Elacestrant is an oral selective estrogen receptor degrader (SERD).

1、 Drug name and main ingredients

1. Common name: Elacestrant

2. Product Name: ORSERDU ™

3. Dosage form: Oral film coated tablets

4. Main ingredients: Each tablet contains 345mg or 86mg of Eloprorelin (corresponding to 400mg and 100mg Eloprorelin Dihydrochloride, respectively)

5. Accessories: Colloidal silica, cross-linked polyvinylpyrrolidone, magnesium stearate (non animal source), microcrystalline cellulose, silicified microcrystalline cellulose, Opadry II Blue (polyvinyl alcohol, titanium dioxide, polyethylene glycol, FD&C Blue 1, talc powder).

2、 Indications

ER positive/HER2 negative, ESR1 mutant breast cancer: used to treat postmenopausal women or adult men with ER positive, HER2 negative, ESR1 mutant advanced or metastatic breast cancer, and the disease progresses after at least first-line endocrine treatment.

3、 Specifications and characteristics

1. Specifications:

345mg tablets: light blue oval shaped double convex tablets without scratches, with "MH" printed on one side.

86m g sheet: light blue circular double convex sheet without scratches, with "ME" printed on one side.

2. Packaging: 30 tablets per bottle, child safety bottle cap.

4、 Usage and dosage

1. Recommended dose: 345mg once daily, taken with meals (to reduce the risk of nausea and vomiting), swallowed whole, not chewed, crushed or divided.

2. Missed or vomited: If missed for more than 6 hours or vomited after taking the medication, skip the dose and take it at the original planned time the next day.

3. Dose adjustment:

First dose reduction: 258mg/day (3 tablets of 86mg);

Secondary reduction: 172mg/day (2 tablets of 86mg);

If further reduction is required, the medication will be permanently discontinued.

Liver injury: Moderate (Child Pugh B) dose reduced to 258mg/day, severe (Child Pugh C) is contraindicated.

5、 Medication precautions

1. Diet: Should be taken with meals to reduce gastrointestinal reactions.

2. Monitoring: Regularly check blood lipids (cholesterol, triglycerides), liver function (ALT/AST), and blood sodium levels before and during treatment.

3. Drug interactions:

Avoid using strong/medium acting CYP3A4 inhibitors (such as itraconazole) or inducers (such as rifampicin) in combination.

The substrates of P-gp/BCRP (such as digoxin and rosuvastatin) need to be reduced.

6、 Medication for special populations

1. Pregnant women: Prohibited, may cause fetal malformation (animal data shows embryotoxicity).

2. Breastfeeding period: Breastfeeding is prohibited during the treatment period and within one week after the last dose.

3. Birth plan: Patients of childbearing age need to take effective contraceptive measures (during treatment and 1 week after discontinuation of medication).

4. Elderly: No need to adjust dosage, but close monitoring is required.

7、 Adverse reactions

1. Common (>10%): musculoskeletal pain (41%), nausea (35%), high cholesterol (30%), high triglycerides (27%), fatigue (26%), vomiting (19%), diarrhea (13%), headache (12%).

2. Serious but rare: hepatotoxicity (ALT/AST elevation), venous thrombosis (6%), embryo fetal toxicity.

8、 Contraindications

There are no absolute contraindications, but it is contraindicated for patients with severe liver injury (Child Pugh C).

9、 Drug interactions

1. CYP3A4 effects: Strong inhibitors (such as clarithromycin) increase exposure to Elasmoles by 5.3 times, while strong inducers (such as rifampicin) reduce exposure by 86%.

2. P-gp/BCRP inhibition: may increase the blood drug concentration of drugs such as digoxin and rosuvastatin.

10、 Storage method

Store at room temperature (20-25 ° C), allow short-term exposure to 15-30 ° C, avoid light and moisture.

Note: If there is persistent nausea, jaundice, or muscle pain during medication, seek medical attention promptly. The specific medication should be combined with the ESR1 mutation test results.

elacestrantinformation