Peringatan Keamanan

There are no data regarding overdosage with nirmatrelvir. Treatment of suspected overdose should consist of general supportive measures as clinically indicated.L39544

Nirmatrelvir

DB16691

small molecule approved investigational

Deskripsi

Nirmatrelvir (PF-07321332) is an orally bioavailable 3C-like protease (3CLPRO) inhibitor that is the subject of clinical trial NCT04756531.L33354 3CLPRO is responsible for cleaving polyproteins 1a and 1ab of SARS-CoV-2.A234224 Without the activity of the SARS-CoV-2 3CLPRO, nonstructural proteins (including proteases) cannot be released to perform their functions, inhibiting viral replication.A234224,A234229,A234234

In 2020, Pfizer was investigating another potential treatment for SARS-CoV-2, PF-07304814.L33359 Both drugs were inhibitors of SARS-CoV-2 3CLPRO, but nirmatrelvir has the advantage of being orally bioavailable.L33359 Nirmatrelvir is advantageous in that it can be prescribed to patients before they require hospitalization, while PF-07304814 requires intravenous administration in hospital.L33359

In December 2021, the FDA granted an emergency use authorization to Paxlovid, a co-packaged product containing both nirmatrelvir and ritonavir, for the treatment of certain patients with mild-to-moderate COVID-19.L39544 It was fully approved by the FDA on May 25, 2023.L46921 Paxlovid was approved for use in Canada in January 2022 for the treatment of adult patients with mild-moderate COVID-19 L39544 and later granted conditional marketing authorization by the European Commission on January 27, 2022.L40094

Struktur Molekul 2D

Berat 499.535
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The mean half-life of nirmatrelvir, administered alongside ritonavir, is 6.05 hours.[L39544]
Volume Distribusi The mean volume of distribution of nirmatrelvir, when given with ritonavir, is 104.7 liters.[L39544]
Klirens (Clearance) The mean oral clearance of nirmatrelvir, administered with ritonavir, is 8.99 L/h.[L39544]

Absorpsi

The median Tmax of nirmatrelvir, when given with ritonavir, is 3 hours.L39544 After a single oral dose of 300mg nirmatrelvir and 100mg ritonavir in healthy subjects, the Cmax and AUCinf of nirmatrelvir were 2.21 µg/mL and 23.01 µg*hr/mL, respectively.L39544

Metabolisme

Nirmatrelvir is a substrate of CYP3A4, but undergoes minimal metabolism when administered alongside ritonavir.L39544

Rute Eliminasi

The major route of nirmaltrevir elimination is via renal elimination, due in part to its coadministration with ritonavir which inhibits its metabolism.L39544 Following oral administration alongside ritonavir, approximately 49.6% of drug-related material was recovered in the feces and 35.3% was recovered in the urine.L39544

Interaksi Makanan

2 Data
  • 1. Avoid St. John's Wort. Co-administration may reduce serum concentrations of niramtrelvir and interfere with virologic efficacy.
  • 2. Take with or without food. Co-administration of nirmatrelvir with food does not significantly alter its pharmacokinetics.

Interaksi Obat

119 Data
Phenytoin The serum concentration of Nirmatrelvir can be decreased when it is combined with Phenytoin.
Pentobarbital The metabolism of Nirmatrelvir can be increased when combined with Pentobarbital.
Carbamazepine The serum concentration of Nirmatrelvir can be decreased when it is combined with Carbamazepine.
Mitotane The metabolism of Nirmatrelvir can be increased when combined with Mitotane.
Primidone The metabolism of Nirmatrelvir can be increased when combined with Primidone.
Rifampin The serum concentration of Nirmatrelvir can be decreased when it is combined with Rifampicin.
Phenobarbital The serum concentration of Nirmatrelvir can be decreased when it is combined with Phenobarbital.
Rifapentine The metabolism of Nirmatrelvir can be increased when combined with Rifapentine.
Dexamethasone The metabolism of Nirmatrelvir can be increased when combined with Dexamethasone.
Fosphenytoin The metabolism of Nirmatrelvir can be increased when combined with Fosphenytoin.
St. John's Wort The serum concentration of Nirmatrelvir can be decreased when it is combined with St. John's Wort.
Midostaurin The metabolism of Nirmatrelvir can be decreased when combined with Midostaurin.
Enzalutamide The serum concentration of Nirmatrelvir can be decreased when it is combined with Enzalutamide.
Lumacaftor The metabolism of Nirmatrelvir can be increased when combined with Lumacaftor.
Apalutamide The serum concentration of Nirmatrelvir can be decreased when it is combined with Apalutamide.
Cyclosporine The metabolism of Nirmatrelvir can be decreased when combined with Cyclosporine.
Fluvoxamine The metabolism of Nirmatrelvir can be decreased when combined with Fluvoxamine.
Fluconazole The metabolism of Nirmatrelvir can be decreased when combined with Fluconazole.
Erythromycin The serum concentration of Nirmatrelvir can be increased when it is combined with Erythromycin.
Ziprasidone The metabolism of Nirmatrelvir can be decreased when combined with Ziprasidone.
Isradipine The metabolism of Nirmatrelvir can be decreased when combined with Isradipine.
Diltiazem The metabolism of Nirmatrelvir can be decreased when combined with Diltiazem.
Clozapine The metabolism of Nirmatrelvir can be decreased when combined with Clozapine.
Haloperidol The serum concentration of Haloperidol can be increased when it is combined with Nirmatrelvir.
Ciprofloxacin The metabolism of Nirmatrelvir can be decreased when combined with Ciprofloxacin.
Voriconazole The metabolism of Nirmatrelvir can be decreased when combined with Voriconazole.
Nicardipine The metabolism of Nirmatrelvir can be decreased when combined with Nicardipine.
Verapamil The metabolism of Nirmatrelvir can be decreased when combined with Verapamil.
Aprepitant The metabolism of Nirmatrelvir can be decreased when combined with Aprepitant.
Isoniazid The metabolism of Nirmatrelvir can be decreased when combined with Isoniazid.
Primaquine The metabolism of Nirmatrelvir can be decreased when combined with Primaquine.
Miconazole The metabolism of Nirmatrelvir can be decreased when combined with Miconazole.
Danazol The metabolism of Nirmatrelvir can be decreased when combined with Danazol.
Fusidic acid The metabolism of Nirmatrelvir can be decreased when combined with Fusidic acid.
Zimelidine The metabolism of Nirmatrelvir can be decreased when combined with Zimelidine.
Dronedarone The metabolism of Nirmatrelvir can be decreased when combined with Dronedarone.
Milnacipran The metabolism of Nirmatrelvir can be decreased when combined with Milnacipran.
Simeprevir The metabolism of Nirmatrelvir can be decreased when combined with Simeprevir.
Isavuconazonium The metabolism of Nirmatrelvir can be decreased when combined with Isavuconazonium.
Desvenlafaxine The metabolism of Nirmatrelvir can be decreased when combined with Desvenlafaxine.
Nilvadipine The metabolism of Nirmatrelvir can be decreased when combined with Nilvadipine.
Seproxetine The metabolism of Nirmatrelvir can be decreased when combined with Seproxetine.
Linagliptin The metabolism of Nirmatrelvir can be decreased when combined with Linagliptin.
Indalpine The metabolism of Nirmatrelvir can be decreased when combined with Indalpine.
Netupitant The metabolism of Nirmatrelvir can be decreased when combined with Netupitant.
Barnidipine The metabolism of Nirmatrelvir can be decreased when combined with Barnidipine.
Benidipine The metabolism of Nirmatrelvir can be decreased when combined with Benidipine.
Venetoclax The metabolism of Nirmatrelvir can be decreased when combined with Venetoclax.
Isavuconazole The metabolism of Nirmatrelvir can be decreased when combined with Isavuconazole.
Fosnetupitant The metabolism of Nirmatrelvir can be decreased when combined with Fosnetupitant.
Berotralstat The metabolism of Nirmatrelvir can be decreased when combined with Berotralstat.
Nelfinavir The metabolism of Nirmatrelvir can be decreased when combined with Nelfinavir.
Indinavir The metabolism of Nirmatrelvir can be decreased when combined with Indinavir.
Terfenadine The metabolism of Nirmatrelvir can be decreased when combined with Terfenadine.
Efavirenz The metabolism of Nirmatrelvir can be decreased when combined with Efavirenz.
Ergotamine The metabolism of Nirmatrelvir can be decreased when combined with Ergotamine.
Amprenavir The metabolism of Nirmatrelvir can be decreased when combined with Amprenavir.
Delavirdine The metabolism of Nirmatrelvir can be decreased when combined with Delavirdine.
Methimazole The metabolism of Nirmatrelvir can be decreased when combined with Methimazole.
Conivaptan The metabolism of Nirmatrelvir can be decreased when combined with Conivaptan.
Tipranavir The metabolism of Nirmatrelvir can be decreased when combined with Tipranavir.
Telithromycin The metabolism of Nirmatrelvir can be decreased when combined with Telithromycin.
Ketoconazole The metabolism of Nirmatrelvir can be decreased when combined with Ketoconazole.
Atazanavir The metabolism of Nirmatrelvir can be decreased when combined with Atazanavir.
Amiodarone The metabolism of Nirmatrelvir can be decreased when combined with Amiodarone.
Nefazodone The metabolism of Nirmatrelvir can be decreased when combined with Nefazodone.
Itraconazole The metabolism of Nirmatrelvir can be decreased when combined with Itraconazole.
Clarithromycin The metabolism of Nirmatrelvir can be decreased when combined with Clarithromycin.
Saquinavir The metabolism of Nirmatrelvir can be decreased when combined with Saquinavir.
Posaconazole The metabolism of Nirmatrelvir can be decreased when combined with Posaconazole.
Darunavir The metabolism of Nirmatrelvir can be decreased when combined with Darunavir.
Lopinavir The metabolism of Nirmatrelvir can be decreased when combined with Lopinavir.
Ditiocarb The metabolism of Nirmatrelvir can be decreased when combined with Ditiocarb.
Nilotinib The metabolism of Nirmatrelvir can be decreased when combined with Nilotinib.
Telaprevir The metabolism of Nirmatrelvir can be decreased when combined with Telaprevir.
Lonafarnib The metabolism of Nirmatrelvir can be decreased when combined with Lonafarnib.
Boceprevir The metabolism of Nirmatrelvir can be decreased when combined with Boceprevir.
Elvitegravir The metabolism of Nirmatrelvir can be decreased when combined with Elvitegravir.
Stiripentol The metabolism of Nirmatrelvir can be decreased when combined with Stiripentol.
Curcumin The metabolism of Nirmatrelvir can be decreased when combined with Curcumin.
Ribociclib The metabolism of Nirmatrelvir can be decreased when combined with Ribociclib.
Danoprevir The metabolism of Nirmatrelvir can be decreased when combined with Danoprevir.
Troleandomycin The metabolism of Nirmatrelvir can be decreased when combined with Troleandomycin.
Pitolisant The serum concentration of Nirmatrelvir can be decreased when it is combined with Pitolisant.
Metreleptin The metabolism of Nirmatrelvir can be increased when combined with Metreleptin.
Cenobamate The serum concentration of Nirmatrelvir can be decreased when it is combined with Cenobamate.
Tucatinib The metabolism of Tucatinib can be decreased when combined with Nirmatrelvir.
Abametapir The serum concentration of Nirmatrelvir can be increased when it is combined with Abametapir.
Satralizumab The serum concentration of Nirmatrelvir can be decreased when it is combined with Satralizumab.
Sotorasib The serum concentration of Nirmatrelvir can be decreased when it is combined with Sotorasib.
Somatrogon The metabolism of Nirmatrelvir can be increased when combined with Somatrogon.
Levoketoconazole The metabolism of Nirmatrelvir can be decreased when combined with Levoketoconazole.
Rubella virus vaccine The therapeutic efficacy of Rubella virus vaccine can be decreased when used in combination with Nirmatrelvir.
Varicella zoster vaccine (live/attenuated) The therapeutic efficacy of Varicella zoster vaccine (live/attenuated) can be decreased when used in combination with Nirmatrelvir.
Bacillus calmette-guerin substrain tice live antigen The therapeutic efficacy of Bacillus calmette-guerin substrain tice live antigen can be decreased when used in combination with Nirmatrelvir.
Bacillus calmette-guerin substrain connaught live antigen The therapeutic efficacy of Bacillus calmette-guerin substrain connaught live antigen can be decreased when used in combination with Nirmatrelvir.
Yellow fever vaccine The therapeutic efficacy of Yellow fever vaccine can be decreased when used in combination with Nirmatrelvir.
Anthrax vaccine The therapeutic efficacy of Anthrax vaccine can be decreased when used in combination with Nirmatrelvir.
Typhoid Vaccine Live The therapeutic efficacy of Typhoid Vaccine Live can be decreased when used in combination with Nirmatrelvir.
BCG vaccine The therapeutic efficacy of BCG vaccine can be decreased when used in combination with Nirmatrelvir.

Target Protein

Replicase polyprotein 1ab rep

Referensi & Sumber

Synthesis reference: Owen DR, Allerton CMN, Anderson AS, Aschenbrenner L, Avery M, Berritt S, Boras B, Cardin RD, Carlo A, Coffman KJ, Dantonio A, Di L, Eng H, Ferre R, Gajiwala KS, Gibson SA, Greasley SE, Hurst BL, Kadar EP, Kalgutkar AS, Lee JC, Lee J, Liu W, Mason SW, Noell S, Novak JJ, Obach RS, Ogilvie K, Patel NC, Pettersson M, Rai DK, Reese MR, Sammons MF, Sathish JG, Singh RSP, Steppan CM, Stewart AE, Tuttle JB, Updyke L, Verhoest PR, Wei L, Yang Q, Zhu Y: An oral SARS-CoV-2 M(pro) inhibitor clinical candidate for the treatment of COVID-19. Science. 2021 Nov 2:eabl4784. doi: 10.1126/science.abl4784.
Artikel (PubMed)
  • PMID: 33098476
    Ionescu MI: An Overview of the Crystallized Structures of the SARS-CoV-2. Protein J. 2020 Dec;39(6):600-618. doi: 10.1007/s10930-020-09933-w. Epub 2020 Oct 24.
  • PMID: 27799534
    Muramatsu T, Takemoto C, Kim YT, Wang H, Nishii W, Terada T, Shirouzu M, Yokoyama S: SARS-CoV 3CL protease cleaves its C-terminal autoprocessing site by novel subsite cooperativity. Proc Natl Acad Sci U S A. 2016 Nov 15;113(46):12997-13002. doi: 10.1073/pnas.1601327113. Epub 2016 Oct 31.
  • PMID: 33460213
    Xiong M, Su H, Zhao W, Xie H, Shao Q, Xu Y: What coronavirus 3C-like protease tells us: From structure, substrate selectivity, to inhibitor design. Med Res Rev. 2021 Jan 18. doi: 10.1002/med.21783.

Contoh Produk & Brand

Produk: 11 • International brands: 0
Produk
  • Paxlovid
    Kit; Tablet, film coated • - • Oral • US
  • Paxlovid
    Kit; Tablet, film coated • - • Oral • US
  • Paxlovid
    Tablet • - • Oral • Canada • Approved
  • Paxlovid
    Kit; Tablet, film coated • - • Oral • US
  • Paxlovid
    Kit; Tablet, film coated • - • Oral • US • Approved
  • Paxlovid
    Kit; Tablet, film coated • - • Oral • US • Approved
  • Paxlovid
    Kit; Tablet, film coated • - • Oral • US • Approved
  • Paxlovid
    Kit; Tablet, film coated • - • Oral • US • Approved
Menampilkan 8 dari 11 produk.

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
© 2025 Digital Pharmacy Research - Universitas Esa Unggul