MedKoo product information:

Satraplatin

Satraplatin (INN, codenamed JM216) is a platinum compound that is currently under investigation as one treatment of patients with advanced prostate cancer who have failed previous chemotherapy. It has not yet received approval from the U.S. Food and Drug Administration. First mentioned in the medical literature in 1993, satraplatin is the first orally active platinum-based chemotherapeutic drug; other available platinum analogues—cisplatin, carboplatin, and oxaliplatin—must be given intravenously. It is made available in the United States jointly by Spectrum Pharmaceuticals and GPC Biotech under the name SPERA (Satraplatin Expanded Rapid Access). The drug has also been used in the treatment of lung and ovarian cancers. The proposed mode of action is that the compound binds to the DNA of cancer cells rendering them incapable of dividing.

According to news published in 8 Jul 2008, GPC Biotech AG  reported that the Company has been informed by its partner for satraplatin in Europe that they plan to withdraw the Marketing Authorization Application (MAA) for satraplatin plus prednisone for the treatment of hormone-refractory prostate cancer patients whose prior chemotherapy has failed. This decision was based on a list of outstanding issues received following review by the Committee for Medicinal Products for Human Use (CHMP) of the European Medicines Agency (EMEA) of the filing, which indicates that the opinion of the Committee is that the application is currently not approvable based on the information provided. see: http://www.medicalnewstoday.com/articles/116301.php.

Current developer:    GPC Biotech

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22: Armstrong AJ, George DJ. Satraplatin in the treatment of hormone-refractory metastatic prostate cancer. Ther Clin Risk Manag. 2007 Oct;3(5):877-83. PubMed PMID: 18473011; PubMed Central PMCID: PMC2376074.

23: Liu W, Qing C, Chen X, Ye Q, Yu Y, Hou S. Preparation, characterization and in vitro anticancer activity of platinum(II) complexes with N-Cyclohexyl-1,3-propanediamine as the carrier. Chem Pharm Bull (Tokyo). 2008 May;56(5):659-62. PubMed PMID: 18451553.

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25: Choy H, Park C, Yao M. Current status and future prospects for satraplatin, an oral platinum analogue. Clin Cancer Res. 2008 Mar 15;14(6):1633-8. Review. PubMed PMID: 18347164.

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29: Harzstark AL, Ryan CJ. Therapies in development for castrate-resistant prostate cancer. Expert Rev Anticancer Ther. 2008 Feb;8(2):259-68. Review. PubMed PMID: 18279066.

30: Choi S, Vastag L, Larrabee YC, Personick ML, Schaberg KB, Fowler BJ, Sandwick RK, Rawji G. Importance of platinum(II)-assisted platinum(IV) substitution for the oxidation of guanosine derivatives by platinum(IV) complexes. Inorg Chem. 2008 Feb 18;47(4):1352-60. Epub 2008 Jan 26. Erratum in: Inorg Chem. 2008 May 5;47(9):3920. PubMed PMID: 18220340.

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32: Bayes M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2007 Oct;29(8):547-83. PubMed PMID: 18040531.

33: Chowdhury S, Burbridge S, Harper PG. Chemotherapy for the treatment of hormone-refractory prostate cancer. Int J Clin Pract. 2007 Dec;61(12):2064-70. Epub 2007 Oct 23. Review. PubMed PMID: 17956560.

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39: Sartor O. Chemotherapy in prostate cancer: an update. Clin Genitourin Cancer. 2007 Jun;5(5):304-5. PubMed PMID: 17645826.

40: Mathew P, Dipaola R. Taxane refractory prostate cancer. J Urol. 2007 Sep;178(3 Pt 2):S36-41. Epub 2007 Jul 20. Review. PubMed PMID: 17644120.

41: Kelland L. The resurgence of platinum-based cancer chemotherapy. Nat Rev Cancer. 2007 Aug;7(8):573-84. Epub 2007 Jul 12. Review. PubMed PMID: 17625587.

42: Kelland L. Broadening the clinical use of platinum drug-based chemotherapy with new analogues. Satraplatin and picoplatin. Expert Opin Investig Drugs. 2007 Jul;16(7):1009-21. Review. PubMed PMID: 17594186.

43: Petrylak DP. New paradigms for advanced prostate cancer. Rev Urol. 2007;9 Suppl 2:S3-S12. PubMed PMID: 17554403; PubMed Central PMCID: PMC1887815.

44: Wosikowski K, Lamphere L, Unteregger G, Jung V, Kaplan F, Xu JP, Rattel B, Caligiuri M. Preclinical antitumor activity of the oral platinum analog satraplatin. Cancer Chemother Pharmacol. 2007 Sep;60(4):589-600. Epub 2007 May 31. PubMed PMID: 17541592.

45: Di Lorenzo G, Autorino R, Figg WD, De Placido S. Hormone-refractory prostate cancer: where are we going? Drugs. 2007;67(8):1109-24. Review. PubMed PMID: 17521214.

46: Martelli L, Di Mario F, Botti P, Ragazzi E, Martelli M, Kelland L. Accumulation, platinum-DNA adduct formation and cytotoxicity of cisplatin, oxaliplatin and satraplatin in sensitive and resistant human osteosarcoma cell lines, characterized by p53 wild-type status. Biochem Pharmacol. 2007 Jun 30;74(1):20-7. Epub 2007 Mar 30. PubMed PMID: 17466278.

47: Kerr C. Satraplatin for hormone-refractory prostate cancer. Lancet Oncol. 2007 Apr;8(4):290. PubMed PMID: 17431954.

48: McKeage MJ. Satraplatin in hormone-refractory prostate cancer and other tumour types: pharmacological properties and clinical evaluation. Drugs. 2007;67(6):859-69. Review. PubMed PMID: 17428104.

49: Di Lorenzo G, Autorino R. Re: Fabio Calabrò and Cora N. Sternberg. Current indications for chemotherapy in prostate cancer patients. Eur urol 2007;51:17-26. Eur Urol. 2007 Aug;52(2):613-4. Epub 2007 Apr 3. PubMed PMID: 17416455.

50: Beekman KW, Bradley D, Hussain M. New molecular targets and novel agents in the treatment of advanced urothelial cancer. Semin Oncol. 2007 Apr;34(2):154-64. Review. PubMed PMID: 17382799.

51: Satraplatin: BMS 182751, BMY 45594, JM 216. Drugs R D. 2007;8(2):125-32. Review. PubMed PMID: 17324011.

52: Oh WK, Tay MH, Huang J. Is there a role for platinum chemotherapy in the treatment of patients with hormone-refractory prostate cancer? Cancer. 2007 Feb 1;109(3):477-86. Review. PubMed PMID: 17186531.

53: Calabrò F, Sternberg CN. Current indications for chemotherapy in prostate cancer patients. Eur Urol. 2007 Jan;51(1):17-26. Epub 2006 Aug 22. Review. PubMed PMID: 17007996.

54: Tan WW. Novel agents and targets in managing patients with metastatic prostate cancer. Cancer Control. 2006 Jul;13(3):194-8. Review. PubMed PMID: 16885915.

55: Martelli L, Di Mario F, Ragazzi E, Apostoli P, Leone R, Perego P, Fumagalli G. Different accumulation of cisplatin, oxaliplatin and JM216 in sensitive and cisplatin-resistant human cervical tumour cells. Biochem Pharmacol. 2006 Sep 14;72(6):693-700. Epub 2006 Jul 17. PubMed PMID: 16844093.

56: Choy H. Satraplatin: an orally available platinum analog for the treatment of cancer. Expert Rev Anticancer Ther. 2006 Jul;6(7):973-82. Review. PubMed PMID: 16831070.

57: Samimi G, Kishimoto S, Manorek G, Breaux JK, Howell SB. Novel mechanisms of platinum drug resistance identified in cells selected for resistance to JM118 the active metabolite of satraplatin. Cancer Chemother Pharmacol. 2007 Feb;59(3):301-12. Epub 2006 Jun 13. PubMed PMID: 16770583.

58: Sova P, Mistr A, Kroutil A, Zak F, Pouckova P, Zadinova M. Comparative anti-tumor efficacy of two orally administered platinum(IV) drugs in nude mice bearing human tumor xenografts. Anticancer Drugs. 2006 Feb;17(2):201-6. PubMed PMID: 16428939.

59: Berry W, Eisenberger M. Achieving treatment goals for hormone-refractory prostate cancer with chemotherapy. Oncologist. 2005;10 Suppl 3:30-9. Review. PubMed PMID: 16368869.

60: Berthold DR, Sternberg CN, Tannock IF. Management of advanced prostate cancer after first-line chemotherapy. J Clin Oncol. 2005 Nov 10;23(32):8247-52. Review. PubMed PMID: 16278480.

61: Bayés M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2005 Sep;27(7):505-22. PubMed PMID: 16258596.

62: Sternberg CN. Satraplatin in the treatment of hormone-refractory prostate cancer. BJU Int. 2005 Nov;96(7):990-4. Erratum in: BJU Int. 2006 Jan;97(1):211. PubMed PMID: 16225514.

63: Carr JL, Tingle MD, McKeage MJ. Satraplatin activation by haemoglobin, cytochrome C and liver microsomes in vitro. Cancer Chemother Pharmacol. 2006 Apr;57(4):483-90. Epub 2005 Sep 20. PubMed PMID: 16172904.

64: Samimi G, Howell SB. Modulation of the cellular pharmacology of JM118, the major metabolite of satraplatin, by copper influx and efflux transporters. Cancer Chemother Pharmacol. 2006 Jun;57(6):781-8. Epub 2005 Sep 17. PubMed PMID: 16170571.

65: McKeage MJ. New-generation platinum drugs in the treatment of cisplatin-resistant cancers. Expert Opin Investig Drugs. 2005 Aug;14(8):1033-46. Review. PubMed PMID: 16050795.

66: Petrylak DP. Future directions in the treatment of androgen-independent prostate cancer. Urology. 2005 Jun;65(6 Suppl):8-12. Review. PubMed PMID: 15939077.

67: Sova P, Mistr A, Kroutil A, Zak F, Pouckova P, Zadinova M. Preclinical anti-tumor activity of a new oral platinum(IV) drug LA-12. Anticancer Drugs. 2005 Jul;16(6):653-7. PubMed PMID: 15930894.

68: Sternberg CN, Whelan P, Hetherington J, Paluchowska B, Slee PH, Vekemans K, Van Erps P, Theodore C, Koriakine O, Oliver T, Lebwohl D, Debois M, Zurlo A, Collette L; Genitourinary Tract Group of the EORTC. Phase III trial of satraplatin, an oral platinum plus prednisone vs. prednisone alone in patients with hormone-refractory prostate cancer. Oncology. 2005;68(1):2-9. Epub 2005 Feb 28. PubMed PMID: 15741753.

69: Ang WH, Khalaila I, Allardyce CS, Juillerat-Jeanneret L, Dyson PJ. Rational design of platinum(IV) compounds to overcome glutathione-S-transferase mediated drug resistance. J Am Chem Soc. 2005 Feb 9;127(5):1382-3. PubMed PMID: 15686364.

70: Latif T, Wood L, Connell C, Smith DC, Vaughn D, Lebwohl D, Peereboom D. Phase II study of oral bis (aceto) ammine dichloro (cyclohexamine) platinum (IV) (JM-216, BMS-182751) given daily x 5 in hormone refractory prostate cancer (HRPC). Invest New Drugs. 2005 Jan;23(1):79-84. PubMed PMID: 15528984.

71: Bayés M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2003 Sep;25(7):565-97. PubMed PMID: 14571286.

72: Vouillamoz-Lorenz S, Buclin T, Lejeune F, Bauer J, Leyvraz S, Decosterd LA. Pharmacokinetics of satraplatin (JM216), an oral platinum (IV) complex under daily oral administration for 5 or 14 days. Anticancer Res. 2003 May-Jun;23(3C):2757-65. PubMed PMID: 12926110.

73: Bayés M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2003 Jan-Feb;25(1):53-76. PubMed PMID: 12690708.

74: Carr JL, Tingle MD, McKeage MJ. Rapid biotransformation of satraplatin by human red blood cells in vitro. Cancer Chemother Pharmacol. 2002 Jul;50(1):9-15. Epub 2002 May 22. PubMed PMID: 12111106.

75: Fokkema E, Groen HJ, Helder MN, de Vries EG, Meijer C. JM216-, JM118-, and cisplatin-induced cytotoxicity in relation to platinum-DNA adduct formation, glutathione levels and p53 status in human tumour cell lines with different sensitivities to cisplatin. Biochem Pharmacol. 2002 Jun 1;63(11):1989-96. PubMed PMID: 12093475.

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77: Jones S, Hainsworth J, Burris HA 3rd, Thompson D, Raefsky E, Johnson V, Calvert S, Bulanhagui C, Lebwohl D, Greco FA. Phase I study of JM-216 (an oral platinum analogue) in combination with paclitaxel in patients with advanced malignancies. Invest New Drugs. 2002 Feb;20(1):55-61. PubMed PMID: 12008664.

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80: Piccart MJ, Lamb H, Vermorken JB. Current and future potential roles of the platinum drugs in the treatment of ovarian cancer. Ann Oncol. 2001 Sep;12(9):1195-203. Review. PubMed PMID: 11697824.

81: George CM, Haraf DJ, Mauer AM, Krauss SA, Hoffman PC, Rudin CM, Szeto L, Vokes EE. A phase I trial of the oral platinum analogue JM216 with concomitant radiotherapy in advanced malignancies of the chest. Invest New Drugs. 2001;19(4):303-10. PubMed PMID: 11561689.

82: Vouillamoz-Lorenz S, Bauer J, Lejeune F, Decosterd LA. Validation of an AAS method for the determination of platinum in biological fluids from patients receiving the oral platinum derivative JM216. J Pharm Biomed Anal. 2001 Jun;25(3-4):465-75. PubMed PMID: 11377026.

83: Xing B, Zhu H, Shi Y, Tang W. In vitro binding of an orally active platinum antitumor drug, JM216 to metallothionein. Biometals. 2001 Mar;14(1):51-7. PubMed PMID: 11368275.

84: Amorino GP, Mohr PJ, Hercules SK, Pyo H, Choy H. Combined effects of the orally active cisplatin analog, JM216, and radiation in antitumor therapy. Cancer Chemother Pharmacol. 2000;46(5):423-6. PubMed PMID: 11127948.

85: Xing B, Zhu H, Wang Y, Tang W. Binding properties of an orally active platinum anti-tumor drug JM216 with metallothionein in vivo. Biometals. 2000 Sep;13(3):203-8. PubMed PMID: 11127891.

86: Kurata T, Tamura T, Sasaki Y, Fujii H, Negoro S, Fukuoka M, Saijo N. Pharmacokinetic and pharmacodynamic analysis of bis-acetato-ammine-dichloro-cyclohexylamine-platinum(IV) (JM216) administered once a day for five consecutive days: a phase I study. Jpn J Clin Oncol. 2000 Sep;30(9):377-84. PubMed PMID: 11095134.

87: Kelland LR. An update on satraplatin: the first orally available platinum anticancer drug. Expert Opin Investig Drugs. 2000 Jun;9(6):1373-82. Review. PubMed PMID: 11060749.

88: Lansiaux A, Bailly C. [JM216, an orally active platine derivative]. Bull Cancer. 2000 Jul;87(7-8):531-6. French. PubMed PMID: 10969209.

89: Britten C, Hammond L, Hidalgo M, Rothenberg ML, Sharma A, Sharma S, Siu L, Villalona-Calero M, Weiss GR. New anticancer agents. Cancer Chemother Biol Response Modif. 1999;18:178-209. Review. PubMed PMID: 10800483.

90: Amorino GP, Freeman ML, Carbone DP, Lebwohl DE, Choy H. Radiopotentiation by the oral platinum agent, JM216: role of repair inhibition. Int J Radiat Oncol Biol Phys. 1999 May 1;44(2):399-405. PubMed PMID: 10760436.

91: Bengtson EM, Rigas JR. New oral chemotherapeutic agents for lung cancer. Drugs. 1999;58 Suppl 3:57-69. Review. PubMed PMID: 10711843.

92: Fokkema E, de Vries EG, Meijer S, Groen HJ. Lack of nephrotoxicity of new oral platinum drug JM216 in lung cancer patients. Cancer Chemother Pharmacol. 2000;45(1):89-92. PubMed PMID: 10647508.

93: Hiorns LR, Seckl MJ, Paradinas F, Sharp SY, Skelton LA, Brunstrom G, Newlands ES, Kelland LR, Leyland-Jones B. A molecular cytogenetic approach to studying platinum resistance. J Inorg Biochem. 1999 Oct;77(1-2):95-104. PubMed PMID: 10626360.

94: Chaney SG, Vaisman A. Specificity of platinum-DNA adduct repair. J Inorg Biochem. 1999 Oct;77(1-2):71-81. PubMed PMID: 10626357.

95: O'Neill CF, Koberle B, Masters JR, Kelland LR. Gene-specific repair of Pt/DNA lesions and induction of apoptosis by the oral platinum drug JM216 in three human ovarian carcinoma cell lines sensitive and resistant to cisplatin. Br J Cancer. 1999 Dec;81(8):1294-303. PubMed PMID: 10604725; PubMed Central PMCID: PMC2362973.

96: Fokkema E, Groen HJ, Bauer J, Uges DR, Weil C, Smith IE. Phase II study of oral platinum drug JM216 as first-line treatment in patients with small-cell lung cancer. J Clin Oncol. 1999 Dec;17(12):3822-7. PubMed PMID: 10577855.

97: Reardon JT, Vaisman A, Chaney SG, Sancar A. Efficient nucleotide excision repair of cisplatin, oxaliplatin, and Bis-aceto-ammine-dichloro-cyclohexylamine-platinum(IV) (JM216) platinum intrastrand DNA diadducts. Cancer Res. 1999 Aug 15;59(16):3968-71. PubMed PMID: 10463593.

98: Leyland-Jones B, Kelland LR, Harrap KR, Hiorns LR. Genomic imbalances associated with acquired resistance to platinum analogues. Am J Pathol. 1999 Jul;155(1):77-84. PubMed PMID: 10393840; PubMed Central PMCID: PMC1866663.

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100: Ferrante K, Winograd B, Canetta R. Promising new developments in cancer chemotherapy. Cancer Chemother Pharmacol. 1999;43 Suppl:S61-8. Review. PubMed PMID: 10357561.

101: Perez JM, Camazón M, Alvarez-Valdes A, Quiroga AG, Kelland LR, Alonso C, Navarro-Ranninger MC. Synthesis, characterization and DNA modification induced by a novel Pt(IV)-bis(monoglutarate) complex which induces apoptosis in glioma cells. Chem Biol Interact. 1999 Jan 29;117(2):99-115. PubMed PMID: 10190571.

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103: Taguchi T. [Gastrointestinal cancer and oral anticancer agents]. Gan To Kagaku Ryoho. 1999 Feb;26(3):284-94. Review. Japanese. PubMed PMID: 10065090.

104: Sessa C, Minoia C, Ronchi A, Zucchetti M, Bauer J, Borner M, de Jong J, Pagani O, Renard J, Weil C, D'Incalci M. Phase I clinical and pharmacokinetic study of the oral platinum analogue JM216 given daily for 14 days. Ann Oncol. 1998 Dec;9(12):1315-22. PubMed PMID: 9932162.

105: Ando Y, Shimizu T, Nakamura K, Mushiroda T, Nakagawa T, Kodama T, Kamataki T. Potent and non-specific inhibition of cytochrome P450 by JM216, a new oral platinum agent. Br J Cancer. 1998 Nov;78(9):1170-4. PubMed PMID: 9820175; PubMed Central PMCID: PMC2062991.

106: Sharp SY, Smith V, Hobbs S, Kelland LR. Lack of a role for MRP1 in platinum drug resistance in human ovarian cancer cell lines. Br J Cancer. 1998 Jul;78(2):175-80. PubMed PMID: 9683290; PubMed Central PMCID: PMC2062892.

107: Beale P, Raynaud F, Hanwell J, Berry C, Moore S, Odell D, Judson I. Phase I study of oral JM216 given twice daily. Cancer Chemother Pharmacol. 1998;42(2):142-8. PubMed PMID: 9654114.

108: DeMario MD, Ratain MJ. Rationale for phase I study of UFT plus leucovorin and oral JM-216. Oncology (Williston Park). 1997 Sep;11(9 Suppl 10):26-9. PubMed PMID: 9348563.

109: van de Vaart PJ, Klaren HM, Hofland I, Begg AC. Oral platinum analogue JM216, a radiosensitizer in oxic murine cells. Int J Radiat Biol. 1997 Dec;72(6):675-83. PubMed PMID: 9416790.

110: McKeage MJ, Raynaud F, Ward J, Berry C, O'Dell D, Kelland LR, Murrer B, Santabárabara P, Harrap KR, Judson IR. Phase I and pharmacokinetic study of an oral platinum complex given daily for 5 days in patients with cancer. J Clin Oncol. 1997 Jul;15(7):2691-700. PubMed PMID: 9215842.

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