In this special issue, an international expert panel of clinicians and basic scientists and our guest editor Prof. Jer-Tsong Hsieh and Ganesh Raj aim to outline current challenges of prostate cancer treatment and discuss every aspect of hormonal metabolism, receptor alteration and mechanism in prostate cancer to pave a way for developing better therapeutic strategy and prognostic tools. Also, a wide range of topics such as cancer metastasis, animal model, molecular imaging and targeted therapy of prostate cancer were included as well.