2. Academic Validation
  3. Discovery of AZD2716: A Novel Secreted Phospholipase A2 (sPLA2) Inhibitor for the Treatment of Coronary Artery Disease

Discovery of AZD2716: A Novel Secreted Phospholipase A2 (sPLA2) Inhibitor for the Treatment of Coronary Artery Disease

  • ACS Med Chem Lett. 2016 Aug 9;7(10):884-889. doi: 10.1021/acsmedchemlett.6b00188.
Fabrizio Giordanetto 1,  Daniel Pettersen 1,  Ingemar Starke 1,  Peter Nordberg 1,  Mikael Dahlström 1,  Laurent Knerr 1,  Nidhal Selmi 1,  Birgitta Rosengren 1,  Lars-Olof Larsson 1,  Jenny Sandmark 1,  Marie Castaldo 1,  Niek Dekker 1,  Ulla Karlsson 1,  Eva Hurt-Camejo 1
Affiliations

Affiliation

  • 1 Cardiovascular and Metabolic Diseases, Innovative Medicines and Early Development Biotech Unit Departments of Medicinal Chemistry, Bioscience, DMPK, Discovery Sciences Departments of Structure & Biophysics, Reagents and Assay Development, and Screening Sciences and Sample Management, Astrazeneca, Mölndal , Pepparedsleden 1, SE-431 83 Mölndal, Sweden.
PMID: 27774123 DOI: 10.1021/acsmedchemlett.6b00188
Abstract

Expedited structure-based optimization of the initial fragment hit 1 led to the design of (R)-7 (AZD2716) a novel, potent secreted Phospholipase A2 (sPLA2) inhibitor with excellent preclinical pharmacokinetic properties across species, clear in vivo efficacy, and minimized safety risk. Based on accumulated profiling data, (R)-7 was selected as a clinical candidate for the treatment of coronary artery disease.

Keywords

Secreted phospholipase A2; atherosclerosis; coronary artery disease; fragment screening; fragment-based drug discovery; inhibitor; sPLA2.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-120078
    sPLA2 Inhibitor