Chemical Structure
The chemical name for ruxolitinib phosphate is (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentyl propane nitrile phosphate.
It has a molecular formula of C17H20N6O.H3PO4 and a molecular weight of 404.370 g/mol.
Mechanism of Action
Ruxolitinib is a JAK1 and JAK2 inhibitor. It inhibits the Janus kinase (JAK) family of enzymes that mediate cytokine signaling involved in hematopoiesis and immune response. In particular it targets JAK1 and JAK2 over JAK3.
Pharmacology
Ruxolitinib phosphate has an oral bioavailability of 97% and is rapidly absorbed, reaching peak plasma levels within 1-2 hours. Its elimination half life is 3-5 hours. Metabolism occurs primarily via CYP3A4 enzymes.
Formulation
Ruxolitinib API is available in tablet dosage forms containing ruxolitinib phosphate as the active ingredient:
- 5mg tablets
- 10mg tablets
- 15mg tablets
- 20mg tablets
- 25mg tablets
Indications
Ruxolitinib phosphate tablets are FDA approved for treatment of:
- Myelofibrosis
- Polycythemia vera
It can reduce spleen size, alleviate disease-related symptoms, and improve outcomes in these blood disorders.
Dosage
For myelofibrosis, the starting oral dose is typically 15-20mg twice daily. For polycythemia vera, the dose is 10mg twice daily. Doses may be adjusted based on response and tolerability.
Adverse Effects
Potential side effects of ruxolitinib phosphate include:
- Thrombocytopenia
- Anemia
- Bruising
- Dizziness
- Headache
Monitoring of blood counts is recommended during treatment.
Warnings
Ruxolitinib phosphate carries warnings for risks of thrombosis, anemia, cytopenias, and infection.
Careful monitoring of complete blood counts is essential during ruxolitinib therapy.
In summary, this overview covers the key facts healthcare professionals need to know about ruxolitinib phosphate. As a leading global ruxolitinib API, AcmeRx supplies high quality ruxolitinib phosphate to support safe and effective therapy.
