Imlunestrant
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From MedlinePlus, U.S. National Library of Medicine
Specialty pharmacy: therapy management checklist, storage and cold chain, dosing calendar, Medicare Part D coverage.
Estrogen Receptor Antagonist
Dosing in kidney impairment
This label has no separate kidney-impairment dosing section. Check warnings and clinical pharmacology in the full label.
Dosing in liver impairment
Dosage in Patients with Hepatic Impairment The recommended dosage of INLURIYO for patients with moderate (Child-Pugh B) or severe (Child-Pugh C) hepatic impairment is 200 mg once daily. Monitor for increased adverse reactions [see Clinical Pharmacology] .
| Grade | INLURIYO Dosage Modifications |
| Persistent or recurrent Grade 2 that does not resolve with maximal supportive measures within 7 days to baseline or Grade 1 | Suspend until toxicity resolves to baseline or ≤Grade 1. Resume INLURIYO at the same dose level. |
| Grade 3 or 4 (except non-hepatic asymptomatic laboratory changes) | Suspend until toxicity resolves to baseline or ≤Grade 1. Resume INLURIYO at next lower dose level. |
Preparation and administration
Recommended Dosage and Administration The recommended dosage of INLURIYO is 400 mg orally once daily until disease progression or unacceptable toxicity. Take on an empty stomach at least 2 hours before food, or 1 hour after food [see Clinical Pharmacology] . Take INLURIYO tablets at approximately the same time daily. Swallow the tablets whole.
Do not split, crush, or chew the tablets. Pre/perimenopausal women and men should receive a gonadotropin-releasing hormone agonist (GnRH) according to current clinical practice standards. If patient misses a dose by 6 or more hours or vomits, instruct the patient to take the next dose the following day at its scheduled time.
Drug interactions
Check interactions
Add the patient's other drugs. Matches come from both FDA labels: by name, drug class, and enzyme or transporter pathway.
- Imlunestrant
Label text (4 paragraphs)
Strong CYP3A Inhibitors: Avoid concomitant use with INLURIYO. If concomitant use cannot be avoided, decrease the INLURIYO dosage. ( 2.5 , 7.1 ) Strong CYP3A Inducers: Avoid concomitant use with INLURIYO. If concomitant use cannot be avoided, increase the INLURIYO dosage ( 2.5 , 7.1 ).
7.1 Effects of Other Drugs on INLURIYO Strong CYP3A Inhibitors Avoid concomitant use of INLURIYO with strong CYP3A inhibitors. If concomitant use cannot be avoided, reduce the dosage of INLURIYO [see Dosage and Administration ( 2.5 ), Clinical Pharmacology ( 12.3 )] . Imlunestrant is a CYP3A substrate. Concomitant use of a strong CYP3A inhibitor increases imlunestrant exposure [see Clinical Pharmacology ( 12.3 )] , which may increase the risk of INLURIYO-associated adverse reactions. Strong CYP3A Inducers Avoid concomitant use of INLURIYO with strong CYP3A inducers.
If concomitant use cannot be avoided, increase the dosage of INLURIYO [see Dosage and Administration ( 2.5 ), Clinical Pharmacology ( 12.3 )]. Imlunestrant is a CYP3A substrate. Concomitant use of a strong CYP3A inducer decreases imlunestrant exposure [see Clinical Pharmacology ( 12.3 )] , which may reduce effectiveness of INLURIYO.
7.2 Effects of INLURIYO on Other Drugs P-gp or BCRP Substrates Avoid concomitant use unless otherwise recommended in the Prescribing Information for P-gp or BCRP substrates where minimal concentration changes may lead to serious adverse reactions. Imlunestrant inhibits both P-gp and BCRP. Imlunestrant increases exposure of P-gp and BCRP substrates, which may increase the risk of adverse reactions related to these substrates [see Clinical Pharmacology ( 12.3 )].
Contraindications
None. None. ( 4 )
Safety data
Reported adverse events (FAERS)
Liver injury (LiverTox)
LiverTox has no chapter for imlunestrant. Check the label's hepatic warnings.
Pregnancy and lactation
Pregnancy
8.1 Pregnancy Risk Summary Based on findings in animals and its mechanism of action, INLURIYO can cause fetal harm when administered to a pregnant woman [see Clinical Pharmacology ( 12.1 )] . There are no available human data on INLURIYO use in pregnant women to inform the drug-associated risk. In an animal reproduction study, oral administration of imlunestrant to pregnant rats during the period of organogenesis led to embryo-fetal mortality and structural abnormalities at maternal exposures below the human exposure at the recommended dose based on AUC ( see Data ). Advise pregnant women and females of reproductive potential of the potential risk to a fetus.
The background risk of major birth defects and miscarriage for the indicated population is unknown. However, the background risk in the U.S. general population of major birth defects is 2 to 4% and of miscarriage is 15 to 20% of clinically recognized pregnancies. Data Animal Data In an embryo-fetal development study, imlunestrant was administered orally to pregnant rats during the period of organogenesis from gestation day 6 to 17 at doses of 0.3, 3, and 30 mg/kg/day. Imlunestrant caused embryo-fetal mortality (increased resorption, reduced number of live fetuses) at ≥0.3 mg/kg/day, approximately 0.1 times the human AUC at the recommended dose.
Early delivery, fetal malformations (including small jaw, protruding tongue, malrotated, and hyperextended hindlimb) and fetal variations (edema localized subcutis) were observed at ≥3 mg/kg/day, approximately 1 time the human AUC at the recommended dose.
Breastfeeding (LactMed)
No information is available on the clinical use of imlunestrant during breastfeeding. The manufacturer recommends not to breastfeed during treatment with imlunestrant and for 1 week after the last dose. If it is used with other agents, breastfeeding should not resume for the longest post-treatment duration recommended for the individual agent(s).
Supply and cost
Drug shortage status
Recalls (last 24 months)
Therapeutic equivalence (Orange Book)
Price ladder
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