Apalutamide

1 Indications and usage erleada: is indicated for the treatment of patients with Metastatic castration-sensitive prostate cancer (mCSPC) Non-metastatic castration-resistant prostate cancer (nmCRPC) ERLEADA is an androgen receptor inhibitor indicated for the treatment of patients with metastatic castration-sensitive prostate cancer. ( 1 ) non-metastatic castration-resistant prostate cancer. ( 1 )

12.1 Mechanism of Action Apalutamide is an Androgen Receptor (AR) inhibitor that binds directly to the ligand-binding domain of the AR. Apalutamide inhibits AR nuclear translocation, inhibits DNA binding, and impedes AR-mediated transcription. A major metabolite, N-desmethyl apalutamide, is a less potent inhibitor of AR, and exhibited one-third the activity of apalutamide in an in vitro transcriptional reporter assay. Apalutamide administration caused decreased tumor cell proliferation and increased apoptosis leading to decreased tumor volume in mouse xenograft models of prostate cancer.

Clinical clearance of Apalutamide (FDA Prescription Therapeutic Agent) relies on hepatic oxidation via cyp3a4/cyp2c9/cyp2c19 followed by renal and biliary excretion of apalutamide metabolites with a Approximately 6–15 hours terminal plasma half-life for Apalutamide half-life; patients absorbing at Estimated 74%–86% oral systemic absorption for Apalutamide bioavailability typically observe target onset around peak plasma concentration (tmax) reached 1–4 hours post-dose for apalutamide.

FDA clinical labeling for Apalutamide restricts administration in known hypersensitivity to apalutamide or structurally related fda prescription therapeutic agent compounds; concomitant contra-labeled cyp/transporter therapies during active apalutamide administration across 60 mg/1 Tablet, Film Coated, 240 mg/1 Tablet, Film Coated, with self-reported patient tracking dominated by fatigue (7.9% of reports), nausea (7.7% of reports), diarrhea (7.5% of reports).