Inluriyo

Inluriyo is used to treat adults with ER-positive, HER2-negative, ESR1-mutated advanced or metastatic breast cancer whose disease has progressed following at least one line of endocrine therapy. This hormone receptor-positive breast cancer treatment is specifically designed for patients with endocrine therapy-resistant breast cancer who have developed ESR1 mutations, a common cause of resistance to other hormone treatments.

Inluriyo (imlunestrant) is an oral SERD (selective estrogen receptor degrader) taken once a day. It can be used on its own (monotherapy) or in combination with abemaciclib (Verzenio).

ESR1 mutation testing is required before starting Inluriyo. This biomarker-driven therapy targets a specific genetic change that occurs in approximately 20-40% of patients with hormone therapy-resistant breast cancer.

Inluriyo is an oral SERD therapy that works through estrogen receptor degradation:

• Imlunestrant attaches to estrogen receptors (ERα) on cancer cells
• Causes receptor breakdown and disappearance
• Blocks estrogen growth signals to cancer cells
• Stops cancer cell multiplication and growth

This mechanism is particularly effective against hormone therapy resistance caused by ESR1 mutations.

In the EMBER-3 Phase 3 clinical trial (NCT04975308), Inluriyo demonstrated significant progression-free survival data:

• 38% reduction in progression or death risk compared to standard endocrine therapy
• Superior progression-free survival vs fulvestrant/exemestane for patients with ESR1-mutated metastatic breast cancer
• Median PFS: 5.5 months (Inluriyo) vs 3.8 months (comparator)
• Hazard ratio 0.62 (95% CI: 0.46-0.82), p=0.0008

Take exactly as prescribed by your healthcare provider

• Take once daily at the same time each day
• Take on an empty stomach (at least 2 hours before food or 1 hour after food)
• Swallow tablets whole. Do not chew, crush, or split.

Missed Dose Instructions

If you miss a dose by 6+ hours or vomit after taking Inluriyo:

• Do not take another dose that day
• Resume your normal dosing schedule the following day.

Tell your healthcare provider about all your medical conditions, including if you have:

• Liver disease
• Plans to become pregnant or are pregnant
• Plans to breastfeed or are breastfeeding.

Pregnancy and Breastfeeding Considerations

Pregnancy: Inluriyo can harm an unborn baby. For females with childbearing potential:

• A pregnancy test is required before starting treatment
• Use effective birth control during treatment and for 1 week after the last dose
• Tell your provider immediately if you become pregnant.

Males with female partners who can become pregnant: Use effective birth control during treatment and for 1 week after the last dose

Breastfeeding: Do not breastfeed during treatment and for 1 week after the last dose.

Fertility: May affect fertility in males and females. Discuss any concerns with your healthcare provider.

Common Side Effects

• Decreased hemoglobin (anemia)
• Muscle and joint pain
• Decreased white blood cell counts
• Increased liver function tests
• Decreased blood calcium levels
• Nausea
• Decreased platelet counts
• Constipation
• Stomach-area (abdominal) pain
• Tiredness
• Diarrhea
• Increased triglyceride and cholesterol blood levels.

Your healthcare provider will monitor your blood levels before and during treatment and may adjust dosing if needed.

Warnings: Inluriyo may cause harm to an unborn baby (see pregnancy and breastfeeding considerations below).

These are not all of the possible side effects of Inluriyo. Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

Dose of Inluriyo for ER+, HER2-, ESR1-mutated Breast Cancer:

• 400 mg once daily
• Take on an empty stomach
• Reduce dosage in moderate to severe liver impairment.

Tell your healthcare provider about all of the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements. Especially tell your healthcare provider about:

• Strong CYP3A Inhibitors, such as ketoconazole, itraconazole, clarithromycin, ritonavir, or nefazodone. Avoid concomitant use with Inluriyo. If concomitant use cannot be avoided, decrease the Inluriyo dosage
• Strong CYP3A Inducers, such as rifampin, carbamazepine, phenytoin, St. John's Wort, and phenobarbital: Avoid concomitant use with Inluriyo. If concomitant use cannot be avoided, increase the Inluriyo dosage.

Inluriyo and other medicines may affect each other, causing side effects. Know the medicines you take. Keep a list of them to show your healthcare provider or pharmacist when you get a new medicine.

• Store Inluriyo at room temperature between 68°F to 77°F (20°C to 25°C).
• Throw away (dispose of) unused Inluriyo by a medicine take-back program if available. If no take-back program is available, visit www.fda.gov/drugdisposal for instructions on how to throw away medicines in the household trash.
• Do not flush Inluriyo down the toilet.
• Keep Inluriyo and all medicines out of the reach of children.

Active ingredient: imlunestrant

Inactive ingredients: croscarmellose sodium, hydroxypropyl cellulose, magnesium stearate, and microcrystalline cellulose. The tablet coating contains polyethylene glycol, polyvinyl alcohol, talc, and titanium dioxide.

Inluriyo is a trademark of Eli Lilly and Company and is marketed by Lilly USA, LLC, Indianapolis, IN 46285, USA.