Drug information of Enzalutamide

Mechanism of effect

Enzalutamide is a competitive androgen receptor inhibitor that effects multiple stages of the signalling pathway. It is able to inhibit androgen binding to its receptor, androgen receptor nuclear translocation, and subsequent interaction with DNA. As a result, proliferation of prostate cancer cells decreases which ultimately leads to apoptosis and decreased tumour volume.

Pharmacodynamic

Enzalutamide is a competitive androgen receptor inhibitor

Pharmacokinetics

Following oral administration, peak plasma concentrations are attained in about 1 hour. Plasma Protein Binding:Enzalutamide: 97–98% (mainly albumin). Metabolized in the liver by CYP2C8 and CYP3A4. Excreted in urine (71%) and feces (14%);Half-life: Enzalutamide: 5.8 days

Drug indications

Prostate Cancer

Dosage

Usual Adult Dose for Prostate Cancer 160 mg (four 40 mg capsules) orally once a day

Drug contraindications

Pregnancy

Side effects

Headache , insomnia , dizziness , fatigue , flushing , Diarrhea , asthenia , Hypertension , paresthesia , Peripheral edema , anxiety , Arthralgia , back pain , Upper respiratory tract infection

Interactions

Amlodipine/Atorvastatine , Citalopram , Medroxyprogesterone , Carbamazepine , Chlordiaze poxide , Solifenacin , Itraconazole , Bosentan , Glutazone , Dihydroergotamine , Cyclosporine , Phenobarbital , Phenytoin , Midazolam , Warfarin , Quinidine , Disulfiram , Bisoprolol , Praziquantel , teriflunomide , Dolasetron , vandetanib , Dofetilide , brigatinib , Efavirenz , Copanlisib , lumacaftor and Ivacaftor , Dabrafenib , Acalabrutinib , Maraviroc , Halofantrine , Grepafloxacin , cobicistat , Delavirdine , Sofosbuvir and velpatasvir , Fostamatinib , Apremilast , Palbociclib , Ixazomib , Tasimelteon , trabectedine , trametinib , Duvelisib , tezacaftor/ivacaftor , Alpelisib , Darolutamide , Pitolisant , atovaquone/proguanil , Clorazepate , Lopinavir and Ritonavir , Cabozantinib , Temsirolimus , ELBASVIR/GRAZOPREVIR , Larotrectinib , glasdegib , Abemaciclib , Eliglustat , Elvitegravir , Bepridil , bedaquiline , Gefitinib , Dasatinib , Cannabidiol , ambrisentan , rolapitant , voxelotor , stiripentol , Fidaxomicin , Netupitant , Capmatinib

Alerts

1-Contraindicated in women who are or may become pregnant. 2-Safety not established in patients with predisposing factors for seizures (e.g., history of seizure, underlying brain injury with loss of consciousness, TIA within past 12 months, cerebrovascular accident, brain metastases, cerebral arteriovenous malformation, concomitant use of drugs that lower seizure threshold)

Points of recommendation

1-Importance of taking enzalutamide as directed and at the same time each day 2-Risk of seizures. Importance of avoiding activities where sudden loss of consciousness could cause serious harm to self or others.

Pregnancy level

X

Related drugs

Apalutamide