Circulating testosterone diffuses into prostatic cells, where it is irreversibly converted into the more potent androgen DHT via the NADPH-dependent reduction catalyzed by the steroid 5α-reductase type II and, to a lesser extent, by steroid 5α-reductase type I. DHT binds to the androgen receptors located on the nuclear membrane. Two DHT–receptor complexes are formed in the nucleus that bind to specific regions of the DNA – the androgen response elements – with high affinity, enhancing the production of regulatory proteins involved in cell proliferation and prostate-specific antigen. Finasteride, a steroid 5α-reductase type II inhibitor, causes an intra-prostatic DHT decrease, ultimately leading to apoptosis. DHT: 5α-dihydrotestosterone; NADP: Nicotinamide adenine dinucleotide; NADPH: Nicotinamide adenine dinucleotide phosphate. Data taken from [125].