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


  • 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


  • 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


  • 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

  • Ilean Chai Associate Director - Business Development, Wuxi Biortus Biosciences Co.Ltd.

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


  • 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

  • Andreas Busch Senior Scientist - Protein Science, Confo Therapeutics


  • 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


  • 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


  • 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


  • 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

  • Zoe Hughes Head of Medical Affairs, Gilgamesh Pharmaceutical


  • 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

4:00 pm Chairs Closing Remarks & End of 3rd Annual GPCRs-Targeted Drug Discovery Summit 2024