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ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › PROTEIN KINASE INHIBITORS › Janus-associated kinase (JAK) inhibitors
ruxolitinib
L01EJ01
Forms & Strengths
- Oral tablets: 5 mg, 10 mg, 15 mg, 20 mg
- Topical cream: 1.5%
Adult Dosing
- Myelofibrosis: 15-20 mg PO BID based on baseline platelet count
- Polycythemia vera: 10 mg PO BID
- Acute graft-versus-host disease: 5 mg PO BID
- Chronic graft-versus-host disease: 10 mg PO BID
- Atopic dermatitis (topical): Apply thin layer BID up to 20% BSA
Pediatric Dosing
- Acute graft-versus-host disease (>=12 years): 5 mg PO BID
- Chronic graft-versus-host disease (>=12 years): 10 mg PO BID
- Atopic dermatitis (>=12 years, topical): Apply thin layer BID up to 20% BSA
Indications
- Intermediate or high-risk myelofibrosis
- Polycythemia vera resistant to or intolerant of hydroxyurea
- Acute graft-versus-host disease steroid-refractory
- Chronic graft-versus-host disease after failure of 1 or 2 lines of therapy
- Atopic dermatitis short-term and intermittent long-term therapy (topical)
Mechanism of Action
- Selective Janus kinase (JAK) inhibitor with high selectivity for JAK1 and JAK2
- Inhibits JAK-STAT signaling pathway, reducing proliferation and inducing apoptosis in malignant cells
- Downregulates inflammatory cytokine production involved in myeloproliferative neoplasms and GVHD
Contraindications
- Severe hepatic impairment
- Active serious infection
- Known hypersensitivity to ruxolitinib
Adverse Reactions
- Thrombocytopenia
- Anemia
- Neutropenia
- Weight gain
- Dizziness
- Headache
- Herpes zoster reactivation
- Urinary tract infections
- Increased risk of malignancies (non-melanoma skin cancer)
Drug Interactions
- Strong CYP3A4 inhibitors (e.g., ketoconazole): Reduce ruxolitinib dose
- Dual CYP3A4 and CYP2C9 inhibitors: Reduce ruxolitinib dose
- Strong CYP3A4 inducers (e.g., rifampin): May decrease ruxolitinib efficacy
- Immunosuppressants: Increased risk of severe infections
Curated Content: Needs Vetting Before Put to Clinical Use