Kutshanje, iGenFleet ibhengeze idatha yamva nje yesiGaba sesiBini sophando lwe-KROCUS, i-fulzerasib (GFH925, i-KRAS G12C inhibitor) kunye ne-cetuximab yonyango lomhlaza wamaphaphu olungengolweseli encinci (NSCLC) lomgca wokuqala, kwisishwankathelo esifutshane kwintetho emfutshane yomlomo yentlanganiso yonyaka yeNkomfa yoMhlaza wamaphaphu yaseYurophu ka-2025 (ELCC).
I-Fulzerasib yi-KRAS G12C inhibitor yokuqala eyenziwe eTshayina eyamkelweyo kwaye yanikwa ukungeniswa kwayo yi-NDA nge-Priority Review Designation yi-NMPA. I-Fulzerasib ikwafumene i-Breakthrough Therapy Designations kulo nyaka yokunyanga izigulane ze-KRAS G12C-mutant NSCLC eziphucukileyo ezifumene ubuncinci unyango olunye lwe-systemic kunye nezigulane ze-CRC ezifumene ubuncinci unyango lwe-systemic ezimbini. Usapho lweprotheyini ye-RAS lunokwahlulwa lube ziindidi ze-KRAS, HRAS kunye ne-NRAS. Utshintsho lwe-KRAS lufunyanwa phantse kwi-90% yomhlaza we-pancreatic, i-30-40% yomhlaza wamathumbu amakhulu, kunye ne-15-20% yezigulane zomhlaza wamaphaphu. Ukwenzeka kwe-KRAS G12C mutation subset kubonwa rhoqo kunezo zine-ALK, ROS1, RET kunye ne-TRK 1/2/3 mutations zidibene. I-GFH925 sisithinteli esitsha, esisebenzayo ngomlomo, esinamandla se-KRAS G12C esenzelwe ukujolisa ngempumelelo kwi-GTP/GDP exchange, inyathelo elibalulekileyo ekusebenzeni kwendlela, ngokuguqula intsalela ye-cysteine yeprotheyini ye-KRAS G12C ngokudibeneyo nangokungenakujikwa. Izifundo zokukhetha i-cysteine zangaphambi kweklinikhi zibonise ukukhetha okuphezulu kwe-fulzerasib kwi-G12C. Emva koko, i-fulzerasib ithintela ngempumelelo indlela yesignali esezantsi ukuze ibangele i-apoptosis yeeseli zethumba kunye nokubanjwa komjikelo weseli.
Izigulane ezingama-47 ze-KRAS G12C-mutant NSCLC ezazingazange zinyangwe ngaphambili zinyangwe nge-fulzerasib kunye ne-cetuximab (fulzerasib 600mg BID + cetuximab 500 mg/m2 Q2W) ukusukela nge-14 kaJanuwari 2025.
Ukusebenza kakuhle: Ukusukela ngomhla wokugqibela wedatha, phakathi kwezigulana ezingama-45 ezifumene ubuncinane uvavanyo olunye emva konyango lwe-tumor, i-ORR yayiyi-80% kwaye i-DCR yayiyi-100%; ama-57.8% ayenokuncipha kwe-≥ 50% ye-tumor. Izigulana ezili-16 (34%) zazinobuchopho obuqhekezekileyo; phakathi kwezigulana ezili-14 eziqhekezekileyo ebuchotsheni ezifumene ubuncinane uvavanyo olunye emva konyango lwe-tumor, i-ORR nge-RECIST 1.1 yayiyi-71.4%. Ubude bexesha eliphakathi lokuphendula (DoR) abukafikelelwa okwangoku, kwaye izigulana ezingama-24 zazisafumana unyango olunexesha eliphakathi lokulandela iinyanga ezili-10.1. I-mPFS yayiyi-12.5 yeenyanga kwaye i-mOS ayifikelelwanga.
Ukhuseleko: Ukususela kumhla wokugqibela wedatha, unyango oludibeneyo lubonise iprofayili yokhuseleko/ukunyamezeleka okuhle. Ii-TRAE zenzeke kwi-87.2% yezigulane kwaye uninzi lwee-TRAE zanikwa amanqaku 1-2; I-14.9% yezigulane zafumana ubuncinane ii-TRAE zebanga lesi-3; azizange zibe ne-TRAE zebanga lesi-4-5. Izigulane ezi-2 zazineziganeko ezimbi ezinzulu ezinxulumene nonyango (TRSAE) kwaye ii-TRSAE zavavanywa ukuba zinxulumene ne-cetuximab kuphela; Izigulane ezi-3 zafumana ii-TRAE, ezingadibaniyo ne-fulzerasib, nto leyo eyakhokelela ekuyekeni kwedosi. I-KROCUS ibonise ukuba kukho ukuvela okuphantsi kokuyekiswa kwedosi okanye ukuncipha phakathi kwezifundo ezahlukeneyo ze-G12C-mutant NSLCL combo ezahlukeneyo. Akukho zimpawu zintsha zokhuseleko ezichongiweyo xa kuthelekiswa ne-fulzerasib okanye i-cetuximab njenge-arhente enye.
Okwangoku, kusekho iimvavanyo ezininzi zeklinikhi zobuchwepheshe obutsha bokulwa nomhlaza eTshayina obufuna izigulane. Iingcebiso ngamayeza amatsha kunye nobuchwepheshe, ungaqhagamshelana neSebe leMicimbi yeZibhedlele ze-Oncology zaseBeijing South Region.
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Ixesha leposi: Epreli-15-2025