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momelotinib (Ojjaara)
Indications:
- treatment of myelofibrosis
Contraindications:
- do not initiate in patients with active infection
- pregnancy: may cause fetal harm
- lactation: breastfeeding not recommended
Dosage: 200 mg PO QD with or without food*
Tablets: 100, 150, 200 mg
* reduced starting dose to 150 mg if severe hepatic impairment
Monitor:
- liver function tests prior to initiation & periodically durinng treatment
Pharmacokinetics:
- metabolized by multiple cytochrome P450 enzymes including: CYP3A4 (36%), CYP2C8 (19%), CYP2C9 (17%), CYP2C19 (19%), & CYP1A2 (9%)
- M21 is an active metabolite with 40% activity of momelotinib
- M21 is formed by CYP followed by aldehyde oxidase metabolism
- 1/2life of momelotinib & M21 is 4-8 hours
Adverse effects:
- bacterial infection
- thrombocytopenia*, neutropenia (reduce dose)
- hepatotoxicity
- major cardiovascular events
- thrombosis
- secondary malignancy, especially smokers
- hemorrhage*
- fatigue*, dizziness*
- nausea*, diarrhea*
* common, >= 20%
Mechanism of action:
- inhibition of JAK1 & JAK2
- inhibition of activin A receptor, type 1 [1]
- inhibits STAT3 phosphorylation
Interactions
drug adverse effects of tyrosine kinase inhibitor(s)
General
Janus kinase inhibitor; JAK inhibitor
References
- Tefferi A, Pardanani A, Gangat N.
Momelotinib (JAK1/JAK2/ACVR1 inhibitor): mechanism of action, clinical trial
reports, and therapeutic prospects beyond myelofibrosis.
Haematologica. 2023 Mar 2.
PMID: 36861402 Free article.
- Highlights of Prescribing Information
OJJAARA (momelotinib) tablets, for oral use
https://gskpro.com/content/dam/global/hcpportal/en_US/Prescribing_Information/Ojjaara/pdf/OJJAARA-PI-PIL.PDF