Ceritinib and Cariprazine: Interaction Details
AI-assisted, pharmacist-reviewed · AI content regenerated Jul 16, 2026 · Source data updated Jul 16, 2026 · Sources: FDA labeling, DDInter 2.0, cited literature
Ceritinib
Cariprazine
How we grade severity & evidence
Severity levels
- Contraindicated: These should generally not be used together.
- Major: Potentially serious — often needs a change or close monitoring.
- Moderate: Can be significant — usually manageable with monitoring.
- Minor: Usually limited clinical impact.
Evidence grades
- Established: Well documented — supported by controlled studies or strong clinical data.
- Probable: Good supporting evidence, though not definitively proven.
- Suspected: Some evidence suggests this interaction, but it is not well established.
- Possible: Limited or conflicting evidence; the interaction may occur.
- Theoretical: Predicted from the drugs' pharmacology; not yet confirmed in people.
Ratings come from the documented interaction literature and are reviewed by a pharmacist. They describe the documented risk of the combination, not what will necessarily happen to you — your dose, timing, and health picture all matter.
These two medicines can interact. Ceritinib (Zykadia) is a cancer medicine that slows down a liver enzyme called CYP3A4. Your body uses that same enzyme to clear out cariprazine (Vraylar). When ceritinib slows the enzyme, cariprazine and its active breakdown product can build up in your body, roughly doubling. That can mean stronger side effects like restlessness, drowsiness, muscle stiffness, or trouble sitting still.
The good news: this is very manageable. Your care team will usually lower your cariprazine dose or spread the doses further apart while you are on ceritinib. Keep taking both exactly as prescribed and talk with your pharmacist or doctor before changing anything.
Mechanism: Ceritinib is a strong CYP3A4 inhibitor; cariprazine is a CYP3A4 substrate (active metabolite didesmethylcariprazine). Inhibition reduces cariprazine clearance, increasing exposure. Direction: increased cariprazine effect.
Magnitude: With ketoconazole, cariprazine AUC and Cmax rose ~100%. Evidence: probable. Severity: major.
Management (per labeling):
- Initiating cariprazine on a strong inhibitor (schizophrenia/bipolar mania): 1.5 mg every 3 days, titrate to 1.5 mg every other day per response.
- Bipolar depression/MDD adjunct: 1.5 mg every 3 days.
- Stable 1.5 or 3 mg daily: reduce to 1.5 mg every 3 days.
- Stable 4.5 or 6 mg daily: reduce to 1.5 mg every other day.
On inhibitor discontinuation, dose may be increased per response. Monitor for EPS, akathisia, sedation.
What happens
Increased exposure to cariprazine and its active metabolite, didesmethylcariprazine
Interaction Deep Dive
When cariprazine (a CYP3A4 substrate) is given together with a potent CYP3A4 inhibitor, exposure to cariprazine as well as its active metabolite, didesmethylcariprazine, may rise. In drug interaction studies, giving cariprazine alongside ketoconazole (a strong CYP3A4 inhibitor) produced roughly a 100% rise in both AUC and Cmax. Consequently, dosing guidance depends on the clinical scenario. For patients beginning cariprazine while already on a strong CYP3A4 inhibitor (in schizophrenia or bipolar mania), the recommended start is 1.5 mg orally every 3 days, which may be raised to 1.5 mg orally every other day if warranted by clinical response and tolerability. For those on a strong CYP3A4 inhibitor being treated for bipolar depression or receiving adjunctive therapy for MDD, the dose is 1.5 mg orally every 3 days. If a strong CYP3A4 inhibitor is added to an established cariprazine regimen, the cariprazine dose must be modified: a patient currently taking 1.5 or 3 mg once daily should be switched to 1.5 mg orally every 3 days when the strong inhibitor is started, whereas a patient currently taking 4.5 or 6 mg once daily should be switched to 1.5 mg orally every other day. Once the strong CYP3A4 inhibitor is stopped, an increase in the cariprazine dose may be required, guided by clinical response and tolerability1.
Why it happens (mechanism)
Inhibition of CYP3A4-mediated metabolism of cariprazine
How to manage this interaction
Keep taking both medicines as prescribed unless your care team tells you otherwise. Because ceritinib raises cariprazine levels, your team will typically tailor your cariprazine dose and watch you more closely.
- They may lower your cariprazine dose or space it further apart (for example, every 3 days or every other day, depending on your current dose and condition).
- They will watch for stronger side effects like restlessness, muscle stiffness, or drowsiness.
- If ceritinib is later stopped, your cariprazine dose may be raised again based on how you respond.
What to do: Tell your pharmacist and prescriber you take both, and report any new or worsening side effects.
Management is individual — confirm any change with your pharmacist or prescriber.
Literature reports
1 report — tap to read
a) In drug interaction studies, giving cariprazine 0.5 mg/day together with ketoconazole 400 mg/day led to an increase in total cariprazine AUC and Cmax of about 100% 1.
Common questions
Can I take Ceritinib and Cariprazine together?
Ceritinib can roughly double cariprazine levels by blocking its breakdown, so your care team will usually reduce or space out your cariprazine dose and monitor you more closely. Keep taking both as prescribed and check with your pharmacist or doctor before changing anything. Always confirm with your pharmacist or prescriber before making any change.
How serious is the Ceritinib and Cariprazine interaction?
It is rated major. Potentially serious — often needs a change or close monitoring.
How quickly could this interaction happen?
The documented onset is "unspecified". The timing of this interaction is not well characterized.
How is the Ceritinib and Cariprazine interaction managed?
Keep taking both medicines as prescribed unless your care team tells you otherwise. Because ceritinib raises cariprazine levels, your team will typically tailor your cariprazine dose and watch you more closely. They may lower your cariprazine dose or space it further apart (for example, every 3 days or every other day, depending on your current dose and condition). They will watch for stronger sid… Management is individual — always follow your own care team's guidance.
How strong is the evidence for this interaction?
The evidence is graded "probable". Good supporting evidence, though not definitively proven.
Questions for your pharmacist
- Does my dose of Ceritinib or Cariprazine need adjusting while I take them together?
- What symptoms should prompt me to call you or my prescriber right away?
- Does the timing of my doses matter for this combination?
- Is there a safer alternative to one of these medications for me?
References (1)
- Product Information: VRAYLAR(R) oral capsules, cariprazine oral capsules. AbbVie Inc. (per FDA), North Chicago, IL, 2024. DailyMed
Keep reading about Ceritinib
Keep reading about Cariprazine
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