Overview

Generic Name(s):
momelotinib
NCI Definition [1]:
An orally bioavailable small-molecule inhibitor of Janus kinases 1 and 2 (JAK1/2) with potential antineoplastic activity. JAK1/2 inhibitor CYT387 competes with JAK1/2 for ATP binding, which may result in inhibition of JAK1/2 activation, inhibition of the JAK-STAT signaling pathway, and so the induction of apoptosis and a reduction of tumor cell proliferation in JAK1/2-expressing tumor cells. JAK2 is the most common mutated gene in bcr-abl-negative myeloproliferative disorders; the JAK2V617F gain-of-function mutation involves a valine-to-phenylalanine modification at position 617. The JAK-STAT signaling pathway is a major mediator of cytokine activity and is often dysregulated in a variety of tumor cell types.

Momelotinib has been investigated in 1 clinical trial, of which 1 is open and 0 are closed. Of the trial investigating momelotinib, 1 is phase 3 (1 open).

KMT2A Fusion, KMT2A-AFF1 Fusion, and KMT2A-ELL Fusion are the most frequent biomarker inclusion criteria for momelotinib clinical trials.

Myelofibrosis transformation in essential thrombocythemia, polycythemia vera, post-polycythemic myelofibrosis phase, and primary myelofibrosis are the most common diseases being investigated in momelotinib clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Momelotinib
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating momelotinib and the cancer types associated with these biomarkers. These numbers are derived from a set of 5,956 clinical trials for which biomarker status defines treatment.

Drug Details

Synonyms [2]:
cyt387, cyt-387, momelotinib, cyt 387, n-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide, momelotinib, gs-0387, jak1/2 inhibitor cyt387, n-(cyanomethyl)-4-(2-((4-(morpholin-4-yl)phenyl)amino)pyrimidin-4-yl)benzamide
Drug Categories [2]:
JAK inhibitors, Tyrosine kinase inhibitors
Drug Target(s) [2]:
JAK1, JAK2
NCIT ID [1]:
C88311

References

1. National Cancer Institute. NCI Thesaurus Version 18.11d. https://ncit.nci.nih.gov/ncitbrowser/. [2018-07-30] [2018-08-02].

2. All assertions and clinical trial landscape data are curated from primary sources. You can read more about the curation process here.