{"entity":{"id":"fulzerasib","kind":"drug","name":"Fulzerasib","aka":[],"tldr":"Fulzerasib was the first KRAS G12C-blocking pill approved in China, for lung cancers carrying that mutation after earlier treatment.","summary":"Discovered by GenFleet Therapeutics and developed in China with Innovent, fulzerasib was approved by the NMPA in August 2024 for KRAS G12C-mutant advanced NSCLC after at least one systemic therapy, on a pivotal single-arm phase 2 study (Journal of Thoracic Oncology 2024) with a confirmed response rate near half of patients. It arrived three years after sotorasib in the US but within weeks of garsorasib, giving China two domestic KRAS G12C inhibitors before either Western drug was approved there. First-line combinations with cetuximab are in trials.","status":"approved","asOf":"2026-09-10","links":[{"label":"GenFleet Therapeutics","url":"https://www.genfleet.com/en/"},{"label":"IBI351 pivotal phase 2 (J Thorac Oncol 2024)","url":"https://doi.org/10.1016/j.jtho.2024.08.005"},{"label":"NMPA (National Medical Products Administration)","url":"https://www.nmpa.gov.cn"}],"tags":["china"],"related":[],"cancers":["nsclc"],"sections":[],"technologies":["kras-inhibitors","kinase-inhibitors"],"targets":["kras"],"drugs":[],"companies":["genfleet","innovent"],"institutions":[],"pathways":["ras-mapk"],"terms":["kras-mutation-subtypes"],"trials":["nct07601048","nct07581912","nct06936644"],"people":["yu-michael"],"bottlenecks":[],"keyPapers":["paper-zhou-j-thorac-oncol"],"journals":[],"dependsOn":[],"notes":[],"brand":"Dupert","code":"GFH925, IBI351","modality":"Small-molecule covalent KRAS G12C inhibitor","mechanism":"Covalent inhibitor locking KRAS G12C in its inactive GDP-bound state, blocking downstream RAF-MEK-ERK signalling.","approvals":[{"region":"China","year":2024,"indication":"KRAS G12C-mutant advanced NSCLC after at least one systemic therapy"}],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[]},"route":"/drugs/fulzerasib/","neighbours":{"cancer":[{"id":"nsclc","kind":"cancer","name":"Non-small-cell lung cancer","route":"/cancers/nsclc/"}],"technology":[{"id":"kras-inhibitors","kind":"technology","name":"KRAS & RAS inhibitors","route":"/technologies/kras-inhibitors/"},{"id":"kinase-inhibitors","kind":"technology","name":"Small-molecule kinase inhibitors","route":"/technologies/kinase-inhibitors/"}],"target":[{"id":"kras","kind":"target","name":"KRAS","route":"/targets/kras/"}],"company":[{"id":"genfleet","kind":"company","name":"GenFleet Therapeutics","route":"/companies/genfleet/"},{"id":"innovent","kind":"company","name":"Innovent Biologics","route":"/companies/innovent/"}],"pathway":[{"id":"ras-mapk","kind":"pathway","name":"RAS / RAF / MEK / ERK (MAPK)","route":"/pathways/ras-mapk/"}],"term":[{"id":"kras-mutation-subtypes","kind":"term","name":"KRAS mutation subtypes (G12C, G12D, G12V)","route":"/terms/kras-mutation-subtypes/"}],"trial":[{"id":"nct06936644","kind":"trial","name":"A Multicenter, Single-arm Phase II Study to Evaluate the Efficacy and Safety of Fulzerasib (IBI351) in Combination With Ivonescimab (AK-112) in First-line Treatment of Advanced or Metastatic Non-small Cell Lung Cancer Patients With KRAS G12C Mutation","route":"/trials/nct06936644/"},{"id":"nct07601048","kind":"trial","name":"A Trial of HRS-7058 in Advanced or Metastatic Non-Small Cell Lung Cancer Patients Who Have Failed Standard Treatment","route":"/trials/nct07601048/"},{"id":"nct07492342","kind":"trial","name":"Fulzerasib Sequential Sintilimab Plus Platinum-Doublet Neoadjuvant Therapy for Resectable KRAS G12C-Mutant NSCLC","route":"/trials/nct07492342/"},{"id":"nct07198841","kind":"trial","name":"IBI351 Plus Cetuximab β in Untreated Advanced Non-small Cell Lung Cancer With KRAS G12C Mutation","route":"/trials/nct07198841/"},{"id":"nct07581912","kind":"trial","name":"Neoadjuvant Treatment of Fulzerasib Plus Cetuximab N01 in KRAS G12C Mutated Locally Advanced Colorectal Cancer With or Without Resectable Metastases","route":"/trials/nct07581912/"}],"person":[{"id":"yu-michael","kind":"person","name":"Michael Yu (Yu De-Chao)","route":"/people/yu-michael/"}],"paper":[{"id":"paper-zhou-j-thorac-oncol","kind":"paper","name":"Efficacy and Safety of KRASG12C Inhibitor IBI351 Monotherapy in Patients With Advanced NSCLC: Results From a Phase 2 Pivotal Study","route":"/key-papers/paper-zhou-j-thorac-oncol/"}]}}