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

: HAO472, the L-alanine-(14-oridonin) ester trifluoroacetate, was conducted first stage human clinical trial (CTR20150246) by a Chinese company, Hengrui Medicine Co. Ltd, to develop 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 natural derived drug candidates. Herein, we sought to overview recent progress of the synthetic, physiological and pharmacological investigations of oridonin and its prodrug HAO472, aiming to disclose the therapeutic potentials and broaden the platform for new anticancer drugs discovery.