Relay Therapeutics, Inc. announced initial clinical data for RLY-4008 (lirafugratinib) in patients with FGFR2-altered solid tumors. The first part of the study (dose escalation) is complete, and the second part of the study (dose expansion) is ongoing at the 70mg QD recommended Phase 2 dose. Most treatment-related adverse events were expected FGFR2 on-target, low-grade, monitorable, generally manage and largely reversible.

There were no observed Grade 4 or 5 adverse events. Off-target toxicities of hyperphosphatemia and diarrhea continued to be clinically insignificant. Lirafugratinib Next Steps: Continue enrollment in the three tumor agnostic cohorts.

The company expects to report additional clinical data and a regulatory update in 2024. Enrollment is complete in the pivotal expansion cohort in patients with FGFR2 -fusion CCA who have not previously received an FGFR inhibitor. Near-term commercial readiness activities for CCA will be paused and aligned with the broader tumor agnostic opportunity.

The company will continue to prioritize and expand further PI3Ka mutant selective development, including: RLY-2608: continue ongoing ReDiscover trial with focus on RLY-2608 + fulvestrant cohorts; Initiate triplet combination with RLY-2608 + fullvestrant + CDK4/6 by the end of 2023; Next PI3Ka clinical data update expected in 2024; Additionally, Relay Therapeutics has decided to pause further development efforts on RLY-2139 (CDK2 inhibitor). Cash Runway Extended: With the decision to pause CCA commercial readiness and RLY-2139 development, Relay Therapeutics expects its cash, cash equivalents and investments will be sufficient to fund its current operating plan into the second half of 2026. Lirafugrat inib is currently being evaluated in a clinical trial in patients with advanced or metastatic FGFR2-altered Solid tumors with a single arm, potentially registration-enabling cohort for FGFRi-naive FGFR2-fusion CCA.

RLY-4008 (Lirafugratinab) is currently being evaluated in a global Phase 1/2 clinical trial (ReFocus) in patients with FGFR 2-altered CCA and multiple other solid tumors including a single-arm, potentially registration-enabling cohorts for FGFRi-naIVE FGFR2-fusionCCA. Any forward-looking statements in this press release are based on management's current expectations and beliefs and are subject to a number of risks, uncertainties and important factors that may cause actual events or results to differ materially from those expressed or implied by any forward-looking statements contained in this press release, including, without limitation, risks associated with: the impact of global economic uncertainty, geopolitical instability, or public health epidemics or outbreaks of an infectious disease, such as COVID-19, on countries or regions in which Relay Therapeutics has operations or does business, as well as on the timing and anticipated results of its clinical trials, strategy, future operations and profitability; the delay of its clinical trials, strategy and profitability; the delay of the study (dose expansion cohort in patients with FG FR2-fusion CCA who have no previously received an FGFR inhibitor; Near-term commercial readiness activities of CCA will be paused and align with the broader tumor agnostic opportunities. Pipeline Updates: The company will continue to prioritize and expand further PI3Ka mutant selective development, including: RLY-2608: continue ongoing ReDiscover trial with focus on RLY-2608 + fulvestrant cohorts Initiate triplet combination with RLY-2608 + fulvestrant + CDK4/6 by the end of 2023 Next PI3Ka clinical data update expected in 2024 Additionally, Relay Therapeutics has decided to pause further development efforts on RLY-2139 (CDK2 inhibitor).