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Ruxolitinib

JAKAFI

Pronunciation: rux-oe-LI-ti-nib (JAK-a-fye)

Ruxolitinib ballicule: receptor binding, kinetics and half-life diagram
Mechanism of action: Ruxolitinib ballicule

What it isJAK1/JAK2 inhibitor; myelofibrosis, polycythemia vera, and graft-versus-host disease.

Why this oneUnlike conventional cytoreductive drugs, it rapidly reduces splenomegaly and constitutional symptoms in myelofibrosis.

What limits itMyelosuppression makes platelets and hemoglobin central to dosing. Abrupt withdrawal can provoke a cytokine-rebound syndrome.

Ruxolitinib molecular structure (skeletal formula)
Molecular structure: Ruxolitinib

Ruxolitinib prescription history

Animated chart of estimated U.S. prescriptions per year, Tyrosine kinase inhibitors (2001–2026). Ruxolitinib enters in 2011 (estimated).

FDA-approved for

Off-label

Principal riskMyelosuppression; cytokine rebound on abrupt withdrawal

Classes and tags

Clinical profile

Therapeutic safety burden3 / 4
Overdose danger2 / 4
Weight-gain liability0 / 4
Sedation liability0 / 4
QT / Torsades0 / 4
Direct muscarinic antagonism0 / 4
Embryofetal risk3 / 4

Legacy pregnancy categoryD

Defining liabilityMyelosuppression and agent-specific hepatic, cardiac, pulmonary, neurologic or reproductive toxicity require oncology monitoring.

FDA label

NO BOXED WARNINGS

FDA dosingPopulationStartTargetMax
MyelofibrosisAdultsPlatelet-based: >200 x10^9/L → 20 mg BID (XR 44 mg QD); 100–200 → 15 mg BID (XR 33 mg QD); 50–<100 → 5 mg BID (XR 11 mg QD)titrate by safety/efficacy25 mg BID
Polycythemia veraAdults10 mg BID (XR 22 mg QD)titrate by safety/efficacy—
Acute graft-versus-host diseaseAdults and pediatric patients5 mg BID (XR 11 mg QD)titrate by safety/efficacy—
Chronic graft-versus-host diseaseAdults and pediatric patients10 mg BID (XR 22 mg QD)titrate by safety/efficacy—

Renal Reduce starting dose or avoid treatment per renal-function recommendations (indication/platelet-based).

Hepatic Reduce starting dose or avoid treatment per hepatic recommendations.

Doses are individualized and modified for thrombocytopenia/neutropenia per label tables.

Instructions

Available strengths

Cautions

Adverse reactions

Pregnancy No human data; animal studies show adverse developmental outcomes at maternally toxic doses.

Lactation Advise not to breastfeed during treatment.

Cost

Ruxolitinib (JAKAFI)
Strength#/mogeneric $/moCostPlus
5 mgtab60 BIDnot offered
10 mgtab60 BIDnot offered
15 mgtab60 BIDnot offered
20 mgtab60 BIDnot offered
25 mgtab60 BIDnot offered
11 mgER tab60 BIDnot offered
22 mgER tab60 BIDnot offered
33 mgER tab60 BIDnot offered
44 mgER tab60 BIDnot offered
55 mgER tab60 BIDnot offered
NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Ruxolitinib is dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.

Generic entry2041 est.

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