title: Rapid disease progression after the administration of bicalutamide in patients with metastatic prostate cancer.
abstract: We report 5 patients with advanced metastatic prostate cancer who took bicalutamide 50 mg/day for "second-line" hormonal manipulation and demonstrated a rapid rise in prostate-specific antigen (PSA) shortly after the initiation of bicalutamide. After discontinuation of the drug, PSA levels declined in 4 patients and stabilized in the fifth. In 2 of the patients, the PSA rise was associated with an increase in pain level, which subsided after the treatment was stopped. The timing of the rapid changes in PSA and pain levels suggests a direct effect of bicalutamide. The most probable explanation for this observation is a very early agonist activation of androgen receptor by bicalutamide, similar to the underlying mechanism of the "antiandrogen withdrawal syndrome."
authors.affiliation: Johns Hopkins Oncology Center, Johns Hopkins University, Baltimore, Maryland, USA.
authors.forename: M
authors.initials: M
authors.lastname: Laufer
authors.forename: V J
authors.initials: VJ
authors.lastname: Sinibaldi
authors.forename: M A
authors.initials: MA
authors.lastname: Carducci
authors.forename: M A
authors.initials: MA
authors.lastname: Eisenberger
mesh_terms: D000368:Aged; D000726:Androgen Antagonists / Q000627:therapeutic use*; D000813:Anilides / Q000627:therapeutic use*; D018931:Antineoplastic Agents, Hormonal / Q000627:therapeutic use*; D001859:Bone Neoplasms / Q000188:drug therapy* / Q000556:secondary*; D018450:Disease Progression; D006801:Humans; D008297:Male; D008875:Middle Aged; D009570:Nitriles; D017430:Prostate-Specific Antigen / Q000097:blood; D011471:Prostatic Neoplasms / Q000097:blood / Q000188:drug therapy* / Q000473:pathology*; D014105:Tosyl Compounds
chemical_list: D000726:Androgen Antagonists; D000813:Anilides; D018931:Antineoplastic Agents, Hormonal; D009570:Nitriles; D014105:Tosyl Compounds; C053541:bicalutamide; D017430:Prostate-Specific Antigen