Luvometinib

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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

Example 6 [WO2014169843]

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

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References

  1.  Cheng Y, Tian H (2017). “Current Development Status of MEK Inhibitors”Molecules22 (10). Basel, Switzerland: 1551. doi:10.3390/molecules22101551PMC 6151813PMID 28954413.
  2.  Keam SJ (2025). “Luvometinib: First Approval”. Drugs85 (9): 1177–1183. doi:10.1007/s40265-025-02217-6PMID 40751881.
Clinical data
Trade names复迈宁 (Fu Mainin)
Other namesFCN-159
Routes of
administration
Oral
Identifiers
IUPAC name
CAS Number2739690-43-6
PubChem CID135210935
IUPHAR/BPS13495
UNIIB2DYT4V89X
Chemical and physical data
FormulaC26H22F2IN5O4S
Molar mass665.45 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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