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Amonafide dihydrochloride

Description of amonafide dihydrochloride: Amonafide dihydrochloride is the dihydrochloride salt of amonafide, an imide derivative of naphthalic acid. Amonafide intercalates into DNA and inhibits topoisomerase II, resulting in protein-associated strand breaks and impaired DNA and RNA synthesis. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

Current developer:    Abbott (Originator), ChemGenex Therapeutics

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2: Lv M, Xu H. Overview of naphthalimide analogs as anticancer agents. Curr Med Chem. 2009;16(36):4797-813. Review. PubMed PMID: 19929786.

3: Zhu H, Miao ZH, Huang M, Feng JM, Zhang ZX, Lu JJ, Cai YJ, Tong LJ, Xu YF, Qian XH, Ding J. Naphthalimides induce G(2) arrest through the ATM-activated Chk2-executed pathway in HCT116 cells. Neoplasia. 2009 Nov;11(11):1226-34. PubMed PMID: 19881958; PubMed Central PMCID: PMC2767224.

4: Mei ZH, Tian ZY, Ma HX, Xie SQ, Zhao J, Wang CJ. [Synthesis and in vitro cytotoxicity of naphthalimide polyamine conjugates as antitumor agents]. Yao Xue Xue Bao. 2009 Jul;44(7):754-7. Chinese. PubMed PMID: 19806915.

5: Allen SL, Kolitz JE, Lundberg AS, Bennett JM, Capizzi RL, Budman DR. Phase I trials of amonafide as monotherapy and in combination with cytarabine in patients with poor-risk acute myeloid leukemia. Leuk Res. 2010 Apr;34(4):487-91. Epub 2009 Sep 12. PubMed PMID: 19748672.

6: Wu A, Xu Y, Qian X, Wang J, Liu J. Novel naphthalimide derivatives as potential apoptosis-inducing agents: design, synthesis and biological evaluation. Eur J Med Chem. 2009 Nov;44(11):4674-80. Epub 2009 Jul 16. PubMed PMID: 19643513.

7: Wang J, Wu A, Xu Y, Liu J, Qian X. M(2)-A induces apoptosis and G(2)-M arrest via inhibiting PI3K/Akt pathway in HL60 cells. Cancer Lett. 2009 Oct 8;283(2):193-202. Epub 2009 May 10. PubMed PMID: 19435648.

8: Ingrassia L, Lefranc F, Kiss R, Mijatovic T. Naphthalimides and azonafides as promising anti-cancer agents. Curr Med Chem. 2009;16(10):1192-213. Review. PubMed PMID: 19355879.

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10: Xie L, Xu Y, Wang F, Liu J, Qian X, Cui J. Synthesis of new amonafide analogues via coupling reaction and their cytotoxic evaluation and DNA-binding studies. Bioorg Med Chem. 2009 Jan 15;17(2):804-10. Epub 2008 Nov 27. PubMed PMID: 19070496.

11: Mijatovic T, Mahieu T, Bruyère C, De Nève N, Dewelle J, Simon G, Dehoux MJ, van der Aar E, Haibe-Kains B, Bontempi G, Decaestecker C, Van Quaquebeke E, Darro F, Kiss R. UNBS5162, a novel naphthalimide that decreases CXCL chemokine expression in experimental prostate cancers. Neoplasia. 2008 Jun;10(6):573-86. PubMed PMID: 18516294; PubMed Central PMCID: PMC2386542.

12: Burcu M, O'Loughlin KL, Ford LA, Baer MR. Amonafide L-malate is not a substrate for multidrug resistance proteins in secondary acute myeloid leukemia. Leukemia. 2008 Nov;22(11):2110-5. Epub 2008 Apr 17. PubMed PMID: 18418409.

13: Ferri N, Beccalli EM, Contini A, Corsini A, Antonino M, Radice T, Pratesi G, Tinelli S, Zunino F, Gelmi ML. Antiproliferative effects on human tumor cells and rat aortic smooth muscular cells of 2,3-heteroarylmaleimides and heterofused imides. Bioorg Med Chem. 2008 Feb 15;16(4):1691-701. Epub 2007 Nov 13. PubMed PMID: 18061459.

14: Norton JT, Witschi MA, Luong L, Kawamura A, Ghosh S, Stack MS, Sim E, Avram MJ, Appella DH, Huang S. Synthesis and anticancer activities of 6-amino amonafide derivatives. Anticancer Drugs. 2008 Jan;19(1):23-36. PubMed PMID: 18043127.

15: Chau M, Christensen JL, Ajami AM, Capizzi RL. Amonafide, a topoisomerase II inhibitor, is unaffected by P-glycoprotein-mediated efflux. Leuk Res. 2008 Mar;32(3):465-73. Epub 2007 Sep 10. PubMed PMID: 17826829.

16: Van Quaquebeke E, Mahieu T, Dumont P, Dewelle J, Ribaucour F, Simon G, Sauvage S, Gaussin JF, Tuti J, El Yazidi M, Van Vynckt F, Mijatovic T, Lefranc F, Darro F, Kiss R. 2,2,2-Trichloro-N-({2-[2-(dimethylamino)ethyl]-1,3-dioxo-2,3-dihydro-1H-benzo[de] isoquinolin- 5-yl}carbamoyl)acetamide (UNBS3157), a novel nonhematotoxic naphthalimide derivative with potent antitumor activity. J Med Chem. 2007 Aug 23;50(17):4122-34. Epub 2007 Jul 21. PubMed PMID: 17658777.

17: Alami N, Paterson J, Belanger S, Juste S, Grieshaber CK, Leyland-Jones B. Comparative analysis of xanafide cytotoxicity in breast cancer cell lines. Br J Cancer. 2007 Jul 2;97(1):58-64. Epub 2007 Jun 5. PubMed PMID: 17551498; PubMed Central PMCID: PMC2359668.

18: Li F, Cui J, Guo L, Qian X, Ren W, Wang K, Liu F. Molecular design, chemical synthesis, and biological evaluation of '4-1' pentacyclic aryl/heteroaryl-imidazonaphthalimides. Bioorg Med Chem. 2007 Aug 1;15(15):5114-21. Epub 2007 May 17. PubMed PMID: 17532640.

19: Pourpak A, Landowski TH, Dorr RT. Ethonafide-induced cytotoxicity is mediated by topoisomerase II inhibition in prostate cancer cells. J Pharmacol Exp Ther. 2007 Jun;321(3):1109-17. Epub 2007 Mar 9. PubMed PMID: 17351106.

20: Zhu H, Huang M, Yang F, Chen Y, Miao ZH, Qian XH, Xu YF, Qin YX, Luo HB, Shen X, Geng MY, Cai YJ, Ding J. R16, a novel amonafide analogue, induces apoptosis and G2-M arrest via poisoning topoisomerase II. Mol Cancer Ther. 2007 Feb;6(2):484-95. PubMed PMID: 17308047.

21: Acevedo O, Jorgensen WL. Influence of inter- and intramolecular hydrogen bonding on kemp decarboxylations from QM/MM simulations. J Am Chem Soc. 2005 Jun 22;127(24):8829-34. PubMed PMID: 15954791.

22: Li Z, Yang Q, Qian X. Novel thiazonaphthalimides as efficient antitumor and DNA photocleaving agents: effects of intercalation, side chains, and substituent groups. Bioorg Med Chem. 2005 Aug 15;13(16):4864-70. PubMed PMID: 15925513.

23: Gil-Alegre ME, Bernabeu JA, Camacho MA, Torres-Suarez AI. Statistical method for evaluation of dissolution stability in the formulation development of solid dosage forms: tablets of amonafide. Pharmazie. 2004 Jul;59(7):541-7. PubMed PMID: 15296092.

24: Braña MF, Cacho M, García MA, de Pascual-Teresa B, Ramos A, Domínguez MT, Pozuelo JM, Abradelo C, Rey-Stolle MF, Yuste M, Báñez-Coronel M, Lacal JC. New analogues of amonafide and elinafide, containing aromatic heterocycles: synthesis, antitumor activity, molecular modeling, and DNA binding properties. J Med Chem. 2004 Mar 11;47(6):1391-9. PubMed PMID: 14998328.

25: Braña MF, Ramos A. Naphthalimides as anti-cancer agents: synthesis and biological activity. Curr Med Chem Anticancer Agents. 2001 Nov;1(3):237-55. Review. PubMed PMID: 12678756.

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28: Dorr RT, Liddil JD, Sami SM, Remers W, Hersh EM, Alberts DS. Preclinical antitumor activity of the azonafide series of anthracene-based DNA intercalators. Anticancer Drugs. 2001 Mar;12(3):213-20. PubMed PMID: 11290869.

29: Wang H, Mao Y, Zhou N, Hu T, Hsieh TS, Liu LF. Atp-bound topoisomerase ii as a target for antitumor drugs. J Biol Chem. 2001 May 11;276(19):15990-5. Epub 2001 Feb 23. PubMed PMID: 11278845.

30: Innocenti F, Iyer L, Ratain MJ. Pharmacogenetics of anticancer agents: lessons from amonafide and irinotecan. Drug Metab Dispos. 2001 Apr;29(4 Pt 2):596-600. PubMed PMID: 11259359.

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32: Sami SM, Dorr RT, Alberts DS, Sólyom AM, Remers WA. Analogues of amonafide and azonafide with novel ring systems. J Med Chem. 2000 Aug 10;43(16):3067-73. PubMed PMID: 10956214.

33: 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.

34: Asbury R, Blessing JA, Reid GC, McGuire WP. A phase II trial of amonafide in patients with endometrial cancer: a Gynecologic Oncology Group Study. Am J Clin Oncol. 1998 Aug;21(4):406-7. PubMed PMID: 9708643.

35: Asbury R, Blessing JA, Podczaski E, Ball H. A phase II trial of amonafide in patients with mixed mesodermal tumors of the uterus: a Gynecologic Oncology Group study. Am J Clin Oncol. 1998 Jun;21(3):306-7. PubMed PMID: 9626805.

36: Asbury R, Blessing JA, Buller R, Malfetano JH, Walker J, Sevin BU. Amonafide in patients with leiomyosarcoma of the uterus: a phase II Gynecologic Oncology Group study. Am J Clin Oncol. 1998 Apr;21(2):145-6. PubMed PMID: 9537200.

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42: Leaf AN, Neuberg D, Schwartz EL, Wadler S, Ritch PS, Dutcher JP, Adams GL. An ECOG phase II study of amonafide in unresectable or recurrent carcinoma of the head and neck (PB390). Eastern Cooperative Oncology Group. Invest New Drugs. 1997;15(2):165-72. PubMed PMID: 9220297.

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45: Bear S, Remers WA. Computer simulation of the binding of amonafide and azonafide to DNA. J Comput Aided Mol Des. 1996 Apr;10(2):165-75. PubMed PMID: 8741020.

46: Ratain MJ, Mick R, Janisch L, Berezin F, Schilsky RL, Vogelzang NJ, Kut M. Individualized dosing of amonafide based on a pharmacodynamic model incorporating acetylator phenotype and gender. Pharmacogenetics. 1996 Feb;6(1):93-101. PubMed PMID: 8845865.

47: Witte RS, Hsieh P, Elson P, Oken MM, Trump DL. A phase II trial of amonafide, caracemide, and homoharringtonine in the treatment of patients with advanced renal cell cancer. Invest New Drugs. 1996;14(4):409-13. PubMed PMID: 9157078.

48: Kreis W, Chan K, Budman DR, Allen SL, Fusco D, Mittelman A, Hock K, Akerman S, Calabro A, Puccio C, Spigelman M. Clinical pharmacokinetics of amonafide (NSC 308847) in 62 patients. Cancer Invest. 1996;14(4):320-7. PubMed PMID: 8689426.

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50: Costanza ME, Berry D, Henderson IC, Ratain MJ, Wu K, Shapiro C, Duggan D, Kalra J, Berkowitz I, Lyss AP. Amonafide: An active agent in the treatment of previously untreated advanced breast cancer--a cancer and leukemia group B study (CALGB 8642). Clin Cancer Res. 1995 Jul;1(7):699-704. PubMed PMID: 9816035.

51: Hayes DF, Henderson IC, Shapiro CL. Treatment of metastatic breast cancer: present and future prospects. Semin Oncol. 1995 Apr;22(2 Suppl 5):5-19; discussion 19-21. Review. PubMed PMID: 7537913.

52: Sami SM, Dorr RT, Sólyom AM, Alberts DS, Remers WA. Amino-substituted 2-[2'-(dimethylamino)ethyl]-1,2-dihydro-3H- dibenz[de,h]isoquinoline-1,3-diones. Synthesis, antitumor activity, and quantitative structure--activity relationship. J Med Chem. 1995 Mar 17;38(6):983-93. PubMed PMID: 7699715.

53: Ratain MJ, Rosner G, Allen SL, Costanza M, Van Echo DA, Henderson IC, Schilsky RL. Population pharmacodynamic study of amonafide: a Cancer and Leukemia Group B study. J Clin Oncol. 1995 Mar;13(3):741-7. PubMed PMID: 7884434.

54: De Isabella P, Zunino F, Capranico G. Base sequence determinants of amonafide stimulation of topoisomerase II DNA cleavage. Nucleic Acids Res. 1995 Jan 25;23(2):223-9. PubMed PMID: 7862525; PubMed Central PMCID: PMC306658.

55: Rosen F, Vokes EE, Lad T, Kies M, Wade J 3rd, Kilton LJ, Blough R, French S, Mullane M, Benson AB 3rd. Phase II study of amonafide in the treatment of patients with advanced squamous cell carcinoma of the head and the neck. An Illinois Cancer Center study. Invest New Drugs. 1995;13(3):249-52. PubMed PMID: 8729954.

56: Chang AY, Tu ZN, Smith JL, Bonomi P, Smith TJ, Wiernik PH, Blum R. Phase II trial of gallium nitrate, amonafide and teniposide in metastatic non-small cell lung cancer. An Eastern Cooperative Oncology Group study (E2588). Invest New Drugs. 1995;13(2):137-41. PubMed PMID: 8617576.

57: Levitt R, Buckner JC, Cascino TL, Burch PA, Morton RF, Westberg MW, Goldberg RM, Gallagher JG, O'Fallon JR, Scheithauer BW. Phase II study of amonafide in patients with recurrent glioma. J Neurooncol. 1995;23(1):87-93. PubMed PMID: 7623074.

58: Marshall ME, Blumenstein B, Crawford ED, Thompson IM, Craig JB, Eisenberger M, Ahmann F. Phase II trial of amonafide for the treatment of advanced, hormonally refractory carcinoma of the prostate. A Southwest Oncology Group study. Am J Clin Oncol. 1994 Dec;17(6):514-5. PubMed PMID: 7977172.

59: Mick R, Ratain MJ. Bootstrap validation of pharmacodynamic models defined via stepwise linear regression. Clin Pharmacol Ther. 1994 Aug;56(2):217-22. PubMed PMID: 8062499.

60: Marschke RF Jr, Wieand HS, O'Connell MJ, Rubin J, Schutt AJ, Burch PA, Kovach JS. Advanced colorectal adenocarcinoma: treatment with amonafide. J Natl Cancer Inst. 1994 Jun 15;86(12):944-5. PubMed PMID: 8196086.

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63: Malviya VK, Liu PY, O'Toole R, Alberts DS, Surwit E, Rosenoff S, Ward JH, Yu A, O'Sullivan J, Craig JB. Phase II trial of amonafide in patients with advanced metastatic or recurrent endometrial adenocarcinoma. A Southwest Oncology Group study. Am J Clin Oncol. 1994 Feb;17(1):37-40. PubMed PMID: 8311005.

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