Tunlametinib

Tunlametinib
Clinical data
Trade names	科露平
Other names	HL-085
Legal status
Legal status	Rx in China;
Identifiers
	IUPAC name 4-Fluoro-5-(2-fluoro-4-iodoanilino)-N-(2-hydroxyethoxy)-1,3-benzothiazole-6-carboxamide;
CAS Number	1801756-06-8;
PubChem CID	71621329;
ChemSpider	115006753;
UNII	IF25NR1PV3;
ChEMBL	ChEMBL5095241;
Chemical and physical data
Formula	C16H12F2IN3O3S
Molar mass	491.25 g·mol−1

Tunlametinib (trade name 科露平) is a pharmaceutical drug for the treatment of cancer. It is an inhbitor of mitogen-activated protein kinase kinase.^[1]

In China, tunlametinib was approved in 2024 for the treatment of patients with NRAS-mutated advanced melanoma who were previously treated with a PD-1/PD-L1 targeting agent.^[2]^[3]

It is also being studied for use in combination with vemurafenib in patients with advanced BRAF V600-mutant solid tumors.^[4]

References

^ "Tunlametinib". NCI Drug Dictionary. National Cancer Institute.
^ "Tunlametinib Wins Approval in China for NRAS+ Advanced Melanoma After PD-1/PD-L1 Therapy". March 18, 2024.
^ Keam, Susan J. (2024). "Tunlametinib: First Approval". Drugs. 84 (8): 1005–1010. doi:10.1007/s40265-024-02072-x. PMID 39034326.
^ Shi, Yuankai; Han, Xiaohong; Zhao, Qian; Zheng, Yulong; Chen, Jianhua; Yu, Xinmin; Fang, Jian; Liu, Yutao; Huang, Dingzhi; Liu, Tianshu; Shen, Hong; Luo, Suxia; Yu, Hongsheng; Cao, Yu; Zhang, Xi; Hu, Pei (2024). "Tunlametinib (HL-085) plus vemurafenib in patients with advanced BRAF V600-mutant solid tumors: An open-label, single-arm, multicenter, phase I study". Experimental Hematology & Oncology. 13 (1): 60. doi:10.1186/s40164-024-00528-0. PMC 11167782. PMID 38867257.

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[1] "Tunlametinib". NCI Drug Dictionary. National Cancer Institute.

[2] "Tunlametinib Wins Approval in China for NRAS+ Advanced Melanoma After PD-1/PD-L1 Therapy". March 18, 2024.

[3] Keam, Susan J. (2024). "Tunlametinib: First Approval". Drugs. 84 (8): 1005–1010. doi:10.1007/s40265-024-02072-x. PMID 39034326.

[4] Shi, Yuankai; Han, Xiaohong; Zhao, Qian; Zheng, Yulong; Chen, Jianhua; Yu, Xinmin; Fang, Jian; Liu, Yutao; Huang, Dingzhi; Liu, Tianshu; Shen, Hong; Luo, Suxia; Yu, Hongsheng; Cao, Yu; Zhang, Xi; Hu, Pei (2024). "Tunlametinib (HL-085) plus vemurafenib in patients with advanced BRAF V600-mutant solid tumors: An open-label, single-arm, multicenter, phase I study". Experimental Hematology & Oncology. 13 (1): 60. doi:10.1186/s40164-024-00528-0. PMC 11167782. PMID 38867257.

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