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A research paper on Renfu Pharmaceutical’s P2X3 antagonist has been published in an internationally renowned journal of medicinal chemistry.
Release time:
2025-09-22 08:56
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On September 14, the innovative drug R&D team at Renfu Pharmaceutical Research Institute published a research paper titled “Development of a P2X3 receptor antagonist derived from eliapixant with improved properties for the treatment of chronic cough” in the internationally renowned journal of medicinal chemistry, the European Journal of Medicinal Chemistry. The paper provides a detailed account of the discovery process of HW091077, a novel, highly effective oral purinergic receptor P2X3 antagonist, and highlights its significant potential in the treatment of refractory chronic cough.
Based on protein models, the innovative drug R&D team at Renfu Pharmaceutical Research Institute analyzed ligand-protein binding sites and key interactions, and designed a series of structurally novel P2X3 receptor antagonists. Through systematic structure-activity relationship (SAR) studies and multiple rounds of structural optimization, they successfully identified the clinical candidate compound HW091077. Preclinical study data indicate that HW091077 exhibits excellent in vitro and in vivo activity, favorable preclinical pharmacokinetic properties, and a high safety profile.
Phase I clinical data indicate that HW091077 exhibits good safety and tolerability, with no serious side effects such as severe loss of taste reported. Moreover, HW091077 is well absorbed in the human body and holds promise for once-daily administration, potentially becoming a “best-in-class” P2X3 receptor antagonist drug globally. A Phase II clinical trial targeting patients with refractory chronic cough is set to begin shortly.
The “European Journal of Medicinal Chemistry” is a journal published by Elsevier and is one of the most influential journals in the field of medicinal chemistry. It is currently listed as a Tier 1, Top Journal by the Chinese Academy of Sciences.
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