Conference Agenda

All Times Below - EST

8:00am | Coffee & Networking

8:55 am Chair’s Opening Remarks

Optimizing Drug Design & Potency to Penetrate the Blood Brain Barrier To Treat Neurodegeneration & Brain Metastasis

9:00 am Pushing the Boundaries of Drug Design to Discover Novel Selective BBB Permeable Kinase Inhibitions as Novel Therapies for Neurological Diseases


  • Understanding the role of the immune system neurological diseases such as Amyotrophic Lateral Sclerosis (ALS), Parkinson’s, Alzheimer’s (AD), and Multiple sclerosis (MS) to discover new therapies
  • Targeting kinases in the CNS to identify clinically validated mechanisms and pathways to expand on the existing biological and clinical knowledge to further our understanding of the causative vs. the consequential effect of the immune system on neurodegeneration
  • Utilizing Structure-Based Drug Design (SBDD), Parallel Medicinal Chemistry (PMC) and Computer Aid Drug Design (CADD) to optimize the physicochemical properties of small molecules inhibitors to enhance brain exposures to treat neurological diseases
  • Discovering novel kinase inhibitors that exhibit excellent kinome selectivity and BBB permeability yet fall outside the drug-like space traditionally targeted when optimizing for improved CNS properties

9:30 am Providing the First Mechanistic Basis for Halting Neurodegenerative Disease: Targeting c-Abl to Reverse Parkinson’s Disease

  • Milton Werner Founder, President & CEO, Inhibikase Therapeutics


  • Discussing the discovery of the biochemical process underlying the initiation and progression of Parkinson’s disease to rationalize c-Abl targeting
  • Optimizing drug design of c-Abl inhibitor IkT-148009 to halt Parkinson’s disease and restore functional loss to effectively reverse Parkinson’s disease
  • Reflecting on preclinical data to supercharge phase 1 trials for IkT-148009

10:00 am Utilizing a CNS Penetrant MasterKey Inhibitor to Access the Blood Brain Barrier to Treat Glioblastoma & Brain Metastasis in NSCLC


  • Revealing BDTX-1535, a CNS penetrant MasterKey inhibitor of EGFR mutations which demonstrates in vivo efficacy and has the potential to treat patients with NSCLC and GBM
  • Targeting unmet medical needs in EGFR-mutated NSCLC EGFR-mutated GBM
  • Presenting preclinical data that support opportunity for progression to clinical studies and therapeutic effect in both indications

10:30 am | Morning Refreshments & Structured Networking

Rationalizing Combination Strategies to Drive Personalized Medicine Approach & Overcome Resistance

11:30 am Uncovering Potential Combinations to Weaponize Kinase Inhibitors Against B Cell Malignancies & Autoimmune Disease


  • Strategically identifying genes and pathways known to drive the abnormal behaviour of B cells
  • Acquiring and optimizing compounds to develop the best-in-class generation of kinase inhibitors
  • Developing complementary and synergistic drug combinations with TG-1701, umbralisib and ublituximab

12:00 pm Rationalizing Kinase Inhibitor Combinations with Immunotherapy to Optimize Tumor Killing


  • Harnessing the patients’ immune systems with novel kinase inhibitors to minimize side effects
  • Assessing the key take-aways from PI3K-PD-1 dual blockade to expand to other kinase inhibitors and checkpoint inhibitors
  • Theorizing the potential for novel kinase inhibitors to act on checkpoint inhibitor resistant cancer types

12:30 pm Expert Panel Discussion: Combining Kinase Inhibitor Therapies for Supercharged Targeting


  • Discussing multiple points of entry of oncogenic pathways to enhance targeting and therapeutic impact
  • Redefining outcomes with combination therapies across indications, from oncology, dermatology, respiratory & autoimmune diseases
  • Assessing the safety issues with polypharmacy of 1 or more kinases and mitigating off-target effects

1:00 pm | Lunch & Networking

Harnessing Biomarkers to Advance Clinical Development of Kinase Inhibitors Which Overcome Resistance

2:00 pm Exploiting Biomarkers for A Personalized Healthcare Approach to the Development of Ipatasertib


  • Advancing understanding of alterations of the PI3K/AKT pathway in human cancer and the differences in frequencies of alterations in different cancer types
  • Determining the role of PI3K/AKT activation in adaptive resistance in current treatment standards to inform future resistance strategies
  • Developing flexible patient selection strategies based on disease and combination context to overcome resistance

2:30 pm Leveraging the Spleen Tyrosine Kinase (SYK) Pathways to Target Inflammatory Signaling in Multiple Diseases with Fostamatinib

  • Esteban Masuda Executive VP, Science and Research , Rigel Pharmaceuticals


  • Treating antibody-mediated platelet destruction with the first kinase inhibitor approved for immune thrombocytopenia
  • Discussing late-stage clinical trial development for autoimmune hemolytic anemia (antibody-mediated RBC destruction)
  • Weaponizing against COVID: discussing the use of fostamatinib in late phase clinical trials for the treatment of hospitalized adults with COVID-19

3:00 pm | Afternoon Refreshments

3:30 pm Reaffirming Kinase Inhibitors in Treatment of Inflammatory Skin Diseases: JAK Inhibitors & Beyond

  • Mehdi Rashighi Founding Director, Connective Tissue Disease Clinic & Research Center, UMass Chan Medical School


  • Reflecting on lessons from the use of JAK inhibitors in dermatology to cultivate targeted skin delivery to improve selectivity and safety profiles
  • Identifying new druggable targets to deliver for unmet clinical needs
  • Optimizing translational approaches to identify early response biomarkers to inform clinical strategy

4:00 pm Harnessing Metabolism to Optimize Kinase Therapeutic Responses & Overcome Resistance

  • George Poulogiannis Team Leader, Signalling & Cancer Metabolism Group, Institute of Cancer Research


  • Deconstructing the metabolic signatures associated with the response of kinase inhibitors to inform target selection
  • Targeting metabolism through a drug and diet combination to enhance the response to targeted therapies and overcome resistance
  • Leveraging pre-clinical data to assess the potential to advance to clinical trials and treat cancer cases, patient by patient

4:30 pm Chairman’s Closing Remarks & Close of Summit