Lenacapavir Tablets
来那卡帕韦片
Strength: 300 mg
Pack size: 5 tablets/box
Lenacapavir is a long-acting HIV-1 capsid inhibitor. It acts at multiple stages of the HIV-1 replication cycle by binding directly to the HIV-1 capsid protein.
Lenacapavir interferes with capsid-mediated nuclear uptake of viral DNA, virus assembly and release, and the formation of a functional capsid core. This helps reduce the amount of HIV-1 in the blood.
Lenacapavir tablets must be used in combination with other antiretroviral medicines. They must not be used alone, because monotherapy may lead to the development of drug resistance.
It is indicated, in combination with other antiretroviral medicines, for the treatment of HIV-1 infection in heavily treatment-experienced adults with multidrug-resistant HIV-1 whose current antiretroviral regimen is failing because of resistance, intolerance or safety considerations.
Active ingredient
Each film-coated tablet contains 300 mg of lenacapavir, equivalent to 306.8 mg of lenacapavir sodium.
Chemical formula
Lenacapavir: C₃₉H₃₂ClF₁₀N₇O₅S₂
Lenacapavir sodium: C₃₉H₃₁ClF₁₀N₇NaO₅S₂
Molecular weight
Lenacapavir sodium: 990.3 g/mol
Water solubility
Lenacapavir sodium is practically insoluble in water.
Appearance
Brown, round, film-coated tablets.
Storage
Store at 20°C–25°C. Excursions between 15°C and 30°C are permitted.
Keep the tablets in the original package and protect them from moisture. Keep out of the reach of children.
Excipients
Copovidone, croscarmellose sodium, magnesium stearate, mannitol, microcrystalline cellulose and poloxamer 407.
The film coating may contain polyvinyl alcohol, polyethylene glycol, talc, titanium dioxide and iron oxides.
● Take lenacapavir tablets exactly as prescribed by the physician.
● Swallow the tablets whole with water. The tablets may be taken with or without food.
● Lenacapavir must always be taken together with an appropriate combination of other antiretroviral medicines.
● Do not stop taking lenacapavir or the accompanying antiretroviral medicines without consulting the physician.
● If a dose is missed or vomiting occurs after administration, contact the treating physician or HIV specialist. Do not take an additional dose unless instructed.
● Inform the physician about all prescription medicines, non-prescription medicines, traditional medicines and herbal products being used.
● Do not use lenacapavir together with strong CYP3A-inducing medicines, such as rifampicin, carbamazepine, phenytoin or St. John’s wort, because these medicines may significantly reduce lenacapavir concentrations and cause loss of antiviral effect.
For the 5-tablet initiation pack, the recommended oral dosing schedule is:
● Day 1: Take 600 mg orally — two 300 mg tablets.
● Day 2: Take 600 mg orally — two 300 mg tablets.
● Day 8: Take 300 mg orally — one 300 mg tablet.
● Day 15: Receive 927 mg of lenacapavir by subcutaneous injection, administered as two 1.5 mL injections by a healthcare professional.
● Maintenance treatment consists of 927 mg by subcutaneous injection every 6 months, in combination with other antiretroviral medicines.
● Do not change the dose, delay a scheduled injection or repeat the initiation regimen without medical instructions.
This 5-tablet pack provides the complete oral initiation doses for Days 1, 2 and 8. Reference: current DailyMed dosing information
The most commonly reported adverse reactions include nausea and injection-site reactions when lenacapavir injection is administered. Injection-site reactions may include pain, redness, swelling, firmness or nodules.
Other possible reactions may include diarrhea, headache or general discomfort.
Patients are advised to follow these precautions:
● Take the medicine strictly according to the prescribed schedule.
● Do not use lenacapavir alone. Continue all accompanying antiretroviral medicines as instructed.
● Seek medical attention immediately if signs of a severe allergic reaction occur, such as facial swelling, difficulty breathing, severe rash or dizziness.
● Contact the physician if injection-site pain, swelling, redness or nodules become severe or persistent.
● Tell the physician immediately if symptoms such as fever, swollen lymph nodes, weakness or worsening of a previous infection occur after starting treatment. These may be signs of immune reconstitution inflammatory syndrome.
● Avoid medicines or herbal products that may interact with lenacapavir unless approved by the physician.
● Keep all scheduled follow-up visits and six-monthly injection appointments. Delayed or discontinued treatment may increase the risk of HIV-1 resistance.
Important: Lenacapavir controls HIV-1 infection but does not cure HIV/AIDS. It must be used under the supervision of an experienced healthcare professional.
