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CNT2130 is a small-molecule, once-daily oral inhibitor of dihydroceramide desaturase 1 (DES1), developed by Centaurus Therapeutics. DES1 is the enzyme responsible for the final step of de novo ceramide synthesis, converting dihydroceramide to ceramide. By inhibiting DES1, CNT2130 aims to reduce excess ceramide production and restore lipid balance in tissues, which is hypothesized to address the underlying pathology of cardio-kidney-metabolic (CKM) diseases. Preclinical studies have shown therapeutic activity across kidney, cardiac, hepatic, and metabolic endpoints. It is currently being evaluated in early-phase clinical trials, including a single ascending dose (SAD) study in healthy volunteers, with a primary focus on diabetic nephropathy.
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