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NAMI-A and KP1019 are two ruthenium anticancer agents that have entered clinical trials.〔Kostova, I., Ruthenium complexes as anticancer agents. Current medicinal chemistry 2006, 13 (9), 1085-1107. 〕 NAMI is an acronym for "New Anti-tumour Metastasis Inhibitor", while the -A suffix indicates that this is the first of a potential series. NAMI-A and KP1019 are based primarily around the use of the metal ruthenium. Ruthenium is unknown to living systems, with a strong complex forming ability with numerous ligands.〔Gopal, Y.; Jayaraju, D.; Kondapi, A., Inhibition of Topoisomerase II Catalytic Activity by Two Ruthenium Compounds: A Ligand-Dependent Mode of Action†. Biochemistry 1999, 38 (14), 4382-4388. 〕 Its partially filled 4d sub-shell allows it to form complexes that are useful for a wide variety of applications including catalysis, electronics, photochemistry, biosensors and anticancer drugs.〔〔Antonarakis, E.; Emadi, A., Ruthenium-based chemotherapeutics: are they ready for prime time? Cancer chemotherapy and pharmacology 2010, 66 (1), 1-9. 3. 〕 Ruthenium, unlike traditional platinum complexes such as cisplatin, shows greater resistance to hydrolysis and more selective action on tumors. == Background == New Anti-tumor Metastasis Inhibitor or NAMI-A is a ruthenium based anti-cancer drug and is one of two ruthenium-based drugs that have entered clinical trials. NAMI-A is considered a pro-drug formulation that becomes active upon hydrolysis. At pH 7.4, a chloride is exchanged with a water molecule, which neutralizes the molecule’s -1 charge. Upon lower pH, imidazole in cleaved and replaced with water. Unlike cisplatin, a platinum based drug, it has been shown in-vivo that NAMI-A doesn’t inhibit primary tumor growth but decreases the speed at which metastasis occurs. 2 It has also been found that when compared to highly cytotoxic platinum compounds, NAMI-A is much less cytotoxic and has a differing mechanism of action. 抄文引用元・出典: フリー百科事典『 ウィキペディア(Wikipedia)』 ■ウィキペディアで「NAMI-A」の詳細全文を読む スポンサード リンク
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