生物活性：Miriplatin hydrate was approved for lipiodolization for the treatment of hepatocellular carcinoma in 2009; it is a lipophilic platinum complex containing myristates as leaving groups, and can be easily suspended in ethyl esters of iodized fatty acids obtained from poppy seed oil.
IC50 Value: 22.3 microg/ml (7-day exposure, in rat ascites hepatoma AH-109A cells) [2]
Target:
in vitro: In monolayer or suspension cell cultures, SM-11355 did not inhibit the cell growth, whereas SM-11355/Lipiodol had dose-dependent growth inhibitory activities, as did CDDP suspended in Lipiodol (CDDP/Lipiodol) [1]. SM-11355 suspended in Lipiodol (SM-11355/Lipiodol) and CDDP suspended in Lipiodol (CDDP/Lipiodol) showed cytotoxic activity against rat ascites hepatoma AH-109A cells in a dose-dependent manner. Their IC50 values following 7-day exposure were 22.3 and 0.40 microg/ml, respectively. Following the subsequent 7-day exposure, from day 7 to day 14 after preparation of the suspension, SM-11355/Lipiodol showed an almost equivalent activity, but CDDP/Lipiodol did not show any activity at all [2].
in vivo: Tumor growth was suppressed in the group that received SM-11355 suspended in Lipiodol (SM-11355/Lipiodol). Mean tumor growth rates in the groups administered 20 microl of Lipiodol containing 0, 0.02, 0.04, 0.1, 0.2, or 0.4 mg of SM-11355 were 244, 86, 110, 81, 51, and 40%, respectively, 1 week after treatment [3].
Clinical trial: Launched drug.
相关文献：
[1]. Kishimoto S, Noguchi T, Yamaoka T, In vitro cytotoxicity of cis[((1R,2R)-1,2-cyclohexanediamine-N,N')bis(myristato)] platinum(II) suspended in lipiodol in rat hepatoma AH-109A cells and human tumor cell lines. Biol Pharm Bull. 2000 Apr;23(4):487-91.
[2]. Kishimoto S, Miyazawa K, Fukushima S, In vitro antitumor activity, intracellular accumulation, and DNA adduct formation of cis-[((1R,2R)-1,2-cyclohexanediamine-N,N')bis(myristato)] platinum (II) suspended in lipiodol. Jpn J Cancer Res. 2000 Jan;91(1):99-104.
[3]. Kishimoto S, Noguchi T, Yamaoka T, Antitumor effects of a novel lipophilic platinum complex (SM-11355) against a slowly-growing rat hepatic tumor after intra-hepatic arterial administration. Biol Pharm Bull. 2000 Mar;23(3):344-8.
