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Fulzerasib was the first KRAS G12C-blocking pill approved in China, for lung cancers carrying that mutation after earlier treatment.
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.
Covalent inhibitor locking KRAS G12C in its inactive GDP-bound state, blocking downstream RAF-MEK-ERK signalling. Connects to KRAS.
1.Fulzerasib slips into a pocket on KRAS.
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| Region | Year | Indication |
|---|---|---|
| China | 2024 | KRAS G12C-mutant advanced NSCLC after at least one systemic therapy |
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Query for this drug: (TITLE:"Fulzerasib" OR ABSTRACT:"Fulzerasib" OR TITLE:"Dupert" OR ABSTRACT:"Dupert" OR TITLE:"GFH925" OR ABSTRACT:"GFH925" OR TITLE:"IBI351" OR ABSTRACT:"IBI351") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about Fulzerasib, not a curated reading list.
Shares A Trial of HRS-7058 in Advanced or Metastatic Non-Small Cell Lung Cancer Patients Who Have Failed Standard Treatment, KRAS mutation subtypes (G12C, G12D, G12V), KRAS & RAS inhibitors, RAS / RAF / MEK / ERK (MAPK) and the tag china.
Shares Michael Yu (Yu De-Chao), Innovent Biologics and the tag china.
Shares RAS / RAF / MEK / ERK (MAPK), Small-molecule kinase inhibitors, Non-small-cell lung cancer and the tag china.
Shares Innovent Biologics, Non-small-cell lung cancer and the tag china.
Shares RAS / RAF / MEK / ERK (MAPK), Small-molecule kinase inhibitors, Non-small-cell lung cancer and the tag china.
Shares Small-molecule kinase inhibitors, Non-small-cell lung cancer and the tag china.
Shares Innovent Biologics and the tag china.
Shares RAS / RAF / MEK / ERK (MAPK), Small-molecule kinase inhibitors and the tag china.