Xocova (ensitrelvir) is filed as SARS-CoV-2 3CL protease inhibitor. The sections below restate public label fields stored for this profile.
1 INDICATIONS AND USAGE XOCOVA is indicated for post-exposure prophylaxis of coronavirus disease 2019 (COVID-19) in adults and adolescents 12 years of age and older following contact with an individual who has COVID-19. XOCOVA, a severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) main protease (M pro : also referred to as 3CL pro or nsp5 protease) inhibitor, is indicated for post-exposure prophylaxis of coronavirus disease 2019 (COVID‑19) in adults and adolescents 12 years of age and older following contact with an individual who has COVID-19. ( 1 )
12.1 Mechanism of Action Ensitrelvir is a severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) antiviral drug [see Microbiology (12.4) ].
5 WARNINGS AND PRECAUTIONS Embryofetal toxicity: Based on animal data, XOCOVA may cause fetal harm. Advise pregnant women and females of reproductive potential that XOCOVA may cause fetal harm. Advise females of reproductive potential to use effective contraception during XOCOVA use and for 2 weeks after the final dose. ( 5.1 , 8.1 , 8.3 ) The concomitant use of XOCOVA and certain other drugs may result in potentially significant drug interactions. Consult the Full Prescribing Information prior to and during treatment for potential drug interactions. ( 5.2 , 7 ) Hypersensitivity reactions, including anaphylaxis, anaphylactic shock, and angioedema, have been reported with XOCOVA. If signs and symptoms of a clinically significant hypersensitivity reaction occur, immediately discontinue XOCOVA and initiate appropriate treatment. ( 5.3 ) 5.1 Embryofetal Toxicity Based on animal reproduction studies, XOCOVA may cause fetal harm when administered to a pregnant woman. In rabbits, embryofetal toxicity (including skeletal malformations and embryofetal lethality) was observed in rabbit offspring following exposure of pregnant rabbits to ensitrelvir at 7 times the human exposures at the recommended human dose (RHD). Likewise in rats, fetal growth retardation, low fetal body weight, skeletal variations, offspring lethality, low body weight in offspring, and retardation of morphological development were observed following exposure during gestation and lactation at exposures 9 times the human exposures at the RHD [see Use in Specific Populations (8.1) ] . Advise pregnant women and females of reproductive potential that XOCOVA may cause fetal harm. Verify pregnancy status of females of reproductive potential prior to initiating XOCOVA. Advise females of reproductive potential to use effective contraception during XOCOVA use and for 2 weeks after the final dose [see Use in Specific Populations (8.1 , 8.3) ] . 5.2 Risk of Serious Adverse Reactions Due to Drug Interactions XOCOVA is a strong CYP3A inhibitor and an inhibitor of P-gp and BCRP. In patients receiving or initiating medications metabolized by CYP3A or transported by P-gp or BCRP, XOCOVA may increase plasma concentrations of those medications and may potentially lead to severe, life-threatening, or fatal events from increased exposure of concomitant medications. In addition, medications that induce CYP3A may decrease concentrations of ensitrelvir, leading to loss of therapeutic effect of XOCOVA. Prior to prescribing XOCOVA, review all medications taken by the patient to assess potential drug-drug interactions and determine if concomitant medications require a dose adjustment, interruption, and/or additional monitoring (e.g., calcineurin inhibitors) [see Contraindications (4) and Drug Interactions (7) ] . Consider the benefit of XOCOVA and whether the risk of potential drug-drug interactions can be appropriately managed [see Drug Interactions (7) ] . 5.3 Hypersensitivity Reactions Including Anaphylaxis Hypersensitivity reactions, including anaphylaxis, anaphylactic shock, and angioedema, have been reported with XOCOVA [see Adverse Reactions (6.2) ] . If signs and symptoms of a clinically significant hypersensitivity reaction occur, immediately discontinue XOCOVA and initiate appropriate treatment.
4 CONTRAINDICATIONS XOCOVA is contraindicated in patients with a history of clinically significant hypersensitivity reactions to ensitrelvir or any other components of the product. XOCOVA is contraindicated in patients taking drugs that are: Primarily metabolized by CYP3A for which elevated concentrations may be associated with serious and/or life-threatening reactions [see Drug Interactions (7.3) ] and Strong CYP3A inducers because they may significantly reduce ensitrelvir plasma concentrations, leading to the potential loss of virologic response [see Drug Interactions (7.3) ] . History of clinically significant hypersensitivity reactions to ensitrelvir or any other components of the product. ( 4 ) Co-administration with drugs primarily metabolized by CYP3A for which elevated concentrations may be associated with serious and/or life-threatening reactions. ( 4 , 7.3 ) Co-administration with strong CYP3A inducers considered to significantly reduce ensitrelvir plasma concentrations and may be associated with the potential for loss of virologic response. ( 4 , 7.3 )
Headache (2.9%); Diarrhea (1.7%); Cough (1.1%)
6 ADVERSE REACTIONS The following clinically significant adverse reactions are described elsewhere in the labeling: Hypersensitivity reactions including anaphylaxis [see Warnings and Precautions (5.3) ] The most common adverse events (regardless of causality) occurring in ≥1% of the XOCOVA group and at a greater frequency compared to placebo were headache, diarrhea, and cough. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Shionogi Inc. at 1-800-849-9707 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. The overall safety profile of XOCOVA is based on data from 2,831 adults and adolescents exposed to the recommended dosage and duration of XOCOVA in controlled clinical trials. Trial SCORPIO-PEP was a randomized, double-blind, placebo-controlled trial in which 1,190 subjects received oral XOCOVA (375 mg [Day 1]/125 mg [Days 2-5]) and 1,187 subjects received oral placebo (Days 1-5). The most common adverse events (regardless of causality) occurring in ≥1% of the XOCOVA group and at a greater frequency compared to placebo were headache (2.9% and 2.6%, respectively), diarrhea (1.7% and 1.3%, respectively), and cough (1.1% and 0.6%, respectively). The proportion of subjects who discontinued study intervention due to an adverse event was <0.1% in both the XOCOVA and placebo groups. Laboratory Abnormalities: Asymptomatic hemoglobin declines from baseline of >2 g/dL occurred in 3% of XOCOVA recipients versus 1% of placebo recipients. 6.2 Postmarketing Experience The following adverse reactions have been identified during post approval use of XOCOVA outside of the United States. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure. Immune system disorders: Anaphylaxis (including anaphylactic shock), angioedema, hypersensitivity, urticaria
2 DOSAGE AND ADMINISTRATION Verify pregnancy status of females of reproductive potential prior to initiating XOCOVA. ( 2.1 ) Begin XOCOVA as soon as possible and within 72 hours following contact with an individual who has COVID-19. ( 2.2 ) Dosage: 375 mg (three 125-mg tablets taken at the same time) orally on Day 1 and 125 mg (one 125-mg tablet) orally on Days 2 to 5 taken with or without food. ( 2.2 ) 2.1 Pregnancy Evaluation Prior to Initiating XOCOVA Verify pregnancy status of females of reproductive potential prior to initiating XOCOVA [see Warnings and Precautions (5.1) and Use in Specific Populations (8.1 , 8.3) ] . 2.2 Recommended Dosage The recommended dosage of XOCOVA in adults and adolescents 12 years of age and older is 375 mg (three 125-mg tablets taken together) orally on Day 1 and 125 mg (one 125-mg tablet) orally on Days 2 to 5 with or without food [see Clinical Pharmacology (12.3) ] . Begin XOCOVA as soon as possible and within 72 hours following contact with an individual who has COVID-19. The tablets should be taken at approximately the same time each day. If a dose of XOCOVA is missed, take the missed dose as soon as possible on the same day, and then take the next dose as scheduled the following day.
7 DRUG INTERACTIONS Co-administration of XOCOVA can alter the plasma concentrations of other drugs, and other drugs may alter the plasma concentrations of XOCOVA. Consider the potential for drug interactions prior to and during XOCOVA use and review concomitant medications during XOCOVA use. ( 4 , 5.2 , 7 , 12.3 ) 7.1 Potential for XOCOVA to Affect Other Drugs Ensitrelvir is a strong inhibitor of CYP3A and an inhibitor of P-gp and BCRP. Co-administration of XOCOVA with drugs that are primarily metabolized by CYP3A or are transported by P-gp or BCRP may result in increased plasma concentrations of such drugs and increase the risk of adverse events [see Contraindications (4) , Warnings and Precautions (5.2) , Drug Interactions (7.3) , and Clinical Pharmacology (12.3) ] . For drugs that are CYP3A substrates and contraindicated with XOCOVA, initiation of XOCOVA should be considered only after careful evaluation of relevant clinical and pharmacokinetic factors related to the concomitant medication. In addition, re-initiation of contraindicated CYP3A substrates should be considered based on an assessment of the duration of CYP3A inhibition and patient‑specific considerations. Refer to individual drug prescribing information for additional information. 7.2 Potential for Other Drugs to Affect XOCOVA Ensitrelvir is a CYP3A substrate; therefore, drugs that induce CYP3A may decrease ensitrelvir plasma concentrations and reduce XOCOVA therapeutic effect [see Drug Interactions (7.3) and Clinical Pharmacology (12.3) ] . Therefore, use of XOCOVA with strong CYP3A4 inducers is contraindicated [see Contraindications (4) ] . No dose adjustment is recommended when XOCOVA is used concomitantly with moderate or weak CYP3A inducers [see Warnings and Precautions (5.2) ] . Refer to individual drug prescribing information for additional information. 7.3 Established and Other Potentially Significant Drug Interactions Table 1 provides examples of drugs that are contraindicated with XOCOVA [see Contraindications (4) and Warnings and Precautions (5.2) ] . Table 1 is provided as a guide and is not a comprehensive list of all possible drugs that may interact with XOCOVA. The healthcare provider should consult other appropriate resources, such as the prescribing information for the interacting drug, for comprehensive information on dosing and monitoring with concomitant use of a strong CYP3A inhibitor, like XOCOVA [see Drug Interactions (7.1) ]. Table 1 Drugs Contraindicated with XOCOVA due to Risk of Potentially Serious or Fatal Interaction [see Contraindications (4) ] Drug Class Drug(s) within Class Effect on Drug Concentration Clinical Comment Antiarrhythmics quinidine ↑ antiarrhythmic Co-administration is contraindicated due to potential for cardiac arrhythmias. Anticancer drugs apalutamide, enzalutamide ↓ ensitrelvir Co-administration is contraindicated due to potential loss of virologic response. Anticonvulsants carbamazepine See Clinical Pharmacology (12.3) , phenytoin ↓ ensitrelvir Co-administration is contraindicated due to potential loss of virologic response. Antigout agents colchicine ↑ colchicine Co-administration is contraindicated due to potential for serious and/or life-threatening reactions in patients with renal and/or hepatic impairment. Antimycobacterials rifampin ↓ ensitrelvir Co-administration is contraindicated due to potential loss of virologic response. Antipsychotics lurasidone, pimozide ↑ lurasidone, pimozide Co-administration is contraindicated due to serious and/or life-threatening reactions, such as cardiac arrhythmias. Cardiovascular drugs eplerenone, ivabradine ↑ eplerenone, ivabradine Co-administration is contraindicated. Cystic fibrosis transmembrane conductance regulator potentiators lumacaftor/ivacaftor ↓ ensitrelvir Co-administration is contraindicated due to potential loss of virologic response. Ergot derivatives dihydroergotamine, ergotamine, methylergonovine ↑ dihydroergotamine, ergotamine, methylergonovine Co-administration is contraindicated due to potential for acute ergot toxicity characterized by vasospasm and ischemia of the extremities and other tissues, including the central nervous system. Herbal products (for depression) St. John's wort ↓ ensitrelvir Co-administration is contraindicated due to potential loss of virologic response. HMG-CoA reductase inhibitors (statins) simvastatin ↑ simvastatin Co-administration is contraindicated. Discontinue use of simvastatin at least 12 hours prior to initiation of XOCOVA. Immunosuppressants voclosporin ↑ voclosporin Co-administration is contraindicated due to potential for acute and/or chronic nephrotoxicity. Microsomal triglyceride transfer protein (MTTP) inhibitors lomitapide ↑ lomitapide Co-administration is contraindicated due to potential for hepatotoxicity and gastrointestinal adverse reactions. Mineralocorticoid receptor antagonists finerenone ↑ finerenone Co-administration is contraindicated due to potential for serious adverse reactions, including hyperkalemia, hypotension, and hyponatremia. Sedatives triazolam ↑ triazolam Co-administration is contraindicated.
17 PATIENT COUNSELING INFORMATION Advise the patient to read the FDA-approved patient labeling (Patient Information). Embryofetal Toxicity Advise pregnant women and females of reproductive potential that XOCOVA may cause fetal harm. Advise females of reproductive potential to inform their healthcare providers of a known or suspected pregnancy. Advise females of reproductive potential to use effective contraception during use of XOCOVA and for 2 weeks after the final dose [see Warnings and Precautions (5.1) and Use in Specific Populations (8.1 , 8.3) ] . Verify Pregnancy Status Before Initiating XOCOVA Inform patients that they need to verify pregnancy status prior to initiating XOCOVA [see Dosage and Administration (2.1) , Warnings and Precautions (5.1) , and Use in Specific Populations (8.1 , 8.3) ]. Drug Interactions Advise patients that XOCOVA can interact with certain drugs and is contraindicated for use with certain drugs; therefore, advise patients to report to their healthcare provider the use of any prescription or non-prescription medication or herbal products [see Contraindications (4) , Warnings and Precautions (5.2) , and Drug Interactions (7) ] . Hypersensitivity Reactions Including Anaphylaxis Advise patients that hypersensitivity reactions, including anaphylaxis, anaphylactic shock, and angioedema, have been reported with XOCOVA and to immediately discontinue XOCOVA and alert the healthcare provider if signs and symptoms of a clinically significant hypersensitivity reaction occur [see Warnings and Precautions (5.3) and Adverse Reactions (6.2) ]. Administration Instructions Advise to begin XOCOVA as soon as possible and within 72 hours following contact with an individual who has COVID-19. Advise patients to take three 125-mg tablets together orally on Day 1 and one 125-mg tablet on Days 2 to 5. Inform patients to take XOCOVA with or without food at approximately the same time each day as instructed [see Dosage and Administration (2.2) ] . Lactation Advise women not to breastfeed while on XOCOVA and for 2 weeks after the final dose [see Use in Specific Populations (8.2) ] .
According to its FDA label, Xocova (ensitrelvir) is approved for: 1 INDICATIONS AND USAGE XOCOVA is indicated for post-exposure prophylaxis of coronavirus disease 2019 (COVID-19) in adults and adolescents 12 years of age and older following contact with an individual who has COVID-19. XOCOVA, a severe acute respiratory syndrome coronavirus 2 (S… For medical advice, please talk to your prescriber or pharmacist.
Xocova (ensitrelvir) belongs to the SARS-CoV-2 3CL protease inhibitor class of medications.
The FDA label lists Xocova (ensitrelvir) as: 3 DOSAGE FORMS AND STRENGTHS Tablets: white to light yellow-white, round tablets containing 125 mg of ensitrelvir, debossed with the Shionogi trademark ( ) above the identifier code "711" on one side and with a "125" on the other side. Tablets: 125 mg of ensitrelvir ( 3 ) Image; oral route. Available strengths and packaging vary by manufacturer.
Not yet. As of the most recent FDA data we ingest, no A-rated generic equivalent is listed for Xocova. Availability changes as patents expire.
Our ingest of the FDA label for Xocova (ensitrelvir) does not include a Boxed Warning at this time. See the full label on DailyMed for the current, authoritative version.
The FDA Enforcement Report does not show an active/ongoing recall for Xocova (ensitrelvir) in our latest ingest. Recall data can change daily — verify at FDA.gov.
The FDA record lists the approval date for Xocova (ensitrelvir) as 2026-05-29.
The FDA label lists Shionogi Inc. as a labeler/manufacturer of Xocova (ensitrelvir). Multiple firms may market generics of the same molecule.
The FDA label states: "Store XOCOVA in the original package at 20°C to 25°C (68°F to 77°F); excursions permitted between 15°C to 30°C (59°F to 86°F) [See USP Controlled Room Temperature]." Follow the packaging insert for the authoritative guidance.
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