CONFERENCE DAY ONE
All times in EDT
7:30 am Registration Opens
8:45 am Chair’s Opening Remarks
9:00 am Panel Discussion: An Overview of the Hippo Pathway Drug Development Landscape
Synopsis
- What indications are showing most promise for therapeutic intervention on the Hippo pathway?
- Will targeted approaches on TEAD isoforms be the key to navigating risk of toxicity from pan-TEADs?
- How do we convince investors Hippo pathway treatments are worth their time when some consider the pathway ‘unvalidated’?
- What are the advantages/risks in targeting YAP/TAZ and TEAD interactions?
Mechanistic Insights into TEAD Palmitoylation to Deepen Functional Understanding of Inhibition
9:45 am Therapeutic Targeting of TEAD Transcription Factors in Cancer
Synopsis
- Understanding how YAP/TAZ-TEAD complex is activated in human cancer
- Demonstrating how TEAD hydrophobic pocket is druggable by small molecules
- Showcasing work on three covalent inhibitors targeting TEAD
10:15 am IAG933, a selective YAP1/TAZ-panTEAD PPI inhibitor
Synopsis
- The development and characterization of a direct pan-TEAD PPI inhibitor, IAG933
- Preclinical data supporting efficacy with IAG933
- Discovery of promising targeted therapy combinations with IAG933
10:45 am Morning Break & Speed Networking
11:45 am Leveraging NMR Fragment Screening Method to Identify Starting Points for Optimization & Disruption of the YAP/TAZ-TEAD Interaction to Develop Structurally Unique Lead-like Chemotypes for TEAD Inhibition
Synopsis
- Pinpointing the approach to develop a streamlined NMR screening platform to identify putative TEAD binders and hit assessment
- Showcasing a pipeline in structural science to allow X-ray structure determination of putative hit fragments
- Highlighting how mode of inhibition and kinetics of TEAD binders are defined based on crystallography and biophysical evaluation
Leveraging Biomarkers to Accelerate Established Hippo Pathway Clinical Drug Development
12:15 pm Biomarker-Guided Drug Development of YAP/TAZ-TEAD inhibitors
Synopsis
- SW-682: preclinical data for a novel TEAD inhibitor for Hippo-mutant cancers
- Overview of potential biomarkers for patient stratification, target engagement and molecular response
- Biomarkers for YAP activation as oncogenic driver or resistance mechanism to targeted therapies
12:45 pm Roundtable Discussion: Exploring What More Needs to be Done to Develop & Establish Hippo Pathway Biomarkers
Synopsis
- How do we find evidence for target/pathway regulation biomarkers?
- Does inhibiting TEAD create a measurable functional effect on disease that could act as a biomarker?
- Are we selecting the right patients with the right TEAD isoform mutations?
- Are there biomarkers of resistance and how do we find them?
- What is the feasibility for clinical biomarker assays?
1:15 pm Lunch & Networking
2:15 pm A Covalent TEAD Inhibitor with Exceptional Anti-cancer Activity & Combination Potential
Synopsis
- Presenting preclinical updates on a lead covalent TEADi including in vivo efficacy
- Harnessing TEAD selectivity to expand into TEADi-responsive indications
- Exploring combination approaches with KRASi
2:45 pm Phase 1 trial of TEAD inhibitor VT3989 : Trial status and future directions
Synopsis
- Exploring Phase 1 clinical data of VT3989
- Detailing translation of preclinical data to clinical results
- Reviewing tuture development directions
3:15 pm Afternoon Break & Networking
Broadening the Toolbox: Indications Showing Most Therapeutic Potential for Targeting the Hippo Pathway
3:45 pm Cardiovascular Conditions & the Hippo Pathway: Where’s the Potential?
Synopsis
- Assessing the data driving hippo pathway aberrations and incidence of cardiovascular conditions to spotlight the potential for drug development
- Characterizing cardio conditions and the existing treatment paradigm of disease
- Hypothesizing a logical approach to drug design to target hippo in cardio indications to inform translation
4:15 pm TEAD Inhibition in Combination to Tackle Targeted Therapy Resistance in Oncology •Evaluating the context in which the Hippo pathway confers resistance to targeted therapies •Considering potential pathways and drugs to use in combination with TEAD inhibit
Synopsis
- Evaluating the context in which the Hippo pathway confers resistance to targeted therapies
- Considering potential pathways and drugs to use in combination with TEAD inhibitors
- Exploring future steps at Ikena
5:15 pm Chair’s Closing Remarks
5:30 pm End of Conference Day One
