Momelotinib for the treatment of myelofibrosis.
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Xu L, Feng J, Gao G, Tang H
Momelotinib for the treatment of myelofibrosis.
Expert Opin Pharmacother. 2019 Nov;20(16):1943-1951. doi: 10.1080/14656566.2019.1657093. Epub 2019 Aug 26.
- PubMed ID
- 31450973 [ View in PubMed]
- Abstract
Introduction: The abnormally activated JAK-STAT pathway plays a central role in the pathogenesis of BCR/ABL-negative myeloproliferative neoplasms (MPNs), simultaneously providing a theoretical and clinical basis for the development of small-molecule compounds targeting JAK. The first approved drug, ruxolitinib, demonstrated a rapid and durable improvement of symptoms and splenomegaly accompanied with better overall survival in myelofibrosis (MF) patients. However, ruxolitinib-related adverse effects and resistance are limitations, so there is an urgent need to develop new JAK inhibitors to retain the efficacy of ruxolitinib and avoid its deficiency. Areas covered: This review discusses the preclinical and clinical studies of momelotinib (MMB) aiming to gain a deeper understanding of the advantages and clinical limitations of this drug. Expert opinion: The clinical trial data available thus far indicate that MMB is not inferior to ruxolitinib in spleen response and symptoms response, with the improvement of anemia surprising. The only obstacle that may slowdown its approval is treatment-emerged peripheral neuropathy (PN). If we can minimize MMB's treatment-related PN by administration optimization, MMB promises to be a good choice of individualized treatment for MF patients mainly manifesting as anemia.
DrugBank Data that Cites this Article
- Drugs
- Drug Targets
Drug Target Kind Organism Pharmacological Action Actions Momelotinib Activin receptor type-1 Protein Humans UnknownInhibitorDetails Momelotinib Non-receptor tyrosine-protein kinase TYK2 Protein Humans UnknownInhibitorDetails Momelotinib Tyrosine-protein kinase JAK1 Protein Humans YesInhibitorDetails Momelotinib Tyrosine-protein kinase JAK2 Protein Humans YesInhibitorDetails Momelotinib Tyrosine-protein kinase JAK3 Protein Humans UnknownInhibitorDetails