Enzalutamide

What is Enzalutamide

• Enzalutamide (Xtandi) is an androgen receptor inhibitor used to treat prostate cancer that is castration resistant (has not responded to treatments that lower testosterone levels).

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Enzalutamide

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Enzalutamide molecule ball

What are the uses of this medicine?

Xtandi is a prescription medicine used to treat men with prostate cancer that:

• no longer responds to a hormone therapy or surgical treatment to lower testosterone
• has spread to other parts of the body and responds to a hormone therapy or surgical treatment to lower testosterone.

How does this medicine work?

• Enzalutamide is an androgen receptor inhibitor that acts on different steps in the androgen receptor signaling pathway.
• Enzalutamide has been shown to competitively inhibit androgen binding to androgen receptors; and consequently, inhibits nuclear translocation of androgen receptors and their interaction with DNA.
• A major metabolite, N‑desmethyl enzalutamide, exhibited similar in vitro activity to enzalutamide.
• Enzalutamide decreased proliferation and induced cell death of prostate cancer cells in vitro, and decreased tumor volume in a mouse prostate cancer xenograft model.

Who Should Not Use this medicine ?

• This medicine have no usage limitations.

What drug interactions can this medicine cause?

• Co‑administration of Xtandi with strong CYP2C8 inhibitors should be avoided if possible. If co-administration of Xtandi with a strong CYP2C8 inhibitor cannot be avoided, reduce the dose of Xtandi
• Avoid co‑administration with strong CYP3A4 inducers as they can decrease the plasma exposure to Xtandi. If co-administration is necessary, increase the dose of Xtandi.
• Avoid co‑administration with CYP3A4, CYP2C9 and CYP2C19 substrates with a narrow therapeutic index, as Xtandi may decrease the plasma exposures of these drugs. If Xtandi is co-administered with warfarin (CYP2C9 substrate), conduct additional INR monitoring.

Is this medicine FDA approved?

• Enzalutamide was developed and marketed by Medivation for the treatment of prostate cancer.
• It was approved by the U.S. Food and Drug Administration (FDA) for the treatment of mCRPC in the United States in August 2012, and for the treatment of non metastatic castration-resistant prostate cancer in July 2018.

How should this medicine be used?

Recommended dosage:

• The recommended dose of Xtandi is 160 mg (two 80 mg tablets or four 40 mg tablets or four 40 mg capsules) administered orally once daily.

Concomitant Strong CYP2C8 Inhibitors

• The concomitant use of strong CYP2C8 inhibitors should be avoided if possible. If patients must be co-administered a strong CYP2C8 inhibitor, reduce the Xtandi dose to 80 mg once daily.

Concomitant Strong CYP3A4 Inducers

• The concomitant use of strong CYP3A4 inducers should be avoided if possible. If patients must be co-administered a strong CYP3A4 inducer, increase the Xtandi dose from 160 mg to 240 mg once daily.

Administration:

• Take your prescribed dose of Xtandi 1 time a day, at the same time each day.
• Your healthcare provider may change your dose if needed.
• Do not change or stop taking your prescribed dose of Xtandi without talking with your healthcare provider first.
• Xtandi can be taken with or without food.
• Swallow Xtandi capsules or tablets whole. Do not chew, dissolve, or open the capsules. Do not cut, crush, or chew the tablets.
• If you are receiving gonadotropin-releasing hormone (GnRH) therapy, you should continue with this treatment during your treatment with Xtandi unless you have had a surgery to lower the amount of testosterone in your body (surgical castration).
• If you miss a dose of Xtandi, take your prescribed dose as soon as you remember that day. If you miss your daily dose, take your prescribed dose at your regular time the next day. Do not take more than your prescribed dose of Xtandi each day.

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

This medicine is available in fallowing doasage form:

• As Capsule 40 mg
• Tablet: 40 mg, 80 mg

This medicine is available in fallowing brand namesː

• Xtandi

What side effects can this medication cause?

The most common side effects of this medicine include:

• weakness or feeling more tired than usual
• back pain
• hot flashes
• constipation
• joint pain
• decreased appetite
• diarrhea
• high blood pressure

Xtandi may cause serious side effects including:

• Seizure
• Posterior Reversible Encephalopathy Syndrome (PRES)
• Allergic Reactions
• Heart disease
• Falls and fracture

What special precautions should I follow?

• Seizure occurred in 0.5% of patients receiving Xtandi. In patients with predisposing factors, seizures were reported in 2.2% of patients. Permanently discontinue Xtandi in patients who develop a seizure during treatment.
• There have been reports of posterior reversible encephalopathy syndrome (PRES) in patients receiving Xtandi. Discontinue Xtandi.
• Hypersensitivity reactions, including edema of the face (0.5%), tongue (0.1%), or lip (0.1%) have been observed with enzalutamide. Discontinue Xtandi.
• Ischemic Heart Disease may occur. Optimize management of cardiovascular risk factors. Discontinue Xtandi for Grade 3-4 events.
• Falls and Fractures occurred in 11% and 10% of patients receiving Xtandi, respectively. Evaluate patients for fracture and fall risk, and treat patients with bone-targeted agents according to established guidelines.
• Xtandi can cause fetal harm and loss of pregnancy. Advise males with female partners of reproductive potential to use effective contraception.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• increased risk of seizure

Management of overdosage:

• In the event of an overdose, stop treatment with Xtandi and initiate general supportive measures taking into consideration the half-life of 5.8 days.

Can this medicine be used in pregnancy?

• The safety and efficacy of Xtandi have not been established in females.
• Based on animal reproductive studies and mechanism of action, Xtandi can cause fetal harm and loss of pregnancy.

Can this medicine be used in children?

• Safety and effectiveness of Xtandi in pediatric patients have not been established.

What are the active and inactive ingredients in this medicine?

Xtandi capsules

• Active ingredient: enzalutamide
• Inactive ingredients: caprylocaproyl polyoxylglycerides, butylated hydroxyanisole, butylated hydroxytoluene, gelatin, sorbitol sorbitan solution, glycerin, purified water, titanium dioxide, black iron oxide.

Xtandi tablets

• Active ingredient: enzalutamide
• Inactive ingredients: hypromellose acetate succinate, microcrystalline cellulose, colloidal silicon dioxide, croscarmellose sodium, and magnesium stearate.
• The tablet film-coat contains hypromellose, talc, polyethylene glycol, titanium dioxide, and ferric oxide.

Who manufactures and distributes this medicine?

• Manufactured for and Distributed by: Astellas Pharma US, Inc., Northbrook, IL
• Marketed by: Astellas Pharma US, Inc., Northbrook, IL 60062 Pfizer Inc., New York, NY

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

• Xtandi capsules and tablets come in a child-resistant bottle.
• Store Xtandi capsules and tablets between 68°F to 77°F (20°C to 25°C).
• Keep Xtandi capsules and tablets dry and in a tightly closed container.

• Dailymed label info on Enzalutamide
• FDA Enzalutamide

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