Cyproterone acetate (CPA) is an antiandrogen that may be used in combination with estradiol in gender reaffirmation therapy...However, its effect appears to be delayed, indicating that cessation alone is suboptimal in cases causing significant mass effect and symptomatology. In such cases, early surgical intervention should be considered.
Our cases highlight the real-world risk of this likely underreported adverse effect and underscore the importance of clinician vigilance for neurological sequelae. We suggest using the lowest dose of CPA that maintains adequate androgen suppression, with consideration of alternative anti-androgens where appropriate.
Finally, we show by exome analysis of breast tumors and meninges that hormone impregnation promotes breast tumor formation without additional somatic oncogenic mutation but is associated with an increased mutational burden on Pik3ca-mutant background. Taken together, these results tend to suggest a prominent role of Pik3ca mutations over hormone impregnation in meningioma tumorigenesis, the exact effect of the latter is still to be discovered.
The effects on cells were compared with that of the antiandrogen cyproterone acetate (CPA)...Likewise, studies on the interaction of new compounds with drug-metabolizing cytochrome P450 3A4 (CYP3A4) showed that 11 was a fourfold stronger inhibitor than 15 (IC of 3 μM and 12 μM, respectively). This suggests that changes in the chemical structure of sterol moieties and the manner of their linkage could largely affect both the antiproliferative activity of androgen dimers and their crossreactivity with CYP3A4.
over 2 years ago
Preclinical • Journal
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CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4)