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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). |
Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
---|---|---|---|---|
Momelotinib | CYT387|CYT-387|GS-0387 | JAK1 Inhibitor - ATP competitive 4 JAK2 Inhibitor - ATP competitive 14 | 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). |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|
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 |
BCOR mut RUNX1 mut | acute myeloid leukemia | predicted - sensitive | Momelotinib | Preclinical - Patient cell culture | Actionable | In a preclinical study, co-occurrence of BCOR and RUNX1 mutations correlated with sensitivity to Momelotinib (CYT387) in patient-derived acute myeloid leukemia samples in an ex vivo assay (PMID: 30333627). | 30333627 |
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 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 |
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 |
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 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 |
CEBPA mutant | acute myeloid leukemia | predicted - sensitive | Momelotinib | Preclinical - Patient cell culture | Actionable | In a preclinical study, patient-derived acute myeloid leukemia (AML) cells harboring biallelic CEBPA mutations demonstrated increased sensitivity to Momelotinib (CYT387) compared to control AML cells in culture (PMID: 27034432). | 27034432 |
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 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 |
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 |
Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
---|---|---|---|---|---|---|
NCT04173494 | Phase III | Danazol Momelotinib | A Study of Momelotinib Versus Danazol in Symptomatic and Anemic Myelofibrosis Patients (MOMENTUM) | Recruiting | USA | CAN | 19 |
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 |
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 |
NCT02244489 | Phase I | Capecitabine Oxaliplatin Momelotinib | Momelotinib Combined With Capecitabine and Oxaliplatin in Adults With Relapsed/Refractory Metastatic Pancreatic Ductal Adenocarcinoma | Terminated | USA | 0 |
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 | Recruiting | USA | 0 |