Therapy Detail

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Therapy Name RLY-4008
Synonyms
Therapy Description

RLY-4008 binds to and inhibits FGFR2, selectively targeting primary oncogenic FGFR2 mutations and leads to decreased FGFR2-dependent signaling, potentially resulting in inhibition of tumor cell proliferation (NCI Drug Dictionary; Journal of Clinical Oncology 39, no. 15_suppl).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
RLY-4008 RLY4008|RLY 4008|Lirafugratinib FGFR2 Inhibitor 22 RLY-4008 binds to and inhibits FGFR2, selectively targeting primary oncogenic FGFR2 mutations and leads to decreased FGFR2-dependent signaling, potentially resulting in inhibition of tumor cell proliferation (NCI Drug Dictionary; Journal of Clinical Oncology 39, no. 15_suppl).

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Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
FGFR2 N549H Advanced Solid Tumor predicted - sensitive RLY-4008 Preclinical - Biochemical Actionable In a preclinical study, RLY-4008 treatment inhibited Fgfr2 phosphorylation in cultured cells expressing FGFR2 N549H (PMID: 37270847). 37270847
FGFR2 L617V Advanced Solid Tumor predicted - sensitive RLY-4008 Preclinical - Biochemical Actionable In a preclinical study, RLY-4008 treatment inhibited Fgfr2 phosphorylation in cultured cells expressing FGFR2 L617V (PMID: 37270847). 37270847
FGFR2 C383R breast cancer sensitive RLY-4008 Preclinical - Cell culture Actionable In a preclinical study, RLY-4008 inhibited proliferation of a breast carcinoma cell line harboring FGFR2 C383R in culture (PMID: 37270847). 37270847
FGFR2 fusion cholangiocarcinoma predicted - sensitive RLY-4008 Phase Ib/II Actionable In a Phase I/II trial (ReFocus), RLY-4008 treatment resulted in radiographic tumor reductions in 64% (74/116) and partial responses/stable disease in 72% (83/116) of patients with advanced solid tumors harboring FGFR2 alterations, and an objective response rate of 52% (13/25) and a disease control rate of 88% (22/25) in FGFR inhibitor-naive cholangiocarcinoma patients harboring FGFR2 fusions or rearrangements (J Clin Oncol 41, 2023 (suppl 16; abstr 4009); NCT04526106). detail...
FGFR2 N549K endometrial cancer predicted - sensitive RLY-4008 Preclinical - Cell culture Actionable In a preclinical study, RLY-4008 treatment led to tumor regression in a cell line xenograft model of endometrial cancer harboring FGFR2 N549K (Cancer Res 2021;81(13_Suppl):Abstract nr 1455). detail...
FGFR2 K641N Advanced Solid Tumor predicted - sensitive RLY-4008 Preclinical - Biochemical Actionable In a preclinical study, RLY-4008 treatment inhibited Fgfr2 phosphorylation in cultured cells expressing FGFR2 K641N (PMID: 37270847). 37270847
FGFR2 Y375C salivary gland carcinoma predicted - sensitive RLY-4008 Case Reports/Case Series Actionable In a Phase I/II trial (ReFocus), RLY-4008 treatment resulted in a partial response with near complete resolution of liver metastases, and regression of lung and adrenal metastases in a patient with metastatic carcinoma of the right parotid salivary gland harboring FGFR2 Y375C (PMID: 37270847; NCT04526106). 37270847
FGFR2 amp colorectal adenocarcinoma sensitive RLY-4008 Preclinical - Cell culture Actionable In a preclinical study, RLY-4008 inhibited proliferation of a colorectal adenocarcinoma cell line with FGFR2 amplification in culture (PMID: 37270847). 37270847
FGFR2 V564F Advanced Solid Tumor predicted - sensitive RLY-4008 Preclinical - Biochemical Actionable In a preclinical study, RLY-4008 treatment inhibited Fgfr2 phosphorylation in cultured cells expressing FGFR2 V564F (PMID: 37270847). 37270847
FGFR2 V564L Advanced Solid Tumor predicted - sensitive RLY-4008 Preclinical - Biochemical Actionable In a preclinical study, RLY-4008 treatment inhibited Fgfr2 phosphorylation in cultured cells expressing FGFR2 V564L (PMID: 37270847). 37270847
FGFR2 K659M Advanced Solid Tumor predicted - sensitive RLY-4008 Preclinical - Biochemical Actionable In a preclinical study, RLY-4008 treatment inhibited Fgfr2 phosphorylation in cultured cells expressing FGFR2 K659M (PMID: 37270847). 37270847
FGFR2 N549D Advanced Solid Tumor predicted - sensitive RLY-4008 Preclinical - Biochemical Actionable In a preclinical study, RLY-4008 treatment inhibited Fgfr2 phosphorylation in cultured cells expressing FGFR2 N549D (PMID: 37270847). 37270847
FGFR2 E565A Advanced Solid Tumor predicted - sensitive RLY-4008 Preclinical - Biochemical Actionable In a preclinical study, RLY-4008 treatment inhibited Fgfr2 phosphorylation in cultured cells expressing FGFR2 E565A (PMID: 37270847). 37270847
FGFR2 K310R FGFR2 N549K endometrial adenocarcinoma sensitive RLY-4008 Preclinical - Cell line xenograft Actionable In a preclinical study, RLY-4008 inhibited proliferation of an endometrial adenocarcinoma cell line harboring FGFR2 N549K and FGFR K310R in culture, and led to tumor regression in a cell line xenograft model (PMID: 37270847). 37270847
FGFR2 amp stomach cancer sensitive RLY-4008 Preclinical - Cell line xenograft Actionable In a preclinical study, RLY-4008 treatment inhibited proliferation of gastric carcinoma cell lines with an FGFR2 amplification in culture, and led to tumor regression in a cell line xenograft model (PMID: 37270847). 37270847

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Clinical Trial Phase Therapies Title Recruitment Status Covered Countries Other Countries
NCT04526106 Phase I RLY-4008 REFOCUS: A First-in-Human Study of Highly Selective FGFR2 Inhibitor, RLY-4008, in Patients With ICC and Other Advanced Solid Tumors Recruiting USA | ITA | GBR | FRA | ESP | DEU | AUS 6


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