Inluriyo (Imlunestrant) instruction manual Chinese introduction

1. [Drug Name]

Product name:Inluriyo

English name:Imlunestrant

Dosage form: oral tablet

2. [Pharmacological effects and mechanisms]

Inluriyo (imlunestrant) is a selective estrogen receptor degrader (SERD) and belongs to a new generation of oral estrogen receptor antagonists. It mainly binds to and degrades the estrogen receptor α protein (encoded by the ESR1 gene), thereby blocking the estrogen signaling pathway and effectively inhibiting the proliferation and survival of tumor cells.

In estrogen receptor-positive (ER+) and human epidermal growth factor receptor 2-negative (HER2-) breast cancer, especially in patients with ESR1 mutations, tumor cells often become resistant to traditional endocrine therapies such as aromatase inhibitors or tamoxifen. Mutations in ESR1 can cause estrogen receptors to remain active, promoting cancer growth even when estrogen levels in the body are extremely low.

Inluriyo achieves sustained ER inhibition by targeting and degrading the mutated receptor, demonstrating significant clinical benefit in endocrine therapy-resistant ESR1-mutated breast cancer.

3. [Indications]

Inluriyo is indicated for adults with advanced or metastatic breast cancer (MBC) who:

Estrogen receptor positive (ER+), HER2 negative (HER2-);

PresenceESR1 gene mutation;

Disease progression after at least one endocrine therapy.

4. [Usage and Dosage]

1. Recommended dosage: 400 mg orally daily.

2. Medication: Take once a day on an empty stomach (at least 2 hours before meals or 1 hour after meals).

3. Course of treatment: Continue medication until the disease progresses or unacceptable adverse reactions occur.

4. If you miss a dose, you should take it as soon as possible; if it is close to the next dose time, skip the missed dose and do not take double dose.

5. [Testing before treatment]

Before starting treatment with Inluriyo, patients should be tested for ESR1 mutations to confirm target positivity. ESR1 mutations typically occur in approximately 20%–40% of patients with ER+ breast cancer that is resistant to hormone therapy. Detection can use plasma cell-free DNA (cfDNA) or tumor tissue gene sequencing.

6. [Adverse reactions]

In clinical trials,Inluriyo was generally well tolerated, with most adverse reactions being mild to moderate. Common laboratory abnormalities include:

Blood system: decreased hemoglobin, neutropenia, and thrombocytopenia;

Liver function:AST (aspartate aminotransferase) and ALT (alanine aminotransferase) are elevated;

Metabolic abnormalities: decreased calcium, increased cholesterol, and increased triglycerides.

Some patients may experience non-specific symptoms such as mild fatigue, nausea or loss of appetite, which are usually relieved without stopping the medication. It is recommended to regularly monitor blood routine and liver function indicators during treatment.

7. [Drug Advantages and Clinical Significance]

1. Precise target: Designed specifically for breast cancer driven by ESR1 mutations, it is a biomarker-guided precision treatment drug.

2. Oral convenience: Take once a day to reduce the frequency of injections and improve patient compliance.

3. Innovative mechanism: Different from traditional endocrine blockers, Inluriyo can directly promote the degradation of estrogen receptors and block signal transmission from the source.

4. Clinical alternatives: New treatment options are provided for patients who have failed treatments such as aromatase inhibitors and Fulvestrant.

8. [Storage Conditions]

Should be stored in a cool, dry place (temperaturebelow 25°C), away from direct sunlight and humid conditions. Please keep out of reach of children.

Reference materials:https://www.drugs.com/inluriyo.html