Momelotinib

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Momelotinib
Names
Preferred IUPAC name
N-(Cyanomethyl)-4-{2-[4-(morpholin-4-yl)anilino]pyrimidin-4-yl}benzamide
Other names
  • CYT-387
  • CYT-11387
  • GS-0387
  • Ojjaara
  • Omjjara
Identifiers
3D model (JSmol)
ChEBI
ChEMBL
ChemSpider
DrugBank
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KEGG
UNII
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  • InChI=1S/C23H22N6O2/c24-10-12-25-22(30)18-3-1-17(2-4-18)21-9-11-26-23(28-21)27-19-5-7-20(8-6-19)29-13-15-31-16-14-29/h1-9,11H,12-16H2,(H,25,30)(H,26,27,28)
    Key: ZVHNDZWQTBEVRY-UHFFFAOYSA-N
  • c1cc(ccc1c2ccnc(n2)Nc3ccc(cc3)N4CCOCC4)C(=O)NCC#N
  • as dihydrochloride: Cl.Cl.O=C(NCC#N)C1=CC=C(C=C1)C1=NC(NC2=CC=C(C=C2)N2CCOCC2)=NC=C1
Properties
C23H22N6O2
Molar mass 414.469 g·mol−1
Pharmacology
L01EJ04 (WHO)
By mouth
Legal status
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
Momelotinib
Clinical data
Other namesMomelotinib hydrochloride hydrate (JAN JP), Momelotinib dihydrochloride (USAN US)
License data
Identifiers
PDB ligand
E number{{#property:P628}}
CompTox Dashboard (EPA)
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Momelotinib, sold under the brand name Ojjaara among others, is an anticancer medication used for the treatment of myelofibrosis.[5] It is a Janus kinase inhibitor and it is taken by mouth.[5]

The most common adverse reactions include dizziness, fatigue, bacterial infection, hemorrhage, thrombocytopenia, diarrhea, and nausea.[8]

Momelotinib was approved for medical use in the United States in September 2023,[5][8][9] and in the European Union in January 2024.[6][10]

Medical uses

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Momelotinib is indicated for the treatment of intermediate or high-risk myelofibrosis in adults with anemia.[5][8][9]

Pharmacology

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Pharmacodynamics

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It is an inhibitor of Janus kinases JAK1 and JAK2, acting as an ATP competitor with IC50 values of 11 and 18 nM, respectively. The inhibitor is significantly less active towards other kinases, including JAK3 (IC50 = 0.16 μM).[11]

Society and culture

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In November 2023, the Committee for Medicinal Products for Human Use (CHMP) of the European Medicines Agency (EMA) adopted a positive opinion, recommending the granting of a marketing authorization for the medicinal product Omjjara, intended for the treatment of disease-related splenomegaly or symptoms in adults with moderate-to-severe anemia who have primary myelofibrosis, post-polycythaemia vera myelofibrosis or post-essential thrombocythaemia myelofibrosis.[12] The applicant for this medicinal product is Glaxosmithkline Trading Services Limited.[12] Momelotinib was approved for medical use in the European Union in January 2024.[6][7]

References

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  • Clinical trial number NCT04173494 for "A Study of Momelotinib Versus Danazol in Symptomatic and Anemic Myelofibrosis Patients (MOMENTUM)" at ClinicalTrials.gov
  • Clinical trial number NCT01969838 for "Momelotinib Versus Ruxolitinib in Subjects With Myelofibrosis (Simplify 1)" at ClinicalTrials.gov

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