TP0473292

TP0473292 is an orally bioavailable prodrug developed to enhance the delivery of its active metabolite, TP0178894, a novel antagonist of metabotropic glutamate 2 and 3 (mGlu2/3) receptors. It is being developed primarily for the treatment of depression, including treatment-resistant depression. Upon oral administration, TP0473292 is rapidly and extensively converted into TP0178894 by carboxylesterase enzymes (primarily CES1 and more efficiently CES2), resulting in high central nervous system penetration. The mechanism involves antagonism at mGlu2/3 receptors, which are implicated in the modulation of glutamatergic neurotransmission relevant to depressive disorders. Preclinical and phase 1 studies have shown that it is safe and well-tolerated with common adverse events including nausea, vomiting, and dizziness[1][5][6]. Clinical development has reached phase 2 for major depressive disorder and treatment-resistant depression[3][7].

Brand names

TS-161TS161TS 161

Other names

TP0473292TP-0473292TP 0473292