Momelotinib

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
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
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
CompTox Dashboard (EPA)

Momelotinib, sold under the brand name Ojjaara among others, 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.[4]

Momelotinib was approved for medical use in the United States in September 2023,[1][4][5] and in the European Union in January 2024.[2][6]

Medical uses

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Momelotinib is indicated for the treatment of intermediate or high-risk myelofibrosis in adults with anemia.[1][4][5]

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).[7]

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.[8] The applicant for this medicinal product is Glaxosmithkline Trading Services Limited.[8] Momelotinib was approved for medical use in the European Union in January 2024.[2][3]

References

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  1. ^ a b c d e "Ojjaara- momelotinib tablet". DailyMed. U.S. National Library of Medicine. 15 September 2023. Archived from the original on 30 November 2023. Retrieved 20 September 2023.
  2. ^ a b c "Omjjara EPAR". European Medicines Agency. 5 August 2011. Retrieved 18 March 2024.
  3. ^ a b "Omjjara Product information". Union Register of medicinal products. 26 January 2024. Retrieved 18 March 2024.
  4. ^ a b c "FDA Roundup: September 19, 2023". U.S. Food and Drug Administration (FDA) (Press release). 19 September 2023. Archived from the original on 21 September 2023. Retrieved 20 September 2023. Public Domain This article incorporates text from this source, which is in the public domain.
  5. ^ a b "Novel Drug Approvals for 2023". U.S. Food and Drug Administration (FDA). 15 September 2023. Archived from the original on 21 January 2023. Retrieved 20 September 2023. Public Domain This article incorporates text from this source, which is in the public domain.
  6. ^ "GSK's Omjjara Authorized in EU for Treating Myelofibrosis With Anemia". MarketWatch. Retrieved 30 January 2024.
  7. ^ 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.
  8. ^ a b "Omjjara: Pending EC decision". European Medicines Agency (EMA). 10 November 2023. Archived from the original on 29 November 2023. Retrieved 5 December 2023.
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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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