TRPM8

TRPM8 (also known as TRPP8) is a calcium ion channel that is triggered by cold temperatures, menthol, and other small molecule agonists. TRPM8 belongs to the melastatin subfamily of TRP proteins. Calcium ions mediate key cellular functions, and activation of TRPM8 channels leads to programmed cell death (apoptosis) in TRPM8-expressing cells.

In normal human tissues, TRPM8 is expressed predominantly in the prostate, a gland in the male reproductive system. It is over-expressed in prostate hyperplasia and multiple types of cancer, including prostate cancer, breast cancer, colon cancer and lung cancer. Dendreon has synthesized small molecule agonists, including D-3263, HCI, which activate the TRPM8 ion channel and induce cell death (apoptosis). The lead investigational molecule, D-3263, HCI, is in a Phase 1 trial for clinical evaluation in patients with solid tumors.