Enzalutamide Bdenza 40 Mg Capsules Xtandi

[Drug Name]

Generic Name: Enzalutamide Capsules

Brand Name: Anketan, XTANDI

English Name: Enzalutamide Capsules

Pinyin: Enzalu’an Jiaonang

Specification: 40 mg/capsule; 112 capsules/box

Manufacturer: BDR Pharmaceuticals

[Composition]

The active ingredient of this product is enzalutamide.

Chemical Name: (R)-4-[3-[4-cyano-3-(trifluoromethyl)phenyl]-5,5-dimethyl-4-oxo-2-thioimidazolidin-1-yl]-2-fluoro-N-methylbenzamide

[Description]

This product is a capsule; the contents are a white powder.

[Indications]

Enzalutamide is an androgen receptor inhibitor indicated for the treatment of:

1.  Castration-resistant prostate cancer (CRPC):

Metastatic castration-resistant prostate cancer in adult men. 

Non-metastatic castration-resistant prostate cancer in adult men who are asymptomatic or mildly symptomatic after failure of androgen deprivation therapy (ADT) and are unwilling or unable to undergo chemotherapy.

2.  Metastatic hormone-sensitive prostate cancer (mHSPC):

In combination with androgen deprivation therapy (ADT) for the treatment of metastatic hormone-sensitive prostate cancer in adult men.

[Dosage and Administration]

Recommended dose: 160 mg (i.e., four 40 mg capsules) taken orally once daily.

Administration method:

Swallow the capsules whole; do not chew, dissolve, or open them.

May be taken with or without food.

Take at approximately the same time each day. 

If a dose is missed, take it as soon as possible; however, if the missed dose is not remembered until the following day, skip the missed dose and take the next dose according to the original schedule. Do not take a double dose.

[Adverse Reactions]

Enzalutamide may cause a range of adverse reactions; the incidence varies from person to person. Common adverse reactions include:

Very common (≥ 1/10):

General: Asthenia/fatigue, arthralgia, hot flushes, hypertension. 

Musculoskeletal: Muscle weakness, musculoskeletal pain. 

Nervous system: Headache, dizziness. 

Psychiatric: Insomnia. 

Gastrointestinal: Nausea, constipation, diarrhea.

Important adverse reactions requiring vigilance:

Seizures: Risk is increased in patients with a history of seizures or predisposing factors. Be alert for symptoms that may precede a seizure (e.g., loss of consciousness, convulsions) during treatment. 

Posterior Reversible Encephalopathy Syndrome (PRES): A rare neurological condition; symptoms include seizures, headache, confusion, and visual disturbances. Discontinue use and seek medical attention immediately if this occurs. 

Hypersensitivity reactions: Severe allergic reactions, such as angioedema, may occur. 

Ischemic heart disease: May increase the risk of myocardial ischemic events. 

Falls and fractures: Risk of falls may increase due to dizziness, fatigue, or asthenia.

【Contraindications】

Contraindicated in patients with a history of severe hypersensitivity to enzalutamide or any of the excipients.

Contraindicated in pregnant women or women of childbearing potential, as the drug may cause fetal harm.

Warning: This drug must not be used by women, particularly pregnant or breastfeeding women. Men handling this drug should not cause their female partners to become pregnant.

【Precautions】

1.  Seizures: Seizures have occurred in patients during clinical trials. Use with caution in patients with a history of seizures or co-morbidities that may lower the seizure threshold.

2.  Drug interactions:

Enzalutamide is a strong CYP3A4 inducer and a moderate inducer of CYP2C9 and CYP2C19. It reduces the plasma concentrations of many drugs metabolized by these enzymes, thereby affecting their efficacy. Drugs requiring special attention include: warfarin (CYP2C9 substrate), certain antiepileptics, antifungals, statins, calcium channel blockers, and certain sedatives/hypnotics. 

Please be sure to inform your doctor of all medications you are currently taking (including prescription drugs, over-the-counter medications, and herbal products) during your consultation.

3.  Laboratory tests: Blood pressure, complete blood count, liver function, etc., should be monitored regularly during treatment.

4.  Effects on the ability to drive and operate machinery: This product may cause fatigue, dizziness, etc.; exercise caution when driving or operating hazardous machinery until you know how this drug affects you.

[Use in Pregnant and Lactating Women]

Contraindicated. As previously stated, this product is not intended for use in women.

[Use in Children]

The safety and efficacy of this product in pediatric patients have not been established.

[Use in the Elderly]

In clinical studies, no overall differences in safety or efficacy were observed between elderly patients (≥65 years) and younger patients; no dose adjustment is required.

[Drug Interactions]

(See [Precautions] for details)

Potent CYP2C8 inhibitors (e.g., gemfibrozil): May increase plasma concentrations of enzalutamide; exercise caution during co-administration.

Potent CYP3A4 inducers (e.g., rifampicin, carbamazepine): May decrease plasma concentrations of enzalutamide; avoid co-administration or consider increasing the enzalutamide dose.

Drugs metabolized by CYP3A4, CYP2C9, or CYP2C19: Enzalutamide reduces plasma concentrations of these drugs; dose adjustments for these drugs may be required during co-administration.

[Overdose]

In clinical trials, patients have received daily doses of up to 480 mg. Reported events were consistent with the drug's adverse reactions.

There is no specific antidote. In the event of overdose, discontinue enzalutamide and initiate general supportive care, including monitoring of vital signs.

[Pharmacology and Toxicology]

Pharmacological action: Enzalutamide is an androgen receptor signaling inhibitor. It works through three key mechanisms: competitively inhibiting the binding of androgens to the receptor; inhibiting nuclear translocation (preventing the receptor from entering the cell nucleus); and inhibiting the binding of the androgen receptor to DNA. Consequently, it suppresses the growth of prostate cancer cells and induces cell death.

[Storage]

Store below 25°C.

Keep out of reach of children.

Specifications

Product Name: Enzalutamide Soft Capsules (Xtandi) 40mg × 112 capsules (Bdenza)

Common Name: Xtandi

Active Ingredient: Enzalutamide

Dosage Form: Capsule

Specification: 40mg/capsule; 112 capsules/box

Manufacturer: BDR Pharmaceuticals

Indication: Indicated for patients with metastatic castration-resistant prostate cancer who have previously received docetaxel therapy.

Dosage and Administration: 160 mg orally once daily. Swallow the capsules whole. Do not chew, dissolve, or open the capsules. May be taken with or without food.