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Please use this identifier to cite or link to this item:
http://ir.nhri.org.tw/handle/3990099045/12219
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| Title: | BPRDP056, a novel small molecule drug conjugate specifically targeting phosphatidylserine for cancer therapy |
| Authors: | Hsu, CY;Chen, YY;Lo, CF;Chiu, TY;Chen, CP;Huang, CL;Huang, CY;Wang, MH;Chao, YS;Shih, JC;Yeh, TK;Tsou, LK;Chen, CT |
| Contributors: | Institute of Biotechnology and Pharmaceutical Research |
| Abstract: | Zinc(II)-dipicolylamine (Zn-DPA) have been described to specifically complex with phosphatidylserine (PS), which has a higher level at the external surface of cancer cells in tumorigenic condition. BPRDP056 is a Zn-DPA-SN38 conjugate designed to provide a PS-targeting drug delivery of cytotoxic payload SN-38 at the tumor microenvironment, thereby, decrease the dosage of SN38, while induce apoptosis in cancer cells. The in vivo therapeutic efficacy of BPRDP056 against the growths of human tumors has been shown significant in mice subcutaneously bearing a tumor type of pancreas, prostate, colon, liver, breast and glioblastoma, as well as in mice with an orthotopic pancreatic tumor. BPRDP056 shrunk tumors at a lower dosing intensity (~20%) of SN38 compared to CPT-11 in all models tested. Micro-Western assays showed that BPRDP056 exhibited apoptotic cell death signal levels similar to those of CPT-11 in the treated tumors in mice. Furthermore, pharmacokinetic and preliminary toxicology studies showed that BPRDP056 has a good stability in circulation with an acceptable therapeutic safety window in mice. BPRDP056 has been demonstrated with a tumor targeting ability and thus increases the cytotoxic payload SN38 concentration in situ for improved efficacy. Its therapeutic spectrum against malignant neoplasm will be expected to cover the PS-rich tumor microenvironment of all cancer types. BPRDP056 is a first-in-class Small Molecule Drug Conjugate for anti-cancer therapy. |
| Date: | 2019-07 |
| Relation: | Cancer Research. 2019 Jul;79(13, Suppl.):Abstract number 227. |
| Link to: | http://dx.doi.org/10.1158/1538-7445.Am2019-227 |
| JIF/Ranking 2023: | http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0008-5472&DestApp=IC2JCR |
| Cited Times(WOS): | https://www.webofscience.com/wos/woscc/full-record/WOS:000488129901405 |
| Appears in Collections: | [陳炯東] 會議論文/會議摘要
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