Irinotecan Injection and Rolapitant: Interaction Details
AI-assisted, pharmacist-reviewed · Source data updated Aug 8, 2026 · Sources: FDA labeling, DDInter 2.0, cited literature
Rolapitant
Irinotecan 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
Increased irinotecan exposure
Interaction Deep Dive
Irinotecan is a substrate of BCRP2 and oral rolapitant is a BCRP inhibitor that can significantly increase substrate exposure and potential for adverse reactions; if concomitant use cannot be avoided, monitor for adverse reactions related to the substrate 1. A post hoc safety analysis supports the tolerability of oral rolapitant in a large number of patients as part of an antiemetic triple-drug regimen prior to cycle 1 of emetogenic chemotherapy comprised of BCRP substrates, which included irinotecan, methotrexate, or topotecan (n=44). There were no differences in toxicities experienced in those treated with rolapitant and BCRP substrate drugs compared with control populations 2.
Why it happens (mechanism)
Inhibition of BCRP-mediated efflux transport of irinotecan by rolapitant
Literature reports
2 reports — tap to read
a) An integrated safety analysis of cycle 1 treatment-emergent adverse effects (TEAE) and serious TEAEs frequencies in patients when oral rolapitant was added to chemotherapy regimens containing CYP2D6 or BCRP substrate drugs compared with non-use of CYP2D6 or BCRP substrate drugs showed no difference in toxicities experienced in those treated with irinotecan, methotrexate, or topotecan and rolapitant (n=44) compared with control (n=42). Common TEAEs and serious TEAEs occurred with comparable frequencies in the rolapitant and control populations when patients were grouped by BCRP substrate drug use (ie, irinotecan, etoposide, epirubicin, docetaxel, DOXOrubicin, fluorouracil, methotrexate, topotecan) vs non-use as well as when grouped by CYP2D6 substrate drug use (ie, ondansetron, metoclopramide, ranitidine) vs non-use. Across 4 phase II and III trials, 53% of patients received CYP2D6 substrate drugs (n=1368) and 63% received BCRP substrate drugs (n=1637) 2.
b) Coadministration of a single oral dose of rolapitant 180 mg (BCRP inhibitor) with sulfasalazine 500 mg (BCRP substrate) on day 1 and sulfasalazine alone on day 8 showed a significantly increased sulfasalazine Cmax by 140% and AUC by 130% on day 1 and on day 8, sulfasalazine Cmax and AUC were still elevated by 17% and 32% 1.
Common questions
Can I take Irinotecan Injection and Rolapitant together?
Increased irinotecan exposure Always confirm with your pharmacist or prescriber before making any change.
How serious is the Irinotecan Injection and Rolapitant 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 "established". Well documented — supported by controlled studies or strong clinical data.
Questions for your pharmacist
- Does my dose of Irinotecan Injection or Rolapitant 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 (2)
- Product Information: VARUBI(R) oral tablets, rolapitant oral tablets. TerSera Therapeutics LLC (per FDA), Deerfield, IL, 2020. DailyMed
- Barbour S, Smit T, Wang X, et al: Integrated safety analysis of rolapitant with coadministered drugs from phase II/III trials: an assessment of CYP2D6 or BCRP inhibition by rolapitant. Ann Oncol 2017; 28(6):1268-1273. PubMed
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