Miriplatin hydrate

Description: IC50 Value: 22.3 microg/ml (7-day exposure, in rat ascites hepatoma AH-109A cells) [2] Miriplatin 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. 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.

Comparison of epirubicin hydrochloride and miriplatin hydrate as anticancer agents for transcatheter arterial chemoembolization of hepatocellular carcinoma.[Pubmed:23046493]

Hepatol Res. 2013 May;43(5):475-80.

AIM: The aim of this retrospective study was to compare the local control effects of transcatheter arterial chemoembolization (TACE) using epirubicin (EPIR) and that using miriplatin (MPT) for hepatocellular carcinoma (HCC). METHODS: Between January 2010 and July 2011, 218 HCC cases were treated with TACE, including 69 cases using EPIR or MPT as initial treatment. All 69 patients were treated with iodized oil and gelatin sponge particles. The local control rate (modified Response Evaluation Criteria in Solid Tumors [RECIST] ver. 1.0), time to treatment failure (Kaplan-Meier and log-rank test) and adverse events were evaluated. RESULTS: Forty-two cases were treated using EPIR, and 27 cases were treated using MPT. All 69 patients had no previous treatment with TACE or hepatic arterial infusion. No serious adverse events were observed in either group. The response rates, including complete response (CR) and partial response (PR), of the EPIR group and the MPT group were 85.7% and 81.5%, respectively, with a time to treatment failure of 5.1 and 7.5 months, respectively. Excluding whole liver TACE cases, time to treatment failure was 5.4 months for the EPIR group and 10.1 months for the MPT group. CONCLUSION: In TACE naive cases, there was no significant difference in local control between EPIR and MPT.

[Transcatheter arterial chemoembolization with a lipophilic platinum complex SM-11355(miriplatin hydrate)--safety and efficacy in combination with embolizing agents].[Pubmed:20154484]

Gan To Kagaku Ryoho. 2010 Feb;37(2):271-5.

SM-11355 is a cisplatin derivative with high affinity for iodized ethyl esters of fatty acids of poppyseed oil. Clinical trials have shown that SM-11355 is effective for treatment of hepatocellular carcinoma. Transcatheter arterial chemoembolization is commonly used in combination with embolizing agents, but concomitant use of SM-11355 and embolizing agents has not been evaluated in previous trials. In this study, the safety and efficacy of SM-11355 in combination with embolizing agents were investigated in 10 patients with hepatocellular carcinoma. An anti-tumor effect of TE4 was achieved in 4 of 9 patients and no serious adverse events were observed, indicating that this therapy can be used safely for hepatocellular carcinoma.