Contents

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
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	US: ℞-only[1] EU: Rx-only[2][3]
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa). Infobox references

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.^[4]

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

Medical uses[edit]

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

Pharmacology[edit]

Pharmacodynamics[edit]

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[edit]

Legal status[edit]

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] The EU gave approval for Omjjara in January 2024.^[9]

References[edit]

^ ^{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. This article incorporates text from this source, which is in the public domain.

^ ^{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. This article incorporates text from this source, which is in the public domain.

External links[edit]

• 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