Treatment of breast cancer with different antiprogestins: Preclinical and clinical studies

Bakker, G.H.; Setyono-Han, Buddy; Portengen, H.; Jong, Frank H. de; Foekens, John A.; Klijn, Jan G.M.

doi:10.1016/0960-0760(90)90421-g

Cited by 81 publications

(20 citation statements)

References 14 publications

(13 reference statements)

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“…When the two antagonists are combined, the inhibition is additive leading to tumor remission similar to that induced by ovariectomy (31). This effect of combined treatment with an antiprogestin and antiestrogen is extremely exciting and has considerable therapeutic promise.…”

Section: Animal Modelsmentioning

confidence: 95%

“…This hypothesis could be tested by the use of an antiestrogen having no agonist activity. Second, among the physiological effects seen in RU486-treated intact female rats are increased plasma levels of LH, prolactin, estradiol, and progesterone, as well as the persistence of numerous and actively secretory corpora lutea associated with hypertrophic pituitaries (30)(31)(32)(33)(34). It has therefore been proposed that the efficacy of simultaneous tamoxifen results from its ability to counteract the proliferative effects of the high estrogen levels induced by RU486.…”

Section: Animal Modelsmentioning

confidence: 99%

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Novel Mechanisms of Antiprogestin Action

Horwitz

Tung²,

Takimoto³

1996

Acta Oncologica

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Section: Animal Modelsmentioning

confidence: 95%

Section: Animal Modelsmentioning

confidence: 99%

Novel Mechanisms of Antiprogestin Action

Horwitz

Tung²,

Takimoto³

1996

Acta Oncologica

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“…In addition to its use in the termination of pregnancy (3,4), recent studies have suggested that RU-486 is effective in providing relief from pain associated with endometriosis (5), and induced a marked reduction in leiomyoma volume (6). Further-more, tumors that have hormone receptors, such as breast cancer and meningiomas, have been reported to respond clinically to RU-486 (7)(8)(9). Its efficacy as an antiglucorticoid also has received attention in the treatment of patients with Cushing's syndrome (10).…”

Section: Introductionmentioning

confidence: 99%

Antioxidant: a new role for RU-486 and related compounds.

Parthasarathy¹,

Morales²,

Murphy³

1994

J. Clin. Invest.

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RU-486 (17 f8-hydroxy 4-dimethylaminophenyl-17-a-propenyl estrone 4,9 diene-3-one; mifepristone) is suggested to act by binding to progesterone and glucocorticoid receptors. Based on its chemical nature, we anticipated that RU-486 may have potent antioxidant properties. We used the oxidation of LDL as our model system. RU-486 and a similar compound, onapristone, at 1-5-IuM concentrations, decreased the formation of oxidized LDL. LDL isolated from plasma of subjects who were orally supplemented with RU-486 was resistant to oxidation, as compared to LDL isolated from control plasma.The antioxidant effect of RU-486 appears to reside in the dimethylaminophenyl side chain moiety. Reduction of the A-ring of the steroid molecule had no effect on its antioxidant property. Analogs of RU-486 which lack the dimethylaminophenyl group, were without antioxidant activity. Levoniorgestrel, which

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“…Although RU 486 can serve as the paradigm for this class of antiprogestins, outcomes must be measured against possible antiglucocorticoid effects (Bertagna et al, 1984). In a study of 11 postmenopausal women with advanced breast cancer RU-486 induced a short-term clinical response in 1 patient and stable disease in 6 others (Bakker et al, 1990). The side effects of RU-486 in this study were mostly related to antiglucocorticoid properties of the drug and increased serum estradiol levels.…”

Section: Prms In Breast Cancer Trialsmentioning

confidence: 99%

Progesterone receptor modulators in breast cancer

Wiehle¹,

2014

Turk J Biol

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Breast cancer has been treated successfully with selective estrogen receptor antagonists (SERMs) such as tamoxifen, receptordepleting agents such as fulvestrant, and aromatase inhibitors such as anastrozole. Selective progesterone receptor modulators (SPRMs or PRMs) have not been studied as much and are currently under investigation for inhibition of mammary carcinogenesis in animal models and breast cancer prevention trials in women. They might follow tamoxifen and aromatase inhibitors in the adjuvant treatment of breast cancers with acquired resistance. These uses have not provoked ground-breaking progress or studies and PRMs do not have a high profile. Most in vitro and in vivo studies indicate that PRMs preferentially suppress cell proliferation and also induce apoptosis. In this review we summarized the data on the effects of PRMs and particularly of the antiprogestins RU-486 (mifepristone) and CDB-4124 (Progenta, Proellex or telapristone acetate) on breast cancer models. Both agents have been employed in preclinical and clinical studies for prevention and treatment of breast cancer. This author believes that PRMs should be investigated more intensely.

show abstract

Treatment of breast cancer with different antiprogestins: Preclinical and clinical studies

Abstract: combined treatment (antiprogestin plus antiestrogen or LHRH-agonist) may be of value in endocrine therapy of breast cancer.

Cited by 81 publications

References 14 publications

Novel Mechanisms of Antiprogestin Action

Novel Mechanisms of Antiprogestin Action

Antioxidant: a new role for RU-486 and related compounds.

Progesterone receptor modulators in breast cancer

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