The Takeda AMPA-R potentiator, TAK-653 , is a glutamate-dependent potentiator that exhibits minimal agonism. AMPA-R agonism is associated with seizure risk and bell-shaped dose-response effects. As reviewer Jake Schwarz notes, companies including Cortex Pharmaceuticals (now RespireRx) and Lilly have been trying to develop AMPA modulators for [...]

Pfizer has announced the FDA-approval of zavegepant ( ZAVZPRET TM , BHV-3500) for the treatment of acute migraine in adults based on positive Ph. II/III results. As the first and only calcitonin gene-related peptide (CGRP) receptor antagonist nasal spray [...]

LTGO-33 is a state-independent NaV1.8 inhibitor with over 600-fold selectivity for the NaV1.8 channel over other sodium channels. Chronic pain affects millions, and existing treatments offer limited efficacy, risk of abuse, and low tolerability. There is an urgent need for new drugs that target validated pain mechanisms such as NaV1.8, which has recently gained increased attention. This article explores the unique pharmacological properties of LTGO-33, setting it apart from earlier NaV1.8 inhibitors.

The Altos Therapeutics /Takeda D2/D3 receptor antagonist, TAK-906 , is a peripherally-restricted, non-BBB penetrant molecule, targeting the stomach and vomiting center in the area postrema to treat gastroparesis. Gastroparesis is a chronic condition characterized by delayed gastric emptying, resulting in nausea, vomiting, pain, and anorexia [...]

Compound 8 is a dual 5-HT2A and 5-HT2C receptor inverse agonist developed to address the limitations of pimavanserin.