Revision Year: 2025
INLURIYO is indicated for the treatment of adults with estrogen receptor (ER)-positive, human epidermal growth factor receptor 2 (HER2)-negative, estrogen receptor-1 (ESR1)-mutated advanced or metastatic breast cancer with disease progression following at least one line of endocrine therapy.
Select patients for treatment of ER-positive, HER2-negative advanced or metastatic breast cancer with INLURIYO based on the presence of ESR1 mutation(s) in a plasma specimen using an FDA-approved test [see Indications and Usage (1) and Clinical Studies (14.1)].
Information on FDA-approved tests for the detection of ESR1 mutations in breast cancer is available at: https://www.fda.gov/CompanionDiagnostics.
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 (12.3)]. 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.
The recommended INLURIYO dosage modifications for adverse reactions are provided in Tables 1 and 2.
The recommended dose reduction is to 200 mg once daily.
Permanently discontinue INLURIYO in patients who are unable to tolerate 200 mg once daily.
Table 1. INLURIYO Dosage Modification - Adverse Reactions (except hepatotoxicity):
| 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. |
Table 2. INLURIYO Dosage Modification - Hepatotoxicity:
| Monitor alanine aminotransferase (ALT)/aspartate aminotransferase (AST) during imlunestrant therapy as clinically indicated. | |
| Liver Transaminase | INLURIYO Dosage Modifications |
| Persistent or Recurrent: AST/ALT >3.0-5.0×ULN | Suspend until toxicity resolves to baseline or to >ULN-3.0×ULN. Resume INLURIYO at the same dose level. |
| If AST/ALT at baseline is within the normal range: AST/ALT >5.0-20×ULN Or If AST/ALT at baseline is above ULN: AST/ALT ≥3 × baseline (if AST/ALT ≥1.5 x ULN at baseline) Or AST/ALT >8 × ULN (whichever is the lower threshold) | Suspend until toxicity resolves to baseline or to >ULN-3.0×ULN. Resume INLURIYO at next lower dose level or discontinue if receiving 200 mg daily. |
| AST/ALT >20.0×ULN Or ALT or AST ≥ 3 × ULN concurrent with TBL ≥ 2 × ULN (if ALT or AST < 1.5 × ULN at baseline), in the absence of cholestasis Or ALT or AST ≥ 2 × baseline concurrent with TBL ≥ 2 × ULN (if ALT or AST ≥ 1.5 × ULN at baseline), in the absence of cholestasis | Discontinue INLURIYO. |
Abbreviation: ALT = alanine aminotransferase, AST = aspartate aminotransferase, TBL = total bilirubin, ULN = upper limit of normal.
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 (12.3)].
Avoid concomitant use with strong CYP3A inhibitors. If concomitant use cannot be avoided, decrease the INLURIYO dosage to 200 mg once daily [see Drug Interactions (7.1)].
Avoid concomitant use with strong CYP3A inducers. If concomitant use cannot be avoided, increase the INLURIYO dosage to 600 mg once daily [see Drug Interactions (7.1)].
Store at 20°C to 25°C (68°F to 77°F). Excursions between 15°C to 30°C (59°F to 86°F) are permitted [see USP Controlled Room Temperature].
Disposal:
Dispose unused medication via a take-back option if available. Otherwise, follow FDA instructions for disposing medication in the household trash, www.fda.gov/drugdisposal. Do NOT flush down the toilet.
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