GPR40 Agonists

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Oral anti-diabetic drug with robust and durable control of hyperglycemia over the long-term.

GPR40 is a free fatty acid receptor that potentiates glucose-induced insulin secretion through changes in intracellular Ca2+ levels/signaling. In addition, it is known to reduce β cell stress and apoptosis. CNX-011-67 is our lead GPR40 agonist showing potential to be the best-in-class anti-diabetic impacting β cell health/function resulting in acute and sustained glycemic control. CNX-011-67 efficacy validated in cellular and animal models of disease shows:

  • Enhancement of phasic insulin secretion in response to stimulatory glucose concentration without hypoglycemia.
  • Improvement in both fasting and post-prandial glycemic levels and significant lowering of HbA1c.
  • Increase in insulin synthesis and content.
  • Reduction in cellular stress and apoptosis.
  • Improvement in insulin action in the periphery, leading to reduction in plasma TG and FFA levels.
  • Significant delay in progression to diabetes.

CNX-011-67 addresses a crucial need in the treatment of T2D patients by providing sustainable benefits to beta cell health and function and is likely to be an improvement over existing insulin secretagogues due to this mechanism, while also providing comparable acute glucose control.

CNX-011-67 is being progressed to enter PI clinical studies and is likely to be one of the early candidates in this class of drugs, while also promising a best-in-class profile.

Key Result:

CNX-011-67enhances glucose stimulated insulin secretion in nSTZ rats

CNX-011-67 improves islet area and insulin content in ZDF rats