Elacestrant

What is Elacestrant?

• Elacestrant (Orserdu), is an estrogen receptor antagonist.

Elacestrant

Elacestrant v.02

What are the uses of this medicine?

• Elacestrant (Orserdu) is a prescription medicine to treat women who have gone through menopause and adult men with estrogen receptor (ER)-positive, human epidermal growth factor receptor 2 (HER2)-negative, ESR1-mutated advanced breast cancer or breast cancer that has spread to other parts of the body (metastatic), and whose disease has progressed after endocrine therapy.

How does this medicine work?

• An orally available, selective estrogen receptor degrader (SERD) and selective estrogen receptor modulator (SERM), with potential antineoplastic and estrogen-like activities.
• Upon oral administration of higher doses of elacestrant, this agent acts as a SERD, which binds to the estrogen receptor (ER) and induces a conformational change that results in the degradation of the receptor.
• This may inhibit the growth and survival of ER-expressing cancer cells.
• At lower doses of this agent, RAD1901 acts as a SERM and has estrogen-like effects in certain tissues, which can both reduce hot flashes and protect against bone loss.
• In addition, elacestrant is able to cross the blood-brain barrier (BBB).

Who Should Not Use this medicine ?

• This medicine have no usage limitations.

What drug interactions can this medicine cause?

• Tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take.
• Orserdu 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.

Be sure to mention any of the following:

• Strong and Moderate CYP3A4 Inducers
• Strong and Moderate CYP3A4 Inhibitors

Is this medicine FDA approved?

• Elacestrant was approved for medical use in the United States in January 2023.

How should this medicine be used?

• Select patients for treatment with Orserdu based on the presence of ESR1 mutations.

Recommended dosage:

• The recommended dosage of Orserdu is 345 mg taken orally with food once daily until disease progression or unacceptable toxicity occurs.
• Dose interruption, reduction, or permanent discontinuation may be required due to adverse reactions.

Administration:

• Take Orserdu exactly as your healthcare provider tells you.
• Do not change your dose or stop taking Orserdu unless your healthcare provider tells you.
• Take Orserdu 1 time each day, at about the same time each day.
• Take Orserdu with food. Taking Orserdu with food may help reduce nausea and vomiting.
• Swallow Orserdu tablets whole. Do not chew, crush or split the tablets before swallowing.
• Do not take any Orserdu tablets that are broken, cracked, or that look damaged.
• If you miss a dose of Orserdu or vomit after taking a dose of Orserdu, do not take another dose of Orserdu on that day. Skip the dose and take your next dose the following day at your regularly scheduled time.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Tablets: 345 mg and 86 mg

This medicine is available in fallowing brand namesː

• Orserdu

What side effects can this medication cause?

The most common side effects of this medicine may include:

• muscle and joint (musculoskeletal) pain
• nausea
• increased cholesterol and triglyceride levels in your blood
• increased liver function tests
• tiredness
• decreased red blood cell counts
• vomiting
• decreased salt (sodium) levels in your blood
• increased kidney function test
• decreased appetite
• diarrhea
• headache
• constipation
• stomach-area (abdominal) pain
• hot flush
• indigestion or heartburn

Less common, but serious side effects may include:

• hypercholesterolemia
• hypertriglyceridemia

What special precautions should I follow?

• Hypercholesterolemia and hypertriglyceridemia occurred in patients taking Orserdu. Advise patients that hypercholesterolemia and hypertriglyceridemia may occur while taking Orserdu. Inform patients that lipid profile monitoring will be performed prior to starting and periodically while taking Orserdu.
• Orserdu can cause fetal harm. Advise pregnant women and females of reproductive potential of the potential risk to a fetus. Advise females to inform their healthcare provider of a known or suspected pregnancy.
• Advise females of reproductive potential to use effective contraception during treatment with Orserdu and for 1 week after the last dose. Advise male patients with female partners of reproductive potential to use effective contraception during treatment with Orserdu and for 1 week after the last dose.
• Advise women not to breastfeed during treatment with Orserdu and for 1 week after the last dose.
• Advise males and females of reproductive potential that Orserdu may impair fertility.

What to do in case of emergency/overdose?

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.

Can this medicine be used in pregnancy?

• Based on findings in animals and its mechanism of action, Orserdu can cause fetal harm when administered to a pregnant woman.
• Orserdu can harm your unborn baby.

Females who are able to become pregnant:

• Your healthcare provider may do a pregnancy test before you start treatment with Orserdu.
• You should use effective (contraception) birth control during treatment with Orserdu and for 1 week after the last dose.
• Tell your healthcare provider right away if you become pregnant or think you may be pregnant during treatment with Orserdu.

Can this medicine be used in children?

• It is not known if Orserdu is safe and effective in children.

What are the active and inactive ingredients in this medicine?

• Active ingredient: elacestrant
• Inactive ingredients: colloidal silicon dioxide, crospovidone, magnesium stearate (non-bovine), microcrystalline cellulose, silicified microcrystalline cellulose and Opadry II Blue (polyvinyl alcohol, titanium dioxide, polyethylene glycol, FD&C Blue #1 and talc).

Who manufactures and distributes this medicine?

• Manufactured for: Stemline Therapeutics, Inc., New York, NY

What should I know about storage and disposal of this medication?

• Store Orserdu at room temperature 68℉ to 77℉ (20℃ to 25℃).

• Dailymed label info on Elacestrant
• FDA Elacestrant