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Investor Presentaiton

2000- 1500- -- Vehicle POLO inhibitor Niraparib POLO inhibitor + Niraparib GSK101 (IDE705): Potential First-in-Class Pol Theta Helicase Inhibitor Phase 1: Targeting First-in-Human in Q4 2023 in Combination with Niraparib (PARPi) Pol Theta Helicase In Vivo Activity GSK101 + PARPI BRCA 1/2 Clinical Reversions Clinical Development Strategy BRCA Reversions Mediated by MMEJ Pol Theta Helicase Inhibitor + PARP Inhibitor Tumor volume (mm³ ± SEM) 1000- 500- Percent reversion events 100% 75% 71% 88% 50% 25% 0% BRCA1- BRCA2- Pol Theta Helicase Inhibitors Disrupt MMEJ Alternative DNA Damage Repair: Inhibit DSB Repair by MMEJ Dysregulate Replication Fork Stabilization 37 0 10 20 30 40 50 60 Study Day 70 80 Observed Deep and Durable Responses in Multiple Xenograft Models IDEAYA / GSK Data Gene Deletion Insertion Other Substitution Wild-type Microhomology deletion Potentiate PARPI Efficacy Prevent PARPI Resistance Overcome PARPI Resistance Cancer Res. 2020, DOI: 10.1158/2159-8290 Potential Clinical Opportunities GSK Strategic Partnership: Global Royalties with GSK covering all Costs, ~$1B Milestones, incl up to $20M Preclinical / Ph1 Clinical Potential Combination with GSK's Zejula™, a PARP Inhibitor BIOSCIENCES IDEAYA
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