Enzalutamide
Enzalutamide Uses, Dosage, Side Effects, Food Interaction and all others data.
Enzalutamide is an androgen receptor inhibitor for the treatment of castration-resistant prostate cancer. FDA approved on August 31, 2012.
Resitance to enzalutamide therapy has been observed. This may occurred due to an upregulation of NF-κB2/p52.
| Trade Name | Enzalutamide |
| Availability | Prescription only |
| Generic | Enzalutamide |
| Enzalutamide Other Names | Enzalutamida, Enzalutamide |
| Related Drugs | estradiol, Premarin, Xtandi, Casodex, Zytiga, Lynparza |
| Weight | 40mg, 40mg, 80mg |
| Type | Oral capsule, oral tablet |
| Formula | C21H16F4N4O2S |
| Weight | Average: 464.436 Monoisotopic: 464.093009286 |
| Protein binding | Enzalutamide is 97% to 98% bound to plasma proteins, primarily albumin. N-desmethyl enzalutamide is 95% bound to plasma proteins. |
| Groups | Approved |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Enzalutamide is an androgen receptor inhibitor used to treat castration-resistant prostate cancer.
Enzalutamide is indicated for the treatment of patients with metastatic castration-resistant prostate cancer who have previously received docetaxel.
Enzalutamide is also used to associated treatment for these conditions: Metastatic Castration Resistant Prostate Cancer
How Enzalutamide works
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.
Toxicity
The most common adverse reactions (≥ 5%) are 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, and hypertension.
Food Interaction
- Avoid St. John's Wort. This herb induces the CYP3A4 metabolism of enzalutamide and may reduce its serum concentration.
- Take with or without food.
Enzalutamide Drug Interaction
Major: tramadolModerate: fexofenadine, sulfamethoxazole / trimethoprim, celecoxib, atorvastatinUnknown: dicyclomine, calcium / vitamin d, calcium carbonate, docusate, leuprolide, ethanol, leuprolide, morphine, bifidobacterium infantis / lactobacillus acidophilus, calcium carbonate, acetaminophen, cyanocobalamin, cholecalciferol, denosumab, goserelin
Enzalutamide Disease Interaction
Volume of Distribution
Apparent volume of distribution (Vd/F), single oral dose = 110 L
Elimination Route
The pharmacokinetic profile of enzalutamide and N-desmethyl enzalutamide (its major active metabolite) is described by a linear two-compartment model with first-order absorption. Enzalutamide also accumulates. Food does not affect its absorption. Tmax, prostate cancer patients = 1 hour (range of 0.5-3 hours); Cmax, steady state, enzalutamide = 16.6 μg/mL; Cmax, steady state, N-desmethyl enzalutamide = 12.7 μg/mL; Time to steady state, daily dosing = 28 days;
Half Life
The mean terminal half-life (t1/2) for enzalutamide in patients after a single oral dose is 5.8 days (range 2.8 to 10.2 days). Following a single 160 mg oral dose of enzalutamide in healthy volunteers, the mean terminal t1/2 for N-desmethyl enzalutamide is approximately 7.8 to 8.6 days.
Clearance
Apparent clearance (CL/F), single oral dose = 0.56 L/h (range of 0.33 - 1.02 L/h)
Elimination Route
Enzalutamide is primarily eliminated by hepatic metabolism. 71% of the dose is recovered in urine (including only trace amounts of enzalutamide and N-desmethyl enzalutamide), and 14% is recovered in feces (0.4% of dose as unchanged enzalutamide and 1% as N-desmethyl enzalutamide).
Innovators Monograph
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