Therapy Detail
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| Therapy Name | Lucitanib |
| Synonyms | |
| Therapy Description |
Lucitanib (E-3810) is a multi-tyrosine kinase receptor inhibitor of VEGFR 1-3, DDR2, PDGFRA, and FGFR1-2, that may inhibit tumor angiogenesis, prevent tumor cell proliferation, and induce tumor cell death (PMID: 27988457, PMID: 24696502). |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| Lucitanib | E-3810|AL3810 | DDR1 Inhibitor 8 DDR2 inhibitor 7 FGFR1 Inhibitor 23 FGFR2 Inhibitor 16 PDGFR-alpha Inhibitor 9 VEGFR Inhibitor (Pan) 32 | Lucitanib (E-3810) is a multi-tyrosine kinase receptor inhibitor of VEGFR 1-3, DDR2, PDGFRA, and FGFR1-2, that may inhibit tumor angiogenesis, prevent tumor cell proliferation, and induce tumor cell death (PMID: 27988457, PMID: 24696502, PMID: 31619444). |
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| FGFR1 over exp | Her2-receptor negative breast cancer | predicted - sensitive | Lucitanib | Phase II | Actionable | In a Phase II (FINESSE) trial, Lucitanib (E-3810) treatment resulted in improved objective response rate (25%, 5/20 vs 8%, 3/39) and median progression-free survival (158 vs 109 days) in patients with metastatic hormone receptor-positive, Erbb2 (Her2)-negative breast cancer with high Fgfr1 expression (H-score>=50) compared to those with low Fgfr1 expression (H-score<50) (PMID: 31619444; NCT02053636). | 31619444 |
| FGFR1 amp | estrogen-receptor positive breast cancer | sensitive | Lucitanib | Preclinical - Cell culture | Actionable | In a preclinical study, an estrogen-receptor positive breast cancer cell line harboring FGFR1 amplification demonstrated sensitivity to treatment with Lucitanib (E-3810) in culture (PMID: 27126994). | 27126994 |
| Unknown unknown | triple-receptor negative breast cancer | not applicable | Lucitanib | Preclinical | Actionable | In a preclinical study, Lucitanib (E-3810) demonstrated antitumor activity in mouse xenograft models of triple negative breast cancer with synergistic effects noted when using Lucatinib plus chemotherapy (PMID: 23270924). | 23270924 |
| DDR2 act mut | lung non-small cell carcinoma | sensitive | Lucitanib | Preclinical | Actionable | In a preclinical study, Lucitanib (E-3810) decreased DDR2 phosphorylation, and inhibited proliferation and induced apoptosis in lung squamous cell carcinoma cells harboring a DDR2 activating mutation in culture (PMID: 24696502). | 24696502 |
| Unknown unknown | breast cancer | not applicable | Lucitanib | Phase II | Actionable | In a Phase II trial, Lucitanib (E-3810) demonstrated acceptable toxicity and activity, resulted in a median progression-free survival of 3.5 and 2.6 months for 10mg and 15mg treatment groups respectively, with no differences in response correlated with FGFR1 and 11q amplification status in metastatic breast cancer patients (Cancer Res 2017;77(4 Suppl):Abstract nr P6-11-03). | detail... |
| FGFR1 amp | Her2-receptor negative breast cancer | predicted - sensitive | Lucitanib | Phase II | Actionable | In a Phase II (FINESSE) trial, Lucitanib (E-3810) treatment resulted in an objective response rate (ORR) of 19% (6/32) and a clinical benefit rate of 41% (13/32) in patients with metastatic hormone receptor-positive, Erbb2 (Her2)-negative breast cancer harboring FGFR1 amplification, ORR was improved (22%, 5/23 vs 9%, 5/53) in patients with high level FGFR1 amplification (FGFR1/centromere ratio>=4) compared to those without (PMID: 31619444; NCT02053636). | 31619444 |
| FGFR1 amp | lung carcinoma | sensitive | Lucitanib | Preclinical - Cell line xenograft | Actionable | in a preclinical study, Lucitanib (E-3810) preferentially inhibited growth of FGFR1-amplified lung carcinoma cell lines in culture and in cell line xenograft models (PMID: 27988457). | 27988457 |
| KDR act mut | Advanced Solid Tumor | predicted - sensitive | Lucitanib | Phase I | Actionable | In a Phase I trial, Lucitanib (E-3810) demonstrated safety and efficacy in patients with FGF-aberrant or angiogenesis-sensitive advanced solid tumors (PMID: 25193991). | 25193991 |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|---|---|---|---|---|---|
| NCT02747797 | Phase II | Lucitanib | Lucitanib (E3810) in Patients With Advanced Cancer and FGFR, VEGFR, or PDGFR Pathway Aberrations | Withdrawn | USA | 0 |
| NCT02109016 | Phase II | Lucitanib | A Study to Assess the Efficacy of the VEGFR-FGFR Inhibitor, Lucitanib, Given to Patients With FGFR1-driven Lung Cancer | Terminated | USA | 4 |
| NCT01283945 | Phase Ib/II | Lucitanib | Study of Oral Lucitanib (E-3810), a Dual VEGFR-FGFR Tyrosine Kinase Inhibitor, in Patients With Solid Tumors | Completed | 3 | |
| NCT02053636 | Phase II | Lucitanib | A Phase II Trial Testing Oral Administration of Lucitanib in Patients With Fibroblast Growth Factor Receptor (FGFR)1-amplified or Non-amplified Estrogen Receptor Positive Metastatic Breast Cancer | Completed | CAN | 8 |
| NCT02202746 | Phase II | Lucitanib | A Study to Assess the Safety and Efficacy of the VEGFR-FGFR Inhibitor, Lucitanib, Given to Patients With FGF Aberrant Metastatic Breast Cancer | Terminated | USA | 0 |
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