined P-gp, UGT1A1, and strong CYP3A inhibitors may significantly increase the plasma concentration; concomitant administration is not recommended.
【USE IN SPECIFIC POPULATIONS】
Pregnancy and Lactation: Lenacapavir is present in human milk. No adverse effects in breastfed infants have been observed. The developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for LuciLena.
Pediatric Use: Safety and effectiveness for PrEP have been established in adolescents weighing at least 35 kg. Safety and effectiveness for Treatment have not been established in pediatric patients.
Renal and Hepatic Impairment: No dosage adjustment is required in patients with mild, moderate, or severe renal impairment (CrCl >= 15 mL/min) or mild to moderate hepatic impairment.
【STORAGE】
Store at 20°C to 25°C, excursions permitted to 15°C to 30°C. Protect from light (keep in the original carton until just prior to preparation).