Apelin / APJ

  • Apelin receptor APJ agonist

  • Lead indication: obesity

An exercise mimetic approach for the treatment of obesity


Apelin is a molecule that is secreted in response to exercise. When activated, the apelin pathway recapitulates many benefits of exercise.

We have shown that agonism of the apelin receptor APJ has the potential to double weight loss and fully restore body composition on an incretin background in preclinical models of obesity.

We believe the combination of an APJ agonist and an incretin is a pharmacological parallel to diet and exercise: one mechanism relies largely on reducing energy intake, the other on increasing energy expenditure.

Program
Mechanism of Action
Target dosing
Indication
Status
APJ
APJ agonist
Oral QD
Obesity
Lead Op pointer
Discoverу Lead Op IND-enabling Ph 1 Ph 2 Ph 3
Program
APJ
Mechanism of Action APJ agonist
Route of administration Oral QD
Indication Obesity
Status
Lead Op pointer
Discoverу Lead Op IND-enabling Ph 1 Ph 2 Ph 3

Mechanism of action

Apelin receptor APJ activates both PI3K and AMPK, key regulators of metabolism

process image

Systemic benefits

  • Balance of lean & fat mass

  • Basal metabolic rate

  • Protein synthesis

  • Mitochondrial biogenesis

  • Insulin sensitivity / glucose metabolism

Preclinical results

We have shown that an APJ agonist can increase overall weight loss and improve body composition co-administered with incretins:

  • 2x weight loss vs. incretin alone

  • Restores body composition and function to that of lean controls 

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