8:00 am Morning Networking Coffee
8:50 am Chair’s Opening Remarks
Addressing Hurdles in Pre-clinical Development to Fast-Track IND-filing & Overcome Bottlenecks in the Approach to the Clinic
9:00 am Discovery & Optimization of Novel GPCR Biologics for CV/Renal Disease
Synopsis
- Development and optimization of the GEODe platform to overcome the structurally dynamic nature and biochemical instability of GPCRs
- Discovery of a GPCR agonist biologic clinically developed in a CV/renal disease indication
- Optimizing the potency, PK, and biophysical characteristics of lead biologic compounds
9:30 am Discovery of Clinical Candidate AZD5462, an Allosteric Oral Small Molecule Agonist for the Treatment of Heart Failure
Synopsis
- Reviewing the optimization of small molecule agonists of the Relaxin Family Peptide Receptor (RXFP1) resulting in discovery of AZD5462
- Exploring mechanism of action and signaling in vitro and in vivo
- Demonstrating the efficacy of AZD5462 in non-human primates
10:00 am Discovering the Next-Generation of GPCR-targeted Therapeutics to Address Metabolic Diseases with Unmet Patient Needs
Synopsis
- Leveraging a novel drug modality and proprietary discovery platform to unlock peptide & protein GPCRs
- Advancing a pipeline of differentiated therapeutics for cardiometabolic and immunological diseases
- Capturing the untapped potential of Class A and Class B GPCRs with novel therapeutic approaches and drug-conjugates
10:30 am Session Reserved for Wuxi Biortus Biosciences
11:00 am Morning Networking Break & Scientific Poster Session
Developing Highly Selective Drug Candidates to Reduce Off-Target Effects & Improve Candidate Safety
12:00 pm Focused & Thoughtful Discovery, a Comprehensive Approach to Anti-GPCR Biologics Discovery & Engineering
Synopsis
- A comparison of antibody discovery methods, technologies and reagents for anti-GPCR biologics discovery.
- Development and engineering of anti-GPCR variable regions to achieve optimal biological activity
- Molecular considerations for anti-GPCR containing multispecifics
12:30 pm Discovery & Validation of a Highly Selective Agonistic VHH
Synopsis
- De novo discovery of potent, full agonistic and highly specific agonistic VHHs
- VHH binding mode as compared to peptide agonists
- Implications for drug discovery
1:00 pm Peptide Agonists to Target GPCRs for Metabolic Disorders to Meet the Growing Patient Need
Synopsis
- Lead optimization of a novel peptide agonist to target Class B GPCRs
- Understanding the functionality of a novel peptide agonist by revealing the mechanisms of action and downstream signaling
- Using structure-based insights to design high affinity and potent drugs
1:30 pm Networking Lunch Break
Advancing Translational Models to Convey the Complex Microenvironments of Native GPCRs & Improve Physiological Relevance
2:30 pm Understanding Receptors for Metabolites Using Novel Transgenic Models
Synopsis
- The development and use of transgenic mouse models that express epitope-tagged and otherwise-modified GPCRs for analysis of function
- The use of phospho-site specific antisera that provide tissue level biomarkers of receptor activation
- How such mouse models can be used in a disease-relevant manner
3:00 pm Discovering & Bringing GPCR-Targeting Drugs to Patients to Tackle Cancer
Synopsis
- Identification of new GPCR targets in I/O field
- POC studies in animal models
- Establishing emerging approaches to tackle identified GPCRs
- Biomarkers to support Drug Discovery and Clinical trials Efforts
3:30 pm Using Translational Techniques to Advance Next Generation 5-HT2A Agonists into the Clinic to Treat Depression
Synopsis
- Developing an optimized small molecule agonist of 5-HT2A receptors
- Utilization of biomarkers with high-translational value to guide dose selection for evaluating the safety and efficacy of small molecules targeting the CNS
- Reviewing 5-HT2A receptor binding in vitro, in vivo and the markers of target engagement from the bench to Phase I clinical trials