APIE Therapeutics Presented Preclinical Findings Supporting Activation of the Apelin Receptor as a Therapeutic Approach for Systemic Sclerosis

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APT-101 is an orally bioavailable small molecule that selectively and potently targets and activates APJ, thus acting upstream of factors that promote fibrosis, representing a potentially disease-modifying approach.

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GlobeNewswire, Inc.

Retrieved on:

Tuesday, August 2, 2022

Information

Geotags:

CARY, NC, US, BOSTON, MA

Organisation:

APIE THERAPEUTICS

Summary

Key Points:

APT-101 is an orally bioavailable small molecule that selectively and potently targets and activates APJ, thus acting upstream of factors that promote fibrosis, representing a potentially disease-modifying approach.
It is in preclinical development for the treatment of SSc-ILD and idiopathic pulmonary fibrosis (IPF).
Systemic sclerosis, sometimes referred to as systemic scleroderma, is a progressive systemic disease of unknown cause characterized by fibrotic scaring in major organ systems including the skin and kidneys.
Currently there are no disease modifying treatment for these patients, representing a critical unmet medical need for this orphan disorder.

Cary, NC, Aug. 02, 2022 (GLOBE NEWSWIRE) -- APIE Therapeutics, a preclinical pharmaceutical company pioneering novel and proprietary anti-fibrotic drugs that target the apelin receptor (APJ), presented results from in vitro and in vivo studies supporting the potential of APT-101 as a therapeutic for interstitial lung disease (ILD), including those cases associated with systemic sclerosis (SSc-ILD). APT-101 is an orally bioavailable small molecule that selectively and potently targets and activates APJ, thus acting upstream of factors that promote fibrosis, representing a potentially disease-modifying approach. It is in preclinical development for the treatment of SSc-ILD and idiopathic pulmonary fibrosis (IPF).

“ILD is a common complication of systemic sclerosis that is associated with poor patient outcomes; yet no treatments exist that provide disease modification by addressing the underlying disease biology,” explained Esther M. Alegría, Ph.D., founder and CEO of APIE Therapeutics, “As we described at the scleroderma workshop, we have promising evidence that APT-101 works upstream to reduce the severe fibrosis that drives ILD in patients with SSc and IPF. We look forward to working with the FDA to advance this novel experimental treatment into clinical trials.”

In a mouse model, prophylactic treatment with APT-101 for 21 days resulted in a statistically significant reduction in the development of fibrosis and apoptosis compared to placebo as well as to active control, pirfenidone, an approved treatment for pulmonary fibrosis. In mice treated after the onset of fibrosis, APT-101 also provided therapeutic benefit, producing a statistically significant decrease in fibrosis at the two highest doses. In both models, treatment was well tolerated and effect was observed to be dose dependent, providing additional evidence of favorable drug-like properties.

Presentation Details:

Oral Presentation:		Development of a Novel Small Molecule Anti-fibrotic and Anti-inflammatory Apelin Agonist, APT101, for the Treatment of Systemic Sclerosis Interstitial Lung Disease
Authors:		Robert N. Willette, PhD; Scott Runyon, PhD; Ronnie Maitra, PhD; Esther Alegria, PhD
Date/Time:		August 2, 2022 / 8:40 – 10:15 a.m. Eastern Time
Location:		Session 10: New Therapeutic Approaches to SSc

The International Workshop of Scleroderma Research is being held July 30 – August 3, 2022 in the Seaport Hotel, in Boston, MA. A copy of the presentation may be found on the company website following the conclusion of the conference.

About APIE Therapeutics

APIE Therapeutics is a preclinical stage pharmaceutical company pioneering the development of a portfolio of small-molecule therapeutic drugs that target the apelinergic signaling pathway to repair and regenerate, post injury, the vasculature niche, which is associated with the pathophysiology of many chronic fibrotic diseases. APIE Therapeutics licensed a portfolio of over 800 compounds from RTI International, a well-known nonprofit research institute and inventors of commercial drugs such as Taxol®, Camptothecin®, EllaOne® and Esmya®.

The company’s lead candidate, APT-101, is at IND-enabling stage. The company is on track to file an IND application with the U.S. Food and Drug Administration to commence a clinical program for the treatment of patients with systemic sclerosis (SSc), including those who have progressed to interstitial lung disease (SSc-ILD). Systemic sclerosis, sometimes referred to as systemic scleroderma, is a progressive systemic disease of unknown cause characterized by fibrotic scaring in major organ systems including the skin and kidneys. Patients often progress to develop interstitial lung disease (ILD), which is the leading cause of early death for patients with SSc. Currently there are no disease modifying treatment for these patients, representing a critical unmet medical need for this orphan disorder.

APIE Therapeutics
Esther Alegria, Ph.D.
[email protected]