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Clinical and endocrine effects of the oral aromatase inhibitor vorozole in postmenopausal patients with advanced breast cancer.

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Vorozole is an orally active, nonsteroidal aromatase inhibitor. Twenty-four postmenopausal patients with advanced breast cancer who had relapsed after treatment with tamoxifen received three separate daily doses of vorozole (1, 2.5, and 5 mg) each for 1 month in a randomized, double-blind, phase II

Endocrine, pharmacokinetic and clinical studies of the aromatase inhibitor 3-ethyl-3-(4-pyridyl)piperidine-2,6-dione ('pyridoglutethimide') in postmenopausal breast cancer patients.

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The aromatase inhibitor, 'pyridoglutethimide' (PyG), has been shown previously to suppress serum oestrogen levels in postmenopausal breast cancer patients and to achieve clinical responses at a dose of 500 mg twice daily (b.d.). This report gives the results of a detailed pharmacokinetic and

Breast cancer and specific types of combined oral contraceptives. The WHO Collaborative Study of Neoplasia and Steroid Contraceptives.

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Data on 2,754 cases and 18,565 controls from a multinational hospital-based, case-control study were analysed to determine whether observed associations between combined oral contraceptives and breast cancer are similar for oral contraceptives with varying types and doses of oestrogens and

Phase I study of the oral nonsteroidal aromatase inhibitor CGS 20267 in postmenopausal patients with advanced breast cancer.

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A phase I study was performed of CGS 20267, an oral nonsteroidal, highly potent, and selective aromatase inhibitor, in 21 postmenopausal patients with advanced breast cancer. The patients were recruited in 3 successive groups of 7, receiving 0.1, 0.5, and 2.5 mg p.o./day, respectively. All patients

Steroidal regulation of oestradiol-17 beta dehydrogenase activity of the human breast cancer cell line MCF-7.

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We have examined the direct effects of progestins, oestrogens, peptide hormones and growth factors on oestradiol-17 beta dehydrogenase (OE2DH) activity of cultures of the human breast cancer cell line MCF-7. Cells were cultured in the presence of steroid or peptide for 6 days, after which the number

Vorozole (R83842) in the treatment of postmenopausal advanced breast cancer: relationship of serum levels of vorozole and clinical results (a study of the EORTC Breast Cancer Cooperative Group).

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The new non-steroidal aromatase inhibitor vorozole (R83842) was administered orally at a single daily dose of 2.5 mg to 27 postmenopausal women with advanced breast cancer in a phase II trial as second-line endocrine treatment. The observed objective response rate of 30% and good tolerability of the

Letrozole. A review of its use in postmenopausal women with advanced breast cancer.

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Letrozole is an oral reversible nonsteroidal aromatase inhibitor. Clinical tracer studies show that it inhibits peripheral aromatase by over 98% and suppresses blood and urinary estrogen levels by over 95% after 2 weeks of treatment in postmenopausal women. Letrozole also significantly inhibits

Steroid hormone profiles in women treated with aminoglutethimide for metastatic carcinoma of the breast.

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Recent evidence suggests that aminoglutethimide (AG), a known inhibitor of adrenal steroidogenesis, is a potent blocker of aromatase and thus of estrogen production. These properties of AG have been exploited clinically to reduce the biosynthesis of adrenal estrogen precursors and extraglandular

Comparison of levels of cytosol estrogen receptors with "arterial" and "venous" concentrations of gonadic steroids in mammary tumors.

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Plasma steroid concentrations measured in the post-menopausal women with breast cancer showed a close correlation between the various androgens. The post-menopausal women exhibited a correlation between estrogen receptors (ER) and "arterial" 17 alpha-hydroxyprogesterone levels in the breast. ER

Role of human adipose tissue in the production and metabolism of steroid hormones.

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Radioimmunological methods have been employed for the simultaneous determination of dehydroepiandrosterone, androstenedione, testosterone, oestrogens (oestradiol + oestrone), progesterone, 17 alpha-hydroxyprogesterone and cortisol in human adipose tissue and peripheral blood to compare the hormone

Inhibition of aromatase with CGS 16949A in postmenopausal women.

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Potent, specific, and nontoxic inhibitors of aromatase would be useful for experimental studies and for use in the treatment of breast cancer and other disorders. We evaluated the effects of CGS 16949A, a nonsteroidal inhibitor of aromatase activity, in 12 postmenopausal women with breast cancer by

Specificity of low dose fadrozole hydrochloride (CGS 16949A) as an aromatase inhibitor.

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CGS 16949A (fadrozole hydrochloride), a potent cytochrome P450-mediated steroidogenesis inhibitor, blocks aromatase at low doses, but other biosynthetic steps at higher concentrations. Recent studies demonstrated inhibition of C11-hydroxylase, corticosterone methyloxidase-II, and deoxycorticosterone

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