Recent Progress of Oridonin and Its Derivatives for the Treatment of Acute Myelogenous Leukemia

Author:

Hu Xu1ORCID,Wang Yan2ORCID,Gao Xiang1ORCID,Xu Shengtao3ORCID,Zang Linghe4ORCID,Xiao Yan1ORCID,Li Zhanlin1ORCID,Hua Huiming1ORCID,Xu Jinyi3ORCID,Li Dahong1

Affiliation:

1. Key Laboratory of Structure-Based Drug Design &Discovery, Ministry of Education, and School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang 110016, China

2. Valiant Co. Ltd., 11 Wuzhishan Road, YEDA Yantai, Shandong 264006, China

3. Department of Medicinal Chemistry and State Key Laboratory of Natural Medicines, China Pharmaceutical University, 24 Tongjia Xiang, Nanjing 210009, China

4. School of Life Science and Biopharmaceutics, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang 110016, China

Abstract

First stage human clinical trial (CTR20150246) for HAO472, the L-alanine-(14-oridonin) ester trifluoroacetate, was conducted by a Chinese company, Hengrui Medicine Co. Ltd, to develop a new treatment for acute myelogenous leukemia. Two patents, WO2015180549A1 and CN201410047904.X, covered the development of the I-type crystal, stability experiment, conversion rate research, bioavailability experiment, safety assessment, and solubility study. HAO472 hewed out new avenues to explore the therapeutic properties of oridonin derivatives and develop promising treatment of cancer originated from naturally derived drug candidates. Herein, we sought to overview recent progress of the synthetic, physiological, and pharmacological investigations of oridonin and its derivatives, aiming to disclose the therapeutic potentials and broaden the platform for the discovery of new anticancer drugs.

Funder

National Natural Science Foundation of China

Natural Science Foundation of Liaoning Province

Department of Education of Liaoning Province

Publisher

Bentham Science Publishers Ltd.

Subject

Drug Discovery,Pharmacology,General Medicine

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