I-Nirmatrelvir iyi-inhibitor ye-SARS-CoV-2 main protease (Mpro), ebizwa nangokuthi i-3C-like protease (3CLpro) noma i-nsp5 protease. Ukuvinjelwa kwe-SARS-CoV-2 Mpro kuyenza ingakwazi ukucubungula izandulela ze-polyprotein, ukuvimbela ukuphindaphinda kwegciwane.

I-Nirmatrelvir ivimbe umsebenzi we-recombinant SARS-CoV-2 Mpro ekuhlolweni kwamakhemikhali e-biochemical ekugxilweni okufinyeleleka ku-vivo. I-Nirmatrelvir itholakale ibophezela ngqo endaweni esebenzayo yakwa-SARS-CoV-2 Mpro nge-X-ray crystallography.

I-Ritonavir iyi-HIV-1 protease inhibitor kodwa ayisebenzi ngokumelene ne-SARS-CoV-2 Mpro. I-Ritonavir ivimbela i-CYP3A-mediated metabolism ye-nirmatrelvir, okuholela ekwandeni kokugxila kwe-nirmatrelvir ku-plasma.

Lo muthi uyatuswa. Inikezwe imvume yokusetshenziswa kwezimo eziphuthumayo yi-FDA yokwelashwa kwesifo se-coronavirus esimaphakathi kuya kokulingene (COVID-19) kubantu abadala nasezigulini zezingane (ezineminyaka eyi-12 nangaphezulu ezinesisindo esingamakhilogremu angama-40 noma cishe amakhilogremu angama-88) imiphumela emihle yokuhlolwa okuqondile kwe-SARS-CoV-2, futhi abasengozini enkulu yokudlulela ku-COVID-19 enzima, okuhlanganisa ukulaliswa esibhedlela noma ukufa. I-Nirmatrelvir/ritonavir kufanele iqalwe ngokushesha ngangokunokwenzeka ngemva kokuxilongwa kwe-COVID-19 futhi zingakapheli izinsuku ezinhlanu izimpawu ziqale.

Izincomo zisekelwe ku-EPIC-HR, uhlolo lwe-Phase2/3 lokulawulwa komtholampilo okungahleliwe oluhlola ukusebenza kahle kwe-nirmaltrelivir/ritonavir vs. placebo ekunciphiseni ukulaliswa esibhedlela noma ukufa ngosuku lwama-28. Ukusetshenziswa kwe-nirmaltrelivir/ritonavir phakathi kwezinsuku ezingu-5 izimpawu ziqale abantu abasengcupheni yokudlulela esifweni esinzima banciphisa ubungozi bokulaliswa esibhedlela noma ukufa ezinsukwini ezingama-28 88%.