Tìm theo
XMT-1001
Thuốc Gốc
Small Molecule
XMT-1001 is a polymer-based prodrug of camptothecin (CPT), a well-characterized topoisomerase I inhibitor with potent anti-tumor activity. It is a water-soluble macromolecular conjugate of camptothecin (CPT). In this novel CPT pro-drug, CPT is conjugated with a 70 kDa biodegradable hydrophilic polyacetal, poly (1-hydroxymethylene hydroxylmethylformal). XMT-1001 has demonstrated an improved therapeutic window as compared with CPT and irinotecan in human tumor xenografts models
Dược Lực Học : In preclinical studies, XMT-1001 was better tolerated and more efficacious than either camptothecin or irinotecan in models of human cancer, showing extended plasma half-life and high concentrations in tumor tissue. The Phase I results show that, in humans, camptothecin, the active agent in XMT-1001, is released gradually from the Fleximer carrier as a pro-drug in a manner that will potentially avoid common safety problems associated with drugs in this class.
Cơ Chế Tác Dụng : XMT-1001 is a polymer-based prodrug of camptothecin (CPT), a well-characterized topoisomerase I inhibitor with potent anti-tumor activity. It is a water-soluble macromolecular conjugate of camptothecin (CPT). In this novel CPT pro-drug, CPT is conjugated with a 70 kDa biodegradable hydrophilic polyacetal, poly (1-hydroxymethylene hydroxylmethylformal). XMT-1001 has demonstrated an improved therapeutic window as compared with CPT and irinotecan in human tumor xenografts models XMT-1001 is Mersana’s most advanced Fleximer®-based product candidate. It utilizes a novel, dual release mechanism to liberate a camptothecin prodrug, which is then converted within cells into camptothecin, a DNA topoisomerase I inhibitor. It is a potent inhibitor of LS174 and A2780 human tumor xenografts in a mouse model.
Chỉ Định : Investigated for use/treatment in solid tumors.
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB06069
... loading
... loading