Therapy Detail
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| Therapy Name | Lestaurtinib |
| Synonyms | |
| Therapy Description |
Lestaurtinib (CEP-701) inhibits JAK2, FLT3 and NTRK1-3, resulting in antiproliferative activity (PMID: 10415871, PMID: 17143529, PMID: 17442779, PMID: 17984313). |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| Lestaurtinib | CEP-701|KT-5555|A-154475|SP924 | CSF1R Inhibitor 23 FLT3 Inhibitor 54 JAK2 Inhibitor - ATP competitive 14 Trk Receptor Inhibitor (Pan) 23 | Lestaurtinib (CEP-701) inhibits JAK2, FLT3 and NTRK1-3, resulting in antiproliferative activity (PMID: 10415871, PMID: 17143529, PMID: 17442779, PMID: 17984313, PMID: 32441887). |
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| JAK2 V617F JAK2 R938L | hematologic cancer | resistant | Lestaurtinib | Preclinical | Actionable | In a preclinical study, immune cells expressing the JAK2 V617F and JAK2 R938L double mutation demonstrated resistance to lestauranib in culture (PMID: 21926964). | 21926964 |
| JAK2 V617F JAK2 G935R | hematologic cancer | resistant | Lestaurtinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing the JAK2 V617F and JAK2 G935R double mutation demonstrated resistance to Lestaurtinib (CEP-701) in culture (PMID: 21926964). | 21926964 |
| FLT3 exon 14 ins FLT3 A627P | hematologic cancer | resistant | Lestaurtinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed hematologic cells co-expressing FLT3 ITD and FLT3 A627P were resistant to treatment with Lestaurtinib (CEP-701) in culture (PMID: 22858906). | 22858906 |
| JAK2 V617F JAK2 Y931C | hematologic cancer | resistant | Lestaurtinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing the JAK2 V617F and JAK2 Y931C double mutation demonstrated resistance to Lestaurtinib (CEP-701) in culture (PMID: 21926964). | 21926964 |
| JAK2 V617F JAK2 M929I | hematologic cancer | predicted - sensitive | Lestaurtinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing the JAK2 V617F and JAK2 M929I double mutation were sensitive to treatment with Lestaurtinib (CEP-701) in culture, demonstrating growth inhibition (PMID: 21926964). | 21926964 |
| FLT3 exon 14 ins FLT3 Y842C | acute myeloid leukemia | sensitive | Lestaurtinib | Preclinical - Cell culture | Actionable | In a preclinical study, acute myeloid leukemia cells harboring a FLT3 internal tandem duplication and expressing FLT3 Y842C demonstrated sensitivity to Lestaurtinib (CEP-701) in culture (Blood 2009 114:3776). | detail... |
| JAK2 V617F JAK2 I960V | hematologic cancer | resistant | Lestaurtinib | Preclinical | Actionable | In a preclinical study, immune cells expressing the JAK2 V617F and JAK2 I960V double mutation demonstrated resistance to Lestauranib in culture (PMID: 21926964). | 21926964 |
| ETV6 - NTRK3 | Advanced Solid Tumor | sensitive | Lestaurtinib | Preclinical | Actionable | In a preclinical study, transformed cells expressing the fusion, ETV6-NTRK3, were treated with Lestaurtinib (CEP-701), which resulted in inhibition of ETV6-NTRK3 autophosphorylation and restoration of Tgf-b1 signaling (PMID: 16258068). | 16258068 |
| FLT3 exon 14 ins FLT3 F691L | acute myeloid leukemia | decreased response | Lestaurtinib | Preclinical - Cell culture | Actionable | In a preclinical study, acute myeloid leukemia cells harboring a FLT3 internal tandem duplication and expressing FLT3 F691L demonstrated a decreased response to Lestaurtinib (CEP-701) compared to treated cells harboring a FLT3 ITD and expressing FLT3 Y842C (Blood 2009 114:3776). | detail... |
| FLT3 exon 14 ins FLT3 F621L | acute myeloid leukemia | sensitive | Lestaurtinib | Preclinical - Cell culture | Actionable | In a preclinical study, acute myeloid leukemia cells harboring a FLT3 internal tandem duplication (ITD) and expressing FLT3 F621L demonstrated sensitivity to Lestaurtinib (CEP-701) in culture (Blood 2009 114:3776). | detail... |
| JAK2 V617F JAK2 E985K | hematologic cancer | resistant | Lestaurtinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing the JAK2 V617F and JAK2 E985K double mutation demonstrated resistance to Lestaurtinib (CEP-701) in culture (PMID: 21926964). | 21926964 |
| Unknown unknown | pancreatic ductal adenocarcinoma | not applicable | Lestaurtinib | Preclinical | Actionable | In preclinical studies, lestaurtinib has been shown to have an antitumor effect in xenograft models of pancreatic ductal adenocarcinoma (PMID: 10473107). | 10473107 |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status |
|---|
CKB BOOST