Can you take Macitentan with Zelboraf?
1 drug interaction and 14 additional warnings found for the following 2 drugs:
- macitentan
- Zelboraf (vemurafenib)
Drug interactions
Moderate drug interactions
Moderate:
vemurafenib macitentan
Applies to: Zelboraf (vemurafenib) and macitentan
Vemurafenib may reduce the blood levels and effects of macitentan. Contact your doctor if your symptoms worsen or your condition changes during treatment with these medications. Your doctor may be able to prescribe alternatives that do not interact, or you may need a dose adjustment or more frequent monitoring to safely use both medications. It is important to tell your doctor about all other medications you use, including vitamins and herbs. Do not stop using any medications without first talking to your doctor
Food/lifestyle interactions
Moderate food/lifestyle interactions
Moderate:
macitentan Food/Lifestyle
Applies to: macitentan
Grapefruit juice may increase the effects of macitentan in some people by increasing its levels in the blood. You should avoid the consumption of grapefruit or grapefruit juice during treatment with macitentan. Contact your doctor if your condition changes or you experience increased side effects. Talk to your doctor or pharmacist if you have any questions or concerns. It is important to tell your doctor about all other medications you use, including vitamins and herbs. Do not stop using any medications without first talking to your doctor.
Disease interactions
13 potential interactions Applies to: 12 conditions, including Heart Failure, Arrhythmia, Anemia, Liver Disease, and Skin Cancer.
Anemia
Moderate:
macitentan
Macitentan has a moderate potential interaction with Anemia.
Clinical studies have shown that most endothelin receptor antagonists decrease hemoglobin concentration and hematocrit levels. There are some postmarketing reports of anemia cases which needed blood transfusion. Hemoglobin and hematocrit levels should be measured prior to treatment initiation and should be monitored periodically thereafter. Initiation of therapy is not recommended in patients with clinically significant anemia.
Arrhythmia
Moderate:
Zelboraf
The vemurafenib in Zelboraf has a moderate potential interaction with Arrhythmia.
Vemurafenib can cause dose dependent QT prolongation which may lead to an increased risk for ventricular arrhythmias, including Torsade de Pointes. It is recommended not to start treatment in patients with uncorrectable electrolyte abnormalities, QTc > 500 ms, or long QT syndrome, or in patients who are taking medicinal products known to prolong the QT interval. Evaluate patients prior to and following treatment initiation or after dose modification for QTc prolongation, evaluate ECG and electrolytes (including potassium, magnesium, and calcium) periodically, and thereafter as clinically indicated. Vemurafenib should be withhold in patients who develop QTc > 500 ms. Upon recovery to QTc <= 500 ms, restart at a reduced dose and it should be permanently discontinued if the QTc interval remains > 500 ms and increased > 60 ms from pre-treatment values after controlling cardiac risk factors for QT prolongation (e.g., electrolyte abnormalities, congestive heart failure, and bradyarrhythmias).
Dermatitis, Drug-Induced
Moderate:
Zelboraf
The vemurafenib in Zelboraf has a moderate potential interaction with Dermatitis, Drug-Induced.
Severe dermatologic reactions, including Stevens-Johnson syndrome, toxic epidermal necrolysis, and mild to severe photosensitivity can occur in patients treated with vemurafenib. Consider dose modifications for intolerable >= Grade 2 photosensitivity. It is recommended to advise patients to avoid sun exposure, wear protective clothing and use a broad-spectrum UVA/UVB sunscreen and a suitable lip balm when outdoors while on vemurafenib treatment. Permanently discontinue vemurafenib in patients who experience a severe dermatologic reaction.
Electrolyte Abnormalities
Moderate:
Zelboraf
The vemurafenib in Zelboraf has a moderate potential interaction with Electrolyte Abnormalities.
Vemurafenib can cause dose dependent QT prolongation which may lead to an increased risk for ventricular arrhythmias, including Torsade de Pointes. It is recommended not to start treatment in patients with uncorrectable electrolyte abnormalities, QTc > 500 ms, or long QT syndrome, or in patients who are taking medicinal products known to prolong the QT interval. Evaluate patients prior to and following treatment initiation or after dose modification for QTc prolongation, evaluate ECG and electrolytes (including potassium, magnesium, and calcium) periodically, and thereafter as clinically indicated. Vemurafenib should be withhold in patients who develop QTc > 500 ms. Upon recovery to QTc <= 500 ms, restart at a reduced dose and it should be permanently discontinued if the QTc interval remains > 500 ms and increased > 60 ms from pre-treatment values after controlling cardiac risk factors for QT prolongation (e.g., electrolyte abnormalities, congestive heart failure, and bradyarrhythmias).
Heart Failure
Moderate:
macitentan
Macitentan has a moderate potential interaction with Heart Failure.
Peripheral edema and fluid retention are known clinical consequences of pulmonary hypertension and also known effects of endothelin receptor antagonists. Caution and monitoring is recommended if these agents are used in patients with underlying left ventricular dysfunction or underlying heart failure, as they have an increased risk for developing significant fluid retention that may need treatment or require discontinuation.
History, Skin Cancer
Moderate:
Zelboraf
The vemurafenib in Zelboraf has a moderate potential interaction with History, Skin Cancer.
Cutaneous squamous cell carcinoma, keratoacanthoma, and melanoma occurred at a higher incidence in patients receiving vemurafenib. Potential risk factors associated included age (> 65 years), prior skin cancer, and chronic sun exposure. It is recommended to perform dermatologic evaluations prior to initiation of therapy and periodically thereafter as clinically indicated. Consider dermatologic monitoring for 6 months following discontinuation of vemurafenib.
Interstitial Lung Disease
Moderate:
Zelboraf
The vemurafenib in Zelboraf has a moderate potential interaction with Interstitial Lung Disease.
The use of certain multikinase inhibitors has been associated with pulmonary toxicity. Serious cases of interstitial lung disease (ILD), including fatal cases and interstitial pneumonitis or pulmonary fibrosis have been reported. Caution is recommended when using these agents in patients with a history of interstitial pneumonitis or pulmonary fibrosis or those patients presenting with acute onset of new or progressive unexplained pulmonary symptoms such as dyspnea, cough, and fever pending diagnostic evaluation. If ILD is confirmed, these agents should be permanently discontinued and appropriate measures should be instituted. Treatment should be immediately withheld in patients diagnosed with ILD/pneumonitis and permanently discontinued if no other potential causes of ILD/pneumonitis have been identified.
Liver Disease
Major:
macitentan
Macitentan has a major potential interaction with Liver Disease.
Endothelin receptor antagonists (ERAs) have been associated with aminotransferase elevations, hepatotoxicity, and cases of liver failure. Hepatic function should be assessed before treatment initiation and closely monitored during treatment. Therapy should be discontinued if aminotransferase elevations are accompanied by increases in bilirubin, or clinical symptoms of hepatotoxicity such as nausea, vomiting, fever, abdominal pain or jaundice. Treatment should be avoided in patients with elevated aminotransferases at baseline as monitoring for hepatotoxicity may be more difficult. In general, the use of ERAs is not recommended for patients with moderate to severe hepatic impairment.
Moderate:
Zelboraf
The vemurafenib in Zelboraf has a moderate potential interaction with Liver Disease.
Liver injury leading to functional hepatic impairment, including coagulopathy or other organ dysfunction may occur with the use of vemurafenib. Based on a population pharmacokinetic analysis to evaluate the effect of hepatic impairment, no dose adjustment is recommended for patients with mild and moderate hepatic impairment. The appropriate dose of vemurafenib has not been established in patients with severe hepatic impairment. It is recommended to monitor transaminases, alkaline phosphatase, and bilirubin before initiation of treatment and monthly during treatment, or as clinically indicated; and to manage laboratory abnormalities with dose reduction, treatment interruption, or treatment discontinuation as appropriate.
Pulmonary Impairment
Moderate:
Zelboraf
The vemurafenib in Zelboraf has a moderate potential interaction with Pulmonary Impairment.
The use of certain multikinase inhibitors has been associated with pulmonary toxicity. Serious cases of interstitial lung disease (ILD), including fatal cases and interstitial pneumonitis or pulmonary fibrosis have been reported. Caution is recommended when using these agents in patients with a history of interstitial pneumonitis or pulmonary fibrosis or those patients presenting with acute onset of new or progressive unexplained pulmonary symptoms such as dyspnea, cough, and fever pending diagnostic evaluation. If ILD is confirmed, these agents should be permanently discontinued and appropriate measures should be instituted. Treatment should be immediately withheld in patients diagnosed with ILD/pneumonitis and permanently discontinued if no other potential causes of ILD/pneumonitis have been identified.
Renal Dysfunction
Moderate:
Zelboraf
The vemurafenib in Zelboraf has a moderate potential interaction with Renal Dysfunction.
Renal failure, including acute interstitial nephritis and acute tubular necrosis may occur with the use of vemurafenib. Based on a population pharmacokinetic analysis, no dose adjustment is recommended for patients with mild and moderate renal impairment. The appropriate dose of vemurafenib has not been established in patients with severe renal impairment. It is recommended to measure serum creatinine before initiation of therapy and periodically during treatment.
Skin Cancer
Moderate:
Zelboraf
The vemurafenib in Zelboraf has a moderate potential interaction with Skin Cancer.
Cutaneous squamous cell carcinoma, keratoacanthoma, and melanoma occurred at a higher incidence in patients receiving vemurafenib. Potential risk factors associated included age (> 65 years), prior skin cancer, and chronic sun exposure. It is recommended to perform dermatologic evaluations prior to initiation of therapy and periodically thereafter as clinically indicated. Consider dermatologic monitoring for 6 months following discontinuation of vemurafenib.
Visual Defect/Disturbance
Moderate:
Zelboraf
The vemurafenib in Zelboraf has a moderate potential interaction with Visual Defect/Disturbance.
Uveitis, blurry vision, and photophobia can occur in patients treated with vemurafenib. Monitor patients for signs and symptoms of uveitis. Care must be exercised when using this agent in patients with ophthalmological complications.
More resources
macitentan
A total of 250 drugs are known to interact with macitentan.
- Macitentan is in the drug class agents for pulmonary hypertension.
- Macitentan is used to treat Pulmonary Arterial Hypertension.
Zelboraf
A total of 644 drugs are known to interact with Zelboraf.
- Zelboraf is in the drug class multikinase inhibitors.
- Zelboraf is used to treat the following conditions:
Drug Interaction Classification
| Highly clinically significant. Avoid combinations; the risk of the interaction outweighs the benefit. | |
| Moderately clinically significant. Usually avoid combinations; use it only under special circumstances. | |
| Minimally clinically significant. Minimize risk; assess risk and consider an alternative drug, take steps to circumvent the interaction risk and/or institute a monitoring plan. | |
| No interaction information available. |
Further information
Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.