Sunlenca
(lenacapavir)Dosage & Administration
| 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. | |
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Sunlenca Prescribing Information
SUNLENCA, in combination with other antiretroviral(s), is indicated for the treatment of human immunodeficiency virus type 1 (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.
Adherence to Treatment Regimen
Prior to starting SUNLENCA, healthcare providers should carefully select patients who agree to the required every 6 month injection dosing schedule and counsel patients about the importance of adherence to scheduled SUNLENCA dosing visits and concomitant oral antiretroviral therapy to help maintain viral suppression and reduce the risk of viral rebound and potential development of resistance with missed doses [see Warnings and Precautions (5.2), Microbiology (12.4)].
Recommended Dosage
SUNLENCA can be initiated using one of the two recommended dosage regimens in Table 1 and Table 2 below. Maintenance dosing is administered by subcutaneous injection every 6 months regardless of the initiation regimen. Healthcare providers should determine the appropriate initiation regimen for the patient. SUNLENCA oral tablets may be taken with or without food [see Clinical Pharmacology (12.3)].
| Treatment Time | |
|---|---|
| |
| Dosage of SUNLENCA: Initiation | |
| 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) |
| Dosage of SUNLENCA: Maintenance | |
| Every 6 months (26 weeks) * +/-2 weeks | 927 mg by subcutaneous injection (2 × 1.5 mL injections) |
| Treatment Time | |
|---|---|
| |
| Dosage of SUNLENCA: Initiation | |
| 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) |
| Dosage of SUNLENCA: Maintenance | |
| Every 6 months (26 weeks) * +/-2 weeks | 927 mg by subcutaneous injection (2 × 1.5 mL injections) |
Recommended Dosing Schedule for Missed Dose
Planned Missed Injections
During the maintenance period, if a patient plans to miss a scheduled 6-month injection visit by more than 2 weeks, SUNLENCA tablets may be taken for up to 6 months until injections resume. Refer to Table 3 below for the recommended dosage after planned missed injections.
| Time since Last Injection | Recommendation |
|---|---|
| 26 to 28 weeks | Maintenance oral dosage of 300 mg taken once every 7 days for up to 6 months. Resume the maintenance injection dosage within 7 days after the last oral dose. |
Unplanned Missed Injections
Patients who miss a scheduled injection visit should be clinically reassessed, including consideration of lenacapavir resistance testing, to ensure resumption of therapy remains appropriate. During the maintenance period, if more than 28 weeks have elapsed since the last injection and SUNLENCA tablets have not been taken, see Table 4 below for the recommended dosage after unplanned missed injections. Adherence to the injection dosing schedule is strongly recommended [see Dosage and Administration (2.1) and Microbiology (12.4)].
| Time since Last Injection | Recommendation |
|---|---|
| More than 28 weeks | Reinitiate with Option 1 (Table 1) or Option 2 (Table 2) and then continue with maintenance injection dosing. |
Preparation and Administration of Subcutaneous Injection
SUNLENCA injection is only for subcutaneous administration into the abdomen by a healthcare provider. Do NOT administer intradermally due to risk of serious injection site reactions [see Warnings and Precautions (5.3)].
Use aseptic technique. Visually inspect the solution in the vials and prepared syringe for particulate matter and discoloration prior to administration. SUNLENCA injection is a yellow solution. Do not use SUNLENCA injection if the solution is discolored or if it contains particulate matter. Once the solution is withdrawn from the vials, the subcutaneous injections should be administered as soon as possible [see How Supplied/Storage and Handling (16)].
There are two available injection kits, which differ only in how SUNLENCA injection is prepared (the components and associated method for withdrawal of the solution from the vials) [see How Supplied/Storage and Handling (16)]. Refer to the figures below for the relevant injection kit.
The injection kit components are for single use only. Two 1.5 mL injections are required for a complete dose.
Vial access device injection kit
Figure 1 identifies the components for use in the administration steps for the vial access device injection kit, and the administration steps are provided in Figure 2. Use of a vial access device is required in this kit.
Figure 1 SUNLENCA Vial Access Device Injection Kit Components
Figure 2 SUNLENCA Injection Steps for Vial Access Device Injection Kit
Withdrawal needle injection kit
Figure 3 identifies the components for use in the administration steps for the withdrawal needle injection kit, and the administration steps are provided in Figure 4. The 18-gauge needle is for withdrawal only in this kit.
Figure 3 SUNLENCA Withdrawal Needle Injection Kit Components
Figure 4 SUNLENCA Injection Steps for Withdrawal Needle Injection Kit
SUNLENCA tablets: Each tablet contains 300 mg of lenacapavir (present as 306.8 mg of lenacapavir sodium). The tablets are beige, capsule-shaped, film-coated, and debossed with 'GSI' on one side of the tablet and '62L' on the other side of the tablet.
SUNLENCA injection: Each single-dose vial contains 463.5 mg/1.5 mL (309 mg/mL) of lenacapavir (present as 473.1 mg/1.5 mL of lenacapavir sodium). The lenacapavir injectable solution is sterile, preservative-free, clear, and yellow with no visible particles.
Pregnancy
Pregnancy Exposure Registry
There is a pregnancy exposure registry that monitors pregnancy outcomes in individuals exposed to SUNLENCA during pregnancy. Healthcare providers are encouraged to register patients by calling the Antiretroviral Pregnancy Registry (APR) at 1-800-258-4263.
Risk Summary
There are insufficient human data on the use of SUNLENCA during pregnancy to inform a drug-associated risk of birth defects and miscarriage. In animal reproduction studies, no adverse developmental effects were observed when lenacapavir was administered to rats and rabbits at exposures (AUC) ≥16 times the exposure in humans at the recommended human dose (RHD) of SUNLENCA (see Data).
The background risk of major birth defects and miscarriage for the indicated population is unknown. The background rate of major birth defects in a U.S. reference population of the Metropolitan Atlanta Congenital Defects Program (MACDP) is 2.7%. The rate of miscarriage is not reported in the APR. The estimated background rate of miscarriage in clinically recognized pregnancies in the U.S. general population is 15 to 20%.
Data
Animal Data
Lenacapavir was administered intravenously to pregnant rabbits (up to 20 mg/kg/day on gestation days (GD) 7 to 19), orally to rats (up to 300 mg/kg/day on GD 6 to 17), and subcutaneously to rats (up to 300 mg/kg on GD 6). No significant toxicological effects on embryo-fetal (rats and rabbits) or pre/postnatal (rats) development were observed at exposures (AUC) approximately 16 times (rats) and 39 times (rabbits) the exposure in humans at the RHD of SUNLENCA.
Lactation
Risk Summary
It is not known whether SUNLENCA is present in human breast milk, affects human milk production, or has effects on the breastfed infant. After administration to pregnant rats, lenacapavir was detected in the plasma of nursing rat pups, without effects on these nursing pups (see Data).
Potential risks of breastfeeding include: (1) HIV-1 transmission (in infants without HIV-1), (2) developing viral resistance (in infants with HIV-1), and (3) adverse reactions in a breastfed infant similar to those seen in adults.
Data
Lenacapavir was detected at low levels in the plasma of nursing rat pups in the pre/postnatal development study (post-natal day 10).
Pediatric Use
The safety and effectiveness of SUNLENCA have not been established in pediatric patients.
Geriatric Use
Clinical studies of SUNLENCA did not include sufficient numbers of participants aged 65 and over to determine whether they respond differently from younger patients.
Renal Impairment
No dosage adjustment of SUNLENCA is recommended in patients with mild, moderate or severe renal impairment (estimated creatinine clearance greater than or equal to 15 mL per minute). SUNLENCA has not been studied in patients with ESRD (estimated creatinine clearance less than 15 mL per minute) [see Clinical Pharmacology (12.3)].
Hepatic Impairment
No dosage adjustment of SUNLENCA is recommended in patients with mild (Child-Pugh Class A) or moderate (Child-Pugh Class B) hepatic impairment. SUNLENCA has not been studied in patients with severe hepatic impairment (Child-Pugh Class C) [see Clinical Pharmacology (12.3)].
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 [see Drug Interactions (7.1)].
Immune Reconstitution Syndrome
Immune reconstitution syndrome has been reported in patients treated with combination antiretroviral therapy. During the initial phase of combination antiretroviral treatment, patients whose immune system responds may develop an inflammatory response to indolent or residual opportunistic infections [such as Mycobacterium avium infection, cytomegalovirus, Pneumocystis jirovecii pneumonia (PCP), or tuberculosis], which may necessitate further evaluation and treatment.
Autoimmune disorders (such as Graves' disease, polymyositis, Guillain-Barré syndrome, and autoimmune hepatitis) have also been reported to occur in the setting of immune reconstitution; however, the time to onset is more variable, and can occur many months after initiation of treatment.
Long-Acting Properties and Potential Associated Risks with SUNLENCA
Residual concentrations of lenacapavir may remain in the systemic circulation of patients for prolonged periods (up to 12 months or longer after the last subcutaneous dose). It is important to counsel patients that maintenance dosing by injection is required every 6 months, because missed doses or non-adherence to injections could lead to loss of virologic response and development of resistance [see Dosage and Administration (2.1)].
Lenacapavir, a moderate CYP3A inhibitor, may increase the exposure to, and therefore potential risk of adverse reactions from, drugs primarily metabolized by CYP3A initiated within 9 months after the last subcutaneous dose of SUNLENCA [see Drug Interactions and Clinical Pharmacology (7.2, 12.3)].
If SUNLENCA is discontinued, to minimize the potential risk of developing viral resistance, it is essential to initiate an alternative, fully suppressive antiretroviral regimen where possible no later than 28 weeks after the final injection of SUNLENCA. If virologic failure occurs during treatment, switch the patient to an alternative regimen if possible [see Dosage and Administration (2.1)].
Injection Site Reactions
Administration of SUNLENCA may result in local injection site reactions (ISRs). If clinically significant ISRs occur, evaluate and institute appropriate therapy and follow-up.
Manifestations of ISRs may include swelling, pain, erythema, nodule, induration, pruritus, extravasation or mass. Nodules and indurations at the injection site may take longer to resolve than other ISRs. In clinical studies, after a median follow-up of 553 days, 30% of nodules and 13% of indurations (in 10% and 1% of participants, respectively) associated with the first injections of SUNLENCA had not fully resolved. Measurements and qualitative assessments of ISRs were not routinely reported. Where described, the majority of the injection site nodules and indurations were palpable but not visible, and had a maximum size of approximately 1 to 4 cm [see Adverse Reactions (6.1)].
The mechanism driving the persistence of injection site nodules and indurations in some patients is not fully understood, but based on available data, they may be related to the presence of the subcutaneous drug depot. In some patients who had a skin biopsy performed of an injection site nodule or induration, dermatopathology revealed foreign body inflammation or granulomatous response.
Improper administration (intradermal injection) has been associated with serious injection site reactions, including necrosis and ulcer [see Adverse Reactions (6)]. Ensure SUNLENCA is only administered subcutaneously in the abdomen [see Dosage and Administration (2.4)].