N- (cyanomethyl)- 4- (2- ((4- (4- morpholinyl)phenyl)amino)- 4- pyrimidinyl)benzamide

01/01/2017 - "Momelotinib is a potent inhibitor of JAK1 and JAK2 that demonstrated efficacy in patients with primary and secondary myelofibrosis. "
06/01/2013 - "Safety and efficacy of CYT387, a JAK1 and JAK2 inhibitor, in myelofibrosis."
07/25/2023 - "Momelotinib long-term safety and survival in myelofibrosis: integrated analysis of phase 3 randomized controlled trials."
01/01/2023 - "Symptomatic benefit of momelotinib in patients with myelofibrosis: Results from the SIMPLIFY phase III studies."
01/01/2023 - "We retrospectively reviewed 72 anemic patients with myelofibrosis (MF; median age 68 years), who were JAK2 inhibitor-naïve at the time of study entry to a phase-1/2 momelotinib clinical trial. "

01/01/2023 - "The current study suggests a short-term survival benefit associated with anemia response in momelotinib-treated patients with MF."
01/01/2022 - "MOMENTUM is an international registration-track phase 3 trial further assessing momelotinib's unique constellation of anemia and other benefits in second-line MF patients; the results of the MOMENTUM trial are keenly awaited and may lead to regulatory approval of momelotinib."
06/01/2017 - "The data from the pivotal trials of momelotinib do not support its approval, although improvement of anemia is an important benefit. "
02/01/2017 - "The JAK1/2 inhibitor momelotinib unexpectedly resulted in reduction of anemia in MF patients during Phase I/II trials. "
04/01/2023 - "Momelotinib may be particularly well suited for patients with significant anemia and novel combination treatments in clinical development may improve the depth and duration of spleen responses. "

01/01/2021 - "In subsequent in vivo experiments, we found that CYT387 inhibited subcutaneous nude mouse tumor growth but had little impact on intracranial orthotopic xenografts, probably due to a limited ability to penetrate the blood-brain barrier (BBB). "
01/01/2021 - "We discovered that CYT387 restrained malignant tumor progression by activating the Hippo pathway in vitro. "
10/15/2019 - "The antiapoptotic, prometastatic JAK-STAT3 pathway was activated in chemoresistant tumors, and treatment with the JAK1/JAK2 inhibitor CYT387 reduced progression of chemoresistant tumors and increased survival. "
03/30/2018 - "The other 50% of mice that developed tumors with ongoing momelotinib treatment also showed significantly increased survival benefit and a smaller tumor burden. "
01/01/2018 - "Momelotinib is a potent and selective small-molecule inhibitor of JAK1/2 that is under investigation for the treatment of myeloproliferative neoplasms. "

11/01/2023 - "In summary, momelotinib represents a safe and effective treatment option for patients with MF and moderate-to-severe thrombocytopenia."
11/01/2023 - "Momelotinib in Myelofibrosis Patients With Thrombocytopenia: Post Hoc Analysis From Three Randomized Phase 3 Trials."
09/01/2023 - "The most common non-haematological treatment-emergent adverse events in momelotinib-treated patients over the entire study period as of the data cutoff were diarrhoea (45 [26%] of 171) and asthenia (28 [16%]); the most common grades 3-4 treatment-emergent adverse events were thrombocytopenia (33 [19%]) and anaemia (19 [11%]). "
02/01/2018 - "The most common grade 3 or worse adverse events were anaemia (14 [14%] of 104 in the momelotinib group vs seven [14%] of 52 in the BAT group), thrombocytopenia (seven [7%] vs three [6%]), and abdominal pain (one [1%] vs three [6%]). "
01/01/2023 - "The most frequent grade 3 or higher treatment-emergent adverse events with momelotinib and danazol were haematological abnormalities by laboratory values: anaemia (79 [61%] of 130 vs 49 [75%] of 65) and thrombocytopenia (36 [28%] vs 17 [26%]). "

01/01/2022 - "Momelotinib, an inhibitor of ACVR1/ALK2, JAK1 and JAK2, demonstrated activity against anemia, symptoms, and splenomegaly in the phase 3 SIMPLIFY trials. "
01/01/2020 - "Momelotinib (MMB) is a JAK1/2 and ACVR1 inhibitor with demonstrated clinical activity in all 3 hallmarks of myelofibrosis (MF): anemia, constitutional symptoms, and splenomegaly. "
12/01/2020 - "Momelotinib does not appear to have an advantage over ruxolitinib with regards to improving splenomegaly in intermediate-/high-risk JAK-inhibitor naive myelofibrosis. "
05/01/2012 - "At present, we have a new generation of inhibitors of JAK2 (Ruxolitinib, CYT387, SB1518, TG101348, with others in development), which have been shown to improve splenomegaly, improve symptomatic burden of illness and improve quality of life. "
07/25/2023 - "Momelotinib is the first inhibitor of Janus kinase 1 (JAK1) and JAK2 shown to also inhibit activin A receptor type 1 (ACVR1), a key regulator of iron homeostasis, and has demonstrated improvements in splenomegaly, constitutional symptoms, and anemia in myelofibrosis (MF). "