



Luvometinib
CAS 2739690-43-6
MF C26H22F2IN5O4S MW665.5 g/mol
CHINA 2025, APPROVALS 2025
N-[3-[6-cyclopropyl-3-fluoro-4-(2-fluoro-4-iodoanilino)-1-methyl-2,5-dioxopyrido[2,3-d]pyridazin-8-yl]phenyl]cyclopropanesulfonamide
N-{3-[6-cyclopropyl-3-fluoro-4-(2-fluoro-4-iodoanilino)-1-methyl-2,5-dioxo-1,2,5,6-tetrahydropyrido[2,3-
d]pyridazin-8-yl]phenyl}cyclopropanesulfonamide
mitogen-activated protein kinase (MEK) inhibitor, antineoplastic, FCN 159, FCN-159, B2DYT4V89X
Luvometinib is a drug for the treatment of various types of cancer. It is a selective, orally administered inhibitor of mitogen-activated protein kinase kinases 1 and 2 (MEK1/MEK2), developed by Fosun Pharma for the treatment of rare malignancies, especially those driven by abnormal abnormal mitogen-activated protein kinase (MAPK) activation.[1][2]
In May 2025, it was approved in China for the treatment of histiocytic neoplasms such as Langerhans cell histiocytosis (LCH) and the genetic disease neurofibromatosis type 1 (NF1).[2]
Luvometinib is an orally bioavailable inhibitor of mitogen-activated protein kinase kinase (MAP2K, MAPK/ERK kinase, or MEK) 1 and 2, with potential antineoplastic activity. Upon administration, luvometinib selectively binds to and inhibits the activity of MEK1 and MEK2, preventing the activation of MEK1/2-dependent effector proteins and transcription factors, which may result in the inhibition of growth factor-mediated cell signaling and tumor cell proliferation. MEK1/2 are dual-specificity threonine/tyrosine kinases that play key roles in the activation of the RAS/RAF/MEK/ERK pathway that regulates cell growth. This pathway is often dysregulated in a variety of tumor cell types through BRAF, KRAS and NRAS mutations.
Luvometinib is a small molecule drug. The usage of the INN stem ‘-tinib’ in the name indicates that Luvometinib is a tyrosine kinase inhibitor. Luvometinib is under investigation in clinical trial NCT07004075 (FCN-159 Monotherapy Versus Chemotherapy by Investigator’s Choice in Pediatric Low-grade Glioma Patients With BRAF Alteration). Luvometinib has a monoisotopic molecular weight of 665.04 Da.
SYN
https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2014169843&_cid=P22-MLD4HW-79323-1
Example 8
N-(3-(6-allyl-3-ƒluoro-4-(2-ƒluoro-4-iodophenylamino)-1-methyl-2,5-dioxo-1,2,5,6- tetrahydropyrido[2,3-d]pyridazin-8-yl)phenyl)cyclopropanesulƒonamide (8)
The title compound 8 was prepared following the same procedure as described for Example 5 by substituting methanesulfonyl chloride with cyclopropanesulfonyl chloride. MS-ESI (m/z): 666 [M + 1]+.
PAT
https://patentscope.wipo.int/search/en/detail.jsf?docId=EP159733179&_cid=P22-MLD4C4-76451-1
Example 8
N-(3-(6-cyclopropyl-3-fluoro-4-(2-fluoro-4-iodophenylamino)-1-methyl-2,5-dioxo-1,2,5,6-tetrahydropyrido[2,3-d]pyridazin-8-yl)phenyl)cyclopropanesulfonamide (8)
[0136] The title compound 8 was prepared following the same procedure as described for Example 5 by substituting methanesulfonyl chloride with cyclopropanesulfonyl chloride. MS-ESI (m/z): 666 [M + 1] +.
PAT
- Protein kinase inhibitorsPublication Number: CN-106905316-BPriority Date: 2013-04-18Grant Date: 2021-06-01
- Certain protein kinase inhibitorsPublication Number: EP-2986611-B1Priority Date: 2013-04-18Grant Date: 2019-02-06
- Certain protein kinase inhibitorsPublication Number: US-10022374-B2Priority Date: 2013-04-18Grant Date: 2018-07-17



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References
- Cheng Y, Tian H (2017). “Current Development Status of MEK Inhibitors”. Molecules. 22 (10). Basel, Switzerland: 1551. doi:10.3390/molecules22101551. PMC 6151813. PMID 28954413.
- Keam SJ (2025). “Luvometinib: First Approval”. Drugs. 85 (9): 1177–1183. doi:10.1007/s40265-025-02217-6. PMID 40751881.
| Clinical data | |
|---|---|
| Trade names | 复迈宁 (Fu Mainin) |
| Other names | FCN-159 |
| Routes of administration | Oral |
| Identifiers | |
| IUPAC name | |
| CAS Number | 2739690-43-6 |
| PubChem CID | 135210935 |
| IUPHAR/BPS | 13495 |
| UNII | B2DYT4V89X |
| Chemical and physical data | |
| Formula | C26H22F2IN5O4S |
| Molar mass | 665.45 g·mol−1 |
| 3D model (JSmol) | Interactive image |
| SMILES | |
| InChI | |
//////////luvometinib, CHINA 2025, APPROVALS 2025, antineoplastic, FCN 159, FCN-159, B2DYT4V89X, ANAX, PTFEON, ADVECT, BLUE JET
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