Goley Pharmaceutical Co., Ltd. tshaj tawm ntawm nws tus as-qhauj wechat thaum sawv ntxov Lub Kaum Hli 10 tias nws theem kuv ntau koob tshuaj nce ntxiv kev soj ntsuam ntawm ASC10, tus tshiab coronavirus qhov ncauj polymerase (RdRp) inhibitor, tau ua tiav hauv National Center for Infectious. Kab mob thiab Thawj Tsev Kho Mob ntawm Zhejiang University Tsev Kawm Ntawv Tshuaj Kho Mob nrog 24 yam kev noj qab haus huv hauv thawj peb pawg.
Qhov kev nce koob tshuaj ntau zaus no kuv sim yuav tso npe rau 72 yam kev noj qab haus huv, suav nrog 60 cov ntsiab lus hauv rau 6 lub koob tshuaj nce ntxiv thiab 12 yam kev kawm hauv kev sim tshuaj noj. Kev tso npe kawm yuav tsum ua kom tiav nyob rau lub quarter thib plaub ntawm 2022. Rau caum yam kev noj qab haus huv yuav raug muab faib ua rau pawg neeg kom tau txais ntau qhov kev nce qib ntawm 50 mg, 100 mg, 200 mg, 400 mg, 600 mg, thiab 800 mg ASC10 ntsiav tshuaj lossis placebo ob zaug. ib hnub (BID) rau 5.5 hnub. Qhov kev sim yog ob qhov muag tsis pom kev thiab cov placebo-tswj los ntsuas kev nyab xeeb, kev zam, thiab cov tshuaj pharmacokinetics (PK) ntawm ASC10 ntsiav tshuaj. Cov 12 cov ntsiab lus ntxiv yuav raug randomized kom tau txais ob koob tshuaj ntawm 800 mg ASC10 ntsiav tshuaj (postprandial lossis yoo mov) txhawm rau ntsuas PK cov nyhuv ntawm cov zaub mov ntawm ASC10 hauv cov kev noj qab haus huv.
Goley yog thawj lub tuam txhab biotechnology Suav tau txais kev pom zoo los ntawm US Food and Drug Administration (FDA) thiab Tuam Tshoj National Medical Products Administration (NDA) los ua qhov kev sim tshuaj tshiab (IND) ntawm qhov ncauj RdRp inhibitor. Thaum Lub Yim Hli 3, 2022, Golly tau tshaj tawm tias FDA tau pom zoo daim ntawv thov IND rau ASC10 los ua Phase Ib qhov kev sim tshuaj rau cov neeg mob uas muaj tus mob me-rau-mob siab COVID-19 (Golly tshaj tawm tias qhov ncauj RdRp inhibitor ASC10 tau txais FDA kev pom zoo los ua ib qho kev sib tw, cov placebo-tswj theem Ib qhov kev sim tshuaj rau cov neeg mob uas mob me-rau-mob COVID-19). Thaum Lub Yim Hli 22, 2022, Golly tau tshaj tawm tias Tuam Tshoj National Food and Drug Administration tau pom zoo daim ntawv thov IND rau ASC10 los ua theem I kev sim tshuaj rau cov kev noj qab haus huv (Golly tshaj tawm tias Tuam Tshoj National Food and Drug Administration tau pom zoo rau daim ntawv thov kuaj mob tshiab rau ASC10. , ib qho tshiab qhov ncauj RdRp inhibitor). Golly yog nyob rau hauv kev sib txuas lus nrog cov neeg saib xyuas kev tswj hwm los tshawb txog qhov muaj peev xwm ntawm kev nthuav dav ntxiv ntawm kev kho mob ntawm ASC10.
ASC10 yog ib qho tshuaj tiv thaiv qhov ncauj nrog cov tshuaj sib txawv tshiab piv rau molnupiravir, ib qho tshuaj. Tom qab kev tswj hwm qhov ncauj, ob qho tib si ASC10 thiab monupivir tau hloov pauv sai thiab ua tiav rau tib lub zog metabolite ASC10-A, tseem hu ua -DN4-hydroxycytidine (NHC) hauv vivo. ASC10 tau tsim los ntawm Golly nws tus kheej. Golly tau foob ntau daim ntawv thov patent rau ASC10 thiab nws siv thoob ntiaj teb. ASC10 ntsiav tshuaj qhov ncauj siv hauv kev tshawb fawb soj ntsuam no yog cov khoom tsim nrog Gollie's proprietary technology.
Los ntawm kev siv lub tswv yim dual prodrug, ASC1{{10}} permeability nyob rau hauv Caco-2 hlwb (tib neeg mob plab adenocarcinoma hlwb) thiab active metabolite raug nyob rau hauv liab yog 3.2-thiab 2. 1-fold siab dua monupivir, feem. Hauv tus qauv nas ntawm tus kab mob COVID-19, ASC10 ntawm 240 mg / kg ob zaug hauv ib hnub txo tus kab mob titer hauv nas ntsws los ntawm tus nqi ntawm 4.0, zoo ib yam nrog cov nyhuv ntawm monupivir ntawm 500 mg / kg ob zaug ib hnub [1 ]. Cov kev tshawb fawb tau pom [2,3] tias ASC10-A (tseem hu ua EIDD-1931) tiv taus Omicron variant virus (BA.1 EC50=0.3 µM; BA. 2 EC50=(xws li 0.25 M; BA. EC50=0.23 (xws li 5 M; BA.2.75 EC50=0.90 µM), Delta variant virus (EC{{31}) }.5 µM) thiab hom kab mob qus (EC50=0.7 µM) tau pom tias muaj zog ntawm cov tshuaj tiv thaiv kab mob hauv cellular. Txoj kev tshawb no kuj pom tias tsis muaj kev sib cuam tshuam ntawm cov tshuaj yeeb tshuaj ntawm ASC10 thiab lwm yam tshuaj siv.
