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Topical toremifene: a new approach for cutaneous melanoma?

Authors :
Maenpaa, Juhani
Dooley, Thomas
Wurz, Gregory
VandeBerg, John
Robinson, Edward
Emshoff, Vernon
Sipila, Pirkko
Wiebe, Valerie
Day, Calvin
DeGregorio, Michael
Maenpaa, J
Dooley, T
Wurz, G
VandeBerg, J
Robinson, E
Emshoff, V
Sipila, P
Wiebe, V
Day, C
DeGregorio, M
Source :
Cancer Chemotherapy & Pharmacology; Sep1993, Vol. 32 Issue 5, p392-395, 4p
Publication Year :
1993

Abstract

The distribution of topically applied toremifene (0.5-1 mg/day for 5 days) in the ultraviolet B (UVB)-induced Monodelphis domestica opossum melanoma model was examined. The mean concentration of toremifene measured in the skin was 1200 nmol/g, or > 500 times that detected in any other tissues (blood, brain, liver, testicles, heart, uterus, eyes). In plasma, toremifene could be detected in only one animal of six (0.04 nmol/ml). Intraperitoneal administration of 0.5 mg toremifene daily for 5 days in three female animals resulted in a mean uterus concentration of 22.9 nmol/g, or 400-fold that achieved by topical administration of 0.5 mg/day in three other female Monodelphis (0.05 nmol/g). The cytostatic effect of toremifene was studied in three human melanoma cell lines and three experimental cell lines derived from UVB-induced melanocytic nevi in M. domestica. Toremifene had a cytostatic effect on all cell lines (50% growth-inhibitory concentrations, 5.8-9.6 microM). Topical toremifene administration yields high local concentration with minimal systemic distribution. In addition, toremifene has a cytostatic effect at achievable concentrations in a variety of melanomatous cell lines. [ABSTRACT FROM AUTHOR]

Details

Language :
English
ISSN :
03445704
Volume :
32
Issue :
5
Database :
Complementary Index
Journal :
Cancer Chemotherapy & Pharmacology
Publication Type :
Academic Journal
Accession number :
71003541
Full Text :
https://doi.org/10.1007/BF00735925