The Development of HEC-866 and Its Analogues for the Treatment of Idiopathic Pulmonary Fibrosis

Overview

Journal RSC Med Chem

Publisher Royal Society of Chemistry

Specialty Chemistry

Date 2021 Aug 6

PMID 34355186

Citations 2

Authors

Runfeng Lin

Zheng Zhang

Shengtian Cao

Wen Yang

Yinglin Zuo

Xinye Yang

Jiancun Zhang

Juan Xu

Jing Li

Xiaojun Wang

Affiliations

Soon will be listed here.

Abstract

Idiopathic pulmonary fibrosis (IPF) is a chronic progressive lung disease with a typical survival time between three to five years. Two drugs, pirfenidone and nintedanib have been approved for the treatment of IPF, but they have limited efficacy. Thus, the development of new drugs to treat IPF is an urgent medical need. In this paper we report the discovery of a series of orally active pyrimidin-4(3)-one analogs which exhibit potent activity in assays. Among them, HEC-866 showed promising efficacy in rat IPF models. Since HEC-866 also had good oral bioavailability, a long half-life and favorable long-term safety profiles, it was selected for further clinical evaluation.

Citing Articles

Highlights on Future Treatments of IPF: Clues and Pitfalls.

Libra A, Sciacca E, Muscato G, Sambataro G, Spicuzza L, Vancheri C Int J Mol Sci. 2024; 25(15).

PMID: 39125962 PMC: 11313529. DOI: 10.3390/ijms25158392.

Synthesis and structure-activity relationships of pirfenidone derivatives as anti-fibrosis agents .

Shi X, Yu Z, Zhu C, Jiang L, Geng N, Fan X RSC Med Chem. 2022; 13(5):610-621.

PMID: 35694690 PMC: 9132227. DOI: 10.1039/d1md00403d.

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