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

Xu Hu, Yan Wang, Xiang Gao, Shengtao Xu, Linghe Zang, Yan Xiao, Zhanlin Li, Huiming Hua, Jinyi Xu, Dahong Li

Journal: Mini reviews in medicinal chemistry 2020;20(6):483-497

PMID: 31660811

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.

Address: 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.; Valiant Co. Ltd., 11 Wuzhishan Road, YEDA Yantai, Shandong 264006, China.; Department of Medicinal Chemistry and State Key Laboratory of Natural Medicines, China Pharmaceutical University, 24 Tongjia Xiang, Nanjing 210009, China.; School of Life Science and Biopharmaceutics, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang 110016, China.

DOI: 10.2174/1389557519666191029121809

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MeSH Terms: Antineoplastic Agents, Phytogenic, Diterpenes, Kaurane, Humans, Leukemia, Myeloid, Acute, Molecular Structure