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Glucokinase activators.

Kevin J Filipski1, Kentaro Futatsugi, Jeffrey A Pfefferkorn

  • 1Cardiovascular, Metabolic & Endocrine Disease Research, Pfizer Worldwide Research & Development, Cambridge, MA 02139, USA.

Pharmaceutical Patent Analyst
|November 19, 2013
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Summary
This summary is machine-generated.

Researchers are developing small-molecule activators for the human glucokinase enzyme as a potential treatment for Type II diabetes. Recent patent filings suggest the field is maturing, with programs moving towards clinical trials.

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Area of Science:

  • Medicinal Chemistry
  • Enzyme Activators
  • Drug Discovery

Background:

  • Glucokinase (GCK) is a key regulator of glucose homeostasis.
  • Small-molecule activators of GCK are being investigated for Type II diabetes mellitus.
  • Novel chemotypes with modified properties are emerging.

Purpose of the Study:

  • To review recent advancements in small-molecule glucokinase activators.
  • To analyze patent literature for trends in GCK activator development.
  • To assess the progress towards a first-in-class GCK activator drug.

Main Methods:

  • Literature review of scientific publications and patents.
  • Analysis of patent filings from December 2009 to November 2011.
  • Translation and examination of foreign patent filings.
  • Characterization of glucokinase activator properties, including tissue selectivity and enzyme kinetics (S0.5, Vmax).

Main Results:

  • Several novel chemotypes of glucokinase activators have been reported.
  • Modifications aim to enhance tissue selectivity and enzyme function parameters.
  • A decrease in patent filings for small-molecule GCK activators was observed.
  • The observed trend may indicate field maturity and progression to clinical stages.

Conclusions:

  • Significant efforts continue towards discovering a GCK activator for Type II diabetes.
  • The field of small-molecule GCK activators is evolving, with new structural motifs and functional modulations.
  • Reduced patent activity likely signifies a transition of programs into clinical development.