Momelotinib

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]

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
CAS Number	1056634-68-4 as dihydrochloride: 1380317-28-1 1841094-17-4
3D model (JSmol)	Interactive image as dihydrochloride: Interactive image
ChEBI	CHEBI:91407
ChEMBL	ChEMBL1078178
ChemSpider	24676202
DrugBank	DB11763 as dihydrochloride: DBSALT003445
IUPHAR/BPS	7791
KEGG	D10315 as dihydrochloride: D10358 D10889
PubChem CID	25062766
UNII	6O01GMS00P as dihydrochloride: RBH995N496 LDX8893L5D
CompTox Dashboard (EPA)	DTXSID801026049
InChI 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
SMILES 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
Chemical formula	C23H22N6O2
Molar mass	414.469 g·mol−1
Pharmacology
ATC code	L01EJ04 (WHO)
Routes of administration	By mouth
Legal status	AU: S4 (Prescription only)[1][2] CA: ℞-only[3][4] US: ℞-only[5] EU: Rx-only[6][7]
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 names	Momelotinib hydrochloride hydrate (JAN JP), Momelotinib dihydrochloride (USAN US)
License data	US DailyMed: Momelotinib
Identifiers
PDB ligand	C87 (PDBe, RCSB PDB)
CompTox Dashboard (EPA)	DTXSID801026049

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

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

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).^[11]

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.^[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]