Momelotinib

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Momelotinib
Names
Other names
  • CYT-387
  • CYT-11387
  • GS-0387
  • Ojjaara
, Momelotinib hydrochloride hydrate (JAN JP), Momelotinib dihydrochloride (USAN US)
Clinical data
Routes of
use		By mouth
Legal
License data
Identifiers
PDB ligand
Chemical and physical data
FormulaC23H22N6O2
Molar mass414.469 g·mol−1
3D model (JSmol)
  • c1cc(ccc1c2ccnc(n2)Nc3ccc(cc3)N4CCOCC4)C(=O)NCC#N
  • 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

Momelotinib, sold under the brand name Ojjaara, is an anticancer medication used to treat myelofibrosis.[1] It is taken by mouth.[1]

Common side effects include include dizziness, fatigue, bacterial infection, hemorrhage, thrombocytopenia, diarrhea, and nausea.[4] It is a Janus kinase inhibitor.

Momelotinib was approved for medical use in the United States in 2023.[1][4][5] It was approved in the EU in 2024.[6]

Medical uses

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

Pharmacology

Momelotinib suppresses hepcidin expression in the liver leading to a rise in circulating iron and hemoglobin levels[7]

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).[8]

Society and culture

Legal status

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.[9] The applicant for this medicinal product is Glaxosmithkline Trading Services Limited.[9] The EU gave approval for Omjjara in January 2024.[10]

References

  1. ↑ 1.0 1.1 1.2 1.3 1.4 "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. ↑ "Omjjara EPAR". European Medicines Agency. 5 August 2011. Archived from the original on 13 March 2024. Retrieved 18 March 2024.
  3. ↑ "Omjjara Product information". Union Register of medicinal products. 26 January 2024. Archived from the original on 29 January 2024. Retrieved 18 March 2024.
  4. ↑ 4.0 4.1 4.2 "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. ↑ 5.0 5.1 "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. Archived from the original on 30 January 2024. Retrieved 30 January 2024.
  7. ↑ Chifotides, Helen T.; Bose, Prithviraj; Verstovsek, Srdan (19 January 2022). "Momelotinib: an emerging treatment for myelofibrosis patients with anemia". Journal of Hematology & Oncology. 15 (1): 7. doi:10.1186/s13045-021-01157-4. ISSN 1756-8722. Retrieved 19 July 2024.
  8. ↑ 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.
  9. ↑ 9.0 9.1 "Omjjara: Pending EC decision". European Medicines Agency (EMA). 10 November 2023. Archived from the original on 29 November 2023. Retrieved 5 December 2023.
  10. ↑ "GSK's Omjjara Authorized in EU for Treating Myelofibrosis With Anemia". MarketWatch. Archived from the original on 30 January 2024. Retrieved 30 January 2024.

External links

Identifiers:
  • 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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