Inventor Zhang Jie (Sichuan Jiuzhang) releasing clinical data on chlorogenic acid for injection at the conference

The China BioMed Innovation and Investment Conference was held at the Suzhou Jinjihu International Conference Center on 14 November 2016, on which Sichuan Jiuzhang released the phased data of chlorogenic acid for injection clinical study.

119 years ago, British scientists Osbome and Cambell discovered an active substance that can blacken sunflower seeds protein. 12 years later, Corter et al. named this active substance as chlorogenic acid (presented as oil-green under certain conditions). 38 years later, i.e. in 1947, half a century after the discovery of chlorogenic acid, Rudkin and Nelson identified the molecular structure of chlorogenic acid (molecular weight: 354.31). 103 years after the discovery of this substance, Sichuan Jiuzhang firstly took the chlorogenic acid monomer as a therapeutic drug for systematical development and had completed all preclinical studies. In 2013, Sichuan Jiuzhang had obtained clinical study approval from CFDA (CHINA FOOD AND DRUG ADMINISTRATION).

 After 2000, Sichuan Jiuzhang realized the kilogram-scale production of chlorogenic acid monomer with the purity over 99% and qualitatively and quantitatively measured the 0.1% impurities in the monomer. As a chlorogenic acid drug substance, it is characterized by low toxicity, low irritation and non-allergenicity.

 With regards to drug research, Sichuan Jiuzhang respects for nature, follows objective laws, explores to understand characteristics of chlorogenic acid and its biological activity. Moreover, Sichuan Jiuzhang has established a close and long-term strategic partnership with the Institute of Materia Medica, Chinese Academy of Medical Sciences, forming a high-end platform for chlorogenic acid research and development. At present, the in-depth and extensive study on the mechanism of action, pharmacodynamics and combination with other anti-tumor drugs of chlorogenic acid has been well underway. Additional data show that chlorogenic acid has an excellent efficacy in treating autoimmune diseases (e.g. erythrodermic psoriasis and systemic lupus erythematosus) and the drug development in the field of such diseases is going well.

According to antitumor mechanism studies, chlorogenic acid is a multichannel and multitargeted natural active substance (monomer), which exerts antitumor effects at both immune and cellular levels. At the immune level, chlorogenic acid features in multi-channel and multi-target and can recognize and regulate multiple immune checkpoints (e.g. LAG-3). In addition, chlorogenic acid can also regulate the tumor-related macrophages, inhibit the proliferation of M2, and promote the transformation of M2 to M1. At the cellular level, chlorogenic acid can induce the differentiation of tumor cells and promote the transformation of tumor cells to a low degree of malignancy.

Prof. Chen Xiaoguang, the Chlorogenic Acid Antitumor Mechanism Investigator, and the Professor of the Institute of Materia Medica, Chinese Academy of Medical Sciences (Left 1)

Sichuan Jiuzhang conducted Phase I clinical trials at Beijing Cancer Hospital, Beijing Shijitan Hospital, and Cancer Hospital Chinese Academy of Medical Science, focusing on dominant tumor spectrum, glioma and administration routes, and the pharmacodynamics against lung cancer. According to present results of the clinical trial, chlorogenic acid had a dominant anti-tumor spectrum in malignant neoplasms like lung cancer, glioma and liver cancer. It showed good safety and tolerability among subjects in the clinical trial and had no obvious clinical side effects. Results of pharmacokinetic studies showed that the drug was rapidly eliminated in vivo with a half-life (t1/2) of 1.15 h, and no accumulation was observed.

Clinical trial data of glioma published at the conference by Prof. Li Wenbin, the principal investigator of the glioma clinical trial (director of the Department of Glioma of Beijing Shijitan Hospital)

For years, Sichuan Jiuzhang had applied for 84 domestic and international invention patents and 1 utility model patent related to key therapeutical areas, relative Derivatives, core process and new dosage form of chlorogenic acid, among which 20 patents had been granted. In the future, we will explore and identify the dominant tumor spectrum based on the broad spectrum of chlorogenic acid anti-tumor so as to carry out international and domestic clinical research on different tumor types and promote the initiation of clinical studies of immune-related disease treatment as soon as possible.