The experimental antitumor agents Phortress and doxorubicin are equiactive against human-derived breast carcinoma xenograft models

Breast Cancer Research and Treatment
Iduna FichtnerTracey D Bradshaw

Abstract

Phortress (the dihydrochloride salt of the lysylamide prodrug of 2-(4-amino-3-methylphenyl)-5-fluoro-benzothiazole (5F 203)) is an experimental antitumor agent with potent and selective activity against human-derived carcinomas of breast, ovarian and renal origin. UK clinical trials of Phortress are scheduled to begin in 2004. The mechanism of action of Phortress is distinct from all classes of chemotherapeutic agents currently in the clinic, and involves metabolic activation by cytochrome P450 (CYP) 1A1 to electrophilic species, which generate DNA adducts in sensitive tumors only. In the present study, the antitumor efficacy of Phortress has been compared with that of doxorubicin (Dox) in nine human-derived mammary carcinoma xenograft models, cultivated subcutaneously in the flanks of nude mice. In addition, cyp1a1 mRNA expression was measured in tumors of control and treated animals. Phortress compared favorably with Dox: significant activity, independent of estrogen receptor (ER) status, was established in 7/9 xenografts; in one xenograft model, Phortress elicited superior antitumor activity; no model demonstrated complete resistance to Phortress. In accordance with this observation, all xenografts available for examination ...Continue Reading

References

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Citations

Aug 4, 2007·Breast Cancer Research and Treatment·Tracey D BradshawMalcolm F G Stevens
Oct 4, 2012·Journal of Enzyme Inhibition and Medicinal Chemistry·Prabodh Chander SharmaDharam Pal Pathak
Sep 10, 2014·Journal of Enzyme Inhibition and Medicinal Chemistry·Leyla YurttaşSeref Demirayak
Aug 16, 2006·Bioorganic & Medicinal Chemistry Letters·Cedric J LionAndrew D Westwell
Jun 25, 2014·Tumour Biology : the Journal of the International Society for Oncodevelopmental Biology and Medicine·Ioannis SpyrouVasilis P Androutsopoulos
Feb 9, 2013·Journal of Enzyme Inhibition and Medicinal Chemistry·Leyla YurttaşŞafak Ulusoylar-Yıldırım
Apr 8, 2015·Organic & Biomolecular Chemistry·Patrique NunesAntónio Paulo
Nov 19, 2015·PloS One·Pantelis StavrinouPeriklis Pappas
Apr 12, 2013·Molecular Cancer Research : MCR·Mariangellys Rodriguez, David A Potter
Aug 31, 2021·Journal of Enzyme Inhibition and Medicinal Chemistry·Livio RacanéSilvana Raić-Malić

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