revumenib   Click here for help

GtoPdb Ligand ID: 11882

Synonyms: Revuforj® | SNDX-5613 | SNDX5613
Approved drug PDB Ligand
revumenib is an approved drug (FDA (2024))
Compound class: Synthetic organic
Comment: The chemical structure for revumenib was revealed in WHO proposed INN list 126 (Jan 2022), in which it was described as an antineoplastic agent. It resolved to Syndax Pharmaceuticals' SNDX-5613 via a PubChem match on SMILES. SNDX-5613 inhbits the Menin-KMT2A protein-protein interaction (binding directly to menin), as a strategy that was originally proposed to treat acute leukemias that are driven by proleukemogenic KMT2A rearrangements [1].
Additional menin inhibitors in development include bleximenib (JNJ-75276617), ziftomenib (KO-539), emilumenib (DS-1594a), enzomenib (DSP-5336) and icovamenib (BMF-219).
2D Structure
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Physico-chemical Properties
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Hydrogen bond acceptors 9
Hydrogen bond donors 1
Rotatable bonds 12
Topological polar surface area 116.35
Molecular weight 630.34
XLogP 4.69
No. Lipinski's rules broken 1

Generated using the Chemistry Development Kit (CDK) (Willighagen EL et al. Journal of Cheminformatics vol. 9:33. 2017, doi:10.1186/s13321-017-0220-4; https://cdk.github.io/)

SMILES / InChI / InChIKey
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Canonical SMILES CCN(C(=O)c1cc(F)ccc1Oc1cncnc1N1CC2(C1)CCN(CC2)C[C@@H]1CC[C@H](CC1)NS(=O)(=O)CC)C(C)C
Isomeric SMILES C(C)S(=O)(=O)N[C@@H]1CC[C@H](CC1)CN1CCC2(CN(C2)c2ncncc2Oc2c(C(=O)N(C(C)C)CC)cc(cc2)F)CC1
InChI InChI=1S/C32H47FN6O4S/c1-5-39(23(3)4)31(40)27-17-25(33)9-12-28(27)43-29-18-34-22-35-30(29)38-20-32(21-38)13-15-37(16-14-32)19-24-7-10-26(11-8-24)36-44(41,42)6-2/h9,12,17-18,22-24,26,36H,5-8,10-11,13-16,19-21H2,1-4H3/t24-,26-
InChI Key FRVSRBKUQZKTOW-YOCNBXQISA-N

Generated using the Chemistry Development Kit (CDK) (Willighagen EL et al. Journal of Cheminformatics vol. 9:33. 2017, doi:10.1186/s13321-017-0220-4; https://cdk.github.io/)

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Summary of Clinical Use Click here for help
Revumenib (SNDX-5613) was advanced to clinical evaluation in defined types of acute lukemia. First approval was granted by the FDA in November 2024, to treat relapsed/refractory acute leukemia with a lysine methyltransferase 2A gene (KMT2A) translocation [3]. It is also under investigation in cancers harbouring mutations in nucleophosmin (NPM1) or nucleoporin 98 and 96 precursor (NUP98) genes, or with dysregulated HOX/MEIS gene expression.
Clinical Trials
Clinical Trial ID Title Type Source Comment References
NCT04065399 A Study of SNDX-5613 in R/R Leukemias Including Those With an MLLr/KMT2A Gene Rearrangement or NPM1 Mutation Phase 1/Phase 2 Interventional Syndax Pharmaceuticals 2
NCT06226571 A Study of SNDX-5613 in Combination With Intensive Chemotherapy in Participants With Acute Myeloid Leukemias Phase 1 Interventional Syndax Pharmaceuticals
NCT06313437 Revumenib in Combination With 7+3 + Midostaurin in AML Phase 1 Interventional Dana-Farber Cancer Institute