SAN DIEGO, CA, USA I November 13, 2018 I Arena Pharmaceuticals, Inc. (Nasdaq: ARNA) presented preclinical data for its recently announced investigational compound, APD418, a first-in-class calcium-independent myofilament derepressor (CMD), ß3 adrenergic receptor (AdrR) selective antagonist, at the American Heart Association Scientific Sessions 2018. APD418 is being developed to improve cardiac contractility with minimal effect on heart rate and blood pressure for decompensated heart failure (DHF).  

“A significant unmet medical need exists in the treatment of decompensated heart failure, the most common hospital diagnosis for patients over the age of 65, which continues to increase with the aging population,” said Preston Klassen, MD, MHS, Executive Vice President, Research and Development and Chief Medical Officer of Arena.  “We are pleased to present new preclinical data demonstrating the potential of our first-in-class compound, APD418, to improve therapeutic options by enhancing cardiac contractility while avoiding the serious adverse events commonly associated with the current standard of care.”

Presentation Details
Session Title:
New Insights into Pharmacological Therapy of CHF
Title: APD418, A Selective Beta3-Adrenergic Receptor Antagonist Enhances Cardiac Positive Inotropic and Lusitropic Responses to Dobutamine in Conscious, Chronically-Instrumented Dogs with Pacing-Induced Heart Failure: Assessment by Pressure-Volume Analysis (Rapid Fire Oral)

Session Title: Kenneth D. Bloch Memorial Lecture
Title: Adverse Functional Significance of Cardiac Beta3-Adrenergic Receptor Activation on Left Ventricular Contractile Performance in Conscious, Chronically-Instrumented Dogs with Pacing-Induced Heart Failure (Oral)

About APD418
APD418 is a first-in-class calcium-independent myofilament derepressor (CMD) for decompensated heart failure (DHF).  APD418 is a ß3 adrenergic receptor (AdrR) selective antagonist designed to improve cardiac contractility with minimal effect on heart rate and blood pressure. Inhibition of ß3 AdrR mediated myofilament repression may provide a unique cardiomyocyte-specific target to enhance cardiac contractile performance while avoiding adverse events associated with current inotrope therapies.  Arena discovered and developed this investigational drug candidate internally. 

APD418 is preclinical, investigational compound that is not approved for any use in any country.

About Arena Pharmaceuticals
Arena Pharmaceuticals is driven to deliver novel, transformational medicines with optimized pharmacology and pharmacokinetics to patients globally. Arena’s proprietary pipeline includes multiple potentially first- or best-in-class assets with broad clinical utility. Ralinepag (APD811) is being evaluated in a Phase 3 program for pulmonary arterial hypertension (PAH).  Etrasimod (APD334), with potential utility in a broad range of immune and inflammatory conditions, is being evaluated with late-stage clinical programs in ulcerative colitis (UC) and Crohn’s disease, as well as progressing programs for primary biliary cholangitis and atopic dermatitis. Arena is also evaluating olorinab (APD371) with a Phase 2 program for gastrointestinal pain. Arena continues to assess other earlier research and development stage drug candidates, including APD418 for decompensated heart failure.

In addition, Arena has several collaborations including with Everest Medicines Limited (ralinepag and etrasimod in Greater China and select Asian countries), Axovant Sciences GmbH (nelotanserin – Phase 2), Boehringer Ingelheim International GmbH (undisclosed target – preclinical), Outpost Medicine, LLC (undisclosed target – preclinical), and Eisai Co., Ltd. and Eisai Inc. (BELVIQ® – marketed product).

SOURCE: Arena Pharmaceuticals