Nirmatrelvir

ʻO ka wehewehe pōkole:

Ka inoa o ka API Hōʻike Mea hana hou Lā Hoʻopau Patent (ʻAmelika)
Nirmatrelvir ʻO ka 3C-Like Protease (3CLPRO) ka mea pale a me ka SARS-Cov-2 Mpro kaohi.    

 


Huahana Huahana

Huahana Huahana

NUI HUA

ʻO Nirmatrelvir kahi mea pale o ka SARS-CoV-2 nui protease (Mpro), i kapa ʻia ʻo 3C-like protease (3CLpro) a i ʻole nsp5 protease. ʻO ka pale ʻana i ka SARS-CoV-2 Mpro ka mea i hiki ʻole ke hana i nā precursors polyprotein, e pale ana i ka hoʻopiʻi viral.

Ua kāohi ʻo Nirmatrelvir i ka hana o ka recombinant SARS-CoV-2 Mpro i kahi hoʻāʻo biochemical i nā ʻike i hiki ke loaʻa i loko o vivo. Ua ʻike ʻia ʻo Nirmatrelvir e hoʻopaʻa pololei i ka pūnaewele ikaika SARS-CoV-2 Mpro e ka X-ray crystallography.

ʻO Ritonavir kahi mea pale protease HIV-1 akā ʻaʻole ikaika e kūʻē iā SARS-CoV-2 Mpro. Hoʻopaʻa ʻo Ritonavir i ka CYP3A-mediated metabolism o nirmatrelvir, ka hopena o ka hoʻonui ʻana i ka plasma concentrations o nirmatrelvir.

Paipai ʻia kēia lāʻau lapaʻau. Ua hāʻawi ʻia ka ʻae ʻia e ka FDA no ka mālama ʻana i ka maʻi coronavirus maʻemaʻe (COVID-19) i nā pākeke a me nā maʻi maʻi pediatric (12 mau makahiki a ʻoi aku paha ma kahi o 40 kilokani a i ʻole 88 paona) me nā hopena maikaʻi o ka hoʻāʻo pololei ʻana iā SARS-CoV-2, a ʻo ka poʻe i ke kūlana kiʻekiʻe no ka piʻi ʻana i ka COVID-19 koʻikoʻi, me ka hoʻokipa a i ʻole ka make. Pono e hoʻomaka koke ʻia ka Nirmatrelvir/ritonavir ma hope o ka hōʻoia ʻana o COVID-19 a i loko o ʻelima mau lā o ka hoʻomaka ʻana o ka hōʻailona.

Hoʻokumu ʻia nā ʻōlelo manaʻo ma ka EPIC-HR, kahi Phase2/3 randomized clinical control trial e loiloi ana i ka pono o ka nirmaltrelivir/ritonavir vs. placebo i ka hōʻemi ʻana i ka hale maʻi a i ʻole ka make a hiki i ka lā 28. ʻO ka hoʻohana ʻana i ka nirmaltrelivir/ritonavir i loko o 5 mau lā o ka hoʻomaka ʻana o ka hōʻailona. ʻO ka poʻe i pilikia no ka piʻi ʻana i ka maʻi koʻikoʻi i hōʻemi i ka pilikia pili o ka haukapila a i ʻole ka make ma o 28 mau lā e 88%.

HOOLAHA ANOAI

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Holo ka nānā ʻana i ka maikaʻi ma ke ola holoʻokoʻa o ka huahana e hōʻoia i ka maikaʻi a me ka hopena therapeutic.

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