Therapy Detail
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| Therapy Name | Momelotinib |
| Synonyms | |
| Therapy Description |
Momelotinib (CYT387) is an ATP-competitive and selective inhibitor of JAK1 and JAK2, which inhibits cell proliferation and promotes apoptosis (PMID: 19295546, PMID: 31733040, PMID: 32394008). |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| Momelotinib | CYT387|CYT-387|GS-0387 | JAK1 Inhibitor - ATP competitive 5 JAK2 Inhibitor - ATP competitive 15 | Momelotinib (CYT387) is an ATP-competitive and selective inhibitor of JAK1 and JAK2, which inhibits cell proliferation and promotes apoptosis (PMID: 19295546, PMID: 31733040, PMID: 32394008). |
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| FLT3 exon 14 ins | acute myeloid leukemia | sensitive | Momelotinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Momelotinib (CYT387) inhibited proliferation of acute myeloid leukemia cell lines and patient-derived cells harboring FLT3-ITD mutations in culture, and resulted in prolonged survival and reduced leukemic burden in cell line xenograft models (PMID: 34768286). | 34768286 |
| JAK2 V617F JAK2 Y931C | hematologic cancer | resistant | Momelotinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing the JAK2 V617F and JAK2 Y931C double mutation demonstrated resistance to Momelotinib in culture (PMID: 21926964). | 21926964 |
| FLT3 exon 14 ins FLT3 Y842H | hematologic cancer | sensitive | Momelotinib | Preclinical - Cell culture | Actionable | In a preclinical study, Momelotinib (CYT387) decreased phosphorylation of Flt3 and Stat5 and inhibited proliferation of transformed cells expressing FLT3-ITD and FLT3 Y842H in culture (PMID: 34768286). | 34768286 |
| JAK2 V617F JAK2 G935R | hematologic cancer | resistant | Momelotinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing the JAK2 V617F and JAK2 G935R double mutation demonstrated resistance to Momelotinib in culture (PMID: 21926964). | 21926964 |
| FLT3 exon 14 ins FLT3 D839G | hematologic cancer | sensitive | Momelotinib | Preclinical - Cell culture | Actionable | In a preclinical study, Momelotinib (CYT387) decreased phosphorylation of Flt3 and Stat5 and inhibited proliferation of transformed cells expressing FLT3-ITD and FLT3 D839G in culture (PMID: 34768286). | 34768286 |
| JAK2 V617F JAK2 R938L | hematologic cancer | resistant | Momelotinib | Preclinical | Actionable | In a preclinical study, immune cells expressing the JAK2 V617F and JAK2 R938L double mutation demonstrated resistance to Momelotinib (CYT387) in culture (PMID: 21926964). | 21926964 |
| JAK2 V617F JAK2 M929I | hematologic cancer | predicted - sensitive | Momelotinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing the JAK2 V617F and JAK2 M929I double mutation were sensitive to treatment with Momelotinib in culture, demonstrating growth inhibition (PMID: 21926964). | 21926964 |
| JAK2 R867Q | hematologic cancer | decreased response | Momelotinib | Preclinical | Actionable | In a preclinical study, immune cells expressing JAK2 R867Q demonstrated decreased response to Momelotinib (CYT387) in culture (PMID: 24398328). | 24398328 |
| JAK2 L583_A586delinsS | hematologic cancer | resistant | Momelotinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing JAK2 L583_A586delinsS demonstrated resistance to inhibition of cell proliferation by Momelotinib (CYT387) in culture (PMID: 31697804). | 31697804 |
| JAK2 V617F | hematologic cancer | sensitive | Momelotinib | Preclinical - Cell culture | Actionable | In a preclinical study, Momelotinib (CYT387) inhibited proliferation of transformed cells expressing JAK2 V617F in culture (PMID: 34768286). | 34768286 |
| JAK2 V617F JAK2 I960V | hematologic cancer | resistant | Momelotinib | Preclinical | Actionable | In a preclinical study, immune cells expressing the JAK2 V617F and JAK2 I960V double mutation demonstrated resistance to Momelotinib in culture (PMID: 21926964). | 21926964 |
| JAK2 V617F JAK2 E985K | hematologic cancer | resistant | Momelotinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing the JAK2 V617F and JAK2 E985K double mutation demonstrated resistance to Momelotinib in culture (PMID: 21926964). | 21926964 |
| FLT3 exon 14 ins | hematologic cancer | sensitive | Momelotinib | Preclinical - Cell culture | Actionable | In a preclinical study, Momelotinib (CYT387) decreased phosphorylation of Flt3 and Stat5 and inhibited proliferation of transformed cells expressing a FLT3-ITD mutation in culture (PMID: 34768286). | 34768286 |
| FLT3 exon 14 ins FLT3 F691L FLT3 D835Y | hematologic cancer | resistant | Momelotinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing FLT3-ITD with FLT3 F691L and D835Y demonstrated resistance to Momelotinib (CYT387) in culture (PMID: 34768286). | 34768286 |
| FLT3 exon 14 ins FLT3 D835Y | hematologic cancer | sensitive | Momelotinib | Preclinical - Cell culture | Actionable | In a preclinical study, Momelotinib (CYT387) decreased phosphorylation of Flt3 and Stat5 and inhibited proliferation of transformed cells expressing FLT3-ITD and FLT3 D835Y in culture (PMID: 34768286). | 34768286 |
| FLT3 exon 14 ins FLT3 F691L | hematologic cancer | resistant | Momelotinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing FLT3-ITD and FLT3 F691L demonstrated resistance to Momelotinib (CYT387) in culture (PMID: 34768286). | 34768286 |
| CSF3R S783fs | chronic neutrophilic leukemia | predicted - resistant | Momelotinib | Preclinical - Patient cell culture | Actionable | In a preclinical study, cells derived from a patient with chronic neutrophilic leukemia harboring CSF3R S783fs did not respond to treatment with Momelotinib (CYT387) in culture (PMID: 23656643). | 23656643 |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|---|---|---|---|---|---|
| NCT02251821 | Phase II | Fludarabine Tacrolimus Mycophenolate mofetil Busulfan Pacritinib Momelotinib Melphalan Methotrexate Ruxolitinib Cyclophosphamide | JAK-2 Inhibitor Before Donor Stem Cell Transplant in Treating Patients With Primary or Secondary Myelofibrosis | Active, not recruiting | USA | 0 |
| NCT02244489 | Phase I | Capecitabine Oxaliplatin Momelotinib | Momelotinib Combined With Capecitabine and Oxaliplatin in Adults With Relapsed/Refractory Metastatic Pancreatic Ductal Adenocarcinoma | Terminated | USA | 0 |
| NCT02101021 | Phase II | Gemcitabine + Nab-paclitaxel Momelotinib | Gemcitabine and Nab-paclitaxel Combined With Momelotinib in Participants With Previously Untreated Metastatic Pancreatic Ductal Adenocarcinoma | Terminated | USA | 0 |
| NCT02258607 | Phase I | Momelotinib Momelotinib + Trametinib | Efficacy and Safety of Momelotinib and Momelotinib Combined With Trametinib in Adults With Metastatic KRAS-mutated Non-Small Cell Lung Cancer (NSCLC) Who Have Failed Platinum-Based Chemotherapy Preceded by a Dose-finding Lead-in Phase | Terminated | USA | 0 |
| NCT03441113 | Phase II | Momelotinib | Extended Access of Momelotinib in Adults With Myelofibrosis | Active, not recruiting | USA | ROU | POL | NLD | ITA | ISR | HUN | GBR | FRA | ESP | DNK | DEU | CAN | BGR | BEL | AUT | AUS | 3 |
| NCT04173494 | Phase III | Danazol Momelotinib | A Study of Momelotinib Versus Danazol in Symptomatic and Anemic Myelofibrosis Patients (MOMENTUM) | Completed | USA | SWE | ROU | POL | NZL | ITA | ISR | HUN | GBR | FRA | ESP | DNK | DEU | CZE | CAN | BGR | BEL | AUT | AUS | 3 |
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