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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, PMID: 31619444).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
Lucitanib E-3810|AL3810 DDR1 Inhibitor 10 DDR2 inhibitor 7 FGFR1 Inhibitor 28 FGFR2 Inhibitor 23 PDGFR-alpha Inhibitor 9 VEGFR Inhibitor (Pan) 36 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 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
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
FGFR1 amp triple-receptor negative breast cancer predicted - sensitive Lucitanib Preclinical - Pdx Actionable In a preclinical study, Lucitanib (E-3810) treatment resulted in reduced tumor volume in FGFR1-amplified triple-negative breast cancer patient-derived xenograft (PDX) models (PMID: 34593528). 34593528
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
FGFR1 W4C FGFR1 amp estrogen-receptor positive breast cancer predicted - sensitive Lucitanib Preclinical - Pdx Actionable In a preclinical study, Lucitanib (E-3810) treatment resulted in reduced tumor volume in an ER-positive breast cancer patient-derived xenograft (PDX) model harboring FGFR1 W4C and FGFR1 amplification (PMID: 34593528). 34593528

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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 | ITA | FRA | ESP | DEU 0
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 ITA | HUN | GBR | FRA | ESP | DEU | CAN | BEL | AUS 0
NCT01283945 Phase Ib/II Lucitanib Study of Oral Lucitanib (E-3810), a Dual VEGFR-FGFR Tyrosine Kinase Inhibitor, in Patients With Solid Tumors Completed ITA | FRA | ESP 0
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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