Switch from antagonist to agonist of the androgen receptor blocker bicalutamide is associated with prostate tumour progression in a new model system
1999

Bicalutamide's Role in Prostate Tumor Progression

publication Evidence: moderate

Author Information

Author(s): Culig Z, Hoffmann J, Erdel M, Eder I E, Hobisch A, Hittmair A, Bartsch G, Utermann G, Schneider M R, Parczyk K, Klocker H

Primary Institution: University of Innsbruck

Hypothesis

Switching from antagonist to agonist of the androgen receptor blocker bicalutamide is associated with prostate tumour progression.

Conclusion

Bicalutamide can acquire agonistic properties during long-term androgen ablation, potentially affecting prostate cancer progression.

Supporting Evidence

  • LNCaP-abl cells showed a hypersensitive proliferative response to androgen until passage 75.
  • Bicalutamide stimulated proliferation of LNCaP-abl cells.
  • AR protein expression in LNCaP-abl cells increased approximately fourfold.
  • Bicalutamide exhibited agonistic effects on AR transactivation activity in LNCaP-abl cells.

Takeaway

When treating prostate cancer, a drug called bicalutamide can start helping tumors grow instead of stopping them after a long time without androgens.

Methodology

A new tumor model was established using androgen-sensitive LNCaP cells kept in androgen-depleted medium, and various androgen levels were tested for their effects on cell proliferation.

Digital Object Identifier (DOI)

10.1038/sj.bjc.6690684

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