Muva nje, i-GenFleet imemezele idatha yakamuva yesigaba sesi-2 socwaningo lwe-KROCUS, i-fulzerasib (GFH925, i-KRAS G12C inhibitor) ngokuhlanganiswa ne-cetuximab yokwelashwa komdlavuza wamaphaphu ongewona amaseli amancane (i-NSCLC) komugqa wokuqala, esifinyezweni esisheshayo esethulweni esincane somlomo somhlangano waminyaka yonke we-European Lung Cancer Conference (ELCC) ka-2025.
I-Fulzerasib ingumvimbeli wokuqala we-KRAS G12C owakhiwe eShayina owamukelwe futhi wanikezwa ukuhanjiswa kwe-NDA nge-Priority Review Designation yi-NMPA. I-Fulzerasib iphinde yathola i-Breakthrough Therapy Designations kulo nyaka yokwelapha iziguli ze-NSCLC eziguquliwe ze-KRAS G12C eziye zathola okungenani ukwelashwa okukodwa kwesistimu kanye neziguli ze-CRC eziye zathola okungenani ukwelashwa okubili kwesistimu. Umndeni wamaprotheni e-RAS ungahlukaniswa ngezigaba ze-KRAS, HRAS kanye ne-NRAS. Ukuguqulwa kwe-KRAS kutholakala cishe ku-90% womdlavuza we-pancreatic, u-30-40% womdlavuza wamathumbu amakhulu, kanye neziguli ezingu-15-20% zomdlavuza wamaphaphu. Ukuvela kwe-KRAS G12C mutation subset kuvame ukubonwa kunalezo ezine-ALK, ROS1, RET kanye ne-TRK 1/2/3 mutations zihlangene. I-GFH925 iyi-KRAS G12C inhibitor entsha, esebenza ngomlomo, enamandla eyenzelwe ukuqondisa ngempumelelo ukushintshaniswa kwe-GTP/GDP, isinyathelo esibalulekile ekusebenzeni kwendlela, ngokushintsha insalela ye-cysteine yeprotheyini ye-KRAS G12C ngokuhambisana nangokungaguquki. Izifundo zokukhetha i-cysteine zangaphambi kokwelashwa zibonise ukukhetha okuphezulu kwe-fulzerasib ku-G12C. Ngemuva kwalokho, i-fulzerasib ivimbela ngempumelelo indlela yesignali engezansi ukuze ibangele ukuqhuma kwamaseli esimila kanye nokuboshwa komjikelezo weseli.
Iziguli ezingu-47 ze-KRAS G12C-mutant NSCLC ezazingelashwanga ngaphambili zelashwe nge-fulzerasib kanye ne-cetuximab (fulzerasib 600mg BID + cetuximab 500 mg/m2 Q2W) kusukela ngomhlaka-14 Januwari 2025.
Ukusebenza kahle: Kusukela ngosuku lokugcina idatha, phakathi kweziguli ezingu-45 ezithole okungenani ukuhlolwa okukodwa kwesimila ngemva kokwelashwa, i-ORR yayingu-80% kanti i-DCR yayingu-100%; abangu-57.8% babene-≥ 50% yesimila esinciphile. Iziguli ezingu-16 (34%) zazine-metastasis yobuchopho; phakathi kweziguli ezingu-14 ezazine-metastatic yobuchopho ezithole okungenani ukuhlolwa okukodwa kwesimila ngemva kokwelashwa, i-ORR nge-RECIST 1.1 yayingu-71.4%. Isikhathi esimaphakathi sokuphendula (i-DoR) asikafinyelelwa, kanti iziguli ezingu-24 zazisathola ukwelashwa ngokulandelana okumaphakathi kwezinyanga ezingu-10.1. I-mPFS yayiyizinyanga ezingu-12.5 kanti i-mOS ayifinyelelwanga.
Ukuphepha: Kusukela ngosuku lokugcina idatha, ukwelashwa okuhlanganisiwe kuveze iphrofayili yokuphepha/ukubekezeleleka okuhle. Ama-TRAE enzeka ku-87.2% weziguli futhi iningi lama-TRAE lafakwa ku-1-2; 14.9% weziguli wabhekana okungenani ne-TRAE eyodwa yebanga lesi-3; azikho i-TRAE zebanga lesi-4-5. Iziguli ezimbili zazinezehlakalo ezimbi kakhulu ezihlobene nokwelashwa (TRSAE) kanti ama-TRSAE ahlolwe ukuthi ahlobene ne-cetuximab kuphela; iziguli ezi-3 zabhekana ne-TRAE, ezingahlobene ne-fulzerasib, okwaholela ekuyekeni komthamo. I-KROCUS ibonise ukwenzeka okuphansi kakhulu kokuyekiswa komthamo noma ukwehla phakathi kwezifundo ezahlukene ze-G12C-mutant NSLCL combo ze-line yokuqala. Azikho izimpawu zokuphepha ezintsha ezitholiwe uma kuqhathaniswa ne-fulzerasib noma i-cetuximab njenge-ejenti eyodwa.
Njengamanje, kusenezivivinyo eziningi zemitholampilo zobuchwepheshe obusha bokulwa nomdlavuza eShayina ezifuna iziguli. Ukubonisana ngemithi emisha kanye nobuchwepheshe, ungaxhumana noMnyango Wezizwe Ngezizwe Wesibhedlela iBeijing South Region Oncology.
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Isikhathi sokuthunyelwe: Ephreli-15-2025