Indications & Uses
Nirmatrelvir with Ritonavir is under an EUA for treating mild-to-moderate coronavirus disease 2019 (COVID-19) in adults and paediatric patients (12 years of age and older weighing at least 40 kg). Nirmatrelvir is a SARS-CoV-2 main protease inhibitor (Mpro, also called 3CLpro or nsp5 protease). Ritonavir is an HIV-1 protease inhibitor and a CYP3A inhibitor. The patient must have a positive result on direct severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) viral testing, and must be at high risk for progression to severe COVID-19, including hospitalization or death. This combination is not authorized for starting treatment in patients who need hospitalization because of severe or critical COVID-19, for pre-exposure or post-exposure prophylaxis to prevent COVID-19, or for use longer than 5 consecutive days.
Pharmacology
Nirmatrelvir is a peptidomimetic inhibitor of the SARS-CoV-2 main protease (Mpro), which is also called 3C-like protease (3CLpro) or nsp5 protease. When Mpro is blocked, the virus can't process its polyprotein precursors, and so it can't replicate. In a biochemical assay, Nirmatrelvir inhibited the activity of recombinant SARS-CoV-2 Mpro with a ki value of 3.1 nM and an IC50 value of 19.2 nM. X-ray crystallography showed that Nirmatrelvir binds directly to the active site of SARS-CoV-2 Mpro.
Ritonavir is an HIV-1 protease inhibitor, but it is not active against SARS-CoV-2 Mpro. Its job here is different. Ritonavir inhibits the CYP3A-mediated metabolism of Nirmatrelvir, and this raises the plasma concentrations of Nirmatrelvir.
Dosage Reference
Reference Information Only
Dosages shown are general references from official sources. Always consult your doctor or pharmacist for personalized dosing.
Adults:
Start this treatment as soon as possible after COVID-19 is diagnosed, and within 5 days of when symptoms began. Swallow the tablets with or without food.
Dosage: 300 mg Nirmatrelvir (two 150 mg tablets) with 100 mg Ritonavir (one 100 mg tablet). All three tablets are taken together, twice daily for 5 days.
Dosage reduction applies in moderate renal impairment (eGFR ≥30 to <60 mL/min). In that case the dose is 150 mg Nirmatrelvir (one 150 mg tablet) with 100 mg Ritonavir (one 100 mg tablet). Both tablets are taken together, twice daily for 5 days.
This treatment is not recommended in patients with severe renal impairment (eGFR <30 mL/min). It is also not recommended in patients with severe hepatic impairment (Child-Pugh Class C).
Side Effects
Nirmatrelvir + Ritonavir caused dysgeusia, diarrhea, hypertension and myalgia in more than 1% of people, and these occurred more often than in the comparison group.
Cautions & Contraindications
Warnings & Precautions
Taking this tablet together with certain other drugs can cause significant interactions. Read the full prescribing information before starting treatment and again during treatment to check for possible drug interactions. Hepatotoxicity: Liver enzyme (hepatic transaminase) levels have risen, and clinical hepatitis and jaundice have occurred, in patients receiving Ritonavir. HIV-1 Drug Resistance: Using this tablet in people with uncontrolled or undiagnosed HIV-1 infection may lead to the HIV-1 developing resistance to HIV protease inhibitors.
Contraindications
Nirmatrelvir + Ritonavir must not be used by anyone who has had a clinically significant hypersensitivity reaction to Nirmatrelvir, Ritonavir or any other component of the medicine. It must also not be given together with drugs that depend heavily on CYP3A to be cleared from the body, where higher levels of those drugs are linked with serious and/or life-threatening reactions. The third situation is use with potent CYP3A inducers. These can lower the plasma levels of Nirmatrelvir or Ritonavir significantly, which may lead to loss of virologic response and possible resistance.
Pregnancy & Breastfeeding
We have no human data on Nirmatrelvir use in pregnancy, so its risk of major birth defects, miscarriage, or other harmful outcomes for the mother or baby can't be judged. For Ritonavir, published observational studies in pregnant women have not found a higher risk of major birth defects. The published studies are not enough to say whether Ritonavir carries a risk of miscarriage. Untreated COVID-19 in pregnancy also carries risks for both the mother and the baby.
Nothing is known about whether Nirmatrelvir passes into human or animal milk, what it does to a breastfed infant, or whether it affects milk production. A mother should weigh the developmental and health benefits of breastfeeding against her own clinical need for Nirmatrelvir and Ritonavir. She should also weigh the possible side effects of these medicines on the infant, and the effects of the illness itself if it goes untreated. Women who are breastfeeding and have COVID-19 should follow clinical guidelines on feeding practices so the infant isn't exposed to COVID-19.
⚠️ Talk to your doctor before taking any medicine during pregnancy or while breastfeeding.
Storage
Store below 30°C in a dry place. Protect it from light and keep it out of the reach of children.
Drug Interactions
Common questions about Jupitavir 150 mg+100 mg
What is Jupitavir 150 mg+100 mg Tablet?
Jupitavir 150 mg+100 mg Tablet is a medicine that contains Nirmatrelvir + Ritonavir. It is made by Incepta Pharmaceuticals Ltd. It belongs to the Anti-viral drugs group of medicines.
What is Jupitavir used for?
Nirmatrelvir with Ritonavir is under an EUA for treating mild-to-moderate coronavirus disease 2019 (COVID-19) in adults and paediatric patients (12 years of age and older weighing at least 40 kg). Nirmatrelvir is a SARS-CoV-2 main protease inhibitor (Mpro, also called 3CLpro or nsp5 protease).
What are the side effects of Jupitavir?
Nirmatrelvir + Ritonavir caused dysgeusia, diarrhea, hypertension and myalgia in more than 1% of people, and these occurred more often than in the comparison group.
Can I take Jupitavir during pregnancy or while breastfeeding?
We have no human data on Nirmatrelvir use in pregnancy, so its risk of major birth defects, miscarriage, or other harmful outcomes for the mother or baby can't be judged. For Ritonavir, published observational studies in pregnant women have not found a higher risk of major birth defects. Talk to your doctor before taking any medicine during pregnancy or while breastfeeding.
How should I store Jupitavir?
Store below 30°C in a dry place. Protect it from light and keep it out of the reach of children.
Can I take other medicines with Jupitavir?
Some medicines can interact with Nirmatrelvir + Ritonavir, for example: Ritonavir. Tell your doctor or pharmacist about every medicine you take.
Do I need a prescription for Jupitavir?
Jupitavir is a prescription (Rx) medicine. Take it as your doctor advises.