Cabazitaxel Injection and Enzalutamide: Interaction Details
AI-assisted, pharmacist-reviewed · Source data updated Aug 8, 2026 · Sources: FDA labeling, DDInter 2.0, cited literature
Enzalutamide
Cabazitaxel Injection
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.
What happens
Decreased cabazitaxel exposure and risk of loss of efficacy
Interaction Deep Dive
Concomitant use of cabazitaxel (a CYP3A4 substrate) and a CYP3A4 inducer may result in subtherapeutic cabazitaxel exposure1. Cabazitaxel exposure was decreased by 17% and clearance was increased 21% in a study when given with rifampin 2 and in another study exposure decreased by 22% when coadministered with enzalutamide. When cabazitaxel is used in lower doses with CYP3A4 inducers, the clinical significance of this interaction may be substantial 3.
Why it happens (mechanism)
Induction of CYP3A4-mediated cabazitaxel metabolism
Literature reports
2 reports — tap to read
a) In a study in patients with metastatic castration-resistant prostate cancer (N=14), exposure of cabazitaxel was decreased by 22% (95% CI, 9% to 34%) when coadministered with enzalutamide (a strong CYP3A inducer). Concomitant administration of cabazitaxel 25 mg/m(2) every 3 weeks for 3 cycles and enzalutamide 160 mg once daily beginning on day 7 after the first cabazitaxel cycle through 8 days after cycle 3 of cabazitaxel, resulted in a significant decrease in cabazitaxel AUC(0 to 24 hours) from 234 to 181 nanograms (ng) x hr/mL between cycles 1 and 3. Additionally, cabazitaxel Cmax significantly decreased from 138 to 96 ng/mL (95% CI, -42 to -16 ng/mL) and t(1/2) decreased from 22 to 18 hours (95% CI, -59 to 64 hours). PSA response of 50% or greater occurred in 62% of 13 patients evaluated 3.
b) Concomitant use of cabazitaxel 15 mg/m(2) plus CISplatin 75 mg/m(2) IV for 70 cycles with rifampin 600 mg orally once daily for a median of 14 days (range, 1 to 28 days) resulted in 21% increase in cabazitaxel clearance (geometric mean ratio [GMR], 1.21 [90% CI, 0.95 to 1.53]) and a 17% decrease in AUC (GMR, 0.83 [90% CI, 0.65 to 1.05]) in a study in patients with advanced solid tumors (n=21; 26.1% breast as primary tumor site). Rifampin had a lower effect during the initial phase of cabazitaxel elimination (0 to 24 hours). Cabazitaxel Cmax increased from 117 to 195 nanograms(ng)/mL, t(1/2) decreased from 78 to 50 hours, and Vd at steady state decreased from 5530 to 4070 L. CISplatin did not contribute to this interaction since it is not a CYP3A inducer 2.
Common questions
Can I take Cabazitaxel Injection and Enzalutamide together?
Decreased cabazitaxel exposure and risk of loss of efficacy Always confirm with your pharmacist or prescriber before making any change.
How serious is the Cabazitaxel Injection and Enzalutamide interaction?
It is rated moderate. Can be significant — usually manageable with monitoring.
How quickly could this interaction happen?
The documented onset is "unspecified". The timing of this interaction is not well characterized.
How strong is the evidence for this interaction?
The evidence is graded "theoretical". Predicted from the drugs' pharmacology; not yet confirmed in people.
Questions for your pharmacist
- Does my dose of Cabazitaxel Injection or Enzalutamide 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 anything you'd monitor while I'm on both?
References (3)
- Product Information: JEVTANA(R) intravenous injection, cabazitaxel intravenous injection. sanofi-aventis US LLC (per FDA), Bridgewater, NJ, 2018. DailyMed
- Sarantopoulos J, Mita AC, Wade JL, et al: Phase I study of cabazitaxel plus cisplatin in patients with advanced solid tumors: study to evaluate the impact of cytochrome P450 3A inhibitors (aprepitant, ketoconazole) or inducers (rifampin) on the pharmacokinetics of cabazitaxel. Cancer Chemother Pharmacol 2014; 74(6):1113-1124. PubMed
- Belderbos BPS, Bins S, van Leeuwen RWF, et al: Influence of enzalutamide on cabazitaxel pharmacokinetics: a drug-drug interaction study in metastatic castration-resistant prostate cancer (mCRPC) patients. Clin Cancer Res 2018; 24(3):541-546. DOI
Keep reading about Enzalutamide
Keep reading about Cabazitaxel Injection
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