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The endopeptidase inhibitor, candoxatril, and its therapeutic potential in the treatment of chronic cardiac failure in man.

Expert opinion on investigational drugs

McDowell G, Nicholls DP.
PMID: 15992061
Expert Opin Investig Drugs. 1999 Jan;8(1):79-84. doi: 10.1517/13543784.8.1.79.

Candoxatril (UK-79300) is the orally-active prodrug of candoxatrilat (UK-73967), the active enantiomer of (+/-)candoxatrilat (UK-69578), a potent neutral endopeptidase (NEP) inhibitor. This article describes the rationale behind the use of such a drug in the treatment of chronic heart...

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McDowell G, Nicholls DP. The endopeptidase inhibitor, candoxatril, and its therapeutic potential in the treatment of chronic cardiac failure in man. Expert Opin Investig Drugs. 1999;8(1):79-84doi: 10.1517/13543784.8.1.79.
McDowell, G., & Nicholls, D. P. (1999). The endopeptidase inhibitor, candoxatril, and its therapeutic potential in the treatment of chronic cardiac failure in man. Expert opinion on investigational drugs, 8(1), 79-84. https://doi.org/10.1517/13543784.8.1.79
McDowell, G, and Nicholls, D P. "The endopeptidase inhibitor, candoxatril, and its therapeutic potential in the treatment of chronic cardiac failure in man." Expert opinion on investigational drugs vol. 8,1 (1999): 79-84. doi: https://doi.org/10.1517/13543784.8.1.79
McDowell G, Nicholls DP. The endopeptidase inhibitor, candoxatril, and its therapeutic potential in the treatment of chronic cardiac failure in man. Expert Opin Investig Drugs. 1999 Jan;8(1):79-84. doi: 10.1517/13543784.8.1.79. PMID: 15992061.
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Effect of Inhibition of Angiotensin-Converting Enzyme and/or Neutral Endopeptidase on Neuropathy in High-Fat-Fed C57Bl/6J Mice.

Journal of obesity

Coppey L, Lu B, Gerard C, Yorek MA.
PMID: 23056927
J Obes. 2012;2012:326806. doi: 10.1155/2012/326806. Epub 2012 Sep 29.

We have demonstrated that treating diet-induced obese (DIO) mice with the vasopeptidase inhibitor ilepatril improved neural function. Vasopeptidase inhibitors block angiotensin-converting enzyme (ACE) and neutral endopeptidase (NEP) activity. We propose that increased activity of ACE and NEP contributes to...

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Coppey L, Lu B, Gerard C, et al. Effect of Inhibition of Angiotensin-Converting Enzyme and/or Neutral Endopeptidase on Neuropathy in High-Fat-Fed C57Bl/6J Mice. J Obes. 2012;2012:326806doi: 10.1155/2012/326806.
Coppey, L., Lu, B., Gerard, C., & Yorek, M. A. (2012). Effect of Inhibition of Angiotensin-Converting Enzyme and/or Neutral Endopeptidase on Neuropathy in High-Fat-Fed C57Bl/6J Mice. Journal of obesity, 2012326806. https://doi.org/10.1155/2012/326806
Coppey, Lawrence, et al. "Effect of Inhibition of Angiotensin-Converting Enzyme and/or Neutral Endopeptidase on Neuropathy in High-Fat-Fed C57Bl/6J Mice." Journal of obesity vol. 2012 (2012): 326806. doi: https://doi.org/10.1155/2012/326806
Coppey L, Lu B, Gerard C, Yorek MA. Effect of Inhibition of Angiotensin-Converting Enzyme and/or Neutral Endopeptidase on Neuropathy in High-Fat-Fed C57Bl/6J Mice. J Obes. 2012;2012:326806. doi: 10.1155/2012/326806. Epub 2012 Sep 29. PMID: 23056927; PMCID: PMC3465928.
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Me-DuPHOS-Rh-Catalyzed Asymmetric Synthesis of the Pivotal Glutarate Intermediate for Candoxatril.

The Journal of organic chemistry

Burk MJ, Bienewald F, Challenger S, Derrick A, Ramsden JA.
PMID: 11674433
J Org Chem. 1999 Apr 30;64(9):3290-3298. doi: 10.1021/jo990145s.

A greatly improved process has been developed for synthesis of the glutarate derivative 2, a key intermediate required for Pfizer's drug candoxatril. The cationic (R,R)-Me-DuPHOS-Rh catalyst was found to allow highly efficient and enantioselective hydrogenation of a unique carboxylate...

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Burk MJ, Bienewald F, Challenger S, et al. Me-DuPHOS-Rh-Catalyzed Asymmetric Synthesis of the Pivotal Glutarate Intermediate for Candoxatril. J Org Chem. 1999;64(9):3290-3298doi: 10.1021/jo990145s.
Burk, M. J., Bienewald, F., Challenger, S., Derrick, A., & Ramsden, J. A. (1999). Me-DuPHOS-Rh-Catalyzed Asymmetric Synthesis of the Pivotal Glutarate Intermediate for Candoxatril. The Journal of organic chemistry, 64(9), 3290-3298. https://doi.org/10.1021/jo990145s
Burk, Mark J., et al. "Me-DuPHOS-Rh-Catalyzed Asymmetric Synthesis of the Pivotal Glutarate Intermediate for Candoxatril." The Journal of organic chemistry vol. 64,9 (1999): 3290-3298. doi: https://doi.org/10.1021/jo990145s
Burk MJ, Bienewald F, Challenger S, Derrick A, Ramsden JA. Me-DuPHOS-Rh-Catalyzed Asymmetric Synthesis of the Pivotal Glutarate Intermediate for Candoxatril. J Org Chem. 1999 Apr 30;64(9):3290-3298. doi: 10.1021/jo990145s. PMID: 11674433.
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Neutral endopeptidase inhibitor suppresses the early phase of atrial electrical remodeling in a canine rapid atrial pacing model.

Indian pacing and electrophysiology journal

Imaki R, Niwano S, Niwano H, Satoh D, Yoshida T, Masaki Y, Izumi T.
PMID: 18379655
Indian Pacing Electrophysiol J. 2008 Apr 01;8(2):102-13.

INTRODUCTION: We examined the acute effects of neutral endopeptidase inhibitor on the hemodynamics and electrical properties of dogs subjected to rapid atrial pacing.METHODS: Ten beagle dogs were used and divided into two groups with and without candoxatril, a neutral...

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Imaki R, Niwano S, Niwano H, et al. Neutral endopeptidase inhibitor suppresses the early phase of atrial electrical remodeling in a canine rapid atrial pacing model. Indian Pacing Electrophysiol J. 2008;8(2):102-13
Imaki, R., Niwano, S., Niwano, H., Satoh, D., Yoshida, T., Masaki, Y., & Izumi, T. (2008). Neutral endopeptidase inhibitor suppresses the early phase of atrial electrical remodeling in a canine rapid atrial pacing model. Indian pacing and electrophysiology journal, 8(2), 102-13.
Imaki, Ryuta, et al. "Neutral endopeptidase inhibitor suppresses the early phase of atrial electrical remodeling in a canine rapid atrial pacing model." Indian pacing and electrophysiology journal vol. 8,2 (2008): 102-13.
Imaki R, Niwano S, Niwano H, Satoh D, Yoshida T, Masaki Y, Izumi T. Neutral endopeptidase inhibitor suppresses the early phase of atrial electrical remodeling in a canine rapid atrial pacing model. Indian Pacing Electrophysiol J. 2008 Apr 01;8(2):102-13. PMID: 18379655; PMCID: PMC2267894.
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Effect of Treatment of Sprague Dawley Rats with AVE7688, Enalapril, or Candoxatril on Diet-Induced Obesity.

Journal of obesity

Davidson EP, Coppey LJ, Dake B, Yorek MA.
PMID: 20847891
J Obes. 2011;2011. doi: 10.1155/2011/686952. Epub 2010 Aug 16.

The objective of this study was to determine the effect of AVE7688, a drug that inhibits both angiotensin converting enzyme (ACE) and neutral endopeptidase (NEP) activity, on neural and vascular defects caused by diet induced obesity (DIO). Rats at...

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Davidson EP, Coppey LJ, Dake B, et al. Effect of Treatment of Sprague Dawley Rats with AVE7688, Enalapril, or Candoxatril on Diet-Induced Obesity. J Obes. 2010;2011doi: 10.1155/2011/686952.
Davidson, E. P., Coppey, L. J., Dake, B., & Yorek, M. A. (2011). Effect of Treatment of Sprague Dawley Rats with AVE7688, Enalapril, or Candoxatril on Diet-Induced Obesity. Journal of obesity, 2011. https://doi.org/10.1155/2011/686952
Davidson, Eric P, et al. "Effect of Treatment of Sprague Dawley Rats with AVE7688, Enalapril, or Candoxatril on Diet-Induced Obesity." Journal of obesity vol. 2011 (2011). doi: https://doi.org/10.1155/2011/686952
Davidson EP, Coppey LJ, Dake B, Yorek MA. Effect of Treatment of Sprague Dawley Rats with AVE7688, Enalapril, or Candoxatril on Diet-Induced Obesity. J Obes. 2011;2011. doi: 10.1155/2011/686952. Epub 2010 Aug 16. PMID: 20847891; PMCID: PMC2933895.
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Effect of Inhibition or Deletion of Neutral Endopeptidase on Neuropathic Endpoints in High Fat Fed/Low Dose Streptozotocin-Treated Mice.

Journal of neuropathology and experimental neurology

Yorek MS, Obrosov A, Lu B, Gerard C, Kardon RH, Yorek MA.
PMID: 27634964
J Neuropathol Exp Neurol. 2016 Nov 01;75(11):1072-1080. doi: 10.1093/jnen/nlw083.

Previously we demonstrated that a vasopeptidase inhibitor of angiotensin converting enzyme and neutral endopeptidase (NEP), a protease that degrades vaso- and neuro-active peptides, improves neural function in diabetic rodent models. The purpose of this study was to determine whether...

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Yorek MS, Obrosov A, Lu B, et al. Effect of Inhibition or Deletion of Neutral Endopeptidase on Neuropathic Endpoints in High Fat Fed/Low Dose Streptozotocin-Treated Mice. J Neuropathol Exp Neurol. 2016;75(11):1072-1080doi: 10.1093/jnen/nlw083.
Yorek, M. S., Obrosov, A., Lu, B., Gerard, C., Kardon, R. H., & Yorek, M. A. (2016). Effect of Inhibition or Deletion of Neutral Endopeptidase on Neuropathic Endpoints in High Fat Fed/Low Dose Streptozotocin-Treated Mice. Journal of neuropathology and experimental neurology, 75(11), 1072-1080. https://doi.org/10.1093/jnen/nlw083
Yorek, Matthew S, et al. "Effect of Inhibition or Deletion of Neutral Endopeptidase on Neuropathic Endpoints in High Fat Fed/Low Dose Streptozotocin-Treated Mice." Journal of neuropathology and experimental neurology vol. 75,11 (2016): 1072-1080. doi: https://doi.org/10.1093/jnen/nlw083
Yorek MS, Obrosov A, Lu B, Gerard C, Kardon RH, Yorek MA. Effect of Inhibition or Deletion of Neutral Endopeptidase on Neuropathic Endpoints in High Fat Fed/Low Dose Streptozotocin-Treated Mice. J Neuropathol Exp Neurol. 2016 Nov 01;75(11):1072-1080. doi: 10.1093/jnen/nlw083. PMID: 27634964; PMCID: PMC7714044.
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Showing 1 to 6 of 6 entries