Here's the Cancer Research abstract:
Title
Chemoprevention of mammary carcinoma by LGD1069 (Targretin): an RXR-selective ligand.
Author
Gottardis MM; Bischoff ED; Shirley MA; Wagoner MA; Lamph WW; Heyman RA
Address
Department of Endocrine Research, Ligand Pharmaceuticals, Inc., San Diego, California
92121, USA.
Source
Cancer Res, 56:5566-70, 1996 Dec 15
Abstract
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. |
