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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