Lenacapavir

Lenacapavir is a prescription medicine used for the treatment of HIV-1 infection.

• Lenacapavir is available under the following different brand names: Sunlenca

Common side effects of Lenacapavir include:

• headache,
• dizziness, and
• sore throat

Serious side effects of Lenacapavir include:

• hives,
• difficulty breathing,
• swelling of the face, lips, tongue, or throat,
• anxiety,
• tremors,
• increased sensitivity to heat,
• weight loss,
• puffy eyes,
• enlarged thyroid,
• muscle pain,
• muscle stiffness,
• muscle weakness,
• joint pain and stiffness,
• difficulty swallowing,
• trouble catching your breath,
• irregular heartbeats,
• difficulty walking,
• problems with coordination,
• difficulty speaking,
• shortness of breath,
• slow reflexes,
• little or no urination,
• facial muscle weakness,
• fatigue,
• abdominal pain or cramping,
• yellowing of the skin and eyes (jaundice),
• nausea,
• vomiting,
• loss of appetite,
• rash,
• loss of menstrual periods, and
• swollen blood vessels in the skin

Rare side effects of Lenacapavir include:

• none

Seek medical care or call 911 at once if you have the following serious side effects:

• Severe headache, confusion, slurred speech, arm or leg weakness, trouble walking, loss of coordination, feeling unsteady, very stiff muscles, high fever, profuse sweating, or tremors;
• Serious eye symptoms such as sudden vision loss, blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights;
• Serious heart symptoms include fast, irregular, or pounding heartbeats; fluttering in the chest; shortness of breath; sudden dizziness, lightheadedness, or passing out. 

This is not a complete list of side effects and other serious side effects or health problems that may occur because of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

Adult dosage

Injection, solution

• 463.5 mg/1.5 mL (309 mg/mL) single-dose vial
• Each kit contains 2 single-dose vials, each containing sufficient volume to provide 927 mg dose

Tablet

• 300 mg

HIV-1 Infection

Adult dosage

• Dose option 1
• Initiation
  • Day 1: 927 mg SC plus 600 mg orally
  • Day 2: 600 mg orally
• Maintenance
  • Every 6 months (26 weeks from last injection) +/- 2 weeks: 927 mg SC
• Dose option 2
• Initiation
  • Day 1: 600 mg orally
  • Day 2: 600 mg orally
  • Day 8: 300 mg orally 
  • Day 15: 927 mg SC
• Maintenance
• Every 6 months (26 weeks from last injection) +/- 2 weeks: 927 mg SC

Dosage Considerations – Should be Given as Follows: 

• See “Dosages”

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider, or pharmacist first.

• Lenacapavir has severe interactions with the following drugs:
  • apalutamide
  • carbamazepine
  • enzalutamide
  • lumacaftor/ivacaftor
  • mitotane
  • phenytoin
  • primidone
  • rifampin
  • St John's Wort
• Lenacapavir has serious interactions with at least 42 other drugs.
• Lenacapavir has moderate interactions with at least 23 other drugs.
• Lenacapavir has minor interactions with no other drugs.

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drug interactions. Therefore, before using this product, tell your doctor or pharmacist about all your products. Keep a list of all your medications with you and share this information with your doctor and pharmacist. Check with your healthcare professional or doctor for additional medical advice, or if you have health questions or concerns.

Contraindications

• Coadministration with strong CYP3A inducers

Effects of drug abuse

• None

Short-Term Effects

• See “What Are Side Effects Associated with Using Lenacapavir?”

Long-Term Effects

• See “What Are Side Effects Associated with Using Lenacapavir?”

Cautions

• Residual concentrations of lenacapavir may remain in systemic circulation for prolonged periods (above 12 months after the last SC dose); counsel patients that maintenance dosing by injection is required every 6 months because missed doses or nonadherence could lead to loss of virologic response and development of resistance
• Local injection site reaction may occur, manifested by swelling, pain, erythema, nodule, induration, pruritus, extravasation, or mass
• Immune reconstitution syndrome
  • Immune reconstitution syndrome reported; during the initial phase of combination antiretroviral therapy (ART), patients whose immune system responds may develop an inflammatory response to indolent or residual opportunistic infections (eg, MAC, CMV, PCP, TB), which will likely require treatment
  • Autoimmune disorders (eg, Grave disease, polymyositis, Guillain-Barré syndrome, autoimmune hepatitis) also reported
• Drug interaction overview
  • Substrate of P-gp, UGT1A1 (minor), and CYP3A (minor)
  • Moderate CYP3A inhibitor
  • Strong CYP3A inducers
• Contraindicated
  • Coadministration of strong CYP3A inducers (eg, carbamazepine, phenytoin, rifampin, St. John’s wort) decreases lenacapavir plasma concentrations, which may result in loss of therapeutic effect and development of resistance
• Moderate CYP3A inducers
  • Not recommended
    • Coadministration of moderate CYP3A inducers (eg, oxcarbazepine, phenobarbital, efavirenz, nevirapine, tipranavir/ritonavir, rifabutin, rifapentine) may decrease lenacapavir plasma concentrations
• Combined P-gp, UGT1A1, and strong CYP3A inhibitors
  • Not recommended
    • Drugs that inhibit P-gp, UGT1A1, and strongly inhibit CYP3A (eg, atazanavir/cobicistat, atazanavir/ritonavir) may significantly increase lenacapavir plasma concentrations
• CYP3A substrates
  • Modify therapy or caution/monitor
  • Owing to the long half-life of lenacapavir SC, coadministration with drugs primarily metabolized by CYP3A may have increased exposure if initiated within 9 months after the last lenacapavir SC dose
  • See prescribing information of sensitive CYP3A substrates (eg, systemic corticosteroids, ergot derivatives) for dosing recommendations with moderate CYP3A inhibitors
• HMG-CoA reductase inhibitors
• Modify dose
  • Coadministration increases lovastatin and simvastatin systemic exposure
  • Initiate lovastatin and simvastatin at the lowest starting dose and titrate carefully while monitoring for safety (eg, myopathy)
  • Opioid analgesics metabolized by CYP3A
  • Decrease dose: Tramadol
  • Careful monitoring: Fentanyl, oxycodone (avoid potentially fatal respiratory depression if coadministered)
  • Narcotic analgesic for the treatment of opioid dependence
  • Effects on buprenorphine or methadone unknown
  • Carefully titrate dependence buprenorphine or methadone dose to desired effect; use the lowest feasible initial or maintenance dose
• Opioid antagonist
  • Avoid coadministration of lenacapavir and naloxegol
  • If unavoidable, decrease naloxegol dose and monitor for adverse effects
• PDE-5 inhibitors
  • Coadministration is not recommended with tadalafil when used for pulmonary hypertension
  • Coadministration with PDE-5 inhibitors when used for erectile dysfunction: Refer to PDE-5 inhibitor prescribing information for dose recommendations
• Sedative/hypnotics
  • Caution/monitor
    • Lenacapavir increases systemic exposure of midazolam or triazolam when coadministered

Pregnancy and Lactation

• There are insufficient data regarding use during pregnancy to inform a drug-associated risk of birth defects and miscarriage
• Healthcare providers are encouraged to register patients by calling the Antiretroviral Pregnancy Registry (APR) at 1-800-258-4263
• Lactation
  • The CDC recommends that HIV-1-infected mothers in the United States not breastfeed their infants to avoid risking postnatal transmission of HIV-1 infection
  • Unknown whether present in human breast milk affects human milk production, or has effects on breastfed infants