Therapy Detail
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| Therapy Name | Merestinib |
| Synonyms | |
| Therapy Description |
Merestinib (LY2801653) inhibits several receptor tyrosine kinases including MET, MST1R (RON), AXL, MERTK, TYRO3, ROS1 fusions, PDGFRA, FLT3, TEK, DDR1/2, MKNK1/2, and NTRK1/2/3 with greatest activity against NTRK1, and may result in decreased tumor growth (PMID: 23275061, PMID: 24305878, PMID: 29568395). |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| Merestinib | LY2801653|LY-2801653 | AXL Inhibitor 27 DDR1 Inhibitor 8 DDR2 inhibitor 7 FLT3 Inhibitor 55 MET Inhibitor 51 RON Inhibitor 10 ROS1 Inhibitor 14 Trk Receptor Inhibitor (Pan) 23 TYRO3 Inhibitor 8 | Merestinib (LY2801653) inhibits several receptor tyrosine kinases including MET, MST1R (RON), AXL, MERTK, TYRO3, ROS1 fusions, PDGFRA, FLT3, TEK, DDR1/2, MKNK1/2, and NTRK1/2/3 with greatest activity against NTRK1, and may result in decreased tumor growth (PMID: 23275061, PMID: 24305878, PMID: 29568395, PMID: 32537847). |
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| ETV6 - NTRK3 | head and neck squamous cell carcinoma | sensitive | Merestinib | Preclinical - Pdx | Actionable | In a preclinical study, a head and neck squamous cell carcinoma patient-derived xenograft (PDX) model harboring ETV6-NTRK3 was sensitive to treatment with Merestinib (LY2801653) compared to vehicle, demonstrating decreased tumor growth (PMID: 29568395). | 29568395 |
| Unknown unknown | lung non-small cell carcinoma | not applicable | Merestinib | Preclinical | Actionable | In a preclinical study, LY2801653 inhibited tumor growth in mouse xenograft models of non-small cell lung cancer (PMID: 24305878). | 24305878 |
| Unknown unknown | colorectal cancer | not applicable | Merestinib | Phase I | Actionable | In a Phase I trial, LY2801653 demonstrated safety and preliminary efficacy in patients with advanced solid tumors, including patients with colorectal cancer (Cancer Res October 1, 2014 74:CT237). | detail... |
| Unknown unknown | Advanced Solid Tumor | not applicable | Merestinib | Phase I | Actionable | In a Phase I trial, LY2801653 demonstrated safety and preliminary efficacy in patients with advanced solid tumors (Cancer Res October 1, 2014 74:CT237). | detail... |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|---|---|---|---|---|---|
| NCT02711553 | Phase II | Ramucirumab Merestinib Cisplatin + Gemcitabine | A Study of Ramucirumab (LY3009806) or Merestinib (LY2801653) in Advanced or Metastatic Biliary Tract Cancer | Active, not recruiting | USA | 18 |
| NCT01285037 | Phase I | Cisplatin Cetuximab Merestinib | A Study of LY2801653 in Advanced Cancer | Completed | USA | 0 |
| NCT03292536 | Phase I | Merestinib | Merestinib on Bone Metastases in Subjects With Breast Cancer | Terminated | USA | 0 |
| NCT02920996 | Phase II | Merestinib | Merestinib In Non-Small Cell Lung Cancer And Solid Tumors | Active, not recruiting | USA | 0 |
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