CVT-10216

CVT-10216 is a **potent and selective, reversible inhibitor of aldehyde dehydrogenase 2 (ALDH2)**, developed as a small molecule therapeutic for alcohol use disorder and related neurobehavioral conditions. Its selectivity for ALDH2 over the cytosolic isoform, ALDH1, is more than 40-fold (IC50 = 29 nM for ALDH2, 1300 nM for ALDH1). CVT-10216 was designed as a synthetic derivative based on structural insights from daidzin, the isoflavone found in kudzu vine, known for its anti-drinking properties, to achieve more efficient and selective interaction with ALDH2[1][6][3][7][9]. **Mechanism of action:** By competitively and reversibly inhibiting ALDH2, CVT-10216 blocks the mitochondrial oxidation of acetaldehyde to acetate, resulting in elevated acetaldehyde levels following ethanol intake—a mechanism exploited for alcoholism therapy. It also disrupts alcohol-induced dopamine release in the nucleus accumbens (NAc), which is thought to reduce reinforcement, craving, and relapse to drinking[1][6][4]. **Pharmacology:** CVT-10216 suppresses voluntary alcohol intake, self-administration, and cue-induced relapse in animal models, showing anxiolytic effects in some studies; it does not cause aversive or rewarding effects on its own[2][5][9]. **Development:** CVT-10216 was initially developed by researchers including David Diamond’s group, building on work at Harvard that characterized daidzin and inspired synthetic ALDH2 inhibitors[6]. **No clinical trials or approval are reported as of 2025; use is limited to preclinical research.**

Brand names

CVT-10216CVT10216CVT 10216

Other names

CVT-10216CVT10216CVT 10216