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ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › PROTEIN KINASE INHIBITORS › Janus-associated kinase (JAK) inhibitors
pacritinib
L01EJ03
Adult Dosing
- Myelofibrosis: 200 mg orally twice daily with or without food
Pediatric Dosing
- Safety and efficacy in pediatric patients have not been established
Indications
- Treatment of adult patients with intermediate- or high-risk myelofibrosis (primary, post-polycythemia vera, or post-essential thrombocythemia) with a platelet count <50 x 10^9/L
Mechanism of Action
- Kinase inhibitor with specificity for Janus kinase 2 (JAK2) and FMS-like tyrosine kinase 3 (FLT3)
- Inhibits signaling of cytokines and growth factors critical for hematopoiesis and immune function
Contraindications
- Concomitant use of strong CYP3A4 inhibitors or inducers
- Known hypersensitivity to pacritinib or any of its components
Adverse Reactions
- Diarrhea
- Thrombocytopenia
- Nausea
- Peripheral edema
- Anemia
- Dizziness
- Hemorrhage
- QT prolongation
Drug Interactions
- Strong or moderate CYP3A4 inhibitors (increase pacritinib exposure)
- Strong or moderate CYP3A4 inducers (decrease pacritinib efficacy)
- CYP3A4 substrates with narrow therapeutic indices
- Drugs that prolong the QT interval
Curated Content: Needs Vetting Before Put to Clinical Use