Lenacapavir
Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Alen Antony Pathil, M.D.[2]
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Overview
Lenacapavir is a HIV 1 antiretroviral agent that is FDA approved for the treatment of Multidrug-resistant Human Immunodeficiency Virus type 1 (HIV-1) infection among adults.. Common adverse reactions include Immune reconstitution syndrome, and Injection site reaction (swelling, erythema, pruritis, pain, nodule, induration)..
Adult Indications and Dosage
FDA-Labeled Indications and Dosage (Adult)
SUNLENCA along with other antiretroviral drugs are used for treating HIV1 infection among adults with multidrug resistance to their current HIV treatment regimen due to resistance, intolerance, or safety considerations.
There are 2 dosage forms: SUNLENCA tablets: Each tablet contains 300 mg of lenacapavir (present as 306.8 mg of lenacapavir sodium).
SUNLENCA injection (subcutaneous): 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)
Off-Label Use and Dosage (Adult)
Pediatric Indications and Dosage
FDA-Labeled Indications and Dosage (Pediatric)
There is limited information regarding Lenacapavir FDA-Labeled Indications and Dosage (Pediatric) in the drug label.
Off-Label Use and Dosage (Pediatric)
Contraindications
SUNLENCA should not be concomitantly administrated with other CYP3A drugs as it decreases the plasma concentration of SUNLENA and this can lead to loss of the therapeutic efficacy of SUNLENCA or the development of resistance to SUNLENCA.
Warnings
1.Immune Reconstitution Syndrome- During the initial phase in combination with other antiretrovirals, the patient's immune system may should inflammatory response to indolent opportunistic infections like Mycobacterium avium infection, cytomegalovirus, Pneumocystis jirovecii pneumonia (PCP), or tuberculosis, which would required further evaluation and treatment. Autoimmune dissorders like Graves' disease, polymyositis, Guillain-Barré syndrome, and autoimmune hepatitis has also been reported due to immune constitution syndrome.
2.Long-Acting Properties and Potential Associated Risks with SUNLENCA- The residual components of lenacapavir remain in the body for a very long period, such as more than 12 months from the last subcutaneous injection dose. lenacapavir being a CYP3A inhibitor, can lead to a decrease in the efficacy of other drugs metabolized by CYP3A, when taken within the 9 months of the last injection dose. Patients are also counseled on the importance of adherence to the treatment regimen, because missed doses or non-adherence can lead to loss of virologic response and development of resistance.
3.Injection Site Reactions Injection site reactions may manifets as swelling, pain, erythema, nodule, induration, pruritus, extravasation, or mass. Nodules and indurations at the injection site may take longer to resolve than other reactions.
Adverse Reactions
Clinical Trials Experience
- Injection site reactions
- swelling
- pain
- erythema
- nodule
- induration
- pruritis
- extravasation
- mass
- nausea
Postmarketing Experience
There is limited information regarding Lenacapavir Postmarketing Experience in the drug label.
Drug Interactions
Lenacapavir is a substrate of P-gp, UGT1A1, and CYP3A.
- Drugs that are strong or moderate inducers of CYP3A when admisntered concomitantly may decrease the plasma concentration of Lenacapavir causing a decrease in the therapeutic efficacy of Lenacapavir .
- Anticonvulsants:carbamazepine, oxcarbazepine, phenobarbital, phenytoin
- efavirenz, nevirapine, tipranavir/ritonavir
- Antimycobacterials: rifabutin, rifampin, rifapentine
- St. John's wort (Hypericum perforatum)
- Lenacapavir is a moderate inhibitor of CYP3A. SUNLENCA may increase the exposure of drugs primarily metabolized by CYP3A initiated within 9 months after the last subcutaneous dose of SUNLENCA, and due to the long half-life this can lead to potential risk of adverse reactions of these unmetabolized drugs.
- Digoxin
- Direct Oral Anticoagulants (DOACs): Rivaroxaban, Dabigatran, Edoxaban
- Dexamethasone, Hydrocortisone/Cortisone
- Dihydroergotamine, Ergotamine, Methylergonovine
- Lovastatin, Simvastatin
- Fentanyl, Oxycodone
- Tramadol
- Naloxegol
- PDE-5 Inhibitors: Sildenafil, Tadalafil, Vardenafil
- Sedatives/Hypnotics: Midazolam (oral), Triazolam
Use in Specific Populations
Pregnancy
Pregnancy Category (FDA): B
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
Pregnancy Category (AUS):
There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Lenacapavir in women who are pregnant.
Labor and Delivery
There is no FDA guidance on use of Lenacapavir during labor and delivery.
Nursing Mothers
It is not known whether SUNLENCA is present in human breast milk, affects human milk production, or has effects on the breastfed infant. However due to the potential for HIV infection transmission to infants, and developing viral resistance in HIV-positive infants, mothers are advised to refrain from breastfeeding.
Pediatric Use
The safety and effectiveness of SUNLENCA have not been established in pediatric patients.
Geriatic Use
There is no FDA guidance on the use of Lenacapavir in geriatric settings.
Gender
There is no FDA guidance on the use of Lenacapavir with respect to specific gender populations.
Race
There is no FDA guidance on the use of Lenacapavir with respect to specific racial populations.
Renal Impairment
No dosage adjustment of SUNLENCA is recommended in patients with mild, moderate or severe renal impairment
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 haptic impairment.
Females of Reproductive Potential and Males
There is no FDA guidance on the use of Lenacapavir in women of reproductive potentials and males.
Immunocompromised Patients
There is no FDA guidance one the use of Lenacapavir in patients who are immunocompromised.
Administration and Monitoring
Administration
There are 2 options for treatment regimen: Option 1:
- Initiation doaage-
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)
- Maintenance dosage-
Every 6 months (26 weeks) +/-2 weeks - 927 mg by subcutaneous injection (2 × 1.5 mL injections)
Option 2:
- Initiation dosage:
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 dosage-
Every 6 months (26 weeks) * +/-2 weeks 927 mg by subcutaneous injection (2 × 1.5 mL injections)
If a dose has been missed and the time elapsed has been more than 28 weeks from last injection during the maintenance phase, it is advised to restart the initiation dosage regimen from Day 1, using either Option 1 or Option 2.
Monitoring
There is limited information regarding Lenacapavir Monitoring in the drug label.
IV Compatibility
There is limited information regarding the compatibility of Lenacapavir and IV administrations.
Overdosage
No data are available on overdose of SUNLENCA in patients.
Pharmacology
There is limited information regarding Lenacapavir Pharmacology in the drug label.
Mechanism of Action
SUNLENCA tablets and SUNLENCA injection contain lenacapavir sodium which is a capsid inhibitor that directly binds to the interface between capsid protein (p24) subunits in hexamers inhibiting HIV-1 replication.
Structure
Lenacapavir sodium has a molecular formula of C39H31ClF10N7NaO5S2, a molecular weight of 990.3.
It is available in two forms:
- SUNLENCA tablets are for oral administration with each film-coated tablet containing 300 mg of lenacapavir (present as 306.8 mg lenacapavir sodium) and the following inactive ingredients like copovidone, croscarmellose sodium, magnesium stearate, mannitol, microcrystalline cellulose, and poloxamer 407.
- SUNLENCA injection is for subcutaneous administration with each single-dose vial containing 463.5 mg/1.5 mL (309 mg/mL) of lenacapavir (present as 473.1 mg/1.5 mL of lenacapavir sodium) as a sterile, preservative-free, clear, yellow solution and the following inactive ingredients: 896.3 mg of polyethylene glycol 300 (as solvent) and water for injection.
Pharmacodynamics
There is limited information regarding Lenacapavir Pharmacodynamics in the drug label.
Pharmacokinetics
There is limited information regarding Lenacapavir Pharmacokinetics in the drug label.
Nonclinical Toxicology
There is limited information regarding Lenacapavir Nonclinical Toxicology in the drug label.
Clinical Studies
There is limited information regarding Lenacapavir Clinical Studies in the drug label.
How Supplied
SUNLENCA 300mg tablets are packaged as follows: SUNLENCA 4-Tablets™ blister pack contains 4 tablets (NDC 61958-3001-1) SUNLENCA 5-Tablets™ blister pack contains 5 tablets (NDC 61958-3001-2)
SUNLENCA injection is packaged in a dosing kit (NDC 61958-3002-1) containing: 2 single-dose clear glass vials, each containing sufficient volume to allow withdrawal of 463.5 mg/1.5 mL (309 mg/mL) of lenacapavir. The injection solution is sterile, preservative-free, clear, and yellow with no visible particles. Vials are sealed with a stopper and aluminium overseal with flip-off cap. 2 vial access devices, 2 disposable syringes, and 2 injection safety needles for subcutaneous injection (22-gauge, ½ inch).
The injections should be administered as soon as possible once the solution has been drawn into the syringes. Discard any unused portion of the solution.
Storage
SUNLENCA tablets are stored at 20 °C – 25 °C (68 °F – 77 °F), excursions permitted to 15 °C – 30 °C (59 °F – 86 °F).
SUNLENCA injection vials are stored at 20 °C – 25 °C (68 °F – 77 °F), excursions permitted to 15 °C – 30 °C (59 °F – 86 °F).
Images
Drug Images
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Package and Label Display Panel
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Patient Counseling Information
There is limited information regarding Lenacapavir Patient Counseling Information in the drug label.
Precautions with Alcohol
Alcohol-Lenacapavir interaction has not been established. Talk to your doctor regarding the effects of taking alcohol with this medication.
Brand Names
There is limited information regarding Lenacapavir Brand Names in the drug label.
Look-Alike Drug Names
There is limited information regarding Lenacapavir Look-Alike Drug Names in the drug label.
Drug Shortage Status
Price
References
The contents of this FDA label are provided by the National Library of Medicine.