Characterization of structural, biochemical, pharmacokinetic, and pharmacodynamic properties of the LSD1 inhibitor bomedemstat in preclinical models.
Sumer JasmineAdel MandlTimothy E G KruegerSusan L DalrympleLizamma AntonyJennifer DiasCassandra A CelatkaAmy E TapperMaria KleppeMayuko KanayamaYuezhou JingValentina SperanziniYuzhuo Z WangJun LuoBruce J TrockSamuel R DenmeadeMichael A CarducciAndrea MatteviHugh Y RienhoffJohn T IsaacsW Nathaniel BrennenPublished in: The Prostate (2024)
Bomedemstat provides enhanced specificity against LSD1, as revealed by structural and biochemical data. PK/PD data display an overall safety profile with manageable side effects resulting from LSD1 inhibition using bomedemstat in preclinical models. Altogether, our results support clinical testing of bomedemstat in the setting of mCRPC.