D-3263

D-3263 is a synthetic small molecule that acts as a potent agonist of the transient receptor potential melastatin member 8 (TRPM8) channel, also known as TRP-P8. It was developed primarily for its antineoplastic (anticancer) activity, particularly targeting prostate cancer and benign prostatic hyperplasia (BPH). By activating TRPM8 channels—calcium-permeable ion channels overexpressed in prostate cancer and BPH—D‑3263 increases calcium and sodium influx into cells, disrupting cellular homeostasis and inducing apoptosis in tumor cells expressing TRPM8. This mechanism may also reduce dihydrotestosterone (DHT) levels, contributing to its effects on prostate tissue. In addition to its anticancer properties, preclinical studies have shown antibacterial activity against Staphylococcus aureus by increasing bacterial membrane permeability. The drug was initially developed by Dendreon Corporation and reached phase 1 clinical trials for advanced solid tumors but development has since been discontinued[1][5][6][7].

Other names

Enteric-Coated TRPM8 Agonist D-3263 Hydrochloride3-(2-Aminoethyl)-1(R)-((2(S)-isopropyl-5(R)-methyl cyclohexanecarbonyl))-5-methoxy-1,3-dihydro-benzoimidazol-2-one hydrochloride