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
Identifiers
3D model (JSmol)
ChEBI
ChEMBL
ChemSpider
DrugBank
KEGG
UNII
  • 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
None
By mouth
Legal status
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
Infobox references
Momelotinib
Clinical data
Other namesMomelotinib hydrochloride hydrate (JAN JP), Momelotinib dihydrochloride (USAN US)
License data
Identifiers
PDB ligand

Momelotinib, sold under the brand name Ojjaara, is an anticancer medication used for the treatment of myelofibrosis.[1] It is a Janus kinase inhibitor and it is taken by mouth.[1]

The most common adverse reactions include dizziness, fatigue, bacterial infection, hemorrhage, thrombocytopenia, diarrhea, and nausea.[2]

Momelotinib was approved for medical use in the United States in September 2023.[1][2][3] In November 2023, momelotinib has received a positive opinion from Europe's CHMP for use in myelofibrosis patients with anemia.[4]

Medical uses

Momelotinib is indicated for the treatment of intermediate or high-risk myelofibrosis in adults with anemia.[1][2][3]

Pharmacology

Pharmacodynamics

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).[5]

References

  1. 1 2 3 4 5 "Ojjaara- momelotinib tablet". DailyMed. U.S. National Library of Medicne. 15 September 2023. Retrieved 20 September 2023.
  2. 1 2 3 "FDA Roundup: September 19, 2023". U.S. Food and Drug Administration (FDA) (Press release). 19 September 2023. Retrieved 20 September 2023. Public Domain This article incorporates text from this source, which is in the public domain.
  3. 1 2 "Novel Drug Approvals for 2023". U.S. Food and Drug Administration (FDA). 15 September 2023. Retrieved 20 September 2023. Public Domain This article incorporates text from this source, which is in the public domain.
  4. ↑ "GSK receives positive CHMP opinion recommending momelotinib for myelofibrosis patients with anaemia | GSK". www.gsk.com. 13 November 2023. Retrieved 30 November 2023.
  5. ↑ Pardanani A, Lasho T, Smith G, Burns CJ, Fantino E, Tefferi A (August 2009). "CYT387, a selective JAK1/JAK2 inhibitor: in vitro assessment of kinase selectivity and preclinical studies using cell lines and primary cells from polycythemia vera patients". Leukemia. 23 (8): 1441–1445. doi:10.1038/leu.2009.50. PMID 19295546. S2CID 26947444.
  • 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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