alicapistat

Description: Alicapistat (also known as ABT-957) is a novel, potent, selective and orally bioactive inhibitor of human calpains 1 and 2 whose overactivation has been linked to Alzheimer disease (AD). It has the potential usefulness in the treatment of Alzheimer's disease (AD). In clinical trials, Alicapistat at 400- or 800-mg twice-daily doses had no effect on REM sleep parameters, whereas the active control, donepezil at 10 mg twice daily, affected sleep parameters. Across all trials, the incidence of treatment-emergent adverse events was similar in the placebo and alicapistat groups. There were no clinically significant changes in vital signs and laboratory measurements. The lack of an effect of alicapistat on sleep suggests that concentrations in the CNS were inadequate or that preclinical studies do not predict alicapistat effects in humans.

References: Clin Pharmacol Drug Dev. 2018 Jul 27.