Business
Relay Therapeutics Announces Interim Clinical Data that Support RLY-4008 as a Highly Selective FGFR2 Inhibitor
Interim data suggest that RLY-4008 is a highly selective FGFR2 inhibitor that has not shown to be limited by off-target toxicities of hyperphosphatemia
About this update from Relay Therapeutics, Inc.
[{"type":"text","content":"Interim data suggest that RLY-4008 is a highly selective FGFR2 inhibitor that has not shown to be limited by off-target toxicities of hyperphosphatemia (FGFR1) and diarrhea (FGFR4) RLY-4008 demonstrated tumor shrinkage in all six pan-FGFR treatment-naïve FGFR2 fusion positive cholangiocarcinoma patients with three achieving confirmed partial responses Interim data support potential clinical benefits of optimized inhibition of FGFR2 regardless of alteration (fusions, mutations, and amplifications), line of treatment or tumor type Relay Therapeutics anticipates selecting a once daily recommended Phase 2 dose and initiating expansion cohorts prior to the end of 2021 Relay Therapeutics to host a conference call today at 12:30 pm E.T. CAMBRIDGE, Mass., Oct. 08, 2021 (GLOBE NEWSWIRE) -- Relay Therapeutics, Inc. (Nasdaq: RLAY), a clinical-stage precision medicine company transforming the drug discovery process by combining leading-edge computational and experimental technologies, today announced interim clinical data for RLY-4008, a highly selective irreversible and oral small molecule inhibitor of FGFR2, in a first-in-human trial in patients with FGFR2-altered cholangiocarcinoma and multiple other solid tumors. The data are being presented today at the virtual AACR-NCI-EORTC Molecular Targets Conference and suggest that RLY-4008 is the first investigational therapy designed to selectively bind to FGFR2 to avoid off‐isoform toxicities for the treatment of patients with FGFR2-altered tumors. As will be presented at the conference, study investigators reported robust inhibition of FGFR2 in the first 49 subjects that was not shown to be limited by off-target toxicities, including hyperphosphatemia and diarrhea, in the interim clinical data. The initial toxicity data suggest that certain dose levels administered can achieve >85% continuous inhibition of FGFR2. At those levels, acute toxicities that would limit dose intensity have generally not been observed to date. The interim clinical data included results from FGFR2-altered solid tumors, with approximately 80% of all patients treated achieving reductions in tumor size at the cut-off date of September 9, 2021. In pan-FGFRi treatment-naïve cholangiocarcinoma patients, RLY-4008 demonstrated tumor shrinkage in all six pan-FGFR treatment-naïve FGFR2 fusion positive cholangiocarcinoma patient...