Tamoxifen as an anti-tumour agent: oestrogen binding as a predictive test for tumour response.
Rats with growing 7,12-dimethylbenz(alpha)anthracene (DMBA)-induced rat mammary carcinomata were biopsied and oestrogen-binding capacity was measured using a Sephadex LH-20 chromatography method. Tumours were measured with calipers and animals were treated for 3 weeks with tamoxifen (50 mug/day, S.C.). Tumour response was determined by the size (cm2) before and after therapy. An increase in tumour regression (ten tumours) was seen with increasing oestrogen-binding sites determined by Scatchard analysis (P less than 0.01). Thirty tumours were used to determine oestrogen binding with a single dose of [3H]-oestradiol. The percentage tumour regression was linearly correlated with oestrogen-binding capacity (P less than 0.01), although some tumours with high oestrogen-binding capacities only partially regressed in response to tamoxifen therapy. The time of the oestrous cycle when biopsy occurred was not a critical factor in determining oestrogen binding for prediction of response. Oestrogen binding was reduced during tamoxifen therapy.
D000818:Animals; D001665:Binding Sites / Q000187:drug effects; D001706:Biopsy; D004958:Estradiol / Q000378:metabolism*; D005260:Female; D008325:Mammary Neoplasms, Experimental / Q000188:drug therapy* / Q000378:metabolism; D051381:Rats; D013267:Stilbenes / Q000627:therapeutic use*; D013629:Tamoxifen / Q000494:pharmacology / Q000627:therapeutic use*
D013267:Stilbenes; D013629:Tamoxifen; D004958:Estradiol