Robert, Your memory serves you right. Here is the abstract (I believe Henry provided an indirect link to same a few posts back):
Cancer Res 1996 Dec 15;56(24):5566-5570
Chemoprevention of mammary carcinoma by LGD1069
(Targretin): an RXR-selective ligand.
Gottardis MM, Bischoff ED, Shirley MA, Wagoner MA, Lamph WW, Heyman RA
Department of Endocrine Research, Ligand Pharmaceuticals, Inc., San Diego, California 92121, USA.
Recently, 9-cis retinoic acid, a high affinity ligand for retinoic acid receptors and retinoid X-receptors (RXRs), was
shown to have efficacy superior to all-trans retinoic acid as a chemopreventive agent in the
N-nitroso-N-methylurea-induced rat mammary carcinoma model. To further explore the specific contribution RXR
activation may play in suppression of carcinogenesis, the efficacy of LGD1069 (Targretin), an RXR-selective
ligand, in the N-nitroso-N-methylurea-induced rat mammary tumor model was studied. LGD1069-treated animals
showed a 90% reduction in tumor burden and tumor incidence compared with vehicle-treated rats with an efficacy
similar to that achieved with tamoxifen. LGD1069 was very well tolerated during 13 weeks of chronic therapy with
no classic signs of "retinoid-associated" toxicities. These data demonstrate that LGD1069, an RXR-selective
ligand, can act as a highly effective and benign chemopreventive agent for mammary carcinoma. |
