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 language | English (US) |
|---|---|
| Pages (from-to) | 392-395 |
| Number of pages | 4 |
| Journal | Cancer Chemotherapy and Pharmacology |
| Volume | 32 |
| Issue number | 5 |
| DOIs | |
| State | Published - Sep 1993 |
| Externally published | Yes |
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ASJC Scopus subject areas
- Pharmacology
- Oncology
- Cancer Research
Cite this
Topical toremifene : a new approach for cutaneous melanoma? / Maenpaa, Juhani; Dooley, Thomas; Wurz, Gregory; VandeBerg, John; Robinson, Edward; Emshoff, Vernon; Sipila, Pirkko; Wiebe, Valerie; Day, Calvin; DeGregorio, Michael.
In: Cancer Chemotherapy and Pharmacology, Vol. 32, No. 5, 09.1993, p. 392-395.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Topical toremifene
T2 - a new approach for cutaneous melanoma?
AU - Maenpaa, Juhani
AU - Dooley, Thomas
AU - Wurz, Gregory
AU - VandeBerg, John
AU - Robinson, Edward
AU - Emshoff, Vernon
AU - Sipila, Pirkko
AU - Wiebe, Valerie
AU - Day, Calvin
AU - DeGregorio, Michael
PY - 1993/9
Y1 - 1993/9
N2 - 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.
AB - 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.
UR - http://www.scopus.com/inward/record.url?scp=0027321521&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=0027321521&partnerID=8YFLogxK
U2 - 10.1007/BF00735925
DO - 10.1007/BF00735925
M3 - Article
C2 - 8339391
AN - SCOPUS:0027321521
VL - 32
SP - 392
EP - 395
JO - Cancer Chemotherapy and Pharmacology
JF - Cancer Chemotherapy and Pharmacology
SN - 0344-5704
IS - 5
ER -