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 24 FGFR2 Inhibitor 18 PDGFR-alpha Inhibitor 9 VEGFR Inhibitor (Pan) 33 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 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 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
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 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 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

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Clinical Trial Phase Therapies Title Recruitment Status Covered Countries Other Countries
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 | FRA | ESP | DEU | CAN | BEL 3
NCT02747797 Phase II Lucitanib Lucitanib (E3810) in Patients With Advanced Cancer and FGFR, VEGFR, or PDGFR Pathway Aberrations Withdrawn USA 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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