|Alias||Xtandi; MDV-3100; ASP-9785|
Enzalutamide is a nonsteroidal antiandrogen (NSAA) medication which is used in the treatment of prostate cancer. It is indicated for use in conjunction with castration in the treatment of metastatic castration-resistant prostate cancer (mCRPC) and nonmetastatic castration-resistant prostate cancer. It is taken by mouth.
Side effects of enzalutamide, when added to castration, include asthenia, back pain, diarrhoea, arthralgia, and hot flashes. Rarely, it can cause seizures. It has a high potential for drug interactions. Enzalutamide is an antiandrogen and acts as an antagonist of the androgen receptor, the biological target of androgens like testosterone and dihydrotestosterone. In doing so, it prevents the effects of these hormones in the prostate gland and elsewhere in the body.
The mechanism of action of enzalutamide is as an Androgen Receptor Antagonist, and Cytochrome P450 3A4 Inducer, and Cytochrome P450 2C9 Inducer, and Cytochrome P450 2C19 Inducer.
Enzalutamide acts as a selective silent antagonist of the androgen receptor (AR), the biological target of androgens like testosterone and dihydrotestosterone (DHT). Unlike the first-generation NSAA bicalutamide, enzalutamide does not promote translocation of AR to the cell nucleus and in addition, prevents binding of AR to deoxyribonucleic acid (DNA) and AR to coactivator proteins. As such, it has been described as an AR signalling inhibitor in addition to the antagonist. The drug is described as a "second-generation" NSAA because it has greatly increased efficacy as an antiandrogen relative to so-called "first-generation" NSAAs like flutamide and bicalutamide. The drug has only 2- to 3-fold lower affinity for the AR relative to DHT, the endogenous ligand of the AR in the prostate gland.
When LNCaP cells (a prostate cancer cell line) engineered to express elevated levels of AR (as found in patients with advanced prostate cancer) were treated with enzalutamide, the expression of androgen-dependent genes PSA and TMPRSS2 was down-regulated in contrast to bicalutamide where the expression was upregulated. In VCaP cells which over-express the AR, enzalutamide induced apoptosis whereas bicalutamide did not. Furthermore, enzalutamide behaves as an antagonist of the W741C mutant AR in contrast to bicalutamide which behaves as a pure agonist when bound to the W741C mutant.
Enzalutamide is a nonsteroidal antiandrogen used to treat metastatic castration-resistant prostate cancer.
Enzalutamide was first described in 2006 and was introduced for the treatment of prostate cancer in 2012. It was the first second-generation NSAA to be introduced. The medication is available widely throughout the world.
Enzalutamide is indicated for the treatment of patients with metastatic castration-resistant prostate cancer who have previously received docetaxel.
Entamtamide (XTANDI) is an oral androgen receptor antagonist currently approved by clinical studies and the US FDA (Food and Drug Administration) for the treatment of metastatic castration-resistant prostate cancer after chemotherapy ( That is, patients with prostate cancer who have cancer or cancer cells still growing after chemotherapy can prolong their survival.
Although antiandrogen therapy has been the treatment of choice for patients with metastatic prostate cancer for 70 years, with the in-depth exploration of the molecular level of the disease, the researchers found that androgen receptors play a role in driving prostate cancer throughout the disease. Important role. A new generation of androgen receptor antagonists such as abiraterone and enzalutamide approved by the FDA has shown that they can benefit patients with advanced prostate cancer after docetaxel chemotherapy.
Enzalutamide has approximately 5- to 8-fold higher binding affinity for the androgen receptor (AR) compared to bicalutamide. One study found an IC50 of 21 nM for enzalutamide and 160 nM for bicalutamide at the AR in the LNCaP cell line (7.6-fold difference), while another found respective IC50 values of 36 nM and 159 nM (4.4-fold difference). In accordance, enzalutamide, at a dosage of 160 mg/day, has been found to produce similar increases in testosterone, estradiol, and luteinizing hormone (LH) levels relative to high-dosage bicalutamide (300 mg/day), and an almost two-fold higher increase in testosterone levels relative to 150 mg/day bicalutamide (114% versus 66%). These findings suggest that enzalutamide is a significantly more potent and effective antiandrogen in comparison. Also, unlike with the first-generation NSAAs (flutamide, nilutamide, and bicalutamide), there has been no evidence of hepatotoxicity or elevated liver enzymes in association with enzalutamide treatment in clinical trials.
Enzalutamide is an androgen receptor inhibitor with a different target than the 2010 approved cabazitaxel and the 2011 approved abiraterone.
Both enzacilide from Astellas in Japan and abiraterone from Johnson and Johnson in the United States are targeted for prostate cancer. According to statistical treatment, there are only a few differences, such as: abiraterone needs to be used together with steroids. However, enzalutamide is not needed; abiraterone needs to limit diet, and enzalutamide does not. Drugs in different countries are only different from the crowd, so there are price differences and the effect is the same.
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