Ngomhla wama-24 ku-Epreli, ngo-2025, iGenFleet Therapeutics yabhengeza ukuba i-US Food and Drug Administration (FDA) ivumile ukusetyenziswa kweyeza elitsha (IND) le-GFH375/VS-7375, i-KRAS G12D (ON/OFF) inhibitor yomlomo, kuvavanyo lweklinikhi lokunyanga izigulane ezine-tumor eqinileyo eziguqukileyo ezine-mutation ye-KRAS G12D. Olu phononongo lucwangciselwe ukuqaliswa liqabane leGenFleet iVerastem Oncology e-US malunga nonyaka ka-2025. Uphononongo lokuqala ebantwini lwe-GFH375 olwaqalwa yiGenFleet eTshayina luye lwaya kwisigaba sesiBini kwaye idatha yokuqala yokusebenza kakuhle kunye nokhuseleko yolu phononongo ikhethwe kwintetho yomlomo ngokukhawuleza kwiNtlanganiso yoNyaka ye-American Society of Clinical Oncology (ASCO) ezayo ka-2025.
Iiproteni ze-RAS, ezikwimo esebenzayo ebotshelelwe kwi-GTP okanye ebotshelelwe kwi-GDP engasebenziyo, zii-binary molecular switches ezilawula iimpendulo zeseli kwiindlela zokubonisa iimpawu kuquka i-RAS-RAF-MEK-ERK kunye ne-PI3K/AKT/mTOR. Iijini ezintathu ze-RAS zivumela ii-isoforms zeproteni, ezizezi: iKirsten Ras (KRAS), iHarvey Ras (HRAS) kunye neNeuroblastoma Ras (NRAS), kwaye i-KRAS yeyona oncogene iguquliweyo rhoqo ebantwini. Phakathi kweenguqu ze-KRAS, i-G12D, i-G12V, kunye ne-G12C zimele ii-alleles ezintathu eziphezulu eziguquliweyo rhoqo. Inguqu ye-KRAS G12D ixhaphake kakhulu kwi-pancreatic ductal adenocarcinoma, umhlaza we-colorectal, kunye ne-lung adenocarcinoma.
Ipesenti enkulu yezigulana ezine-KRAS G12D mutation zifunyanwa zingenambali yokutshaya kwaye zingasabela kakuhle kwii-PD-1 inhibitors. Ii-mutant-selective G12D inhibitors zinezithembiso zokunceda amaqela amakhulu ezigulana ze-PDAC eziqhutywa yi-KRAS kuba utshintsho lwe-KRAS G12D lolona tshintsho lwe-somatic oluhlala lusenzeka kwizigulana ze-PDAC (malunga nama-40%) ezixelwe ukuba zinezinga lokusinda leminyaka emi-5 elingaphantsi kwe-10%.
I-GFH375 sisithinteli se-KRAS G12D (ON/OFF) esisebenza ngomlomo, esinamandla, nesikhetha kakhulu i-KRAS G12D (ON/OFF) esenzelwe ukujolisa kwi-GTP/GDP exchange, ngaloo ndlela siphazamisa ukusebenza kweendlela ezisezantsi kwaye sithintele ngempumelelo ukwanda kweeseli ze-tumor. Izifundo zangaphambi kweklinikhi zibonise ukuthintelwa okuxhomekeke kwidosi kwiimodeli ezine-KRAS G12D mutation; I-GFH375 ikwabonise umngcipheko ophantsi ongekho kwithagethi ekukhetheni i-kinase kunye novavanyo lokhuseleko.
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.
Inombolo yefowuni: 4008803716
Email：myimmnet@163.com
Ixesha leposi: Epreli-25-2025