Anti-HIV drug development on the fast track

An international cooperation deal was made recently in Shanghai on developing a new anti-HIV drug based on the research results of CAS scientists and their preclinical studies, marking a breakthrough progress for China's research in the field.

According to the agreement inked on 15 April between TargetDrug, a Shanghai-based drug firm backed by CAS, and Avexa, a Melbourne-based pharmaceutical company, the two sides will join forces in the follow-up development of Nifeviroc, a promising drug candidate for the treatment of AIDS, and its global distribution.

The anti-HIV drugs now commonly used in clinical practice are to act on the life cycle of the HIV virus after their invasion of the healthy cells, with an objective of reducing complications of the patients and elongating their lives. However, they have defects, such as low bioavailability, high toxicity, unbearable side effects, high costs and rapid development of viral resistance. Recently, scientists are thinking to develop new drugs against the initial entry of the virus into human cells.

Set to be China's first entry-inhibitor for HIV-virus, Nifeviroc works by restraining CCR5, a protein that commonly exists on the surface of human immune cells. The protein plays a critical role in mediating the HIV virus entry and facilitating viral fusion with the cells, which is the initiation of life cycle of HIV. As a mall molecular compound, the anti-HIV capacity of Nifeviroc was jointly approved in 2003 by PEI Gang from the Institute of Biochemistry and Cell Biology under the CAS Shanghai Institutes for Biological Sciences (SIBS) and MA Dawei from the Shanghai Institute of Organic Chemistry (SIOC). The researchers attribute the feat to the interdisciplinary studies of biology and chemistry, which enable them to ferret out several bio-molecules as promising candidates for anti-HIV drugs.

Preclinical study results indicate that Nifeviroc is of both potent efficacy and impressive safety profiles, according to researchers. It also shows, in pharmacodynamic studies, strong anti-viral activity against various HIV strains, especially when tested against those that are multi-drug resistant. Further pharmacokinetic studies confirm its oral bioavailability, and safety studies find that it causes no serious treatment-related toxicity either in an acute study or in a chronic state.

In order to speed up the follow-up development, Targetdrug was established as a spin-off of SIBS and SIOC. The firm has completed pre-clinic research work on Nifeviroc and received endorsement from the National Food and Drug Administration for clinical research to begin early this year. So far, Targetdrug has applied for patents for Nifeviroc in 14 countries and regions, including the United States, Japan and the European Union.

"In the field of basic research," Prof. Ma comments, "there is a group of competent Chinese scientists who have made research fruits up to the advanced international level. But, what we are lacking hereby is a success in commercialization of their results as we need to have an institutional mechanism sound enough and compatible with the conventional practice exercised by the international community in this regard."

"Through cooperation with Avexa, we hope to bring our brainchild into the world market in an efficient way," notes Prof. Pei, who is also SIBS president.

Following the agreement with Avexa, Targetdrug will possess the rights for developing Nifeviroc in China. Avexa will take charge of post-research expenses, develop it in the international marketplace and share global benefits with Targetdrug.

"The provisions in the protocol were formulated in line with the international conventions in the course when a new drug is being developed. Our objective is to speed up the developing tempo of the candidate by taking advantage of a professional and overseas R&D platform with a higher starting point;" notes CEO of TargetDrug CHEN Li, "On the other hand, this is an attempt to blaze a new trail, unclogging a channel accessible to the international market."

Source from CAS