Drug intelligence / Profile preview

AF-130

Development stage
Phase 1
Lead developer
Merck
Modality
Small Molecules
Administration
Oral
01

Overview

AF-130 is an orally available, first-in-class, small molecule drug that acts as a selective antagonist of the purinergic P2X3 receptor. It was initially developed by Afferent Pharmaceuticals and later acquired by Merck. The drug has shown promise in preclinical studies for improving heart function and preventing sleep apnea in animal models of heart failure. Its mechanism involves reducing sympathetic nerve activity, decreasing inflammation (notably lowering interleukin-1β), and preventing increases in natural killer cells associated with heart failure progression. By targeting the P2X3 receptor, AF-130 aims to address mechanisms that worsen heart failure and are not targeted by current therapies. It has also been considered for other indications such as treatment-resistant hypertension, migraine, and visceral pain[1][3][4][5][8].

02

Targets

P2X3 (P2X purinoceptor 3)

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