Back to products

Browse products

Approved anticancer agents

Anticancer agents in trials

Anticancer molecular libraries

MedKoo product information:

Elsamitrucin

Description of Elsamitrucin: Elsamitrucin is a heterocyclic antineoplastic antibiotic isolated from the bacterium Actinomycete strain J907-21. Elsamitrucin intercalates into DNA at guanine-cytosine (G-C)-rich sequences and inhibits topoisomerase I and II, resulting in single-strand breaks and inhibition of DNA replication. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

Current developer:  Spectrum Pharmaceuticals, Inc.

In a phase II trial, : Elsamitrucin showed modest activity in patients with relapsed or refractory non-Hodgkin's lymphoma. Toxicity was relatively mild, consisted mainly of asthenia, nausea and vomiting and did not include myelosuppression. The activity of elsamitrucin in this group of patients and its lack of myelosuppression suggest utility in this disease especially when combined with other proven agents. see http://www.ncbi.nlm.nih.gov/pubmed/8913843.

In another phase II trial to test the antitumor activity of Elsamitrucin in metastatic cancer of the breast, colon and rectum, non-small cell lung and ovary. Patients with colorectal or non-small cell lung cancer could not have received prior chemotherapy. Treatment consisted of Elsamitrucin 25 mg/m2/week given as a 5-10 min infusion for at least 3-6 weekly doses. RESULTS: One hundred and five patients entered the studies, 97 were eligible, 94 are evaluable for toxicity and 75 for response. Toxicity mainly consisted of mild nausea/vomiting, and less frequently reversible hepatotoxicity and malaise. No objective responses were seen. CONCLUSION: Elsamitrucin at this dose and schedule is not an active drug in metastatic breast cancer, colorectal cancer, non-small cell lung cancer or ovarian cancer. see http://www.ncbi.nlm.nih.gov/pubmed/8075039.

 1: Barceló F, Portugal J. Elsamicin A binding to DNA. A comparative thermodynamic characterization. FEBS Lett. 2004 Oct 8;576(1-2):68-72. PubMed PMID: 15474012.

2: Portugal J. Chartreusin, elsamicin A and related anti-cancer antibiotics. Curr Med Chem Anticancer Agents. 2003 Nov;3(6):411-20. Review. PubMed PMID: 14529449.

3: van Acker FA, van Acker SA, Haenen GR, Bast A, van der Vijgh WJ. In vitro screening of antitumour agents for cardiotoxicity by means of isolated mouse left atria. Anticancer Res. 2000 Nov-Dec;20(6B):4483-7. PubMed PMID: 11205292.

4: Shen LL. DNA-unwinding test using eukaryotic DNA topoisomerase I. Methods Mol Biol. 2001;95:149-60. PubMed PMID: 11089228.

5: Costanza ME, Weiss RB, Henderson IC, Norton L, Berry DA, Cirrincione C, Winer E, Wood WC, Frei E 3rd, McIntyre OR, Schilsky RL. Safety and efficacy of using a single agent or a phase II agent before instituting standard combination chemotherapy in previously untreated metastatic breast cancer patients: report of a randomized study--Cancer and Leukemia Group B 8642. J Clin Oncol. 1999 May;17(5):1397-406. PubMed PMID: 10334524.

6: Vaquero A, Portugal J. Modulation of DNA-protein interactions in the P1 and P2 c-myc promoters by two intercalating drugs. Eur J Biochem. 1998 Jan 15;251(1-2):435-42. PubMed PMID: 9492315.

7: Rodríguez-Campos A, Azorín F, Portugal J. Influence of elsamicin A on the activity of mammalian topoisomerase I. Biochemistry. 1996 Aug 27;35(34):11177-82. PubMed PMID: 8780522.

8: Allen SL, Schacter LP, Lichtman SM, Bukowski R, Fusco D, Hensley M, O'Dwyer P, Mittelman A, Rosenbloom B, Huybensz S. Phase II study of elsamitrucin (BMY-28090) for the treatment of patients with refractory/relapsed non-Hodgkin's lymphoma. Invest New Drugs. 1996;14(2):213-7. PubMed PMID: 8913843.

9: Portugal J. Abortive transcription of the T7 promoter induced by elsamicin A. Anticancer Drug Des. 1995 Jul;10(5):427-38. PubMed PMID: 7639931.

10: Alhambra C, Luque FJ, Portugal J, Orozco M. Molecular dynamics study of the binding of elsamicin A to DNA. Eur J Biochem. 1995 Jun 1;230(2):555-66. PubMed PMID: 7607229.

11: Verweij J, Wanders J, Nielsen AL, Pavlidis N, Calabresi F, ten Bokkel Huinink W, Bruntsch U, Piccart M, Franklin H, Kaye SB. Phase II studies of Elsamitrucin in breast cancer, colorectal cancer, non-small cell lung cancer and ovarian cancer. EORTC Early Clinical Trials Group. Ann Oncol. 1994 Apr;5(4):375-6. PubMed PMID: 8075039.

12: Goss G, Letendre F, Stewart D, Shepherd F, Schacter L, Hoogendoorn P, Eisenhauer E. Phase II study of elsamitrucin in non-small cell lung cancer. Invest New Drugs. 1994;12(4):315-7. PubMed PMID: 7775132.

13: Klein I, Welink J, van der Vijgh WJ. Determination of Elsamitrucin (BMY-28090) in plasma and urine by high-performance liquid chromatography with fluorescence detection. J Chromatogr. 1993 Dec 22;622(2):249-53. PubMed PMID: 8150873.

14: Lorico A, Long BH. Biochemical characterisation of elsamicin and other coumarin-related antitumour agents as potent inhibitors of human topoisomerase II. Eur J Cancer. 1993;29A(14):1985-91. PubMed PMID: 8280493.

15: Silvestrini R, Sanfilippo O, Zaffaroni N, De Marco C, Catania S. Activity of a chartreusin analog, elsamicin A, on breast cancer cells. Anticancer Drugs. 1992 Dec;3(6):677-81. PubMed PMID: 1288737.

16: Jiménez-García E, Portugal J. Elsamicin A can convert the Z-form of poly[d(G-C)] and poly[(G-m5C)] back to B-form DNA. Biochemistry. 1992 Nov 24;31(46):11641-6. PubMed PMID: 1445900.

17: Párraga A, Orozco M, Portugal J. Experimental and modelling studies on the DNA cleavage by elsamicin A. Eur J Biochem. 1992 Sep 1;208(2):227-33. PubMed PMID: 1325899.

18: Ichikawa A, Kuboya T, Aoyama T, Sugiura Y. Activation of DNA cleavage by dynemicin A in a B-Z conformational junction. Biochemistry. 1992 Jul 28;31(29):6784-7. PubMed PMID: 1379070.

19: Uesugi M, Sugiura Y. Product analyses in DNA strand scission by antitumor antibiotic elsamicin A. Biochem Biophys Res Commun. 1992 Jul 15;186(1):580-7. PubMed PMID: 1321617.

20: Párraga A, Portugal J. Detection of elsamicin-DNA binding specificity by restriction enzyme cleavage. FEBS Lett. 1992 Mar 23;300(1):25-9. PubMed PMID: 1312486.

21: Raber MN, Newman RA, Newman BM, Gaver RC, Schacter LP. Phase I trial and clinical pharmacology of elsamitrucin. Cancer Res. 1992 Mar 15;52(6):1406-10. PubMed PMID: 1540949.

22: Salas X, Portugal J. Map of chartreusin and elsamicin binding sites on DNA. FEBS Lett. 1991 Nov 4;292(1-2):223-8. PubMed PMID: 1959610.

23: Uesugi M, Sekida T, Matsuki S, Sugiura Y. Selective DNA cleavage by elsamicin A and switch function of its amino sugar group. Biochemistry. 1991 Jul 9;30(27):6711-5. PubMed PMID: 1648389.

24: Uesugi M, Sugiura Y. Switch-function of amino sugar on elsamicin A, a DNA binding antitumor antibiotic. Nucleic Acids Symp Ser. 1990;(22):33-4. PubMed PMID: 2101907.

25: Lam KS, Veitch JA, Forenza S, Combs CM, Colson KL. Biosynthesis of elsamicin A, a novel antitumor antibiotic. J Nat Prod. 1989 Sep-Oct;52(5):1015-21. PubMed PMID: 2607345.

26: Schurig JE, Bradner WT, Basler GA, Rose WC. Experimental antitumor activity of BMY-28090, a new antitumor antibiotic. Invest New Drugs. 1989 Jul;7(2-3):173-8. PubMed PMID: 2793369.

27: Gaver RC, Deeb G, George AM. Validated HPLC procedures for the analysis of MBY-28090 in human plasma and urine. Cancer Chemother Pharmacol. 1989;25(3):195-201. PubMed PMID: 2598411.

28: Otake N. [The structure and antitumor activity of antitumor antibiotics--recent progress]. Gan To Kagaku Ryoho. 1988 Mar;15(3):369-79. Review. Japanese. PubMed PMID: 3279909.

29: Konishi M, Sugawara K, Kofu F, Nishiyama Y, Tomita K, Miyaki T, Kawaguchi H. Elsamicins, new antitumor antibiotics related to chartreusin. I. Production, isolation, characterization and antitumor activity. J Antibiot (Tokyo). 1986 Jun;39(6):784-91. PubMed PMID: 3733527.