Zhengzhou University sells a cardiovascular candidate to Ausun for RMB 45 million

A few days earlier, Zhengzhou University out-licensed a cardiovascular candidate called BZP (布罗佐喷钠) to Ausun Pharmaceutical (奥翔药业). The drug was discovered by Junbiao Chang (常俊标) who is the vice principal of Zhengzhou University.

BZP is a patented compound derived from butylphthalide (NBP)[1] which was originally isolated from celery (芹菜). In 2002, CSPC Pharmaceutical launched butylphthalide in China for the treatment of mild to moderate acute ischemic stroke.

Junbiao Chang has filed two patent applications (CN100554259, CN101402565) related to butylphthalide derivatives. The best compound claimed in the two patents is 5-bromo-2-(1-hydroxypentyl)benzoate, a bromine substituted compound of 2-(1-hydroxypentyl) benzoate (PHPB).

PHPB, the ring-opening derivative of NBP, has been patented by Chinese Academy of Medical Sciences (WO03095412)[2]. Recently, Biovalley Pharmaceutical (生物谷药业) initiated a placebo-controlled Phase IIa trial (CTR20132923) to evaluate the safety and efficacy of PHPB in patients with acute ischemic stroke.

It is surprising that the patent WO03095412 doesn’t cover the halogenated derivatives of PHPB. Anyway, in my opinion, it is not a good idea to develop such a belated me-too drug with a highly similar structure to the lead compound.

Moreover, Zhengzhou University out-licensed the nucleoside analog reverse-transcriptase inhibitor azvudine (FNC)[3], another me-too candidate identified by Junbiao Chang, to 北京兴宇中科 for RMB 40 million in 2011. Last year, the CFDA approved the IND application of azvudine within 3 months. It is uncommon for the CFDA to review an IND  so fast. 河南真实生物科技 is currently testing the drug in HIV patients in the Phase I trial (CTR20140526).

[1] 乔地, 苏雨. 郑州大学研发一类新药卖了四千五百万元. 科技日报. 2014-11-30.

[2] J Pharmacol Exp Ther. 2006, 317(3), 973-979.

[3] PLoS One. 2014, 9(8), e105617.

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