Transplatin is the less-active isomer of the DNA damanging, platinum antitumor drug cisplatin, which is used in the treatment of a variety of solid tumors. However, it has been reported that the antitumor activity of transplatin can be photo-activated. Several trans-platinum compounds have excellent anticancer bioactivity that overcomes cisplatin resistance, making transplatin an excellent starting place for the development of novel anticancer agents.