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
IDEAYAView entire presentation