Drug reference

Ruxolitinib

Immunosuppressant · Targeted therapy responsive malignancy

Also known as Jakavi, Ruxolitinib phosphate

ImmunosuppressantTargeted therapy responsive malignancy

CDSCO approvedSchedule H

EXCRETION

—

not curated

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

Avoid—toxicity in animal studies. Contraceptive advice required.

FDA category + note

Top interactionssee all 12 →

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Mechanism

Ruxolitinib is a selective inhibitor of the Janus-associated tyrosine kinases JAK1 and JAK2. It blocks signaling through common cytokine receptors and attenuates signaling by pro-inflammatory cytokines.

Indications

Disease-related splenomegaly or symptoms in patients with primary myelofibrosis, post-polycythaemia vera myelofibrosis, or post-essential thrombocythaemia myelofibrosis (specialist use only)Polycythaemia vera in patients resistant to, or intolerant of, hydroxyurea (specialist use only)rheumatoid arthritisgraft-versus-host diseasemyelofibrosispolycythemia verapolycythemia vera (inadequate response to hydroxyurea)steroid-refractory, acute graft-versus-host disease (>12 years of age)Atypical Chronic Myeloid Leukemia (limited efficacy)PCM1::JAK2 or BCR::JAK2 or other JAK2 partners fusionHemophagocytic Lymphohistiocytosis (HLH)

Dosing

Adult: Consult product literature or local protocols
Renal adjustment: Reduce dose in severe impairment (consult product literature)
Hepatic adjustment: Manufacturer advises caution; initial dose reduction—consult product literature

Pharmacokinetics

Half-life

3 h (elimination)

Bioavailability

95% (oral)

Metabolism

hepatic CYP3A4

Excretion

largely in the urine (products)

Contraindications

Active serious infections (do not initiate treatment until resolved)
nonuse during breastfeeding
concurrent use of live vaccines

Side effects

Common

Anaemiabruisingconstipationdizzinessdyslipidaemiaflatulencehaemorrhageheadachehypertensionincreased risk of infectionneutropeniathrombocytopeniaweight increasedanemiaincreased risk of infections (upper respiratory, sinus, common cold, hepatitis c virus)

Serious

Intracranial haemorrhage
sepsis
progressive multifocal leucoencephalopathy
Tuberculosis
increased risk of serious bacterial, fungal, viral, and opportunistic infections leading to hospitalization or death
higher rate of all-cause mortality, including sudden cardiovascular death
higher rate of certain cancers
higher rate of thrombosis, cardiovascular death, myocardial infarction, and stroke
basal cell carcinoma
squamous cell skin carcinoma