Pfizer tau thov rau Tebchaws Meskas rau kev siv thaum muaj xwm txheej ceev ntawm Paxlovid' cov tshuaj tiv thaiv kab mob rau lub hlis no, uas tau pom tias muaj txiaj ntsig zoo hauv kev tiv thaiv kev mus pw hauv tsev kho mob thiab kev tuag ntawm cov neeg mob uas muaj kev pheej hmoo siab. Ntawm cov neeg mob uas muaj kev pheej hmoo siab nrog cov kab mob tshiab uas tau txais kev kho mob tsis pub dhau peb hnub ntawm qhov pib tshwm sim, Pfizer cov tshuaj tau pom tias yuav txo tau mus pw hauv tsev kho mob lossis tuag los ntawm 89%. Hnub tim 19 lub hlis no, tsoomfwv Meskas tau tshaj tawm tias nws yuav siv $ 5.3 nphom (33.8 billion yuan) los yuav 10 lab Pfizer cov tshuaj tshiab. Pfizer yuav pib muab cov ntsiav tshuaj tshiab no rau tsoomfwv Meskas tom qab lub xyoo no thiab txuas ntxiv mus txog xyoo 2022. Thaum xaus ntawm lub xyoo (tau kawg, seb nws puas tuaj yeem siv tau yog nyob ntawm kev pom zoo los ntawm US Food and Drug Administration).
Cov khoom tseem ceeb ntawm Paxlovid yog PF-073213322. Kev tshawb fawb thiab kev loj hlob ntawm PF-073213322 pib thaum SARS. Lub sijhawm ntawd, Pfizer tau tsim PF-00835231, tab sis nrog rau qhov kawg ntawm SARS, txoj kev loj hlob tau raug txiav. Thaum tus kabmob tshiab no tau tshwm sim xyoo 2020, cov kws tshawb nrhiav pom tias cov noob caj ces ntawm tus kabmob tshiab no yog tib yam li qhov chaw tseem ceeb ntawm tus kabmob SARS' lub ntsiab protease, ua rau nws siv tau cov tshuaj SARS PF. -00835231 hauv kev tshawb fawb txog tus kabmob tshiab no, yog li Pfizer siv PF-00835231 ua lub hauv paus, rov pib tshawb nrhiav thiab txhim kho tshuaj.
PF-00835231 (Compound 1) inhibits kev ua ntawm lub ntsiab protease ntawm tus kab mob. Nws cov tshuaj tiv thaiv muaj zog heev, tab sis nws cov dej solubility thiab cov ntaub so ntswg nqus tsis zoo. Nws tuaj yeem tsuas yog siv los ntawm qhov ncauj, tsuas yog los ntawm kev txhaj tshuaj intravenous. Txhawm rau txhim kho qhov permeability thiab qhov ncauj muaj nyob ntawm 1, cov kws tshawb fawb tau hloov pauv α-hydroxymethyl ketone ntawm 1 mus rau cyano kom tau txais cov ntsiab lus 2. Cov txiaj ntsig tau pom tias qhov sib xyaw cyano no txhim kho cov dej-soluble absorbability ntawm cov tshuaj, thaum tseem txo qis. nws antiviral zog. Tom qab ntawd, cov kws tshawb fawb tau qhia txog azabicyclo thiab benzothiazole kom tau txais cov khoom sib xyaw 3. Lub permeability ntawm compound 3 yog qhov zoo dua, tab sis cov kev ua tau qis dua 1. Cov kws tshawb fawb tau hloov cov indole rau methyl sulfonamide kom tau cov compound 4. Tom qab kev txhim kho ntxiv, compound 5 muaj trifluoroacetamide tau txais. Hloov cov benzothiazole ntawm 5 rau cyano kom tau PF-07321332 (xws li compound 6). Thaum kawg, xav txog cov compound' s bioavailability, antiviral kev ua haujlwm, thiab muaj peev xwm tsim tau, cov compound 6 tau siv los ua cov tshuaj nquag ua haujlwm rau kev sim tshuaj.
Thaum kawm txog cov tshuaj metabolism, cov kws tshawb fawb pom tias cytochrome P4503A4 enzyme oxidizes ntau qhov chaw ntawm PF-07321332 kom inactivate nws. Ntxiv cytochrome P4503A4 enzyme inhibitor, tus nqi inactivation ntawm PF-07321332 hauv tib neeg lub cev yuav raug txo kom tsawg. Yog li, cov kws tshawb fawb tau siv kev sib koom ua ke nrog cov muaj zog cytochrome P450 3A4 enzyme inhibitor ritonavir (RTV) kom nce cov tshuaj tiv thaiv kab mob ntawm PF-07321332 hauv tsev kho mob. Cov txiaj ntsig tau pom tias kev sib koom ua ke tuaj yeem ua kom cov ntshav siab ntawm cov tshuaj hauv qhov ncauj, yog li txhim kho cov kab mob zoo thiab txhim kho kev kho mob.
Tus kab mob SARS thiab tus kabmob tshiab no muaj nyob rau tib hom B coronavirus, tab sis lawv cov caj ces homology tsis siab heev. Tab sis hmoov zoo, lawv cov proteases zoo sib xws. Piv nrog rau cov kab mob sib txawv sib txawv, cov kab mob sib kis tau zoo heev yog cov hom phiaj tseem ceeb tshaj plaws thiab muaj txiaj ntsig zoo ntawm tus kab mob.
Tib lub sijhawm, raws li Reuters, Pfizer tau hais tias nws tau kos npe rau daim ntawv cog lus nrog" Medical Patent Pas (MPP)" tau txais kev txhawb nqa los ntawm United Nations tso cai rau cov chaw muag tshuaj los tsim cov tshuaj generic rau tus kabmob tshiab uas tsim los ntawm nws. Raws li kev pom zoo, tsuav yog Paxlovid tau tso cai siv los ntawm cov koom haum tswj hwm hauv ntau lub teb chaws, cov tuam txhab tshuaj tsim nyog tau tso cai los ntawm MPP yuav tuaj yeem muab cov tshuaj rau 95 lub teb chaws, uas yuav tsum tau them txog 53% ntawm lub ntiaj teb [ GG] #39;s pej xeem.
Seb Paxlovid, nrog rau nws cov khoom zoo thiab cov txiaj ntsig ntawm kev kho mob, tuaj yeem dhau los ua tus txiav tawm ntawm Covid-19 uas tau kis mus rau lub ntiaj teb, thiab dhau los ua kev cia siab ntawm tib neeg, cia peb tos thiab saib!
Qhov chaw:Official Account Pharmaceutical Affairs
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