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Inhibition of the methionine aminopeptidase 2 enzyme for the treatment of obesity

Authors Joharapurkar A, Dhanesha N, Jain M

Received 1 November 2013

Accepted for publication 9 January 2014

Published 28 February 2014 Volume 2014:7 Pages 73—84

DOI https://doi.org/10.2147/DMSO.S56924

Checked for plagiarism Yes

Review by Single-blind

Peer reviewer comments 4


Amit A Joharapurkar, Nirav A Dhanesha, Mukul R Jain

Department of Pharmacology and Toxicology, Zydus Research Centre, Cadila Healthcare Limited, Ahmedabad, India

Abstract: Worldwide prevalence of obesity has nearly doubled since 1980. Obesity is the result of interactions among the environmental factors, genetic predisposition, and human behavior. Even modest weight reduction in obese patients provides beneficial health outcomes. For effective weight reduction, a drug should either increase energy expenditure or decrease energy intake without causing serious adverse effects. To overcome lack of efficacy and central nervous system related side effects, exploitation of the peripheral mechanism of anti-obesity action is needed. Inhibition of pathological angiogenesis in adipose tissue is one such peripheral mechanism that has attracted the attention of researchers in this area. Although originally developed as anti-cancer agents, methionine aminopeptidase (MetAP2) inhibitors induce significant and sustained weight reduction. Here, we review preclinical and clinical pharmacology of MetAP2 inhibitors. Beloranib is a prototype MetAP2 inhibitor, and currently in advanced clinical trials for the treatment of obesity. Clinical data of beloranib indicate that MetAP2 inhibitors could be a future treatment option for weight reduction without serious adverse effects. Further clinical data from Phase III trials will add to our growing knowledge of MetAP2 inhibitor potential for anti-obesity therapy.

Keywords: angiogenesis, beloranib, body weight, MetAP2, anti-obesity

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