Issue 7, 2021

The development of HEC-866 and its analogues for the treatment of idiopathic pulmonary fibrosis

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(3H)-one analogs which exhibit potent activity in in vitro 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.

Graphical abstract: The development of HEC-866 and its analogues for the treatment of idiopathic pulmonary fibrosis

Supplementary files

Article information

Article type
Research Article
Submitted
25 Jan 2021
Accepted
14 Apr 2021
First published
02 Jun 2021

RSC Med. Chem., 2021,12, 1222-1231

The development of HEC-866 and its analogues for the treatment of idiopathic pulmonary fibrosis

R. Lin, Z. Zhang, S. Cao, W. Yang, Y. Zuo, X. Yang, J. Zhang, J. Xu, J. Li and X. Wang, RSC Med. Chem., 2021, 12, 1222 DOI: 10.1039/D1MD00023C

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