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Tunlametinib is a Chinese MEK inhibitor approved in 2024 for advanced melanoma with an NRAS mutation, a group with no targeted therapy elsewhere in the world, and in phase 3 trials with vemurafenib for BRAF-mutant disease and for colorectal cancer.
Shanghai Kechow Pharma's tunlametinib (HL-085) received NMPA approval in 2024 for advanced NRAS-mutant melanoma after prior immunotherapy, a first for that molecular group. NRAS mutations are common in the acral and mucosal melanomas that predominate in East Asia. Phase 3 trials test tunlametinib with vemurafenib in BRAF V600-mutant melanoma and in combinations for metastatic colorectal cancer.
An allosteric inhibitor of MEK1 and MEK2 that shuts off the MAPK pathway downstream of RAS and RAF, the route NRAS-mutant melanoma depends on. Connects to MEK1/2.
1.Tunlametinib slips into a pocket on MEK1/2.
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| Region | Year | Indication |
|---|---|---|
| CN | 2024 | Advanced NRAS-mutant melanoma after prior immunotherapy |
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Query for this drug: (TITLE:"Tunlametinib" OR ABSTRACT:"Tunlametinib" OR TITLE:"HL-085" OR ABSTRACT:"HL-085") 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 Tunlametinib, not a curated reading list.
Shares NRAS, Mucosal melanoma, Melanoma and the tag pipeline.
Shares Advanced melanoma (unresectable stage III and stage IV), Melanoma and the tag pipeline.
Shares Advanced melanoma (unresectable stage III and stage IV), Melanoma and the tag pipeline.
Shares NRAS, Colorectal cancer and the tag pipeline.
Shares Advanced melanoma (unresectable stage III and stage IV), Melanoma and the tag pipeline.
Shares Advanced melanoma (unresectable stage III and stage IV), Melanoma and the tag pipeline.
Shares Advanced melanoma (unresectable stage III and stage IV), Melanoma and the tag pipeline.
Shares Advanced melanoma (unresectable stage III and stage IV), Melanoma and the tag pipeline.