Fulzerasib

Fulzerasib
Clinical data
Other names	Dupert; GFH-925; IBI-351
Legal status
Legal status	Rx in China;
Identifiers
	IUPAC name (7R)-16-chloro-15-(2-fluoro-6-hydroxyphenyl)-7,9-dimethyl-12-(4-methyl-2-propan-2-yl-3-pyridinyl)-5-prop-2-enoyl-2,5,9,12,14-pentazatetracyclo[8.8.0.02,7.013,18]octadeca-1(10),13,15,17-tetraene-8,11-dione;
CAS Number	2641747-54-6;
PubChem CID	167713279;
IUPHAR/BPS	12393;
DrugBank	DB21609;
ChemSpider	129307087;
UNII	6D5B7F245W;
ChEBI	CHEBI:759169;
ChEMBL	ChEMBL5314463;
Chemical and physical data
Formula	C33H32ClFN6O4
Molar mass	631.11 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CC1=C(C(=NC=C1)C(C)C)N2C3=NC(=C(C=C3C4=C(C2=O)N(C(=O)[C@@]5(N4CCN(C5)C(=O)C=C)C)C)Cl)C6=C(C=CC=C6F)O;
	InChI InChI=InChI=1S/C33H32ClFN6O4/c1-7-23(43)39-13-14-40-28-19-15-20(34)26(24-21(35)9-8-10-22(24)42)37-30(19)41(27-18(4)11-12-36-25(27)17(2)3)31(44)29(28)38(6)32(45)33(40,5)16-39/h7-12,15,17,42H,1,13-14,16H2,2-6H3/t33-/m1/s1; Key:BRWVQEWFJJFLIQ-MGBGTMOVSA-N;

Fulzerasib is a drug that is approved in China to treat KRAS G12C-positive non-small cell lung cancer (NSCLC).^[2]^[1]^[3]

Prior to marketing approval, fulzerasib had received two breakthrough therapy designations, the first for advanced G12C-mutant NSCLC and a second, for colorectal cancer (CRC) from the Center for Drug Evaluation (CDE) of the Chinese National Medical Products Administration (NMPA).^[4]

References

1 2 Lamb YN (December 2024). "Fulzerasib: First Approval". Drugs. 84 (12): 1665–1671. doi:10.1007/s40265-024-02120-6. PMID 39587006.
↑ "Fulzerasib - GenFleet Therapeutics". AdisInsight. Springer Nature Switzerland AG.
↑ Jiang T, Lin C, Le S, Zhang L, Liang T, Cai L, et al. (August 2025). "Discovery of Fulzerasib (GFH925) for the Treatment of KRAS G12C-Mutated Solid Tumors". Journal of Medicinal Chemistry. 68 (15) acs.jmedchem.4c03183: 15386–15402. doi:10.1021/acs.jmedchem.4c03183. PMID 40701936.
↑ "Fulzerasib Phase II KROCUS Study | ASCO 2024". DelveInsight Business Research LLP. 2025.

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[Lamb_2024-1] 1 2 Lamb YN (December 2024). "Fulzerasib: First Approval". Drugs. 84 (12): 1665–1671. doi:10.1007/s40265-024-02120-6. PMID 39587006.

[AdisInsight-2] "Fulzerasib - GenFleet Therapeutics". AdisInsight. Springer Nature Switzerland AG.

[Jiang_2025-3] Jiang T, Lin C, Le S, Zhang L, Liang T, Cai L, et al. (August 2025). "Discovery of Fulzerasib (GFH925) for the Treatment of KRAS G12C-Mutated Solid Tumors". Journal of Medicinal Chemistry. 68 (15) acs.jmedchem.4c03183: 15386–15402. doi:10.1021/acs.jmedchem.4c03183. PMID 40701936.

[4] "Fulzerasib Phase II KROCUS Study | ASCO 2024". DelveInsight Business Research LLP. 2025.

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References