Uses
Lobaplatin (D-19466) is a diastereometric mixture of platinum(II) complexe. Lobaplatin arrests cell cycle at G1 and G2/M phase. Lobaplatin induces apoptosis by increasing expressions of caspase and Bax, decreasing expression of Bcl-2. Lobaplatin can be used for research of cancer[1][2][3].
Biological Activity
Lobaplatin (D-19466) is a third-generation platinum anticancer agent in vitro and in vivo, consisting of ~50:50 mixture of the two trans-1,2-cyclobutanedimethanamine diastereomers in complex with L-lactic acid. Llobaplatin shows antitumor efficacy against various human cancer cancer xenografts and significantly prolongs the survival of mice bearing P388 leukemia (mean life span increase post single i.p. in mg/kg = 46%/4.64 & 77/14.7). Compared to first and second generation platinum compounds, lobaplatin appears to be more stable, less toxic, have a better therapeutic index and may overcome tumor resistance.
in vivo
Lobaplatin (5 and 10 mg/kg; i.p.; once a week, for 3 weeks) suppresses tumor growth of esophageal squamous cell carcinoma (ESCC) xenograft[1].
| Animal Model: | Male BALB/c nude mice (4-6 weeks) with ESCC xenograft[1] |
| Dosage: | Intraperitoneal injection; once a week, for 3 weeks |
| Administration: | 5 and 10 mg/kg |
| Result: | Suppressed tumor volumes in a dose-dependent manner.
Increased expressions of Bax and decreased expressions of Bcl-2.
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References
[1] Du L, et, al. Antitumor activity of Lobaplatin against esophageal squamous cell carcinoma through caspase-dependent apoptosis and increasing the Bax/Bcl-2 ratio. Biomed Pharmacother. 2017 Nov;95:447-452. DOI:
10.1016/j.biopha.2017.08.119[2] Wu Q, et, al. Lobaplatin arrests cell cycle progression in human hepatocellular carcinoma cells. J Hematol Oncol. 2010 Oct 31;3:43. DOI:
10.1186/1756-8722-3-43[3] McKeage MJ. Lobaplatin: a new antitumour platinum drug. Expert Opin Investig Drugs. 2001 Jan;10(1):119-28. DOI:
10.1517/13543784.10.1.119
