Cinnamic acid derivatives are good candidates to satisfy this unmet medical need

Executive Summary

BioNutrigen, Inc (“BioNutrigen”) was organized in 1999 by scientists from the Korean Research Institute of Bioscience and Biotechnology. BioNutrigen has been focused on developing non-toxic natural products and materials from vegetables and fruits for prevention or treatment of adult disease such as obesity, diabetes and CV diseases.

Cinnamic acid derivatives were extracted from natural sources (e.g., apple, tea, potato, coffee, grape, plum and etc) and used to prevent and treat blood lipid level-related diseases such as hyperlipidemia, arteriosclerosis, angina pectoris, stroke and fatty liver. Use of novel cinnamic acid derivatives to treat or prevent Metabolic Syndrome are protected by worldwide patents held by BioNutrigen.

It estimates that there are nearly 86 million Metabolic Syndrome patients in the six major markets. There are no medicines approved for treatment for Metabolic Syndrome and the lack of a safe and effective medicine for this indication creates an unmet medical need in major global markets around the world.

Fig.1 Cinnamic acid derivatives

Cinnamic acid derivatives are good candidates to satisfy this unmet medical need. Promising preclinical data generated over the past 8 years by BioNutrigen scientists makes cinnamic acid derivatives a “first-in-class” series of compounds targeted at the Metabolic Syndrome indication. BioNutrigen is seeking co-development partners or licensing partners to fund the clinical development an innovative and promising medicine, cinnamic acid derivatives.

Key Technology Highlights

Lowering blood cholesterol level

Cinnamic acid derivatives can improve lipid metabolism and liver function. These drugs also inhibit plaque formation in the endothelium of the main artery and diminish formation of fatty liver, as shown below compared to other commercial agents.

Group	TC (mg/dl)	TG (mg/dl)	HDL-C (mg/dl)	HDL/TC (%)	GOT (IU/l)	GPT (IU/l)	Fatty streak (%)	A
Control	1995+ 472	170 +30	50 + 11	2.5 + 0.4	161+ 71	96 + 46	80 + 8	3.2 + 0.3
Lovastatin	1446 + 263	153 + 95	58 + 23	4.9 + 2.6	43 + 12	81 + 44	15 + 3	3.4 + 0.5
4-hydroxycinnamic acid	1517 + 417	167 + 43	57 + 28	3.7 + 1.3	59 + 45	74 + 49	24 + 11	2.7 + 0.3
3,4-dihydroxycinnamic acid	1559 + 347	139 + 46	53 + 13	3.4 + 0.4	99 + 49	40 + 27	13 + 5	2.6 + 0.3
3,4-dihydroxyhydrocinnamic acid	1256 + 150	108 + 22	80 + 23	6.3 + 1.6	55 + 20	90 + 83	16 + 1	2.6 + 0.3

Inhibition of HMG-CoA reductase activity

HMG-CoA reductase activities observed with the 4-hydroxycinnamic acid, 3,4-dihydroxycinnamic acid and 3,4-dihydroxyhydrocinnamic acid groups are lower than that of the Control group by 31 to 70%.

Group	Inhibition of HMG-CoA reductase activity (%)
Control	0
4-hydroxycinnamic acid	31
3,4-dihydroxycinnamic acid	44

Early Stage

BioNutrigen is seeking co-development partners or licensing partners to fund the clinical development an innovative and promising medicine, cinnamic acid derivatives.

US6313171; EP1113790; CN1148176; CA2344053