When the currently available pharmacotherapeutic principles used for treatment of male lower urinary tract symptoms (LUTS) fail, transurethral resection of the prostate still remains the widely applied gold-standard therapy, since the majority of minimally invasive therapies have not achieved the same efficacy and/or lack an evidence base to support their routine use. Intraprostatic injection therapy, which probably is the oldest minimally invasive surgical treatment, has not been widely used, but recent reports of successful treatments with several new agents have renewed interest in this approach. Anhydrous ethanol still seems to be one of the most extensively studied injectables to date, but intraprostatic injection of botulinum toxin has received much recent attention, with regard to both its mechanism of action and efficacy. In addition, other agents such as NX-1207 and PRX302 have been reported to have promising effects. Injection therapy, using the transperineal, transrectal and transurethral routes for delivery of the active compounds, seems to be an effective minimally invasive surgical therapy for LUTS associated with benign prostatic hyperplasia (BPH). However, further studies on mechanisms of action of the novel agents used, and controlled clinical trials documenting their efficacy and side-effects (which are largely lacking), are needed before their place in the treatment of BPH/LUTS can be properly assessed.