← Search & browse all drugs
ANTIINFECTIVES FOR SYSTEMIC USE › ANTIVIRALS FOR SYSTEMIC USE › DIRECT ACTING ANTIVIRALS › Protease inhibitors
ensitrelvir
J05AE16
Adult Dosing
- COVID-19: 375 mg (three 125 mg tablets) orally once daily on day 1, followed by 125 mg orally once daily on days 2 through 5 (initiated within 5 days of symptom onset)
Pediatric Dosing
- Safety and efficacy not established in pediatric patients under 12 years of age or weighing less than 40 kg
- Adolescents (12 years and older, weighing 40 kg or more): Same as adult dosing
Indications
- Treatment of SARS-CoV-2 infection (COVID-19)
Mechanism of Action
- Inhibits the SARS-CoV-2 3C-like protease (3CLpro), preventing viral replication
Contraindications
- Known hypersensitivity to ensitrelvir or any of its components
- Concomitant use with strong CYP3A inducers
- Pregnancy or plans to become pregnant
- Patients requiring concurrent administration of certain drugs dependent on CYP3A for clearance and for whom elevated concentrations are associated with serious/life-threatening events
Adverse Reactions
- Dysgeusia
- Diarrhea
- Headache
- Nausea
- Decreased high-density lipoprotein (HDL)
- Increased serum triglycerides
Drug Interactions
- Strong CYP3A inducers (e.g., rifampin, carbamazepine, St. John's wort) significantly decrease ensitrelvir plasma concentrations
- CYP3A substrates (e.g., midazolam, statins) may have increased exposure, potentially increasing toxicity
- Hormonal contraceptives may have reduced efficacy; alternative non-hormonal contraception recommended during treatment
- Potential interactions with P-glycoprotein and BCRP substrates
Curated Content: Needs Vetting Before Put to Clinical Use