I-Nirmatrelvir sisithinteli se-SARS-CoV-2 main protease (Mpro), ekwabizwa ngokuba yi-3C-like protease (3CLpro) okanye i-nsp5 protease. Ukuthintelwa kwe-SARS-CoV-2 Mpro kuyenza ingakwazi ukujongana ne-polyprotein precursors, ukuthintela ukuphindaphinda kwentsholongwane.

I-Nirmatrelvir ithintele umsebenzi we-SARS-CoV-2 Mpro kwakhona kuvavanyo lwe-biochemical ekugxininiseni okufikelelekayo kwi-vivo. I-Nirmatrelvir yafunyanwa ibophelela ngqo kwindawo esebenzayo ye-SARS-CoV-2 Mpro ngeX-ray crystallography.

I-Ritonavir yi-HIV-1 protease inhibitor kodwa ayisebenzi ngokuchasene ne-SARS-CoV-2 Mpro. I-Ritonavir inqanda i-CYP3A-mediated metabolism ye-nirmatrelvir, ekhokelela ekunyuseni kwe-plasma ye-nirmatrelvir.

Eli yeza liyacetyiswa. Inikwe isigunyaziso sosetyenziso olungxamisekileyo yi-FDA kunyango lwesifo se-coronavirus esisezantsi ukuya-kumodareyitha (COVID-19) kubantu abadala nakwizigulana zabantwana (abaneminyaka eli-12 ubudala nangaphezulu abanobunzima obumalunga neekhilogram ezingama-40 okanye malunga neekhilogram ezingama-88) iziphumo ezincumisayo zovavanyo oluthe ngqo lwe-SARS-CoV-2, kwaye abo basemngciphekweni omkhulu wokuqhubela phambili ukuya kwi-COVID-19 eqatha, kubandakanya ukulaliswa esibhedlele okanye ukufa. I-Nirmatrelvir/ritonavir kufuneka iqalwe ngokukhawuleza emva kokufunyaniswa kwe-COVID-19 kwaye zingaphelanga iintsuku ezintlanu emva kokuba iimpawu ziqale.

Izindululo zisekelwe kwi-EPIC-HR, i-Phase2/3 yolingo lonyango olungenamkhethe oluvavanya ukusebenza kwe-nirmaltrelivir/ritonavir vs. placebo ekunciphiseni ukulaliswa esibhedlele kunye okanye ukufa ngosuku lwama-28. Ukusetyenziswa kwe-nirmaltrelivir/ritonavir phakathi kweentsuku ezi-5 zokuqalisa kweempawu abantu abasemngciphekweni wokuqhubela phambili kwisifo esiqatha bawunciphisa umngcipheko wokulaliswa esibhedlele okanye wokusweleka ngeentsuku ezingama-28 88%.