Therapy Detail
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| Therapy Name | Fedratinib |
| Synonyms | |
| Therapy Description |
Inrebic (fedratinib) binds and inhibits JAK2, FLT3, and RET kinases, which may inhibit cell proliferation and tumor growth (PMID: 17541402). Inrebic (fedratinib) is FDA approved for use in patients with myelofibrosis (FDA.gov). |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| Fedratinib | Inrebic | SAR302503|TG101348 | FLT3 Inhibitor 69 JAK2 Inhibitor - ATP competitive 15 RET Inhibitor 53 | Inrebic (fedratinib) binds and inhibits JAK2, FLT3, and RET kinases, which may inhibit cell proliferation and tumor growth (PMID: 17541402). Inrebic (fedratinib) is FDA approved for use in patients with myelofibrosis (FDA.gov). |
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| JAK2 V617F JAK2 G935R | hematologic cancer | resistant | Fedratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing the JAK2 V617F and JAK2 G935R double mutation demonstrated resistance to Inrebic (fedratinib) in culture (PMID: 21926964). | 21926964 |
| JAK2 V617F JAK2 R947Q | hematologic cancer | sensitive | Fedratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Inrebic (fedratinib) inhibited proliferation of a cell line expressing JAK2 V617F and R947Q in culture (PMID: 39091915). | 39091915 |
| JAK2 V617F JAK2 L902Q JAK2 E1028K | hematologic cancer | resistant | Fedratinib | Preclinical - Cell culture | Actionable | In a preclinical study, a cell line expressing JAK2 V617F, L902Q, and E1028K was resistant to Inrebic (fedratinib) in culture (PMID: 39091915). | 39091915 |
| JAK2 V617F JAK2 Q959H JAK2 L983F | hematologic cancer | sensitive | Fedratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Inrebic (fedratinib) inhibited Stat5 signaling and proliferation in a cell line expressing JAK2 V617F, L983F, and Q959H in culture (PMID: 39091915). | 39091915 |
| JAK2 V617F JAK2 Y931C JAK2 S1025C | Advanced Solid Tumor | resistant | Fedratinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing JAK2 V617F, Y931C and S1025C demonstrated resistance to Inrebic (fedratinib) treatment in culture (PMID: 26419724). | 26419724 |
| JAK2 V617F JAK2 I960V | hematologic cancer | resistant | Fedratinib | Preclinical - Cell culture | Actionable | In a preclinical study, immune cells expressing the JAK2 V617F and JAK2 I960V double mutation demonstrated resistance to Inrebic (fedratinib) in culture (PMID: 21926964). | 21926964 |
| JAK2 V617F JAK2 Q959H | hematologic cancer | sensitive | Fedratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Inrebic (fedratinib) inhibited proliferation of a cell line expressing JAK2 V617F and Q959H in culture (PMID: 39091915). | 39091915 |
| JAK2 V617F JAK2 R938E | hematologic cancer | sensitive | Fedratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Inrebic (fedratinib) inhibited proliferation of a cell line expressing JAK2 V617F and R938E in culture (PMID: 39091915). | 39091915 |
| JAK3 V718L | esophagus adenocarcinoma | sensitive | Fedratinib | Preclinical - Patient cell culture | Actionable | In a preclinical study, Inrebic (fedratinib) inhibited viability of cells derived from the brain metastases of a patient with esophagus adenocarcinoma harboring JAK3 V718L in culture (PMID: 38985431). | 38985431 |
| JAK2 rearrange | myeloid neoplasm | sensitive | Fedratinib | Guideline | Actionable | Inrebic (fendratinib) is included in guidelines for patients with a myeloid/lymphoid neoplasm with eosinophilia harboring a JAK2 rearrangement (NCCN.org). | detail... |
| JAK2 V617F JAK2 Y931C | hematologic cancer | resistant | Fedratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing the JAK2 V617F and JAK2 Y931C double mutation demonstrated resistance to Inrebic (fedratinib) in culture (PMID: 21926964). | 21926964 |
| JAK2 V617F JAK2 Y931C | hematologic cancer | resistant | Fedratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Inrebic (fedratinib) inhibited Stat5 signaling and proliferation in a cell line expressing JAK2 V617F and Y931C in culture (PMID: 39091915). | 39091915 |
| JAK2 V617F JAK2 L902Q | hematologic cancer | resistant | Fedratinib | Preclinical - Cell culture | Actionable | In a preclinical study, a cell line expressing JAK2 V617F and L902Q was resistant to Inrebic (fedratinib) in culture (PMID: 39091915). | 39091915 |
| JAK2 V617F JAK2 E985K | hematologic cancer | resistant | Fedratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing the JAK2 V617F and JAK2 E985K double mutation demonstrated resistance to Inrebic (fedratinib) in culture (PMID: 21926964). | 21926964 |
| JAK2 V617F JAK2 L983F | hematologic cancer | sensitive | Fedratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Inrebic (fedratinib) inhibited Stat5 signaling and proliferation in a cell line expressing JAK2 V617F and L983F in culture (PMID: 39091915). | 39091915 |
| JAK2 V617F | hematologic cancer | sensitive | Fedratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Inrebic (fedratinib) inhibited Stat5 signaling and proliferation in a cell line expressing JAK2 V617F in culture (PMID: 39091915). | 39091915 |
| JAK2 V617F JAK2 R938L | hematologic cancer | resistant | Fedratinib | Preclinical - Cell culture | Actionable | In a preclinical study, immune cells expressing the JAK2 V617F and JAK2 R938L double mutation demonstrated resistance to Inrebic (fedratinib) in culture (PMID: 21926964). | 21926964 |
| JAK2 V617F JAK2 Y931C JAK2 Y1045W | Advanced Solid Tumor | resistant | Fedratinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing JAK2 V617F, Y931C and Y1045W demonstrated resistance to Inrebic (fedratinib) treatment in culture (PMID: 26419724). | 26419724 |
| JAK2 V617F JAK2 L902Q JAK2 R947Q | hematologic cancer | resistant | Fedratinib | Preclinical - Cell culture | Actionable | In a preclinical study, a cell line expressing JAK2 V617F, L902Q, and R947Q was resistant to Inrebic (fedratinib) in culture (PMID: 39091915). | 39091915 |
| JAK2 V617F JAK2 Y931C JAK2 V1075F | Advanced Solid Tumor | resistant | Fedratinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing JAK2 V617F, Y931C and V1075F demonstrated resistance to Inrebic (fedratinib) treatment in culture (PMID: 26419724). | 26419724 |
| JAK2 V617F JAK2 M929I | hematologic cancer | predicted - sensitive | Fedratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing the JAK2 V617F and JAK2 M929I double mutation were sensitive to treatment with Inrebic (fedratinib) in culture, demonstrating growth inhibition (PMID: 21926964). | 21926964 |
| JAK2 R867Q | hematologic cancer | decreased response | Fedratinib | Preclinical - Cell culture | Actionable | In a preclinical study, immune cells expressing JAK2 R867Q demonstrated decreased response to Inrebic (fedratinib) in culture (PMID: 24398328). | 24398328 |
| JAK2 V617F JAK2 Y931C JAK2 F1061W | Advanced Solid Tumor | resistant | Fedratinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing JAK2 V617F, Y931C and F1061W demonstrated resistance to Inrebic (fedratinib) treatment in culture (PMID: 26419724). | 26419724 |
| JAK2 V617F JAK2 L902Q JAK2 R938E | hematologic cancer | resistant | Fedratinib | Preclinical - Cell culture | Actionable | In a preclinical study, a cell line expressing JAK2 V617F, L902Q, and R938E was resistant to Inrebic (fedratinib) in culture (PMID: 39091915). | 39091915 |
| JAK2 V617F JAK2 Y931C | Advanced Solid Tumor | sensitive | Fedratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Inrebic (fedratinib) treatment inhibited colony formation and proliferation of transformed cells expressing JAK2 V617F and Y931C in culture (PMID: 26419724). | 26419724 |
| JAK2 V617F JAK2 E1028K | hematologic cancer | sensitive | Fedratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Inrebic (fedratinib) inhibited proliferation of a cell line expressing JAK2 V617F and E1028K in culture (PMID: 39091915). | 39091915 |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|---|---|---|---|---|---|
| NCT03952039 | Phase III | Fedratinib | An Efficacy and Safety Study of Fedratinib Compared to Best Available Therapy in Subjects With DIPSS-intermediate or High-risk Primary Myelofibrosis, Post-polycythemia Vera Myelofibrosis, or Post-essential Thrombocythemia Myelofibrosis and Previously Treated With Ruxolitinib (FREEDOM2) | Active, not recruiting | POL | NLD | ITA | IRL | HUN | GBR | FRA | ESP | DEU | CZE | BEL | AUT | AUS | 3 |
| NCT05127174 | Phase Ib/II | Fedratinib | Maintenance Fedratinib to Prevent Post-Transplant Relapse in Myeloproliferative Neoplasms | Active, not recruiting | USA | 0 |
| NCT03755518 | Phase III | Fedratinib | An Efficacy and Safety Trial of Fedratinib in Subjects With DIPSS, Intermediate or High-Risk Primary Myelofibrosis, Post-Polycythemia Vera Myelofibrosis, or Post-Essential Thrombocythemia Myelofibrosis and Previously Treated With Ruxolitinib (FREEDOM) | Completed | USA | CAN | 0 |
| NCT05177211 | Phase II | Fedratinib | Fedratinib in Myelodysplastic /Myeloproliferative Neoplasms (MDS/MPNs) and Chronic Neutrophilic Leukemia (CNL) | Active, not recruiting | USA | 0 |
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