Ruxolitinib (Jakafi)

General information

Class/mechanism: Kinase inhibitor of Janus Associated Kinases (JAKs) JAK1 and JAK2. Modulates gene expression by interfering with the JAK signaling pathway, which involves recruitment, activation, and localization of STATs (signal transducers and activators of transcription) to cytokine receptors and the nucleus.
Route: PO
Extravasation: n/a

For conciseness and simplicity, HemOnc.org currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, UpToDate (courtesy of Lexicomp), or the prescribing information.

Diseases for which it is established

• Graft versus host disease
• Myelofibrosis
• Polycythemia vera

Diseases for which it is used

• Acute myeloid leukemia
• Chronic lymphocytic leukemia
• Essential thrombocythemia
• Hypereosinophilic syndrome

Patient drug information

• Patient information may be found in the Ruxolitinib (Jakafi) package insert
• Ruxolitinib (Jakafi) patient drug information (Chemocare)
• Ruxolitinib (Jakafi) patient drug information (UpToDate)

History of changes in FDA indication

• 2011-11-16: Initial FDA approval for treatment of patients with intermediate or high-risk myelofibrosis, including primary myelofibrosis, post-polycythemia vera myelofibrosis and post-essential thrombocythemia myelofibrosis. (Based on COMFORT-I and COMFORT-II)
• 2014-12-04: Indication expanded for the treatment of patients with polycythemia vera (PV) who have had an inadequate response to or are intolerant of hydroxyurea (HU). (New disease entity; based on RESPONSE)
• 2019-05-24: Indication expanded for steroid-refractory acute graft-versus-host disease (GVHD) in adult and pediatric patients 12 years and older. (New condition; based on REACH1)
• 2021-09-21: Approved for chronic graft-versus-host disease (cGVHD) after failure of one or two lines of systemic therapy in adult and pediatric patients 12 years and older. (Based on REACH3)

History of changes in EMA indication

• 2012-08-23: Initial authorization

History of changes in Health Canada indication

• 2012-06-19: Initial notice of compliance

History of changes in PMDA indication

• 2014-07-04: Initial approval for the treatment of myelofibrosis.
• 2015-09-24: New additional indication and a new dosage for the treatment of polycythemia vera (use only when conventional therapies are not sufficiently effective or inappropriate).

Also known as

• Code name: INCB018424
• Generic name: ruxolitinib phosphate
• Brand names: Jakafi, Jakavi