Tìm theo
AP5346
Thuốc Gốc
Small Molecule
AP5346 is designed to target a diaminocyclohexane platinum (Pt) moiety to tumors through pH-sensitive linkage to a 25 kDa hydroxypropylmethacrylamide polymer. It is being pursued by Access Pharmaceuticals, Inc.
Dược Lực Học : Preclinical studies of the delivery of platinum to tumors in an animal model has shown that, compared with oxaliplatin at equitoxic doses, AP5346 delivers in excess of 16 times more platinum to the tumor. An analysis of tumor DNA, which is the main target for anti-cancer platinum agents, has shown that in excess of 13 times more platinum tumor DNA complexes were formed from AP5346 than oxaliplatin in these studies. Results from preclinical efficacy studies conducted in the B16 and other tumor models have also shown that AP5346 is superior to oxaliplatin in inhibiting the growth of tumors.
Cơ Chế Tác Dụng : AP5346 is designed to target a diaminocyclohexane platinum (Pt) moiety to tumors through pH-sensitive linkage to a 25 kDa hydroxypropylmethacrylamide polymer. It is being pursued by Access Pharmaceuticals, Inc. Utilizing the biocompatible water-soluble polymer HPMA as a drug carrier, AP5346 links DACH platinum to the polymer in a manner which permits the selective release of platinum in tumors. The polymer capitalizes on the biological differences in the permeability of blood vessels at tumor sites versus normal tissue. In this way, tumor selective delivery and platinum release is achieved. Once delivered to the tumor, platinum binds preferentially to the guanine and cytosine moieties of DNA, leading to cross-linking of DNA, thus inhibiting DNA synthesis and function.
Chỉ Định : For the treatment of various forms of cancer.
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : ProLindac
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB04992
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