Enzalutamide – Targeted Therapy
Enzalutamide is a potent second-generation selective androgen receptor signaling inhibitor. The drug is specifically designed to treat advanced prostate cancer and acts at several stages of the signaling pathway that stimulates tumor cell growth under the influence of male sex hormones.
The mechanism of action of enzalutamide is multi-step. Unlike earlier antiandrogens, it not only competitively inhibits the binding of androgens to receptors but also prevents the translocation of the activated receptor into the cell nucleus and blocks its interaction with DNA. This effectively halts the transcription of genes responsible for cancer cell division and survival. As a result, tumor growth slows down, and levels of prostate-specific antigen (PSA) in the blood decrease.
The drug is intended for oral administration and possesses high bioavailability. Enzalutamide significantly extends the time to disease progression and increases overall survival in patients both before and after receiving chemotherapy.
Indications
Enzalutamide is used in urologic oncology for the therapy of progressive forms of prostate cancer:
- Metastatic Castration-Resistant Prostate Cancer (mCRPC): treatment of adult men when hormonal therapy has failed.
- Non-metastatic Castration-Resistant Prostate Cancer (nmCRPC): therapy for patients at high risk of developing metastases.
- Metastatic Hormone-Sensitive Prostate Cancer (mHSPC): use in combination with androgen deprivation therapy.
- Therapy Resistance: the drug is effective in patients previously treated with docetaxel and in those for whom chemotherapy has not yet been prescribed.
Dosage and administration
The enzalutamide dosing regimen requires regularity and adherence to the established dosage.
- Standard Dose: 160 mg (four 40 mg capsules or tablets) once daily.
- Administration Rules: the drug is taken orally as a whole, with or without food. It is important to take the dose at the same time every day.
- Missed Dose: if a dose is missed, it should be taken as soon as possible on the same day. If the next day has arrived, the missed dose should not be taken.
- Drug Interactions: enzalutamide is a strong inducer of CYP3A4 enzymes, which can reduce the efficacy of many concomitantly administered medications.
- Duration of Treatment: therapy continues as long as a clinical benefit is maintained or until signs of unacceptable toxicity appear.