2. Academic Validation
  3. Optimization of METTL3 Inhibitors for the Treatment of Solid Tumors and AML

Optimization of METTL3 Inhibitors for the Treatment of Solid Tumors and AML

  • J Med Chem. 2026 Apr 23;69(8):9585-9602. doi: 10.1021/acs.jmedchem.6c00474.
Guillaume Dutheuil 1,  Killian Oukoloff 1,  François Lenoir 1,  Julien Korac 1,  Mohamed El Bousmaqui 1,  Nicolas Probst 1,  Alexey Lapin 1,  Galina Nakhabina 1,  Nicolas Parmentier 1,  Catherine Sorlet 1,  Graeme L Fraser 1
Affiliations

Affiliation

  • 1 Epics Therapeutics SA, rue Adrienne Bolland 47, 6041 Gosselies, Belgium.
PMID: 41978353 DOI: 10.1021/acs.jmedchem.6c00474
Abstract

Further lead optimization of our series of METTL3 inhibitors is disclosed where aggregative replacements of the α-methylpyridone core and 5-dimethylaminopyridin-3-yl-1,2,3-triazole hinge moiety with an oxetan-3-yl-pyridin-3-yl core and 5-cyclopropylpyridin-3-yl-1,3,4-thiadiazol-2-yl hinge moiety, respectively, improved oral bioavailability while decreasing lipophilicity, thereby translating into oral efficacy in mouse tumor models. This research culminates in the discovery of EP102, a compound with a clear selectivity profile and a favorable ADME/PK profile in addition to robust efficacy in AML and solid tumor models. EP102 has entered clinical development for the treatment of advanced solid tumors.

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