Nemorubicin is a doxorubicin derivative that differs significantly from its parent drug in terms of spectrum of antitumor activity, metabolism and toxicity profile. The drug is active on tumors resistant to alkylating agents, topoisomerase II inhibitors and platinum derivatives. It works primarily through topoisomerase I inhibition. Of note, Nemorubicin is active in cells with upregulation of the nucleotide excision repair (NER) pathway, where current therapies fail.

Nemorubicin is biotransformed in the liver into cytotoxic metabolites that may further contribute to render this drug highly active against primary liver tumors or liver metastases. In addition, Nemorubicin was minimally cardiotoxic at therapeutic doses in animals.

Clinical trials were conducted in Europe, US and China with Nemorubicin given at different dose-schedules and by different routes of administration: as single agent by systemic IV route, oral route and by intra-hepatic artery (IHA) infusion alone or in combination with cisplatin.

A Phase II study with Nemorubicin in combination with cisplatin via IHA administration has been recently concluded with success in Europe.

Selected References

  • Fiore F, Gadaleta CD, Granetto C, et al. Phase II trial of Nemorubicin hydrocloride (Nemorubicin) in combination with cisplatin (cDDP) in patients (pts) with hepatocellular carcinoma (HCC): First step results, American Society of Clinical Oncology Annual Meeting 2009,May 31(Abs 4593)
  • Sun Y,Yang J, Luo P, et al. Efficacy of Nemorubicin (MMDX) administered with iodinated oil via hepatic artery (IHA) to patients with unresectable primary hepatocellular carcinoma (HCC): phase II trial. EJC 2004; vol.2 (8), Abstract 470.
  • Geroni C, Quintieri L, Valota O, et al. Preclinical activity against liver metastases of nemorubicin, a DNA-intercalating cytotoxic agent for the treatment of hepatocellular carcinoma. Eur J Cancer, 38(7): 45, S19, 2002.
  • Quintieri L, Rosato A, Napoli E, et al. In vivo antitumor activity and host toxicity of methoxymorpholinyl doxorubicin: role of cytochrome P450 3A., Cancer Res. 2000 Jun 15;60(12):3232-8
  • Sessa C,  Zucchetti M, Ghielmini M, et al.   Phase I clinical and pharmacological study of oral methoxymorpholinyl doxorubicin (PNU 152243)., Cancer Chemother Pharmacol. 1999;44(5):403-10        
  • Bakker M, Droz JP, Hanauske AR, et al. Broad phase II and pharmacokinetic study of methoxy-morpholino doxorubicin (FCE 23762-MMRDX) in non-small-cell lung cancer, renal cancer and other solid tumour patients., Br J Cancer. 1998;77(1):139-46     
  • Danesi R, Agen C, Grandi M, et al.  3'-Deamino-3'-(2-methoxy-4-morpholinyl)-doxorubicin  (FCE  23762):  a new  anthracycline  derivative with enhanced cytotoxicity and reduced cardiotoxicity. Eur J Cancer, 29A:1560-5, 1993.
  • Ripamonti M, Pezzoni G, Pesenti E, at al. In vivo antitumour activity of FCE23762, a methoxy morpholinyl derivative of doxorubicin active on doxorubicin-resistant tumour cells.  Br J Cancer, 65:703-7, 1992.
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