Therapeutic Pipeline

Targeting the Apelinergic signaling pathway to drive improved health outcomes

Therapeutic Drug Development Pipeline

Using the vast library of selective oral small molecules, APIE Therapeutics’ robust development program is targeting several primary indications.

Drug
Primary Indication
Research
Preclinical
IND Enabling
Clinical
APT-101
Idiopathic Pulmonary Fibrosis (IPF)
Kidney Nephrotic Syndrome
Scleroderma
APT-102
Heart Failure
APT-103
Metabolic Syndrome (Liver Steatosis; Glucose Utilization; Weight Loss)
APT-C
Covid19-Endothelium Organ Vascular Damage (prophylactic)
APT-D
Pulmonary Dysplasia (BPD)

The Initial Challenge

Discovering active, potent, and highly selective agonists to the Apelin Receptor (APJ) is challenging because endogenous apelin peptides are non-selective with a short half-life that limits their utility.

APIE Therapeutics Apelin Receptor (APJ) Agonists Discovery Platform

RTI International (RTI), a well-known research organization and investors of commercial drugs such as Taxol®, Camptothecin®, EllaOne®, and Esmya®, with NIH funding support, pioneered the design and discovery of a novel Apelin drug-like agonist scaffold that selectively binds to the Apelin receptor. Modifications were then made to the core scaffold to generate over 800 synthetic analogs spanning several chemotypes with varying potency and selectivity for the Apelin-APJ receptor. Challenge conquered!
We are continually evaluating the therapeutic effects of our lead compounds to create a portfolio of drug development programs that can be moved into clinical trials via investments and/or partnerships.
APIE Therapeutics Apelin Receptor (APJ) Agonists Discovery Platform

IP Portfolio

APIE Therapeutics has a strong IP portfolio of several issued patents with broad supported claims covering many variations on the base scaffold including the lead compound of interest. These patents have long patent life remaining (2037 and beyond) and have been filed extensively internationally. The patent portfolio contains several family members with different structural classes and methods of use filed later to provide additional patent protection and term.

  • US10100059B2

    Granted 10/16/2018

  • US20190322644A1

    Pub. 10/24/2019

  • US20190315693A1

    Pub. 10/17/2019