Ruxolitinib with Tocilizumab Interaction Details
Brand Names Associated with Ruxolitinib
- Jakafi
- Ruxolitinib
Brand Names Associated with Tocilizumab
- Actemra®
- Tocilizumab Injection
Medical Content Editor Dr. Brian Staiger, PharmD
Last updated
Dec 27, 2023
Interaction Effect
Reduced CYP3A4 substrate exposure and reduced efficacy of CYP3A4 substrate
Interaction Summary
Concurrent administration of tocilizumab and a CYP3A4 substrate with a narrow therapeutic index (NTI) may reduce the exposure of the substrate. Monitor therapeutic effect or drug concentrations and adjust the individual dose of the CYP3A4 NTI substrate as needed upon initiation or discontinuation of tocilizumab, in patients being treated with CYP3A4 NTI substrate. The effect of tocilizumab on CYP450 enzyme activity may persist for several weeks after stopping therapy. Use caution when coadministering tocilizumab with CYP3A4 substrate drugs like oral contraceptives, lovastatin, atorvastatin etc. where decrease in effectiveness is undesirable.
Severity
Major
Onset
Unspecified
Evidence
Probable
How To Manage Interaction
Concurrent administration of tocilizumab and a CYP3A4 substrate with a narrow therapeutic index (NTI) may reduce the exposure of the substrate. Monitor therapeutic effect or drug concentrations and adjust the individual dose of the CYP3A4 NTI substrate as needed upon initiation or discontinuation of tocilizumab, in patients being treated with CYP3A4 NTI substrate. The effect of tocilizumab on CYP450 enzyme activity may persist for several weeks after stopping therapy. Use caution when coadministering tocilizumab with CYP3A4 substrate drugs like oral contraceptives, lovastatin, atorvastatin etc. where decrease in effectiveness is undesirable.
Mechanism Of Interaction
Induction of CYP3A4-substrate metabolism by tocilizumab
Literature Reports
A) In clinical studies, omeprazole, metabolized by CYP2C19 and CYP3A4, and simvastatin, metabolized by CYP3A4, showed up to a 28% and 57% decrease in exposure one week following a single dose of tocilizumab, respectively .
Ruxolitinib Overview
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Ruxolitinib is used to treat myelofibrosis (a cancer of the bone marrow in which the bone marrow is replaced by scar tissue and causes decreased blood cell production). It is also used to treat polycythemia vera (PV; a slow growing cancer of the blood in which the bone marrow makes too many red blood cells) in people who were not able to be treated successfully with hydroxyurea. Ruxolitinib is also used to treat acute graft versus host disease (aGVHD; a complication of hematopoietic stem-cell transplant [HSCT; a procedure that replaces diseased bone marrow with healthy bone marrow] that usually develops within the first months after HSCT) in adults and children 12 years of age and older who were treated unsuccessfully with steroid medications. It is also used to treat chronic GVHD (cGVHD; a complication of HSCT that usually develops at least 3 months after HSCT) in adults and children 12 years of age and older who were treated unsuccessfully with 1 or 2 other treatments. Ruxolitinib is in a class of medications called kinase inhibitors. It works to treat myelofibrosis and PV by blocking the signals that cause cancer cells to multiply. This helps to stop the spread of cancer cells. It works to treat GVHD by blocking the signals of the cells that cause GVHD.
Tocilizumab Overview
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Tocilizumab injection is used alone or in combination with other medications to relieve the symptoms of certain types of arthritis and other conditions including:
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rheumatoid arthritis (a condition in which the body attacks its own joints, causing pain, swelling, and loss of function) in adults who have not been helped by other disease-modifying antirheumatic drugs (DMARDs),
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giant cell arteritis (a condition that causes swelling of blood vessels, especially in the scalp and head) in adults,
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systemic sclerosis-associated interstitial lung disease (SSc-ILD; also known as scleroderma-associated ILD: a lung disease that involves scarring of the lungs) in adults,
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polyarticular juvenile idiopathic arthritis (PJIA; a type of childhood arthritis that affects five or more joints during the first six months of the condition, causing pain, swelling, and loss of function) in children 2 years of age or older.
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systemic juvenile idiopathic arthritis (SJIA; a condition in children that causes inflammation in different areas of the body, causing fever, joint pain and swelling, loss of function, and delays in growth and development) in children 2 years of age or older,
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cytokine release syndrome (a severe and possibly life-threatening reaction) in adults and children 2 years of age or older after receiving certain immunotherapy infusions.
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Tocilizumab injection is in a class of medications called interleukin-6 (IL-6) receptor inhibitors. It works by blocking the activity of interleukin-6, a substance in the body that causes inflammation.
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Definitions
Severity Categories
Contraindicated
These drugs, generally, should not be used together simultaneously due to the high risk of severe adverse effects. Combining these medications can lead to dangerous health outcomes and should be strictly avoided unless otherwise instructed by your provider.
Major
This interaction could result in very serious and potentially life-threatening consequences. If you are taking this drug combination, it is very important to be under close medical supervision to minimize severe side effects and ensure your safety. It may be necessary to change a medication or dosage to prevent harm.
Moderate
This interaction has the potential to worsen your medical condition or alter the effectiveness of your treatment. It's important that you are monitored closely and you potentially may need to make adjustments in your treatment plan or drug dosage to maintain optimal health.
Minor
While this interaction is unlikely to cause significant problems, it could intensify side effects or reduce the effectiveness of one or both medications. Monitoring for changes in symptoms and your condition is recommended, and adjustments may be made if needed to manage any increased or more pronounced side effects.
Onset
Rapid: Onset of drug interaction typically occurs within 24 hours of co-administration.
Delayed: Onset of drug interaction typically occurs more than 24 hours after co-administration.
Evidence
Level of documentation of the interaction.
Established: The interaction is documented and substantiated in peer-reviewed medical literature.
Theoretical: This interaction is not fully supported by current medical evidence or well-documented sources, but it is based on known drug mechanisms, drug effects, and other relevant information.
How To Manage The Interaction
Provides a detailed discussion on how patients and clinicians can approach the identified drug interaction as well as offers guidance on what to expect and strategies to potentially mitigate the effects of the interaction. This may include recommendations on adjusting medication dosages, altering the timing of drug administration, or closely monitoring for specific symptoms.
It's important to note that all medical situations are unique, and management approaches should be tailored to individual circumstances. Patients should always consult their healthcare provider for personalized advice and guidance on managing drug interactions effectively.
Mechanism Of Interaction
The theorized or clinically determined reason (i.e., mechanism) why the drug-drug interaction occurs.
Disclaimer: The information provided on this page is for informational purposes only and should not be considered medical advice. Always consult with a qualified healthcare professional regarding your specific circumstances and medical conditions.
Where Does Our Information Come From?
Information for our drug interactions is compiled from several drug compendia, including:
The prescribing information for each drug, as published on DailyMED, is also used.
Individual drug-drug interaction detail pages contain references specific to that interaction. You can click on the reference number within brackets '[]' to see what reference was utilized.
The information posted is fact-checked by HelloPharmacist clinicians and reviewed quarterly.