Topical toremifene: a new approach for cutaneous melanoma?

Juhani Maenpaa, Thomas Dooley, Gregory Wurz, John VandeBerg, Edward Robinson, Vernon Emshoff, Pirkko Sipila, Valerie Wiebe, Calvin Day, Michael DeGregorio

Research output: Contribution to journalArticle

14 Scopus citations

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 μM). 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.

Original languageEnglish (US)
Pages (from-to)392-395
Number of pages4
JournalCancer Chemotherapy and Pharmacology
Volume32
Issue number5
DOIs
StatePublished - Sep 1993
Externally publishedYes

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ASJC Scopus subject areas

  • Pharmacology
  • Oncology
  • Cancer Research

Cite this

Maenpaa, J., Dooley, T., Wurz, G., VandeBerg, J., Robinson, E., Emshoff, V., Sipila, P., Wiebe, V., Day, C., & DeGregorio, M. (1993). Topical toremifene: a new approach for cutaneous melanoma? Cancer Chemotherapy and Pharmacology, 32(5), 392-395. https://doi.org/10.1007/BF00735925