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MedKoo product information:
Picoplatin
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MedKoo Code#: 202230
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Name: Picoplatin
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CAS#: 181630-15-9
Synonym:
Code names: AMD473; NX 473; ZD0473. Chemical structure
names: * Cis-Amminedichloro (2-Methylpyridine) Platinum.
IUPAC/Chemical name:
Cis-Amminedichloro (2-Methylpyridine) Platinum.
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Chemical structure |
Theoretical analysis
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Chemical Formula: C6H10Cl2N2Pt
Molecular Weight: 376.15
Elemental Analysis: C, 19.16; H, 2.68; Cl,
18.85; N, 7.45; Pt, 51.86
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Availability and price:
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Information about this agent
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Picoplatin is a
new generation organic platinum analog with an extended spectrum of
antineoplastic activity. Designed to overcome platinum drug resistance,
picoplatin alkylates DNA, forming both inter- and intra-strand
cross-linkages, resulting in inhibition of DNA replication and
transcription, and the induction of apoptosis. Check for
active clinical trials or
closed clinical trials using this agent. (NCI
Thesaurus)
Picoplatin is a new generation platinum chemotherapy
agent that has an improved safety profile compared to existing
platinum-based chemotherapeutics and was designed to overcome platinum
resistance. Picoplatin has been evaluated in approximately 1100 patients
and has demonstrated activity in multiple indications with no evidence
of significant kidney, nerve toxicity or hearing loss. (Source:
Poniard's website).
Picoplatin is a cytotoxic platinum compound in
clinical development by Poniard Pharmaceuticals (previously NeoRx) for
the treatment of patients with solid tumors. In Phase I and Phase II
clinical trials, picoplatin demonstrated activity in a variety of solid
tumors, including lung, ovarian, colorectal and hormone-refractory
prostate cancer. However, in Phase III trials, picoplatin failed to hit
its primary endpoint for advanced small cell lung cancer. Hopes are now
pinned on its use for metastatic colorectal cancer. (source:
wikipedia.com).
Current developer:
Poniard Pharmaceuticals.
1: Wheate NJ, Walker S, Craig GE, Oun R. The
status of platinum anticancer drugs in the clinic and in clinical
trials. Dalton Trans. 2010 Jun 30. [Epub ahead of print] PubMed PMID:
20593091.
2: Margiotta N, Denora N, Ostuni R, Laquintana V, Anderson A, Johnson
SW, Trapani G, Natile G. Platinum(II) complexes with bioactive carrier
ligands having high affinity for the translocator protein. J Med Chem.
2010 Jul 22;53(14):5144-54. PubMed PMID: 20568783.
3: More SS, Li S, Yee SW, Chen L, Xu Z, Jablons DM, Giacomini KM.
Organic cation transporters modulate the uptake and cytotoxicity of
picoplatin, a third-generation platinum analogue. Mol Cancer Ther. 2010
Apr;9(4):1058-69. Epub 2010 Apr 6. PubMed PMID: 20371711.
4: Olszewski U, Hamilton G. A better platinum-based anticancer drug yet
to come? Anticancer Agents Med Chem. 2010 May 1;10(4):293-301. Review.
PubMed PMID: 20187870.
5: Eckardt JR, Bentsion DL, Lipatov ON, Polyakov IS, Mackintosh FR,
Karlin DA, Baker GS, Breitz HB. Phase II study of picoplatin as
second-line therapy for patients with small-cell lung cancer. J Clin
Oncol. 2009 Apr 20;27(12):2046-51. Epub 2009 Mar 16. PubMed PMID:
19289620.
6: Shah N, Dizon DS. New-generation platinum agents for solid tumors.
Future Oncol. 2009 Feb;5(1):33-42. Review. PubMed PMID: 19243296.
7: Tomillero A, Moral MA. Gateways to clinical trials. Methods Find Exp
Clin Pharmacol. 2008 Oct;30(8):643-72. PubMed PMID: 19088949.
8: Tomillero A, Moral MA. Gateways to clinical trials. July-August 2008.
Methods Find Exp Clin Pharmacol. 2008 Jul-Aug;30(6):459-95. PubMed PMID:
18850047.
9: Teicher BA. Newer cytotoxic agents: attacking cancer broadly. Clin
Cancer Res. 2008 Mar 15;14(6):1610-7. Review. PubMed PMID: 18347161.
10: Bayés M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods
Find Exp Clin Pharmacol. 2007 Dec;29(10):697-735. PubMed PMID: 18200333.
11: Bayes M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods
Find Exp Clin Pharmacol. 2007 Oct;29(8):547-83. PubMed PMID: 18040531.
12: 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.
13: 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.
14: Battle AR, Choi R, Hibbs DE, Hambley TW. Platinum(IV) analogues of
AMD473 (cis-[PtCl2(NH3)(2-picoline)]): preparative, structural, and
electrochemical studies. Inorg Chem. 2006 Aug 7;45(16):6317-22. PubMed
PMID: 16878941.
15: Bayés M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods
Find Exp Clin Pharmacol. 2004 Nov;26(9):723-53. PubMed PMID: 15632957.
16: Plasencia C, Abad A, Martinez-Balibrea E, Taron M. Antiproliferative
effects of ZD0473 (AMD473) in combination with 5-fluorouracil or SN38 in
human colorectal cancer cell lines. Invest New Drugs. 2004
Nov;22(4):399-409. PubMed PMID: 15292710.
17: Gelmon KA, Stewart D, Chi KN, Chia S, Cripps C, Huan S, Janke S,
Ayers D, Fry D, Shabbits JA, Walsh W, McIntosh L, Seymour LK. A phase I
study of AMD473 and docetaxel given once every 3 weeks in patients with
advanced refractory cancer: a National Cancer Institute of
Canada-Clinical Trials Group trial, IND 131. Ann Oncol. 2004
Jul;15(7):1115-22. PubMed PMID: 15205207.
18: Raaphorst GP, Yang DP, Li LF, Malone S. Comparison of human tumour
cell responses to cisplatin and ZD0473 with and without irradiation.
Anticancer Res. 2004 Mar-Apr;24(2B):613-8. PubMed PMID: 15161002.
19: Flaherty KT, Stevenson JP, Redlinger M, Algazy KM, Giatonio B,
O'Dwyer PJ. A phase I, dose escalation trial of ZD0473, a novel platinum
analogue, in combination with gemcitabine. Cancer Chemother Pharmacol.
2004 May;53(5):404-8. PubMed PMID: 15129676.
20: Bayés M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods
Find Exp Clin Pharmacol. 2004 Mar;26(2):129-61. PubMed PMID: 15071612.
21: Bayés M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods
Find Exp Clin Pharmacol. 2003 Jul-Aug;25(6):483-506. PubMed PMID:
12949633.
22: Oe T, Tian Y, O'Dwyer PJ, Roberts DW, Bailey CJ, Blair IA.
Determination of the platinum drug cis-amminedichloro(2-methylpyridine)platinum(II)
in human urine by liquid chromatography-tandem mass spectrometry. J
Chromatogr B Analyt Technol Biomed Life Sci. 2003 Jul 25;792(2):217-27.
PubMed PMID: 12860029.
23: Twelves C, Reck M, Anthoney A, Gatzemeier U, Kaye S. A phase I study
of ZD0473 combined with paclitaxel for the treatment of solid
malignancies. Cancer Chemother Pharmacol. 2003 Oct;52(4):277-81. Epub
2003 Jun 25. PubMed PMID: 12827291.
24: Kanzawa F, Akiyama Y, Saijo N, Nishio K. In vitro effects of
combinations of cis-amminedichloro (2-methylpyridine) platinum (II)
(ZD0473) with other novel anticancer drugs on the growth of SBC-3, a
human small cell lung cancer cell line. Lung Cancer. 2003
Jun;40(3):325-32. PubMed PMID: 12781432.
25: Munk VP, Diakos CI, Ellis LT, Fenton RR, Messerle BA, Hambley TW.
Investigations into the interactions between DNA and conformationally
constrained pyridylamineplatinum(II) analogues of AMD473. Inorg Chem.
2003 Jun 2;42(11):3582-90. PubMed PMID: 12767196.
26: Medina-Gundrum L, Cerna C, Gomez LR, Yochmowitz M, Weitman S. AMD473
(ZD0473) exhibits marked in vitro anticancer activity in human tumor
specimens taken directly from patients. Anticancer Drugs. 2003
Apr;14(4):275-80. PubMed PMID: 12679731.
27: Beale P, Judson I, O'Donnell A, Trigo J, Rees C, Raynaud F, Turner
A, Simmons L, Etterley L. A Phase I clinical and pharmacological study
of cis-diamminedichloro(2-methylpyridine) platinum II (AMD473). Br J
Cancer. 2003 Apr 7;88(7):1128-34. PubMed PMID: 12671715; PubMed Central
PMCID: PMC2376375.
28: Smith CJ, Wilson ID, Abou-Shakra F, Payne R, Parry TC, Sinclair P,
Roberts DW. A comparison of the quantitative methods for the analysis of
the platinum-containing anticancer drug [cis-[amminedichloro(2-methylpyridine)]platinum(II)]
(ZD0473) by HPLC coupled to either a triple quadrupole mass spectrometer
or an inductively coupled plasma mass spectrometer. Anal Chem. 2003 Mar
15;75(6):1463-9. PubMed PMID: 12659211.
29: Gelmon KA, Vandenberg TA, Panasci L, Norris B, Crump M, Douglas L,
Walsh W, Matthews SJ, Seymour LK. A phase II study of ZD0473 given as a
short infusion every 3 weeks to patients with advanced or metastatic
breast cancer: a National Cancer Institute of Canada Clinical Trials
Group trial, IND 129. Ann Oncol. 2003 Apr;14(4):543-8. PubMed PMID:
12649098.
30: Giaccone G, O'Brien ME, Byrne MJ, Bard M, Kaukel E, Smit B. Phase II
trial of ZD0473 as second-line therapy in mesothelioma. Eur J Cancer.
2002 Dec;38 Suppl 8:S19-24. PubMed PMID: 12647701.
31: Douillard JY, Schiller J. ZD0473 combined with other
chemotherapeutic agents for the treatment of solid malignancies. Eur J
Cancer. 2002 Dec;38 Suppl 8:S25-31. PubMed PMID: 12645909.
32: Treat J, Schiller J, Quoix E, Mauer A, Edelman M, Modiano M, Bonomi
P, Ramlau R, Lemarie E. ZD0473 treatment in lung cancer: an overview of
the clinical trial results. Eur J Cancer. 2002 Dec;38 Suppl 8:S13-8.
PubMed PMID: 12645908.
33: Gore ME, Atkinson RJ, Thomas H, Cure H, Rischin D, Beale P, Bougnoux
P, Dirix L, Smit WM. Results of ZD0473 in platinum-pretreated ovarian
cancer: analysis according to platinum free interval. Eur J Cancer. 2002
Dec;38 Suppl 8:S7-12. PubMed PMID: 12645907.
34: Murakami H, Tamura T, Yamada Y, Yamamoto N, Ueda Y, Shimoyama T,
Saijo N. ZD0473 pharmacokinetics in Japanese patients: a Phase I
dose-escalation study. Eur J Cancer. 2002 Dec;38 Suppl 8:S1-5. PubMed
PMID: 12645906.
35: Lansiaux A, Bailly C. [Perspectives on the oncologist
pharmacopoeia]. Bull Cancer. 2003 Jan;90(1):25-30. French. PubMed PMID:
12609801.
36: Gore ME, Atkinson RJ, Thomas H, Cure H, Rischin D, Beale P, Bougnoux
P, Dirix L, Smit WM. A phase II trial of ZD0473 in platinum-pretreated
ovarian cancer. Eur J Cancer. 2002 Dec;38(18):2416-20. PubMed PMID:
12460786.
37: Sharp SY, O'Neill CF, Rogers P, Boxall FE, Kelland LR. Retention of
activity by the new generation platinum agent AMD0473 in four human
tumour cell lines possessing acquired resistance to oxaliplatin. Eur J
Cancer. 2002 Nov;38(17):2309-15. PubMed PMID: 12441268.
38: Lin X, Okuda T, Holzer A, Howell SB. The copper transporter CTR1
regulates cisplatin uptake in Saccharomyces cerevisiae. Mol Pharmacol.
2002 Nov;62(5):1154-9. Erratum in: Mol Pharmacol. 2003 Apr;63(4):957.
PubMed PMID: 12391279.
39: Kawamura-Akiyama Y, Kusaba H, Kanzawa F, Tamura T, Saijo N, Nishio
K. Non-cross resistance of ZD0473 in acquired cisplatin-resistant lung
cancer cell lines. Lung Cancer. 2002 Oct;38(1):43-50. PubMed PMID:
12367792.
40: Rogers P, Boxall FE, Allott CP, Stephens TC, Kelland LR.
Sequence-dependent synergism between the new generation platinum agent
ZD0473 and paclitaxel in cisplatin-sensitive and -resistant human
ovarian carcinoma cell lines. Eur J Cancer. 2002 Aug;38(12):1653-60.
PubMed PMID: 12142057.
41: Daud A, Munster P, Munster P, Spriggs DR. New drugs in gynecologic
cancer. Curr Treat Options Oncol. 2001 Apr;2(2):119-28. Review. PubMed
PMID: 12057130.
42: Oe T, Tian Y, O'Dwyer PJ, Roberts DW, Malone MD, Bailey CJ, Blair
IA. A validated liquid chromatography/tandem mass spectrometry assay for
cis-amminedichloro(2-methylpyridine)platinum(II) in human plasma
ultrafiltrate. Anal Chem. 2002 Feb 1;74(3):591-9. PubMed PMID: 11838680.
43: Hay MP. ZD-0473 AstraZeneca. Curr Opin Investig Drugs. 2000
Oct;1(2):263-6. PubMed PMID: 11249584.
44: Holford J, Beale PJ, Boxall FE, Sharp SY, Kelland LR. Mechanisms of
drug resistance to the platinum complex ZD0473 in ovarian cancer cell
lines. Eur J Cancer. 2000 Oct;36(15):1984-90. PubMed PMID: 11000581.
45: Judson I, Kelland LR. New developments and approaches in the
platinum arena. Drugs. 2000;59 Suppl 4:29-36; discussion 37-8. Review.
PubMed PMID: 10864228.
46: Kelland LR, Sharp SY, O'Neill CF, Raynaud FI, Beale PJ, Judson IR.
Mini-review: discovery and development of platinum complexes designed to
circumvent cisplatin resistance. J Inorg Biochem. 1999
Oct;77(1-2):111-5. Review. PubMed PMID: 10626362.
47: 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.
48: 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.
49: Raynaud FI, Boxall FE, Goddard PM, Valenti M, Jones M, Murrer BA,
Abrams M, Kelland LR. cis-Amminedichloro(2-methylpyridine) platinum(II)
(AMD473), a novel sterically hindered platinum complex: in vivo
activity, toxicology, and pharmacokinetics in mice. Clin Cancer Res.
1997 Nov;3(11):2063-74. PubMed PMID: 9815598.
50: Pestell KE, Medlow CJ, Titley JC, Kelland LR, Walton MI.
Characterisation of the p53 status, BCL-2 expression and radiation and
platinum drug sensitivity of a panel of human ovarian cancer cell lines.
Int J Cancer. 1998 Sep 11;77(6):913-8. PubMed PMID: 9714063.
51: 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.
52: Holford J, Raynaud F, Murrer BA, Grimaldi K, Hartley JA, Abrams M,
Kelland LR. Chemical, biochemical and pharmacological activity of the
novel sterically hindered platinum co-ordination complex, cis-[amminedichloro(2-methylpyridine)]
platinum(II) (AMD473). Anticancer Drug Des. 1998 Jan;13(1):1-18. PubMed
PMID: 9474239.
53: Holford J, Sharp SY, Murrer BA, Abrams M, Kelland LR. In vitro
circumvention of cisplatin resistance by the novel sterically hindered
platinum complex AMD473. Br J Cancer. 1998;77(3):366-73. PubMed PMID:
9472630; PubMed Central PMCID: PMC2151285.
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