Patients at high risk for the development of multiple non-melanoma skin cancers, especially those receiving immunosuppressive medications following solid organ transplantation, are candidates for chemoprophylaxis. In patients where photo-protection and topical medications are insufficient to prevent the growth of new cancers, there is considerable evidence that oral retinoids, including vitamin A, and synthetics such as isotretinoin, etretinate and acitretin are efficacious in this regard. This manuscript is a review of the literature regarding the use of these agents for chemoprophylaxis of non-melanoma skin cancer. Also included is anecdotal evidence that bexarotene, a rexinoid, may be as effective as acitretin in terms of chemoprevention, with a comparable side effects at doses recommended for chemoprophylaxis.