Source: European Medicines Agency (EU) Revision Year: 2026 Publisher: Eli Lilly Nederland B.V., Papendorpseweg 83, 3528 BJ Utrecht, The Netherlands
Inluriyo is indicated as monotherapy for the treatment of adult patients with oestrogen receptor (ER)-positive, HER2-negative, locally advanced or metastatic breast cancer with an activating ESR1-mutation, who have disease progression following prior treatment with an endocrine based regimen (for biomarker-based patient selection, see section 4.2).
In pre- or perimenopausal women, or men, Inluriyo should be combined with a luteinising hormone-releasing hormone (LHRH) agonist.
Treatment should be initiated and supervised by a physician experienced in the use of anticancer therapies.
Patients with ER-positive, HER2-negative advanced breast cancer should be selected for treatment based on the presence of an activating ESR1-mutation in tumour or in plasma specimens, using a CE-marked in vitro diagnostic (IVD) with the corresponding intended purpose. If the CE-marked IVD is not available, the presence of an activating ESR1-mutation should be assessed by an alternative validated test.
The recommended dose of imlunestrant is 400 mg orally (two 200 mg film-coated tablets), once daily.
It is recommended that treatment is continued as long as the patient is deriving clinical benefit from therapy or until unacceptable toxicity occurs.
If a dose is missed, it can be taken up to 6 hours after the time it is usually taken. After more than 6 hours, the dose should be skipped for that day. An additional dose should not be taken. On the next day, the dose should be taken at the usual time.
If the patient vomits after taking the dose, the patient should not take an additional dose on that day and should resume the usual dosing schedule the next day at the usual time.
If dose reduction is necessary, the dose should be decreased by 200 mg. Management of some adverse reactions may require dose interruption and/or dose reduction as shown in Tables 1 and 2. The treatment should be discontinued for patients unable to tolerate 200 mg once daily.
Table 1. Recommended dose modification for increased ALT and AST:
| Toxicitya | Dose modification |
| Persistent or Recurrent Grade 2 AST or ALT, if baseline was normal | Suspend until toxicity resolves to baseline or Grade 1 if baseline was normal. Dose reduction is not required. |
| Grade 3 AST or ALT if baseline was normal Or Grade 2 or above AST or ALT if baseline was abnormal Or AST or ALT > 8 × ULN (whichever is the lower threshold) | Suspend until toxicity resolves to baseline or Grade 1 if baseline was normal. Resume at 200 mg dose level or discontinue if receiving 200 mg daily. |
| Grade 4 AST or ALT if baseline was normal | Discontinue dosing. |
| AST or ALT ≥ 3 × ULN concurrent with total bilirubin (TBL) ≥ 2 × ULN if baseline was normal in the absence of cholestasis Or AST or ALT ≥ 2 × baseline concurrent with TBL ≥ 2 × ULN if baseline was abnormal, in the absence of cholestasis | Discontinue dosing. |
a NCI CTCAE v5.0
ULN: upper limit of normal
Alanine aminotransferase (ALT) and aspartate aminotransferase (AST) should be monitored during treatment, and as clinically indicated.
Table 2. Recommended dose modification for adverse reactions (except increased ALT and AST):
| Toxicitya | Dose 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. Dose reduction is not required. |
| Grade 3 (except non-hepatic asymptomatic laboratory changes) | Suspend until toxicity resolves to baseline or ≤ Grade 1. Resume at next lower dose level or discontinue if receiving 200 mg daily. |
| Grade 4 (except non-hepatic asymptomatic laboratory changes) | Suspend until toxicity resolves to baseline or ≤ Grade 1. Resume at next lower dose level or discontinue if receiving 200 mg daily. Closely monitor on resuming treatment. |
a NCI CTCAE 5.0
Concomitant use of strong CYP3A inducers should be avoided. If strong CYP3A inducers cannot be avoided, the imlunestrant dose should be increased by 200 mg once daily (see section 4.5).
Concomitant use of strong CYP3A inhibitors should be avoided. If strong CYP3A inhibitors cannot be avoided, the imlunestrant dose should be decreased by 200 mg once daily (see section 4.5).
No dose adjustment is required on the basis of patient age (see section 5.2). Limited data are available in patients ≥75 years of age (see section 5.2).
No dose adjustment is recommended for patients with mild hepatic impairment (Child-Pugh A). The dose should be reduced to 200 mg once daily in patients with moderate (Child-Pugh B) or severe (Child-Pugh C) hepatic impairment.
No dose adjustment is necessary in patients with mild or moderate renal impairment. Limited data indicates that the exposure of imlunestrant may be increased in patients with severe renal impairment, end stage renal disease, or in patients on dialysis (see section 5.2). Treatment should be administered with caution in patients with severe renal impairment, with close monitoring for signs of toxicity.
There is no relevant use of imlunestrant in the paediatric population in the indication of locally advanced breast cancer.
Inluriyo is for oral use.
Patients should take their dose at approximately the same time each day.
The tablets should be taken on an empty stomach at least 2 hours before or 1 hour after food (see section 5.2). The tablets should be swallowed whole (patients should not split, crush, or chew the tablets before swallowing). The effects of splitting, crushing, or chewing the tablets have not been investigated and may impact the safety, efficacy, or stability of the product. Exposure to the active substance could be harmful for caregivers.
Symptoms of overdose have not been established. The ADRs reported in association with doses higher than the recommended dose were consistent with the established safety profile (see section 4.8). The most frequent ADRs at higher doses were diarrhoea, nausea, fatigue and arthralgia. There is no known antidote for an overdose of imlunestrant. Patients should be closely monitored, and supportive care should be provided.
3 years.
This medicinal product does not require any special storage conditions.
Polychlorotrifluoroethylene (PCTFE)/Polyvinylchloride (PVC) blister sealed with aluminium foil in packs of 14, 28, 42, 56, 70 or 168 film-coated tablets.
Not all pack sizes may be marketed.
Any unused medicinal product or waste material should be disposed of in accordance with local requirements.
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