An inhibitor of steroid 5α-reductase
Dutasteride?(Avodart) is an inhibitor of dual 5-alpha-reductase for treating benign prostatic hyperplasia (BPH).
Dutasteride has been reported to inhibit conversion of?3H-testosterone to?3H-DHT by more than 99% in LNCaP cells. Dutasteride strongly reduces growth, proliferation, and viability of LNCaP cells as well. Dutasteride increased the enzymatic activities of caspase 7 and caspase 8 dose-dependently at 48 hours, providing functional significance and confirming that the?apoptotic and survival pathways are being activated by dutasteride treatment in LNCaP cells [1].
In vivo, dutasteride, which inhibits both 5αR1/5αR2, is efficacious in blocking prostate cancer development or progression in C57BL/6 TRAMP x FVB mice [2].
参考文献:
[1] Schmidt LJ1,?Murillo H,?Tindall DJ. Gene expression in prostate cancer cells treated with the dual 5 alpha-reductase inhibitor dutasteride. J Androl.?2004 Nov-Dec;25(6):944-53.
[2] Opoku-Acheampong AB1,?Unis D,?Henningson JN,?Beck AP,?Lindshield BL.Preventive and therapeutic efficacy of finasteride and dutasteride in TRAMP mice. PLoS One.?2013 Oct 18;8(10):e77738. doi: 10.1371/journal.pone.0077738. eCollection 2013.
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