Intraprostatic injection therapy is a minimally invasive treatment of patients with lower urinary tract symptoms suggestive of benign prostatic hyperplasia and could be a therapeutic alternative in increasingly older and co-morbid patients. Nowadays only botulinum neurotoxin A (BoNT/A), absolute ethanol, NX-1207 and PRX302 are of relevance but none of these substances has yet been authorized for treatment use (off-label use). There have been only three randomized, placebo-controlled trials (RCTs) for BoNT/A, whereas none exist for ethanol and the results of existing studies are inconsistent and without convincing proof of efficacy. NX-1207 is a protein with selective pro-apoptotic properties and non-inferiority compared to finasteride has been demonstrated. PRX302 is a modified proaerolysin that can be activated by prostate-specific antigen and is therefore (prostate) cell-specific. Safety and efficacy are well documented; however, intraprostatic injection therapy should presently only be performed in clinical trials, irrespective of the substance used.