Effect and efficacy of Androxal

Androxal is a second-generation anti-androgen drug that blocks the activity of androgens and androgen receptors (AR) in prostate cancer. Due to the normal physiology of prostate cells, AR activity is closely related to prostate cancer progression, providing the rationale for androgen deprivation therapy (ADT). However, due to the accumulation of mutations, including changes in constitutive activity mutations, AR overexpression, and AR splicing variants, resistance eventually emerges after the onset of ADT 2-3 years later. Therefore, Androxal was designed to take advantage of these mutations. In vitro experiments with human prostate cancer cell line VCaP have shown that Androxal inhibits cell growth and induces apoptosis, while other anti-androgen drugs such as bicalutamide do not.

Clinical trials in prostate cancer patients have shown that Androxal can lead to a reduction in serum PSA for at least 12 weeks, although this response may be short-lived and thus lead to Androxal resistance. Patients treated with Androxal also had a 37 percent lower risk of death compared with placebo.

Effect and efficacy of Androxal

Androxal should be avoided with which drugs?

Clinical research

Effects of CYP2C8 inhibitors on XTANDI: Co-administration of XTANDI 160mg with gemferozil (a strong CYP2C8 inhibitor) increased the AUC of Androxal plus n-demethylAndroxal by a factor of 2.2, with minimal effect on C. max.

Effects of CYP3A4 and CYP2C8 inducers on XTANDI: Co-administration of XTANDI 8mg after multiple oral rifampicin (strong CYP160A3 and moderate CYP4C2 inducers) reduced the AUC of Androxal plus n-demethylAndroxal by 37%, with no effect on C. max.