Congratulations to the team that leads the project: “Pre-clinical investigation of the anti-cancer multi-kinase inhibitor:DBPR114”from IBPR for receiving the 26th Wang Ming-Ning Award by the Wang Ming-Ning memorial foundation.

Leading by Dr. Hsing-Pang Hsieh, the DBPR114 team has achieved the milestone on  “Pre-clinical investigation of the anti-cancer multi-kinase inhibitor:DBPR114”. Comprehensive studies on structural-activity and property relationships were performed by using three lead optimization strategies: scaffold hopping, side-chain modification and solubilizing group implementation. With more than 1,300 compounds synthesized, over 100 compounds conducted for pharmacokinetic (PK) study and acute toxicity test, 30 potent compounds were further examined for pharmacological evaluations. These work led the team to identify DBPR114 that exhibited potent inhibition activities both in vitro and in vivo. DBPR114, a multiple kinase inhibitor as an anticancer agent, provided excellent in vitro inhibitory activities against multiple oncogenic enzymes and various cancer cell lines.

With funding supports from the National Research Program for Biopharmaceuticals (NRPB), and National Health Research Institutes (NHRI), the development program of DBPR114 is aiming to accomplish a comprehensive program of pre-clinical development and file IND in Taiwan and in the USA . IBPR integrates various disciplines for DBPR114 discovery and development, such as, cancer biology, medicinal chemistry, pharmacology, pharmacokinetics/metabolism, formulation development, toxicological studies, clinical trial planning, and project management. Kilogram scale-up of compound synthesis and toxicity studies were accomplished in 2016. Global patents of DBPR114 have been filed and the territories of ROC, USA, Europe and China have already been granted. The investigational new drug (IND) applications for TFDA and FDA will be submitted in the first half of 2017.The clinical trial of DBPR114 will particularly focus on the cancers classified as high prevalence, high mortality rate and lower 5-years survival rate in Taiwan, such as pancreatic, liver, stomach, and colorectal cancers.

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