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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
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
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 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
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
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 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
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 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
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
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 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 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 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
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
JAK3 V718L esophagus adenocarcinoma sensitive Momelotinib Preclinical - Patient cell culture Actionable In a preclinical study, Momelotinib (CYT387) inhibited viability of cells derived from the brain metastases of a patient with esophagus adenocarcinoma harboring JAK3 V718L in culture (PMID: 38985431). 38985431
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
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
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
NCT02244489 Phase I Capecitabine Oxaliplatin Momelotinib Momelotinib Combined With Capecitabine and Oxaliplatin in Adults With Relapsed/Refractory Metastatic Pancreatic Ductal Adenocarcinoma 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
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
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


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