Apaziquone - CAS 114560-48-4
Catalog number:
114560-48-4
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
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Description:
Apaziquone is an indolequinone bioreductive prodrug and analog of mitomycin C with potential antineoplastic and radiosensitization activities. Apaziquone is converted to active metabolites in hypoxic cells by intracellular reductases, which are present in greater amounts in hypoxic tumor cells. Apaziquone may selectively sensitize hypoxic tumor cells to radiocytotoxicity.
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Synonyms:
EO9; NSC 382459; EOquin; aziridinylquinone; Neoquin; Eoquin; NOR-701.
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Current Developer:
Spectrum Pharmaceuticals, Inc.
1.Phase 2 study of adjuvant intravesical instillations of apaziquone for high risk nonmuscle invasive bladder cancer.
Hendricksen K1, Cornel EB, de Reijke TM, Arentsen HC, Chawla S, Witjes JA. J Urol. 2012 Apr;187(4):1195-9. doi: 10.1016/j.juro.2011.11.101. Epub 2012 Feb 14.
PURPOSE: We studied the safety and efficacy of multiple adjuvant apaziquone instillations in patients with high risk nonmuscle invasive bladder cancer.
2.The orthotopic Fischer/AY-27 rat bladder urothelial cell carcinoma model to test the efficacy of different apaziquone formulations.
Arentsen HC1, Hendricksen K, Hulsbergen-van de Kaa CA, Reddy G, Oosterwijk E, Alfred Witjes J. Urol Oncol. 2012 Jan-Feb;30(1):64-8. doi: 10.1016/j.urolonc.2009.10.002. Epub 2009 Nov 27.
OBJECTIVES: Apaziquone used intravesically showed significant activity in phase I and II marker lesion studies in non-muscle-invasive bladder cancer. The objective of this study was to assess antitumor activity and safety of 3 different formulations of intravesical apaziquone in an orthotopic rat bladder cancer model.
3.EO9 (Apaziquone): from the clinic to the laboratory and back again.
Phillips RM1, Hendriks HR, Peters GJ; EORTC-Pharmacology and Molecular Mechanism Group. Br J Pharmacol. 2013 Jan;168(1):11-8. doi: 10.1111/j.1476-5381.2012.01996.x.
EO9 (Apaziquone) is a bioreductive drug that has a chequered history. It underwent clinical trial but failed to show activity in phase II clinical trials when administered i.v. Poor drug delivery to tumours caused by a combination of rapid pharmacokinetic elimination and poor penetration through avascular tissue were the major factors responsible for EO9's poor efficacy. Based upon an understanding of why EO9 failed, a further clinical trial against patients with superficial transitional cell carcinoma of the bladder was conducted. The rationale for this was that intravesical administration directly into the bladder would circumvent the drug delivery problem, and any drug reaching the blood supply would be rapidly cleared thereby reducing the risk of systemic exposure. EO9 was well tolerated, and clinical activity against marker lesions was recorded in both phase I and II clinical trials. This article charts the pharmacological history of EO9 and discusses the potential implications that 'the EO9 story' has for the development of other loco-regional therapies.
4.Apaziquone as an intravesical therapeutic agent for urothelial non-muscle-invasive bladder cancer.
Yutkin V1, Chin J. Expert Opin Investig Drugs. 2012 Feb;21(2):251-60. doi: 10.1517/13543784.2012.646081. Epub 2011 Dec 21.
INTRODUCTION: Urothelial carcinoma of the bladder is a disease prone to recurrence. A new cytotoxic drug, apaziquone, is an analog of mitomycin C. Given via intravesical instillations it has the ability to specifically target cancer cells.
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CAS 114560-48-4 Apaziquone

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