Ocera Therapeutics fka OCRX

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Constrained Peptides and Macrocyclics Drug Discovery

Novel Peptide Therapeutics

April 16-17, 2013
Macrocyclic-Based Drug Candidates

1:25 Chairperson’s Remarks

Julio Camarero, Ph.D., Associate Professor, Pharmacology and Chemistry, University of Southern California

1:30 SOM230: A New Therapeutic Modality for Cushing’s Disease

Ian Lewis, Ph.D., Research Chemist, Global Discovery Chemistry, Novartis

SOM230 has recently shown promise as the first effective pituitary directed medical treatment for Cushing’s disease. Indeed, the multiple high affinity binding of SOM230 to somatostatin receptor subtypes enables much more effective inhibition of ACTH release in vitro and in vivo. Recent clinical studies involving treatment of Cushing’s disease with SOM230 have demonstrated that SOM230 produced a decrease in urinary free cortisol (UFC) levels in 76% of patients during 15 days, with direct effects on ACTH release, establishing a new therapeutic modality for Cushing’s disease.

2:00 Discovery of Stereochemically Complex Macrocyclic Hsp90 Inhibitors

Christoph Zapf, Ph.D., Principal Scientist, Worldwide Medicinal Chemistry, Pfizer

We wish to disclose the design and synthesis of a series of stereochemically complex, rule-of-five compliant small molecule macrocycles that were fine-tuned to be metabolically stable and devoid of hERG activity. The compounds showed impressive biomarker activity 24 hours post dosing in different cell lines. When studied in a lung cancer xenograft model, the macrocycles demonstrated prolonged exposure in tumors and significant tumor size reduction.

2:30 Discovery of TZP-102, a Macrocycle-Based Oral Ghrelin Receptor Agonist and GI Prokinetic Agent for the Treatment of Diabetic Gastroparesis

Helmut Thomas, Ph.D., Senior Vice President, Research and Preclinical Development, Tranzyme Pharma

3:00 Sponsored Presentation (Opportunity Available)

3:15 Refreshment Break in the Exhibit Hall with Poster Viewing

4:00 Macrocycles for Drug Discovery - Identification of Small Molecule Synthetic Macrocycle Antagonists of Human IL17A

Nick Terrett, Ph.D., CSO, Ensemble Therapeutics Corp.

Ensemble Therapeutics has developed a DNA-programmed chemistry platform for the rapid synthesis and screening of macrocycles (EnsemblinsTM). Using this platform, small molecule macrocyclic compounds have been discovered that are nanomolar inhibitors of the interaction of the IL17A cytokine with its receptor. These compounds are anti-inflammatory in IL17-dependent animal inflammatory models and optimized for oral bioavailability
http://www.drugdiscoverychemistry.com/Constrained-Peptide-Therapeutics/