Nirmatrelvir

Nkọwa dị mkpirikpi:

Aha API Ngosipụta Onye mmepụta ihe Ụbọchị Mmebi Ikikere (US)
Nirmatrelvir 3C-dị ka Protease (3CLPRO) Inhibitor na SARS-Cov-2 Mpro Inhibitor    

 


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Nirmatrelvir bụ onye na-egbochi SARS-CoV-2 isi protease (Mpro), nke a na-akpọkwa 3C-dị ka protease (3CLpro) ma ọ bụ nsp5 protease. Mgbochi nke SARS-CoV-2 Mpro na-eme ka ọ bụrụ enweghị ike ịhazi polyprotein precursors, na-egbochi nje virus.

Nirmatrelvir gbochiri ọrụ nke recombinant SARS-CoV-2 Mpro na nyocha biochemical na mkpokọta enwere ike nweta na vivo. Achọpụtara Nirmatrelvir ka ọ na-ejikọ ozugbo na saịtị SARS-CoV-2 Mpro na-arụ ọrụ site na X-ray crystallography.

Ritonavir bụ onye na-egbochi nje HIV-1 mana ọ naghị arụ ọrụ megide SARS-CoV-2 Mpro. Ritonavir na-egbochi usoro mgbasa ozi CYP3A nke nirmatrelvir, na-ebute mmụba plasma nke nirmatrelvir.

A na-akwado ọgwụ a. Enyerela ya ikike iji ihe mberede mee ihe mberede site n'aka FDA maka ọgwụgwọ nke ọrịa coronavirus dị nro na-agafeghị oke (COVID-19) na ndị okenye na ndị ọrịa ụmụaka (afọ 12 na karịa na-eru opekata mpe kilogram 40 ma ọ bụ ihe dị ka kilogram 88) Nsonaazụ dị mma nke nnwale SARS-CoV-2 ozugbo, yana ndị nọ n'ihe egwu dị elu maka ịga n'ihu na COVID-19 siri ike, gụnyere ụlọ ọgwụ ma ọ bụ ọnwụ. Ekwesịrị ibido Nirmatrelvir/ritonavir ozugbo enwere ike ka achọpụtara COVID-19 yana n'ime ụbọchị ise nke mgbaàmà mmalite.

Ndụmọdụ sitere na EPIC-HR, usoro nlekọta ahụike na-ahụ maka usoro nke Phase2 / 3 na-enyocha ịdị irè nke nirmaltrelivir / ritonavir vs. placebo na mbelata ụlọ ọgwụ na ma ọ bụ ọnwụ site na ụbọchị 28. Ojiji nirmaltrelivir / ritonavir n'ime ụbọchị 5 nke mgbaàmà mmalite. Ndị mmadụ nọ n'ihe ize ndụ maka ịga n'ihu na ọrịa siri ike belatara ohere ịnọ n'ụlọ ọgwụ ma ọ bụ ọnwụ site na ụbọchị 28 site na 88%.

Asambodo

2018 GMP-2
原料药GMP证书201811 (captopril, thalidomide wdg)
GMP-of-PMDA-in-Chanyoo-平成28年08月03日 Nantong-Chanyoo-Pharmatech-Co
Akwụkwọ ozi FDA-EIR-201901

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