Ruxolitinib (Systemic)
Class: Antineoplastic Agents
VA Class: AN900
Chemical Name: (βR)-β-Cyclopentyl-4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazole-1-propanenitrile phosphate
Molecular Formula: C17H18N6•H3PO4
CAS Number: 1092939-17-7
Brands: Jakafi
Introduction
Antineoplastic agent; selective inhibitor of Janus kinase (JAK) 1 and 2.
Uses for Ruxolitinib (Systemic)
Intermediate- or High-Risk Myelofibrosis
Treatment of intermediate- or high-risk myelofibrosis, including primary myelofibrosis, post-polycythemia vera myelofibrosis, and post-essential thrombocythemia myelofibrosis (designated an orphan drug by FDA for this use).
Ruxolitinib (Systemic) Dosage and Administration
General
Perform CBC, including platelet count, prior to initiating therapy, every 2–4 weeks until dosage is stabilized, and then as clinically indicated.
Restricted Distribution Program
Must be obtained through the Incyte Connecting to Access, Reimbursement, Education, and Support (IncyteCARES) program.
Clinician and patient must jointly complete a prescription and reimbursement application. Following verification of prescription information and review of healthcare benefits, an authorized specialty pharmacy ships ruxolitinib directly to the patient.
To enroll in this program, call 855-452-5234 or visit [Web].
Administration
Oral Administration
Administer orally; take with or without food.
NG Tube
Disperse in approximately 40 mL of water, stir for approximately 10 minutes, and administer within 6 hours through an NG tube (8 French or larger) using an appropriate syringe. Following administration, rinse tube with approximately 75 mL of water.
Dosage
Available as ruxolitinib phosphate; dosage expressed in terms of ruxolitinib.
Adults
Intermediate- or High-Risk Myelofibrosis
Oral
Platelet count >200,000/mm3: Initially, 20 mg twice daily.
Platelet count 100,000–200,000/mm3: Initially, 15 mg twice daily.
Titrate dosage based on efficacy and safety. (See Dosage Modification for Thrombocytopenia and also Dosage Modification for Insufficient Clinical Response under Dosage and Administration.)
Dosage adjustment required if used concomitantly with a potent CYP3A4 inhibitor. (See Drugs Affecting Hepatic Microsomal Enzymes under Interactions.)
When discontinuing ruxolitinib for reasons other than thrombocytopenia, taper dosage gradually (e.g., by 5 mg twice daily on a weekly basis).
Dosage Modification for Thrombocytopenia
Interrupt treatment in patients with platelet counts <50,000/mm3.
Restart therapy or increase dosage following recovery of platelet counts to acceptable levels. When restarting therapy, use dosage at least 5 mg twice daily below the original dosage. For maximum dosages when restarting ruxolitinib, see Table 1.
