Discovery of lirafugratinib (RLY-4008), a highly selective irreversible small-molecule inhibitor of FGFR2
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Publications
Discovery and clinical proof-of-concept of RLY-2608, a first-in-class mutant-selective allosteric PI3Ka inhibitor that decouples anti-tumor activity from hyperinsulinemia
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Oral Presentation: Clinical activity of lirafugratinib (RLY-4008), a highly selective FGFR2 inhibitor, in patients with advanced FGFR2-altered solid tumors: the ReFocus study
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Poster: Clinical activity of lirafugratinib (RLY-4008), a highly selective FGFR2 inhibitor, in patients with advanced FGFR2-altered solid tumors: the ReFocus study
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Updated Dose Escalation Results for ReFocus: A First-In-Human Study of Highly Selective FGFR2 Inhibitor, RLY-4008, in Cholangiocarcinoma and Other Solid Tumors
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RLY-4008, the first highly selective FGFR2 inhibitor with activity across FGFR2 alterations and resistance mutations
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Pan-mutant and isoform selective PI3K⍺ inhibitor, RLY-2608, demonstrates selective targeting in a first-in-human study of PIK3CA-mutant solid tumor patients: ReDiscover trial
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A food effect and esomeprazole drug–drug interaction study of RLY-4008, a highly selective FGFR2 inhibitor, in healthy subjects
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First-in-human global multi-center study of RLY-2608, a pan mutant and isoform selective PI3Kα inhibitor, as a single agent in advanced solid tumor patients and in combination with fulvestrant in patients with advanced breast cancer
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ReFocus: A Phase 1/2 study of the highly selective FGFR2 inhibitor RLY-4008 in patients with advanced solid tumors, including breast cancer
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Identifying FGFR2 fusions/rearrangements in cholangiocarcinoma patients using a novel cfDNA algorithm for treatment with RLY-4008, a highly selective irreversible FGFR2 inhibitor
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Efficacy of RLY-4008, a highly selective FGFR2 inhibitor in patients with an FGFR2 fusion or rearrangement, FGFR inhibitor-naïve cholangiocarcinoma: ReFocus trial
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Discovery and Characterization of the Potent, Allosteric SHP2 inhibitor GDC-1971 for the Treatment of RTK/RAS Driven Tumors
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RLY-2608: the first allosteric mutant- and isoform-selective inhibitor of PI3Kα, is efficacious as a single agent and drives regressions in combination with standard of care therapies in PIK3CA mutant breast cancer models
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First Results of RLY-4008, a Potent and Highly Selective FGFR2 Inhibitor in a First-in-Human Study in Patients with FGFR2-Altered Cholangiocarcinoma and Multiple Solid Tumors
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Discovery and characterization of RLY-2608, the first allosteric, mutant, and isoform-selective inhibitor of PI3Kα
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First-in-human study of the highly selective FGFR2 inhibitor, RLY-4008, in patients with intrahepatic cholangiocarcinoma and other advanced solid tumors
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RLY‑4008, a Novel Precision Therapy for FGFR2‑Driven Cancers Designed to Potently and Selectively Inhibit FGFR2 and FGFR2 Resistance Mutations
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