You can buy Apnat at the lowest price in the online pharmacy Nextgen.ooo . Apalutamide is an androgen receptor inhibitor used to treat non-metastatic, castration-resistant prostate cancer.
 
Apalutamide is a potent androgen receptor (AR) antagonist that selectively binds to the ligand-binding domain of the AR and blocks nuclear translocation of the AR or binding to androgen response elements. With its antitumor activity, apalutamide blocks the action of androgens that promote tumor growth. It targets the ligand-binding domain of the AR and prevents nuclear translocation of the AR, DNA binding, and transcription of AR target genes in prostate tumors. In mice bearing human CRPC xenograft models, treatment with apalutamide resulted in tumor regression in a dose-dependent manner, which was more effective than treatment with bicalutamide or enzalutamide. Unlike bicalutamide, apalutamide antagonized AR-mediated signaling in human CRPC cell lines overexpressing AR.
 
Androgen deprivation or hormone therapy can be used as part of maintenance therapy for patients with non-metastatic prostate cancer. Although most patients achieve a therapeutic response with initial hormonal therapy, many patients develop non-metastatic castration-resistant (hormone therapy resistant) prostate cancer, which is the second leading cause of cancer death in American men. Castration-resistant prostate cancer is often incurable, posing significant clinical challenges for patients. Approximately 10 to 20% of prostate cancers are castration-resistant, and up to 16% of these patients have no evidence of metastatic cancer at the time of diagnosis of castration resistance. Apalutamide has shown a good tolerability and safety profile in clinical studies.
 
Apalutamide was approved by the FDA in February 2018 for the treatment of patients with non-metastatic prostate cancer that is resistant to hormonal therapy (castration-resistant prostate cancer). It is available as an oral tablet. Apalutamide is the first FDA-approved treatment for non-metastatic castration-resistant prostate cancer.
Persistent androgen receptor (AR) signaling is a common feature of castration-resistant prostate cancer (CRPC) and is associated with AR gene amplification, AR gene mutation, AR overexpression, or increased androgen biosynthesis in prostate tumors. Apalutamide is an AR antagonist that binds to a binding site in the ligand-binding domain of the receptor with an IC50 of 16 nM. Upon binding, apalutamide disrupts AR signaling, inhibits DNA binding, and interferes with AR-mediated gene mark transcription. Apalutamide interferes with the translocation of AR from the cytoplasm to the nucleus, thereby reducing the concentration of AR available for interaction with androgen response elements (AREs). Its major metabolite, N-desmethylapalutamide, is a less potent AR inhibitor and has been shown to be one-third as active as apalutamide in an in vitro reporter transcription assay.