Annual Review of Pharmacology and Toxicology Vol. 51 (Volume publication date February 2011)
Department of Medicine, Division of Endocrinology, Stanford University School of Medicine, Stanford, CA 94305
Department of Medicine, Division of Endocrinology, Stanford University School of Medicine, Stanford, CA 94305-5103
Calcitriol, the hormonally active form of vitamin D is currently being evaluated in clinical trials as an anti-cancer agent. Calcitriol exerts multiple anti-proliferative, pro-apoptotic and pro-differentiating actions on various malignant cells and retards tumor growth in animal models of cancer. Calcitriol also exhibits several anti-inflammatory effects including suppression of prostaglandin (PG) action, inhibition of p38 stress kinase signaling and the subsequent production of pro-inflammatory cytokines and inhibition of NF?B signaling. Calcitriol also decreases the expression of aromatase, the enzyme catalyzing estrogen synthesis in breast cancer directly and indirectly by reducing PGs, which are major stimulators of aromatase. Other important effects include the suppression of tumor angiogenesis, invasion and metastasis. These calcitriol actions provide a basis for its potential use in cancer therapy and chemoprevention. We summarize the current status of trials of calcitriol and its analogs used alone or in combination with known anti-cancer agents.
Expected final online publication date for the Annual Review of Pharmacology and Toxicology Volume 51 is January 6, 2011. Please see http://www.annualreviews.org/catalog/pubdates .aspx for revised estimates.