Trilostane - CAS 13647-35-3
Catalog number: B0084-057927
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
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Trilostane is an inhibitor of 3β-hydroxysteroid dehydrogenase used in the treatment of Cushing’s syndrome.
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B0084-057927 1 g $199 In stock
B0084-057927 5 g $299 In stock
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1. Trilostane in the Treatment of Advanced Breast Cancer
C. G. Beardwell, A. C. Hindley, P. M. Wilkinson. Cancer Chemother Pharmacol (1983) 10:158-160
Side-effects were frequent in this series, although many patients could tolerate the drug without particular difficulty. However, it is possible that the dose selected initially (960 rag/day) was too high and was responsible for the necessity to discontinue treatment, as side-effects in subsequent patients treated with 480 mg/day were negligible. The elevations in serum androstenedione and falls in serum oestrone observed were similar whether doses of 480 mg or 960 mg trilostane daily were given. Further studies are in progress to confirm the above results,to elucidate more fully the mode of action of trilostane, and to define the sub-groups of patients most likely to benefit from its uses.
2. Trilostane with hydrocortisone in treatment of metastatic breast cancer
Ping S. Chu, Aman U. Buzdar and Gabriel N. Hortobagyi. Breast Cancer Research and Treatment 13:117-121 (1989)
Trilostane (4α,5α-epoxy-3,17β-dihydroxy-androst-2-ene-2-carbonitrile) has been shown to inhibit 3β- hydroxysteroid dehydrogenase: △5,4-isomerase enzyme system specifically and competitively. This leads to decreased conversion of pregnenolone to progesterone, as well as dehydroepiandrosterone to androstenedione, precursor of the estrogens in postmenopausal women. Trilostane alone causes an increase in the △5 adrenal steroids (pregnenolone, 17-hydroxypregnenolone, and dehydroepiandrosterone), elevation in androstenedione and testosterone, and unexpectedly, elevation in plasma and urine estrogens. The production of hydrocortisone is also diminished, necessitating that patients receiving trilostane should receive replacement therapy. Administration of hydrocortisone also prevents the compensatory feedback mechanism interfering with the treatment. A study by Beardwell suggested that trilostane may inhibit the aromatase system and reduce circulating estrone levels in postmenopausal women, but data on this aspect are scanty. Treatment with trilostane in combination with hydrocortisone has been evaluated in a few studies of metastatic breast cancer. These studies demonstrated significant antitumor activity (25-32% overall response rate) in postmenopausal women.
3. Biological effects of trilostane in vitro on oocyte maturation and fertilization in the hamster
S. Suzuki, Y. Endo, R. Miura and R. Iizuka. Experientia 40 (1984)
Cumulus-oocyte complexes and denuded oocytes of the experimental groups were incubated in microdrops containing 10-6 M trilostane at which concentration inhibition of △5-3β-HSD activity seemed to occur in the denuded oocytes. Trilostane was dissolved in sterilized water adjusted to pH 8.5 by adding 0.1 N NaOH solution, because of its poor solubility in water. The stock solution of 10-3M trilostane was neutralized to pH 7.4 by 0.1 N HC1 and diluted with the GH-2 medium. Following incubation, the oocytes were mounted on a glass slide in 1-2 lal of medium, compressed gently with a coverslip smeared with vaseline at the corners, and examined under a Nomarski differential interference contrast microscope. The oocytes were fixed with 2.5% glutaraldehyde in phosphate buffered saline for 1 min and then transferred to 10% neutral formalin overnight. After fixation, the slides were washed, dehydrated and stained with 0.25% lacmoid solution for chromosome observation. The oocytes were classified according to the following stages: degenerated; immature stage with an intact germinal vesicle (GV); germinal vesicle breakdown without polar bodies (GVBD) and polar body extrusions (PB). The oocytes were assessed as degenerated when nonspherical, brown in color, fragmented or vacuolated.
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CAS 13647-35-3 Trilostane

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