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mk-8245

Development stage: Phase 2
Lead developer: Merck
Modality: Small Molecules
Administration: Oral

Overview

MK-8245 is a potent, orally active, liver-targeted small molecule inhibitor of stearoyl-CoA desaturase 1 (SCD1), developed by Merck for the treatment of type 2 diabetes mellitus. It selectively inhibits SCD1 with nanomolar potency (IC50 = 1 nM for human SCD1) and demonstrates anti-diabetic and anti-dyslipidemic efficacy in preclinical models. The compound was designed to target the liver via organic anion transporting polypeptides (OATPs), aiming to maximize therapeutic effects while minimizing adverse events associated with SCD inhibition in other tissues such as skin and eye. Clinical development reached Phase 2 trials for type 2 diabetes but was subsequently discontinued[1][3][4][6][7][8].

Other names: MK-8245MK8245MK 8245

Targets

SCD1 (Stearoyl-CoA desaturase 1)

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