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Boehringer Ingelheim thiab Mirati Cov Kev Kho Mob Tshaj Tawm tau tshaj tawm tias lawv tau mus cuag kev soj ntsuam kev koom tes los soj ntsuam Boehringer Ingelheim' s yias-KRAS inhibitor BI1701963 nrog Mirati' s KRAS G12C xaiv cov tshuaj tiv thaiv MRTX849 rau kev kho mob ntawm KRAS G12C cov kev ua kom tau txais txiaj ntsig ntawm cov neeg mob uas hlav cov hlav hlav. Qhov kev koom tes no yuav tshawb nrhiav qhov muaj peev xwm ntawm qhov kev sib koom ua ke no los muab cov lus teb tau zoo dua thiab siv tau ntev dua rau cov neeg mob ntsws thiab txoj hnyuv laus uas tam sim no muaj cov kev xaiv kho tsawg.
MRTX849 tsim los ntawm Mirati yog ib qho tshwj xeeb inhibitor ntawm KRAS G12C mutant. Los ntawm covalently khi rau KRAS G12C mutant, nws xauv lub KRAS G12C mutant nyob rau hauv lub xeev tsis muaj zog, thiaj li tiv thaiv KRAS cov haujlwm. MRTX849 raug soj ntsuam nyob rau ntu 1/2 chaw kuaj mob los kho cov neeg mob nrog KRAS G12C zoo kawg ua cov qog.
Boehringer Ingelheim' s BI1701963 yog hom tshiab ntawm qhov ncauj me me uas khi rau catalytic thaj tsam ntawm SOS1 kom nws tsis txhob cuam tshuam nrog lub xeev tsis muaj sia nyob ntawm KRAS thiab tib lub sijhawm thaiv cov lus tawm tswv yim tsav los ntawm SOS1. Qhov no txo qhov tsim ntawm KRAS kev ua haujlwm hauv xeev, yog li thaiv txoj haujlwm ntawm MAPK cov paib hais qhia nyob rau hauv KRAS-qog nqaij hlav. Los ntawm kev xaiv tiv thaiv SOS1, kev ua haujlwm ntawm ntau yam ntawm KRAS hloov pauv tuaj yeem tsis hais qhov twg ntawm KRAS kev hloov pauv (pan-KRAS inhibition).
Cov ntaub ntawv tshaj tawm qhia tau hais tias kev sib xyaw ntawm KRAS G12C inhibitor thiab yias-KRAS inhibitor BI1701963 tuaj yeem txhim kho kev tiv thaiv qog ua haujlwm raws li kev sib xyaw ua ke ntawm cov tshuaj tiv thaiv cov qog ntshav. BI1701963 tuaj yeem ua rau ntau dua KRAS G12C hloov pauv nyob rau hauv lub xeev tsis muaj zog los ntawm hloov KRAS qhov sib npaug ntawm lub xeev qhib rau lub xeev tsis muaj sia, thiab txhawb lawv txoj kev khi nrog covalent KRAS G12C inhibitors.
![(S) - 3, 4-Dihydro-4-hydroxy-2 - (3 - methoxypropyl) -2H-thieno [3, 2-e] -1,2-thiazine -6-sulfonamide 1, 1-dioxide CAS 1 54127-42-1](/uploads/202022606/small/s-3-4-dihydro-4-hydroxy-2-3-methoxypropyl-2h17065155349.png?size=264x0)
