Enzalutamide

About Enzalutamide

• Enzalutamide, initially granted regulatory approval in 2012, received authorization for individuals with metastatic castration-resistant prostate cancer (mCRPC) who had undergone prior docetaxel treatment. 
• Enzalutamide operates through three primary mechanisms of action. First, it functions as a robust and competitive binder of androgens at the androgen receptor (AR) level. 
• Second, it obstructs the translocation of AR from the cytoplasm to the nucleus. 
• Lastly, within the nucleus, it inhibits AR binding to chromosomal DNA, effectively preventing the further transcription of tumor genes.

Strength: 

Enzalutamide capsules are available in strengths of 40 mg. 

Recommended Dosage:

In the event of Grade 3 or higher toxicity or if the patient encounters an intolerable side effect, suspend the dosing for a week or until symptoms ameliorate to Grade 2 or below. Following this, recommence the treatment at either the same dosage or a reduced dose (120 mg or 80 mg), depending on the circumstances. Consult your doctor for more information. 

• The prescribed dosage for Enzalutamide is 160 mg, which corresponds to four 40 mg capsules taken orally once daily. Enzalutamide can be ingested with or without food. 
• It is crucial to swallow the capsules whole and avoid chewing, dissolving, or opening them.
• It is advisable to refrain from concurrently using potent CYP2C8 inhibitors if possible. Should it be necessary to co-administer a strong CYP2C8 inhibitor, consider reducing the daily Enzalutamide dose to 80 mg. 
• Upon discontinuation of the co-administered strong inhibitor, the Enzalutamide dosage should be reverted to the level used before initiating the potent CYP2C8 inhibitor.

Important:

Ensuring precise adherence to prescribed Enzalutamide protocols is crucial for effective treatment. Healthcare providers should maintain vigilant monitoring and swift management of any potential adverse reactions. Regular follow-up assessments, combined with transparent communication, contribute to a responsible and effective treatment approach. It is essential to inform your doctor about any pre-existing conditions before starting treatment to proactively address the possibility of adverse effects.

Warnings & Precaution:

• Do not take Enzalutamide  if you are pregnant because Enzalutamide carries a risk of fetal harm during pregnancy due to its mechanism of action. It is contraindicated in women, and use during pregnancy or if the patient becomes pregnant may lead to potential harm to the fetus and an increased risk of pregnancy loss.
• Enzalutamide, in a clinical trial, led to seizures in 0.9% of patients (7 out of 800), occurring 31 to 603 days after initiation, with none in the placebo group. Those affected were permanently discontinued, and all seizures were resolved. 
• Re-administration after seizures lacks trial data. Safety in patients with seizure predisposition is unknown, as they were excluded based on criteria like a history of seizures or brain injuries. 
• Due to seizure risk, caution is advised, particularly in activities where sudden loss of consciousness could pose harm to individuals or others.

Common Enzalutamide Side Effects:

• Asthenia/Fatigue
• Back Pain
• Diarrhea
• Arthralgia
• Hot Flush
• Peripheral Edema
• Musculoskeletal Pain
• Headache
• Upper Respiratory Infection
• Muscular Weakness
• Dizziness
• Insomnia
• Lower Respiratory Infection
• Spinal Cord Compression and Cauda Equina Syndrome
• Hematuria
• Paresthesia
• Anxiety
• Hypertension

Use in Specific Population

• Do not use Enzalutamide if you are pregnant. Before starting the medicine inform your doctor if you are pregnant or planning to get pregnant. 
• Enzalutamide is not approved for use in women, and the presence of enzalutamide in human milk remains unknown. 
• Given that various medications are excreted in breast milk, and considering the potential for severe adverse reactions in nursing infants exposed to Enzalutamide, a decision must be carefully considered, weighing the drug’s importance to the mother against the potential risks. 
• Patients should be alerted to the potential harm Enzalutamide may pose to a developing fetus. If engaging in sexual activity with a pregnant woman, it is advisable to use a condom. 
• In cases where the patient is sexually involved with a woman capable of childbearing, a condom along with another reliable form of contraception should be employed. 
• These precautions are mandatory throughout the treatment period and for three months following the completion of Enzalutamide therapy.
• The safety and effectiveness of Enzalutamide in pediatric patients have not been established. 
• No discernible differences in safety or efficacy were noted between these patients and their younger counterparts. 
• Initial dosage adjustments are unnecessary for patients with mild to moderate renal impairment. However, the suitability of Enzalutamide for individuals with baseline severe hepatic impairment (Child-Pugh Class C) or end-stage renal disease remains unassessed.

Storage and Handling

• Store Enzalutamide capsules in a dry location at temperatures between 20°C to 25°C (68°F to 77°F), ensuring the container is tightly closed. 
• Excursions within the range of 15°C to 30°C (59°F to 86°F) are permitted.
• Bottles of 120 capsules
• Do not freeze the medicine. 
• Keep the medicine away from pets and children.