Tìm theo
AZD3409
Thuốc điều trị ung thư
Thuốc Gốc
Small Molecule
AZD3409 is a farnesyl-transferase inhibitor (FAR) indicated for the treatment of solid tumors. Phase I trials were initiated January 2003, and were ongoing as of February 2004. As of February 2007 the development of AZD3409 had been discontinued.
Dược Lực Học : AZD3409 is a novel, oral, antitumor agent that acts as a prenyl transferase inhibitor. It has potentially broad antitumor activity both as monotherapy and in combination with other anticancer treatments. AZD3409 is a double pro-drug; its metabolism involves conversion to a thiol-ester intermediate, then, intracellularly, to a thiol-acid active species. Phase I trials were initiated January 2003, and were ongoing as of February 2004. Recent studies have shown that AZD3409 is a potent inhibitor of both prostate epithelial cell proliferation and cellular invasion, without an associated bone marrow cellular toxicity.
Cơ Chế Tác Dụng : AZD3409 is a farnesyl-transferase inhibitor (FAR) indicated for the treatment of solid tumors. Phase I trials were initiated January 2003, and were ongoing as of February 2004. As of February 2007 the development of AZD3409 had been discontinued. In preclinical studies, AZD3409 achieves up to 90% inhibition of FTase in tumors at well tolerated doses. In enzyme studies AZD3409 is also known to inhibit GGTase-1.
Dược Động Học :

▧ Metabolism :
AZD3409 is converted to a thiol-ester intermediate, then, intracellularly, to a thiol-acid active species.
▧ Half Life :
15–20 hours for the thiol-ester intermediate and 15–30 hours for the active thiol-acid metabolite.
Chỉ Định : For the treatment of solid tumors.
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB04893
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