BPH is thought to occur when accumulated testosterone in the prostate is converted to dihydrotestosterone, stimulating cells to multiply excessively and causing the prostate to enlarge. Clinical studies have shown that when a steroidal enzyme called 5-a-reductase is inhibited, the hormone testosterone will not be converted within the prostate to dihydrotestosterone, and the prostate generally atrophies (shrinks glandular hyperplasia), subsequently deobstructing the urethra for easier urinary flow, and thereafter preventing the development of incontinence because of exhaustive bladder failure.

Saw Palmetto is also a research candidate as a potential deterrent to prostate cancer. Also, Taxus Brevifolia (the Pacific Yew Tree), yet another ingredient in Prostatin+, contains "taxol" which has demonstrated high cytotoxic effect on prostatic cancer cells, or in other words, has been found to be phytomedicinally active against prostate cancer.