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 15 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 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 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
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
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
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 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

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Clinical Trial Phase Therapies Title Recruitment Status
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
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
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
NCT02747797 Phase II Lucitanib Lucitanib (E3810) in Patients With Advanced Cancer and FGFR, VEGFR, or PDGFR Pathway Aberrations Withdrawn
NCT01283945 Phase Ib/II Lucitanib Study of Oral Lucitanib (E-3810), a Dual VEGFR-FGFR Tyrosine Kinase Inhibitor, in Patients With Solid Tumors Completed


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