生物活性

• 描述Lobaplatin (D-19466) is a diastereometric mixture of platinum(II) complexes containing a 1,2-bis(aminomethyl)cyclobutane stable ligand and lactic acid as the leaving group. Its antitumour activity results from the formation of DNA-drug adducts, mainly as GG and AG intra-strand cross-links. Lobaplatin influences the expression of the c-myc gene, which is involved in oncogenesis, apoptosis and cell proliferation^[3]. Lobaplatin and paclitaxel inhibited SGC-7901 cell growth in a concentration and timedependent manner, with IC25 values at 48h of 1.97±0.17µg/ml and 1.98±0.19 ng/ml, respectively. Lobaplatin did not affect cyclin D1 and CDK4 protein expression, while cyclin E1 and CDK2 levels were significantly increased, with cyclin B1 amounts markedly decreased (p<0.05). More S phase cells were observed after lobaplatin treatment compared with controls (60.03±1.25 vs. 18.69±0.96%; p<0.05). Lobaplatin and paclitaxel combination did not affect cyclin D1 and CDK4 protein levels (p>0.05); meanwhile, cyclin E1 and CDK2 levels were increased, with reduced cyclin B1 amounts, compared with control values (p<0.05)^[4].Lobaplatin inhibited proliferation of human HCC cells in a dose-dependent manner. For the most sensitive SMMC-7721 cells, lobaplatin arrested cell cycle progression in G1 and G2/M phases time-dependently which might be associated with the down-regulation of cyclin B, CDK1, CDC25C, phosphorylated CDK1 (pCDK1), pCDK4, Rb, E2F, and pRb, and the up-regulation of p53, p21, and p27^[5].Lobaplatin inhibited the proliferation of human gastric cancer cells and induced apoptosis, which may be associated with the up-regulation of Bax expression, poly(ADP-ribose) polymerase (PARP) cleavage, p53 expression and the reduction of Bcl-2 expression^[6].
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT03731442	Esophageal Cancer	Phase 3	Recruiting	October 31, 2027	China, Beijing ... more >> Department of Radiation Oncology, National Cancer Center/National Clinical Research Center for Cancer/Cancer Hospital, Chinese Academy of Medical Sciences (CAMS) and Peking Union Medical College (PUMC) Recruiting Beijing, Beijing, China, 100021 Contact: Zefen Xiao, MD Collapse <<
  NCT03328234	IMRT With or Without Concurren... more >>t Chemotherapy for Esophageal Cancer Collapse <<	Phase 3	Recruiting	December 31, 2022	China ... more >> Department of Radiation Oncology, Cancer Hospital, National Cancer Center, Chinese Academy of Medical Sciences (CAMS) and Peking Union Medical College (PUMC) Recruiting Beijing, China, 100021 Contact: Xin Wang, MD    +861013311583220    beryl_wx2000@163.com Collapse <<
  NCT03308552	Esophageal Neoplasms	Phase 3	Recruiting	August 30, 2021	China, Beijing ... more >> Department of Radiation Oncology, Cancer Hospital, National Cancer Center, Chinese Academy of Medical Sciences (CAMS) and Peking Union Medical College (PUMC) Recruiting Beijing, Beijing, China, 100021 Contact: Zefen Xiao, MD Collapse <<

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• 参考文献

• [1] Welink J, Boven E, et al. Pharmacokinetics and pharmacodynamics of lobaplatin (D-19466) in patients with advanced solid tumors, including patients with impaired renal of liver function. Clin Cancer Res. 1999 Sep;5(9):2349-58.

  [2] Gietema JA, Veldhuis GJ, et al. Phase II and pharmacokinetic study of lobaplatin in patients with relapsed ovarian cancer. Br J Cancer. 1995 Jun;71(6):1302-7.

  [3] M J McKeage. Lobaplatin: a new antitumour platinum drug. Expert Opin Investig Drugs. 2001 Jan;10(1):119-28.

  [4] Suhang Hua,et al. Anticancer Mechanism of Lobaplatin as Monotherapy and in Combination with Paclitaxel in Human Gastric Cancer. Curr Mol Pharmacol. 2018;11(4):316-325.

  [5] Qiong Wu,et al. Lobaplatin arrests cell cycle progression in human hepatocellular carcinoma cells. J Hematol Oncol. 2010 Oct 31;3:43.

  [6] Chu-Yang Yin,et al. Lobaplatin inhibits growth of gastric cancer cells by inducing apoptosis. World J Gastroenterol.2014 Dec 14;20(46):17426-33.

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