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Inluriyo ™ (imlunestrant) tablets
200 mg
This information is provided in response to your request. Resources may contain information about doses, uses, formulations and populations different from product labeling. See Prescribing Information above, if applicable.
Are there any drug-drug interactions with Inluriyo™ (imlunestrant)?
Statistically significant increases in the AUC0-∞ and Cmax were observed for P-gp, and BCRP substrates when coadministered with imlunestrant. Caution is advised when coadministering imlunestrant with these substrates.
Potential Drug-Drug Interactions
Clinical Trials
Three open-label, fixed-sequence, crossover, phase 1 trials were conducted to evaluate the drug-drug interaction potential of imlunestrant in healthy female participants aged 18 to 65 years who are of nonchildbearing potential. These studies aimed to assess the tolerability, safety, and pharmacokinetics of imlunestrant when administered alone or in combination with other drugs.1
Pharmacokinetic parameters were determined using standard noncompartmental analyses. Log-transformed maximum plasma concentrations (Cmax) and area under the plasma concentration-time curve from zero to infinity (AUC0-∞) parameters were analyzed using a linear mixed-effects model with a fixed effect for treatment and random effect for participant.1
Geometric least-squares mean ratios and corresponding 90% confidence intervals were reported.1
Statistically significant increases in the AUC0-∞ and Cmax were observed for dextromethorphan (a cytochrome P450 [CYP] 2D6 substrate), digoxin (a p-glycoprotein [P-gp] substrate), and rosuvastatin (a breast cancer resistance protein [BCRP] substrate) when coadministered with imlunestrant (Summary of Imlunestrant Drug-Drug Interactions as a Precipitant and Object). No significant effects on the time to reach maximum plasma concentration values were observed.1,2
Precipitant | Object | AUC0-∞ Ratio | Cmax Ratio GLSM (90% CI) | Statistically Significanta |
Imlunestrant | Repaglinide | 1.02 (0.97-1.08) | 0.93 (0.79-1.10) | NA |
Imlunestrant | Omeprazole | 1.10 (0.97-1.24) | 1.28 (1.05-1.57) | Cmax |
Imlunestrant | Hydroxyomeprazole | 1.03 (0.96-1.11) | 1.15 (0.99-1.32) | NA |
Imlunestrant | Dextromethorphan | 1.33 (1.22-1.46) | 1.43 (1.24-1.65) | AUC0-∞, Cmax |
Imlunestrant | Dextrorphan | 1.01 (0.86-1.18) | 1.10 (0.97-1.25) | NA |
Imlunestrant | Midazolam | 0.93 (0.85-1.02) | 1.07 (0.99-1.16) | NA |
Imlunestrant | Hydroxymidazolam | 0.82 (0.78-0.87) | 0.96 (0.83-1.12) | AUC0-∞ |
Imlunestrant | Digoxin | 1.39 (1.22-1.59) | 1.60 (1.34-1.91) | AUC0-∞, Cmax |
Imlunestrant | Rosuvastatin | 1.49 (1.14-1.97) | 1.65 (1.28-2.13) | AUC0-∞, Cmax |
Itraconazole | Imlunestrant | 2.11 (1.77-2.53) | 1.87 (1.62-2.17) | AUC0-∞, Cmax |
Carbamazepine | Imlunestrant | 0.58 (0.49-0.69) | 0.71 (0.60-0.85) | AUC0-∞, Cmax |
Quinidine | Imlunestrant | 0.87 (0.76-1.00) | 0.87 (0.72-1.06) | AUC0-∞ |
Abbreviations: AUC0-∞ = area under the plasma concentration-time curve from zero to infinity; Cmax = maximum plasma concentration; GLSM = geometric least-squares mean.
aParameter for which a statistically significant change was observed (CI excluded 1).
Avoid coadministration of imlunestrant with P-gp or BCRP substrates, where a small change in substrate plasma concentration may lead to serious toxicities.2
Coadministration of imlunestrant with itraconazole (a strong CYP3A inhibitor) significantly increased the AUC0-∞ and Cmax of imlunestrant (Summary of Imlunestrant Drug-Drug Interactions as a Precipitant and Object). Avoid coadministering imlunestrant with strong CYP3A inhibitors. If concomitant use cannot be avoided, decrease the imlunestrant dose to 200 mg once daily.1,2
Additionally, coadministration of imlunestrant with carbamazepine (a strong CYP3A inducer) significantly decreased the AUC0-∞ and Cmax of imlunestrant (Summary of Imlunestrant Drug-Drug Interactions as a Precipitant and Object). Avoid concomitant use of strong CYP3A inducers with imlunestrant. If concomitant use is unavoidable, increase the imlunestrant dose to 600 mg once daily.1,2
There were no clinically meaningful effects on the pharmacokinetics of imlunestrant when coadministered with omeprazole (a gastric acid-reducing agent) or quinidine (a P-gp inhibitor).2,3
Imlunestrant had no clinically meaningful effects on the pharmacokinetics of
- midazolam (a CYP3A substrate)
- repaglinide (a CYP2C8 substrate)
- omeprazole (a CYP2C19 substrate), or
- dextromethorphan (a CYP2D6 substrate).1-3
In Vitro Study
Imlunestrant is not a substrate of
- BCRP
- organic cation transporter 1 (OCT1)
- organic anion transporting polypeptide (OATP) 1B1, or
- OATP1B3.2
Enclosed Prescribing Information
References
The published references below are available by contacting 1-800-LillyRx (1-800-545-5979).
1Datta-Mannan A, Shanks E, Yuen E, et al. Pharmacokinetic drug-drug interactions of imlunestrant in healthy female participants of nonchildbearing potential. Poster presented at: Annual Meeting of the American Association of Pharmaceutical Scientists (AAPS) PharmSci 360; October 20-23, 2024; Salt Lake City, UT. Accessed February 13, 2026. https://aaps2024.eventscribe.net/ajaxcalls/PosterInfo.asp?PosterID=679226
2Inluriyo [package insert]. Indianapolis, IN: Eli Lilly and Company; 2025.
3Datta-Mannan A, Shanks E, Yuen E, et al. Phase 1 study evaluating the effect of food and omeprazole-induced gastric pH change on the pharmacokinetics and safety of imlunestrant in healthy females. Clin Ther. 2026;48(1):81-87. https://doi.org/10.1016/j.clinthera.2025.10.007
Date of Last Review: April 15, 2026