Ngo-Ephreli 24, 2025, i-GenFleet Therapeutics yamemezela ukuthi i-US Food and Drug Administration (FDA) ivumile ukusetshenziswa kwesidakamizwa esisha (IND) se-GFH375/VS-7375, i-KRAS G12D (ON/OFF) inhibitor yomlomo, yokuhlolwa kwezokwelapha iziguli ezine-tumor eqinile ezigugile ezine-mutation ye-KRAS G12D. Lolu cwaningo luhlelwe ukuthi luqalwe ngumlingani we-GenFleet i-Verastem Oncology e-US cishe maphakathi no-2025. Ucwaningo lokuqala kubantu lwe-GFH375 olwaqalwa yi-GenFleet eShayina luye lwaqhubekela esigabeni sesi-2 futhi idatha yokuqala yokusebenza kahle nokuphepha yalolu cwaningo ikhethwe ekubonisweni okusheshayo komlomo eMhlanganweni Wonyaka we-American Society of Clinical Oncology (ASCO) ka-2025.
Amaprotheni e-RAS, ngesimo esisebenzayo esiboshelwe yi-GTP noma esingasebenzi se-GDP, angama-binary molecular switch alawula izimpendulo zamaseli ezindleleni zokubonisa izimpawu okuhlanganisa i-RAS-RAF-MEK-ERK kanye ne-PI3K/AKT/mTOR. Ama-gene amathathu e-RAS afaka ikhodi yama-isoforms e-protein, okungukuthi i-Kirsten Ras (KRAS), i-Harvey Ras (HRAS) kanye ne-Neuroblastoma Ras (NRAS), kanti i-KRAS iyi-oncogene eguquliwe kakhulu kubantu. Phakathi kwezinguquko ze-KRAS, i-G12D, i-G12V, kanye ne-G12C zimelela ama-allele amathathu aphezulu aguquliwe kakhulu. Ukuguqulwa kwe-KRAS G12D kuvame ukutholakala ku-pancreatic ductal adenocarcinoma, umdlavuza we-colorectal, kanye ne-lung adenocarcinoma.
Iphesenti elikhulu leziguli ezine-KRAS G12D mutation zitholakala zingenawo umlando wokubhema futhi zinempendulo embi kuma-PD-1 inhibitors. Ama-G12D inhibitors akhetha i-mutant anezithembiso zokuzuzisa izingxenye ezinkulu zeziguli ze-PDAC eziqhutshwa yi-KRAS njengoba izinguquko ze-KRAS G12D ziyizinguquko ezenzeka kakhulu ezigulini ze-PDAC (cishe ama-40%) okubikwa ukuthi zinesilinganiso sokusinda seminyaka emi-5 esingaphansi kwama-10%.
I-GFH375 iyisivimbeli se-KRAS G12D (ON/OFF) esisebenza ngomlomo, esinamandla, nesikhetha kakhulu i-KRAS G12D (ON/OFF) esiklanyelwe ukuqondisa ukushintshaniswa kwe-GTP/GDP, ngaleyo ndlela siphazamise ukusebenza kwezindlela ezingezansi futhi sivimbele ngempumelelo ukwanda kwamaseli esimila. Izifundo zangaphambi kokwelashwa zibonise ukuvinjelwa okuncike kumthamo kumamodeli ane-KRAS G12D mutation; I-GFH375 iphinde yabonisa ingozi ephansi ngaphandle kwenhloso ekukhetheni kwe-kinase kanye nokuhlolwa kokuphepha kwenhloso.
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-25-2025