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, PMID: 32441887). |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| Lestaurtinib | CEP-701|KT-5555|A-154475|SP924 | CSF1R Inhibitor 28 FLT3 Inhibitor 64 JAK2 Inhibitor - ATP competitive 15 Trk Receptor Inhibitor (Pan) 31 | 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 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 Lestaurtinib (CEP-701) in culture (PMID: 21926964). | 21926964 |
| 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 D835V | hematologic cancer | sensitive | Lestaurtinib | Preclinical - Cell culture | Actionable | In a preclinical study, Lestaurtinib (CEP-701) inhibited proliferation of transformed cells expressing FLT3-ITD and FLT3 D835V in culture (PMID: 34768286). | 34768286 |
| 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 |
| 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 |
| 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 D835A | hematologic cancer | sensitive | Lestaurtinib | Preclinical - Cell culture | Actionable | In a preclinical study, Lestaurtinib (CEP-701) inhibited Flt3 autophosphorylation and viability in transformed cells expressing FLT3 D835A in culture (PMID: 28077790). | 28077790 |
| 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 Lestaurtinib (CEP-701) in culture (PMID: 21926964). | 21926964 |
| FLT3 exon 14 ins FLT3 D839G | hematologic cancer | sensitive | Lestaurtinib | Preclinical - Cell culture | Actionable | In a preclinical study, Lestaurtinib (CEP-701) inhibited proliferation of transformed cells expressing FLT3-ITD and FLT3 D839G in culture (PMID: 34768286). | 34768286 |
| FLT3 exon 14 ins FLT3 F691L | hematologic cancer | resistant | Lestaurtinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing FLT3-ITD and FLT3 F691L demonstrated resistance to Lestaurtinib (CEP-701) in culture (PMID: 34768286). | 34768286 |
| FLT3 I836S | hematologic cancer | sensitive | Lestaurtinib | Preclinical - Cell culture | Actionable | In a preclinical study, Lestaurtinib (CEP-701) inhibited Flt3 autophosphorylation and viability in transformed cells expressing FLT3 I836S in culture (PMID: 28077790). | 28077790 |
| FLT3 I836T | hematologic cancer | sensitive | Lestaurtinib | Preclinical - Cell culture | Actionable | In a preclinical study, Lestaurtinib (CEP-701) inhibited Flt3 autophosphorylation and viability in transformed cells expressing FLT3 I836T in culture (PMID: 28077790). | 28077790 |
| FLT3 exon 14 ins FLT3 D835Y | hematologic cancer | sensitive | Lestaurtinib | Preclinical - Cell culture | Actionable | In a preclinical study, Lestaurtinib (CEP-701) inhibited proliferation of transformed cells expressing FLT3-ITD and FLT3 D835Y in culture (PMID: 34768286). | 34768286 |
| FLT3 Q575del | hematologic cancer | sensitive | Lestaurtinib | Preclinical - Cell culture | Actionable | In a preclinical study, Lestaurtinib (CEP-701) decreased downstream signaling and proliferation in transformed cells expressing FLT3 Q575del in culture (PMID: 33914060). | 33914060 |
| 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 |
| FLT3 E573del | hematologic cancer | sensitive | Lestaurtinib | Preclinical - Cell culture | Actionable | In a preclinical study, Lestaurtinib (CEP-701) decreased proliferation in transformed cells expressing FLT3 E573del in culture (PMID: 33914060). | 33914060 |
| FLT3 D835K FLT3 D835L | hematologic cancer | sensitive | Lestaurtinib | Preclinical - Cell culture | Actionable | In a preclinical study, Lestaurtinib (CEP-701) inhibited Flt3 autophosphorylation and viability in transformed cells expressing FLT3 D835L and D835K in culture (PMID: 28077790). | 28077790 |
| 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... |
| FLT3 D835G | hematologic cancer | sensitive | Lestaurtinib | Preclinical - Cell culture | Actionable | In a preclinical study, Lestaurtinib (CEP-701) inhibited Flt3 autophosphorylation and viability in transformed cells expressing FLT3 D835G in culture (PMID: 28077790). | 28077790 |
| FLT3 D835N | hematologic cancer | sensitive | Lestaurtinib | Preclinical - Cell culture | Actionable | In a preclinical study, Lestaurtinib (CEP-701) inhibited Flt3 autophosphorylation and viability in transformed cells expressing FLT3 D835N in culture (PMID: 28077790). | 28077790 |
| 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... |
| FLT3 I836D FLT3 I836L | hematologic cancer | sensitive | Lestaurtinib | Preclinical - Cell culture | Actionable | In a preclinical study, Lestaurtinib (CEP-701) inhibited Flt3 autophosphorylation and viability in transformed cells expressing FLT3 I836D and I836L in culture (PMID: 28077790). | 28077790 |
| FLT3 Y572del | hematologic cancer | sensitive | Lestaurtinib | Preclinical - Cell culture | Actionable | In a preclinical study, Lestaurtinib (CEP-701) decreased proliferation in transformed cells expressing FLT3 Y572del in culture (PMID: 33914060). | 33914060 |
| FLT3 S574del | hematologic cancer | sensitive | Lestaurtinib | Preclinical - Cell culture | Actionable | In a preclinical study, Lestaurtinib (CEP-701) decreased proliferation in transformed cells expressing FLT3 S574del in culture (PMID: 33914060). | 33914060 |
| FLT3 exon 14 ins FLT3 Y842H | hematologic cancer | sensitive | Lestaurtinib | Preclinical - Cell culture | Actionable | In a preclinical study, Lestaurtinib (CEP-701) inhibited proliferation of transformed cells expressing FLT3-ITD and FLT3 Y842H in culture (PMID: 34768286). | 34768286 |
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- Use quotes to match on a longer phrase with spaces (i.e. "mtor c1483f")
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|
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