Preclinical profile and phase I clinical trial of a novel androgen receptor antagonist GT0918 in castration-resistant prostate cancer.

•GT0918 has high binding affinity to androgen receptor.•GT0918 reduces the androgen receptor protein level effectively.•GT0918 inhibits transcriptional activity of androgen receptor with mutations.•GT0918 is well tolerated with a favourable pharmacokinetics profile.•GT0918 has promising antitumour activity in castration-resistant prostate cancer.