ATC Group: L02BB Anti-androgens

Apalutamide is an orally administered, selective Androgen Receptor (AR) inhibitor that binds directly to the ligand-binding domain of the AR. Apalutamide treatment decreases tumor cell proliferation and increases apoptosis leading to potent antitumor activity.

Bicalutamide is a non-steroidal antiandrogen, devoid of other endocrine activity. It binds to androgen receptors without activating gene expression, and thus inhibits the androgen stimulus. Regression of prostatic tumours results from this inhibition.

Darolutamide is an androgen receptor (AR) inhibitor with a flexible polar-substituted pyrazole structure that binds with high affinity directly to the receptor ligand binding domain. Darolutamide competitively inhibits androgen binding, AR nuclear translocation, and AR mediated transcription. A major metabolite, keto-darolutamide, exhibited similar in vitro activity to darolutamide. Darolutamide treatment decreases prostate tumour cell proliferation leading to potent antitumour activity.

Enzalutamide is a potent androgen receptor signalling inhibitor that blocks several steps in the androgen receptor signalling pathway. Enzalutamide treatment decreases the growth of prostate cancer cells and can induce cancer cell death and tumour regression.

Flutamide is a non-steroidal, highly specific, orally active anti-androgenic agent. The pharmacologically active metabolite, hydroxyflutamide, is believed to exert an anti-androgenic effect directly on the target tissues, either by inhibiting androgen uptake or by blocking cytoplasmic and nuclear binding of androgen. Flutamide is indicated for the treatment of advanced prostatic carcinoma in which suppression of testosterone effects is indicated.