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PR-104A

 
National Institutes of Health

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1 relation

Broader (1)

Nitrogen Mustard Compounds

Papers overview

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2015
2015
Pre-clinical activity of PR-104 as monotherapy and in combination with sorafenib in hepatocellular carcinoma
PR-104 is a clinical stage bioreductive prodrug that is converted in vivo to its cognate alcohol, PR-104A. This dinitrobenzamide… Expand
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2013
2013
The Role of Bystander Effects in the Antitumor Activity of the Hypoxia-Activated Prodrug PR-104
Activation of prodrugs in tumors (e.g., by bioreduction in hypoxic zones) has the potential to generate active metabolites that… Expand
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Highly Cited
2012
Highly Cited
2012
Diflavin Oxidoreductases Activate the Bioreductive Prodrug PR-104A under Hypoxia
The clinical agent PR-104 is converted systemically to PR-104A, a nitrogen mustard prodrug designed to target tumor hypoxia… Expand
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Highly Cited
2011
Highly Cited
2011
A phase I trial of PR-104, a pre-prodrug of the bioreductive prodrug PR-104A, given weekly to solid tumour patients
BackgroundThe phosphate ester PR-104 is rapidly converted in vivo to the alcohol PR-104A, a nitrogen mustard prodrug that is… Expand
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Highly Cited
2009
Highly Cited
2009
DNA cross-links in human tumor cells exposed to the prodrug PR-104A: relationships to hypoxia, bioreductive metabolism, and cytotoxicity.
PR-104, currently in clinical trial, is converted systemically to the dinitrobenzamide nitrogen mustard prodrug PR-104A, which is… Expand
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Highly Cited
2009
Highly Cited
2009
Roles of DNA repair and reductase activity in the cytotoxicity of the hypoxia-activated dinitrobenzamide mustard PR-104A
PR-104 is a dinitrobenzamide mustard currently in clinical trial as a hypoxia-activated prodrug. Its major metabolite, PR-104A… Expand
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Highly Cited
2009
Highly Cited
2009
A phase I trial of PR-104, a nitrogen mustard prodrug activated by both hypoxia and aldo-keto reductase 1C3, in patients with solid tumors
PurposePR-104 is a “pre-prodrug” designed to be activated to a dinitrobenzamide nitrogen mustard cytotoxin by nitroreduction in… Expand
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Highly Cited
2007
Highly Cited
2007
Mechanism of Action and Preclinical Antitumor Activity of the Novel Hypoxia-Activated DNA Cross-Linking Agent PR-104
Purpose: Hypoxia is a characteristic of solid tumors and a potentially important therapeutic target. Here, we characterize the… Expand
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Highly Cited
2007
Highly Cited
2007
Identification of human reductases that activate the dinitrobenzamide mustard prodrug PR-104A: a role for NADPH:cytochrome P450 oxidoreductase under hypoxia.
Hypoxia is a common trait found in many solid tumours and thus represents a therapeutic target with considerable potential. PR… Expand
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2007
2007
Oxygen dependence and extravascular transport of hypoxia-activated prodrugs: comparison of the dinitrobenzamide mustard PR-104A and tirapazamine.
PURPOSE To compare oxygen dependence and tissue transport properties of a new hypoxia-activated prodrug, PR-104A, with… Expand
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