What is Apalutamide used for?
Apalutamide is used to treat patients with metastatic castration-sensitive prostate cancer (prostate cancer that responds to medical or surgical treatments that lower testosterone and has spread to other parts of the body), and non-metastatic castration-resistant prostate cancer (prostate cancer that is resistant to …
What generation is Apalutamide?
Apalutamide is a third-generation AR-targeted therapy which competitively blocks the AR and prevents AR dimerization, nuclear internalization, thereby avoiding cancer progression. Early studies have demonstrated that apalutamide was safe and demonstrated clinical benefit.
Is apalutamide better than enzalutamide?
Apalutamide also outperformed enzalutamide in terms of PSA90 response at the 9-month mark (70.4% vs 62.5%; HR, 1.49; 95% CI, 1.05-2.11; P = . 024).
What is the difference between bicalutamide and apalutamide?
Apalutamide binds AR in the same ligand-binding domain as bicalutamide but with greater affinity, and unlike bicalutamide, retains full antagonist activity in the setting of AR overexpression (48). Furthermore, apalutamide was shown to be selective for AR over other nuclear hormone receptors (48).
What is the difference between bicalutamide and enzalutamide?
Purpose: Enzalutamide, a potent oral androgen receptor inhibitor, improves survival in men with metastatic castration-resistant prostate cancer (CRPC) before and after chemotherapy. Bicalutamide, a nonsteroidal antiandrogen, is widely used to treat men with nonmetastatic or metastatic CRPC.
How long does xtandi extend life?
How long does Xtandi extend life? In the AFFIRM trial, treatment with Xtandi extended life by almost 5 months. Treatment with Xtandi resulted in a median overall survival time of 18.4 months (95% CI 17.3 to not yet reached) compared with 13.6 months (95% CI 11.3 to 15.8) in the placebo recipients (p<0.001).
Is xtandi a type of chemotherapy?
XTANDI is an androgen receptor inhibitor; it is not a chemotherapy. Androgens are a group of hormones that includes testosterone. Androgen receptor inhibitors interfere with the connection between androgens and androgen receptors. This can help slow cancer cell growth.
Is Apalutamide similar to enzalutamide?
Both apalutamide and enzalutamide are next-generation androgen receptor inhibitors. Enzalutamide was approved by the FDA on December 16, 2019, and apalutamide was approved in this indication on September 17, 2019.
What is the difference between bicalutamide and Apalutamide?
Is Apalutamide an anti androgen?
Apalutamide (ARN-509) is an antiandrogen that binds selectively to androgen receptors (AR) and does not show antagonist-to-agonist switch like bicalutamide.
What is ARN-509?
ARN-509: a novel antiandrogen for prostate cancer treatment Continued reliance on the androgen receptor (AR) is now understood as a core mechanism in castration-resistant prostate cancer (CRPC), the most advanced form of this disease.
What is the difference between ARN-509 and bicalutamide?
ARN-509 was optimized for inhibition of AR transcriptional activity and prostate cancer cell proliferation, pharmacokinetics, and in vivo efficacy. In contrast to bicalutamide, ARN-509 lacked significant agonist activity in preclinical models of CRPC.
Is the androgen receptor still a core mechanism in castration-resistant prostate cancer?
Continued reliance on the androgen receptor (AR) is now understood as a core mechanism in castration-resistant prostate cancer (CRPC), the most advanced form of this disease. While established and novel AR pathway-targeting agents display clinical efficacy in metastatic CRPC, dose-limiting side effe …