Bdenza — Enzalutamide 40 mg (112 Capsules)

Bdenza is available in the form of oral capsules containing a strictly calibrated dose of the active pharmaceutical ingredient:

• Active Compound: Enzalutamide — 40 mg in each capsule.
• Excipients: Caprylocaproyl macrogolglycerides, butylhydroxyanisole, butylhydroxytoluene, gelatin, sorbitol, sorbitan solution, glycerin, titanium dioxide, purified water.
• Appearance: Soft gelatin oblong capsules with an oily filling, packed in blisters and enclosed in a branded cardboard box.

Pharmacodynamics: Enzalutamide is a potent inhibitor of the androgen receptor signaling pathway. It competitively binds to androgen receptors, blocks their nuclear translocation (transfer of the complex into the cell nucleus), and prevents its binding to DNA, which deprives the tumor of stimuli for division.

Pharmacokinetics: The drug is rapidly absorbed in the gastrointestinal tract, reaching peak plasma concentrations within 1–2 hours after ingestion. It is metabolized in the liver with the involvement of CYP2C8 and CYP3A4 isoenzymes to form an active metabolite. Excretion occurs primarily via the kidneys and intestines, with a half-life of approximately 5.8 days.

Bdenza 40 mg is used as prescribed by a specialized professional (oncologist or urologist) for the treatment of the following conditions:

• 🔹 Metastatic Castration-Resistant Prostate Cancer (mCRPC): In patients whose disease progresses during or following standard androgen deprivation therapy.
• 🔹 Non-Metastatic Castration-Resistant Prostate Cancer (nmCRPC): In men with a high risk of developing metastases (characterized by a rapidly rising prostate-specific antigen — PSA level).
• 🔹 Metastatic Hormone-Sensitive Prostate Cancer (mHSPC): In combination with androgen deprivation therapy to achieve maximum control over the tumor process.

Administration of the drug is carried out strictly under medical supervision. Alteration of the recommended dosages without prior consultation is not permitted:

• Recommended Daily Dose: Is 160 mg, which is equivalent to taking 4 capsules of 40 mg simultaneously once daily.
• Method of Administration: Capsules are taken orally, swallowed whole and washed down with a sufficient amount of water. Capsules must not be chewed, bitten, or dissolved.
• Relation to Food: The drug can be taken independently of food intake (either before or after meals), preferably at the same fixed time of day.
• Dose Adjustments: Upon development of severe toxicity or intolerable side effects, the treating physician may temporarily interrupt treatment or reduce the daily dose to 120 mg or 80 mg.

The use of Bdenza capsules is strictly prohibited in the presence of the following contraindications or medical conditions:

• ⛔ Hypersensitivity: Individual intolerance to enzalutamide or any of the excipients included in the shell and core of the capsule.
• ⛔ Female Gender: The drug is developed exclusively for the treatment of men and is strictly contraindicated in women, particularly during pregnancy and lactation.
• ⛔ Severe Hepatic Impairment: Severe liver function disorders (Child-Pugh Class C).
• ⛔ Age Restrictions: Children and adolescents under 18 years of age (safety and efficacy of use in children have not been established).

Enzalutamide actively interacts with many liver enzymes, requiring caution when selecting concomitant therapy:

• ❌ CYP2C8 Inhibitors: Drugs that inhibit this isoenzyme (e.g., gemfibrozil) can increase the systemic concentration of enzalutamide in the blood, requiring a dose reduction.
• ❌ CYP3A4 and CYP2C8 Inducers: Agents that induce these enzymes (e.g., rifampicin, St. John's wort) can reduce the clinical efficacy of enzalutamide.
• ⚠️ Effect on Other Medications: Enzalutamide is a strong CYP3A4 inducer, which can significantly lower plasma concentrations of concomitant drugs metabolized by this enzyme (including certain anticoagulants and statins).

The drug is not intended for use in women, however, its strong teratogenic properties impose obligations on male patients:

• Risks to the Fetus: Entry of the active substance into a pregnant woman's body can cause severe developmental defects or fetal death.
• Contraceptive Rules: If the patient is sexually active with a woman of childbearing potential, a condom must be used in combination with another highly effective method of contraception during treatment and for 3 months after its completion.
• Protection of Pregnant Partners: If the patient's partner is pregnant, the use of a condom is mandatory to prevent fetal exposure to the drug during sexual contact.

Enzalutamide therapy can lead to the development of side effects, the severity of which requires regular monitoring of the patient's condition:

• 🟢 General Disorders (Very Common): Severe fatigue, general weakness, hot flashes, increased blood pressure (arterial hypertension).
• 🟡 Musculoskeletal System: Joint pain (arthralgia), muscle weakness, back pain, increased risk of bone fractures.
• 🟡 Gastrointestinal and Metabolism: Decreased appetite, altered taste sensations, dry skin, headache.
• 🟠 Neurological Complications: Memory impairment, cognitive disorders, anxiety. In rare cases (less than 1%), the development of seizures is possible.
• ⚠️ Urgent Medical Attention: If seizures, severe confusion, sudden memory loss, or a sharp uncontrolled spike in blood pressure occur, stop taking the medication immediately and seek hospital care.

Cases of acute enzalutamide overdose in medical practice are limited, but exceeding the dose increases the risks of toxicity:

• Main Manifestations: The primary expected symptom of an overdose is a significant increase in the frequency and severity of seizures, as well as an increase in the severity of general fatigue.
• First Aid: Discontinuation of the drug, immediate gastric lavage (if a superdose was ingested recently), and administration of sorbents.
• Treatment: No specific antidote exists. Supportive and symptomatic therapy is prescribed under medical supervision. Given the long half-life, long-term monitoring of the patient is established.

Maintaining the original storage conditions ensures the therapeutic stability of the soft capsules throughout their entire shelf life:

• 🌡️ Temperature Regimen: Store in a dry place at a stable room temperature not exceeding 25°C. Do not allow freezing or overheating.
• 📦 Environmental Protection: Keep the capsules in their original blisters inside the factory cardboard pack to prevent exposure to moisture and direct sunlight.
• 👶 Accessibility: The medicinal product must be kept in a safe, locked place entirely out of reach of children and pets.
• ⏳ Package Contents: The original package contains 4 blisters with 28 capsules each, totaling 112 capsules, designed for a standard 28-day course of treatment.