rislenemdaz

Rislenemdaz (CERC-301) is an orally active, selective antagonist of the N-methyl-D-aspartate (NMDA) receptor subunit 2B (GluN2B). It was originally developed by Merck & Co and later by Cerecor (now Avalo Therapeutics). The drug is a small molecule designed to act as an adjunctive therapy for treatment-resistant depression (TRD) and major depressive disorder (MDD), with additional investigation in neurogenic orthostatic hypotension. Rislenemdaz binds specifically to the GluN2B subunit of the NMDA receptor, preventing endogenous glutamate from activating this site. This selectivity aims to mitigate depressive symptoms rapidly while minimizing off-target effects. Clinical trials have shown rapid onset of action but failed to demonstrate significant efficacy in MDD primary endpoints; however, it showed promising results in improving blood pressure in patients with neurogenic orthostatic hypotension[1][3][5][8].

Other names

rislenemdaz