Ruxolitinib

JAKAFI

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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

FDA-approved for

myelofibrosis (2011)
polycythemia vera, graft-versus-host disease

Off-label

steroid-refractory graft-versus-host disease beyond label
vitiligo (topical form is approved)

FDA label

Read the full label on DailyMed ↗

FDA dosing	Population	Start	Target	Max
Myelofibrosis	Adults	Platelet-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/efficacy	25 mg BID
Polycythemia vera	Adults	10 mg BID (XR 22 mg QD)	titrate by safety/efficacy	—
Acute graft-versus-host disease	Adults and pediatric patients	5 mg BID (XR 11 mg QD)	titrate by safety/efficacy	—
Chronic graft-versus-host disease	Adults and pediatric patients	10 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

JAKAFI (IR) taken twice daily; JAKAFI XR taken once daily; XR tablets swallowed whole
Perform CBC before starting and every 2–4 weeks until doses are stabilized
Do not interrupt/discontinue abruptly — use supportive care and consider resuming to avoid symptom exacerbation
Screen for infections (TB, HBV, HSV, herpes zoster) before starting

Available strengths

tab 5, 10, 15, 20, 25 mg
ER tab 11, 22, 33, 44, 55 mg
cream 1.5 %

Cautions

Thrombocytopenia, anemia, neutropenia
Serious infections (bacterial, mycobacterial/TB, fungal, viral; HBV reactivation)
Symptom exacerbation on interruption/discontinuation
Non-melanoma skin cancer
Lipid elevations
MACE, thrombosis, and secondary malignancies (JAK inhibitor class)

Adverse reactions

Thrombocytopenia
Anemia
Neutropenia
Bruising
Dizziness
Headache
Diarrhea
Infections
Edema

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		#/mo	CostPlus
5 mg	tab	60 BID	not offered
10 mg	tab	60 BID	not offered
15 mg	tab	60 BID	not offered
20 mg	tab	60 BID	not offered
25 mg	tab	60 BID	not offered
11 mg	ER tab	60 BID	not offered
22 mg	ER tab	60 BID	not offered
33 mg	ER tab	60 BID	not offered
44 mg	ER tab	60 BID	not offered
55 mg	ER tab	60 BID	not 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.

NO BOXED WARNINGS

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.

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