Informational only — Not medical advice. Always consult a licensed healthcare provider.

Community data Updated 22 hours ago

Indications

Enzalutamide is used to treat patients with castration-resistant prostate cancer (CRPC) and metastatic castration-sensitive prostate cancer (mCSPC).

⚠️ Always consult a registered physician before taking any medicine.

Pharmacology

Enzalutamide is an androgen receptor inhibitor, and it works on several steps of the androgen receptor signaling pathway. It competes with androgens for binding to the androgen receptors. Because of this, the receptors can't move into the cell nucleus and can't interact with DNA.

A major metabolite, N-desmethyl enzalutamide, showed similar activity to enzalutamide in vitro. In vitro, enzalutamide reduced the growth of prostate cancer cells and caused them to die. In a mouse prostate cancer xenograft model, it also decreased tumor volume.

Pregnancy & Breastfeeding

Enzalutamide has not been shown to be safe or effective in females. Animal reproductive studies and the way the medicine works suggest it can harm the fetus and cause loss of pregnancy. There are no human data on its use in pregnant females. When pregnant mice were given enzalutamide by mouth during organogenesis, it caused adverse developmental effects at doses lower than the maximum recommended human dose.

Safety and efficacy in females have not been established for breastfeeding either. Nobody knows whether enzalutamide passes into human milk, what it does to a breastfed infant, or whether it affects milk production. In lactating rats, enzalutamide and/or its metabolites were found in the milk.

⚠️ Talk to your doctor before taking any medicine during pregnancy or while breastfeeding.

Dosage Reference

⚠️ Reference ranges from official sources only. Consult your doctor for personalized dosing.

Adults: The recommended dose of Enzalutamide is 160 mg taken by mouth once a day, with or without food. Swallow the capsules or tablets whole. Don't chew, dissolve or open the capsules, and don't cut, crush or chew the tablets. Dosage Modifications for Adverse Reactions If a patient has a ≥Grade 3 adverse reaction, or one they can't tolerate, Enzalutamide should be withheld for one week or until symptoms improve to ≤Grade 2. After that, treatment can restart at the same dose or at a reduced dose (120 mg or 80 mg) if warranted. Strong CYP2C8 Inhibitors Avoid giving Enzalutamide together with strong CYP2C8 inhibitors. If they can't be avoided, reduce the Enzalutamide dose to 80 mg once daily. If the strong inhibitor is later stopped, increase Enzalutamide back to the dose used before the inhibitor was started. Strong CYP3A4 Inducers Avoid giving Enzalutamide together with strong CYP3A4 inducers. If they can't be avoided, increase the Enzalutamide dose from 160 mg to 240 mg orally once daily. If the strong inducer is later stopped, decrease Enzalutamide to the dose used before the inducer was started. Pediatric Use The safety and effectiveness of Enzalutamide in children have not been established. Renal Impairment No dose change is recommended for patients with mild to moderate renal impairment. Hepatic Impairment No dose change is recommended for patients with mild, moderate or severe hepatic impairment.

Side Effects & Interactions

Side Effects

No side-effect data recorded yet.