Therapy Detail

Therapy Name Momelotinib
Therapy Description

Momelotinib (CYT387) is an ATP-competitive and selective inhibitor of JAK1 and JAK2, which inhibits cell proliferation and promotes apoptosis (PMID: 19295546).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
Momelotinib CYT387 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).
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
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
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 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
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 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
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
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
NCT02244489 Phase I Capecitabine Oxaliplatin Momelotinib Momelotinib Combined With Capecitabine and Oxaliplatin in Adults With Relapsed/Refractory Metastatic Pancreatic Ductal Adenocarcinoma Terminated
NCT02101021 Phase II Nab-paclitaxel + Gemcitabine Momelotinib Gemcitabine and Nab-paclitaxel Combined With Momelotinib in Participants With Previously Untreated Metastatic Pancreatic Ductal Adenocarcinoma Terminated