Abstract

ADVANCING THE MEDICINAL CHEMISTRY OF ZAVEGEPANT: KEY SAR STUDIES AND OPTIMIZATION

Libis Linga Siva Subbu Raj P.* and Aiswaria M. S.

ABSTRACT

Zavzpret is the drug name which has an active ingredient zavegepant. Zavegepant, also known as BHV-3500. It is indicated for the acute treatment of migraine with or without aura in adults. Zavegepant is a small molecule of the calcitonin gene-related peptide (CGRP) receptor antagonist that is being developed as a potential treatment for migraine headaches. The initial hit compound was identified from a high-throughput screening campaign and underwent multiple rounds of optimization to improve potency, selectivity, and pharmacokinetic properties. The SAR studies revealed that the presence of a heterocyclic ring system and a carboxylic acid moiety were critical for activity. This review summarizes the medicinal chemistry efforts that lead to the discovery and optimization of zavegepant, highlighting key structure-activity relationships (SAR) and the optimization of physicochemical properties to improve drug-like properties.

Keywords: activity. This review summarizes the medicinal chemistry efforts that lead to the discovery and optimization of zavegepant, highlighting key structure-activity relationships (SAR) and the optimization of physicochemical properties to improve drug-like pr