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 23 | 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). |
Filtering
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- Separate multiple filter terms with a space. Any order may be used (i. e. a b c and c b a are equivalent )
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- Use quotes to match on a longer phrase with spaces (i.e. "mtor c1483f")
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| 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 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 |
| 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 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 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 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 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 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 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 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 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 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 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 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 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 |
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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 | Active, not recruiting | USA | NLD | ITA | GBR | FRA | ESP | DEU | AUS | 5 |
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