Clinical evaluation of an oral progestin contraceptive, R-2323, 5mg, administered at weekly intervals

Mora, Gabriel; Faúndes, Aníbal; Pastore, Umberto

doi:10.1016/0010-7824(74)90070-5

Cited by 35 publications

(5 citation statements)

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“…Gestrinone is a synthetic trienic 19-norsteroid compound with potent anti-estradiolic and antigonadotropic properties. The compound also inhibits gonadotropin secretion and ovulation, which prevents the occurrence of menstruation [26] . Gestrinone was developed originally as a long-acting contraceptive.…”

Section: Introductionmentioning

confidence: 99%

Effects of gestrinone on uterine leiomyoma and expression of c-Src in a guinea pig model

Zhu

Qiu

Wang

et al. 2007

Acta Pharmacologica Sinica

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Aim: To investigate the effect of gestrinone on uterine leiomyomas and the expression of c-Src, estradiol receptors (ER), and progesterone receptors (PR) in a guinea pig model. Methods: After being oophorectomized, the guinea pigs were allocated into random groups. The model group was treated with estradiol benzoate (E 2 ) for 16 weeks. In the gestrinone-treated groups, the animals were treated with E 2 for 6 weeks in advance, and then in combination with gestrinone for 10 weeks. Histological examination was performed to evaluate whether there were leiomyoma features in the animals. The protein levels of c-Src, phospho-416 Src, ER, and PR were assayed by Western blotting and an immunohistochemical method. Results: Morphological changes were observed in the myometrium of the guinea pig model, including an increase of uterine weights, proliferation of uterine smooth muscles, and the formation of nodules. High protein levels of c-Src, phospho-416 Src, ER, and PR were observed in the myometrium of the guinea pig model. In the gestrinone-treated group, there were no nodules observed. The histological features of the myometrium were similar to that of the control group. Low protein levels of c-Src, phospho-416 Src, ER, and PR were observed in the gestrinonetreated group. Conclusion: The upregulation of c-Src and phospho-416 Src indicated that the activity of c-Src is augmented in the uterine leiomyoma model. c-Src was associated with the formation of uterine leiomyomas in the model, and gestrinone markedly suppressed the growth of uterine leiomyomas in the model. Gestrinone inhibited not only the protein expression of ER and PR, but also c-Src and the autophosphorylation of c-Src in the guinea pig leiomyoma model.

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Section: Introductionmentioning

confidence: 99%

Effects of gestrinone on uterine leiomyoma and expression of c-Src in a guinea pig model

Zhu

Qiu

Wang

et al. 2007

Acta Pharmacologica Sinica

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“…Gestrinone, 13β‐ethyl‐17λ‐ethynyl‐17‐hydroxygona‐4,9,11‐trien‐3‐one, is a synthetic 19‐norsteroid that was originally developed as an oral contraceptive for women 1,. 2 The efficacy and safety in the cyclical mastalgla of gestrinone, which has androgenic, anti‐oestrogenic and antiprogestagenic properties, were investigated 3. This drug is a possible anabolic steroid doping agent, although no misuse of it has been reported by any International Olympic Committee accredited laboratories.…”

mentioning

confidence: 99%

Determination and excretion study of gestrinone in human urine by high performance liquid chromatography and gas chromatography/mass spectrometry

Kim

Lee

Kim

et al. 2000

Rapid Commun. Mass Spectrom.

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“…Gestrinone, 13β‐ethyl‐17λ‐ethynyl‐17‐hydroxygona‐4,9,11‐trien‐3‐one, is a synthetic 19‐norsteroid that was originally developed as an oral contraceptive for women 1,. 2 The efficacy and safety in cyclical mastalgia of gestrinone, which has androgenic, anti‐oestrogenic and antiprogestagenic properties, have been investigated 3. This drug is a possible anabolic steroid doping agent, although no misuse of it has been reported by any International Olympic Committee accredited laboratories.…”

mentioning

confidence: 99%

Determination of the metabolites of gestrinone in human urine by high performance liquid chromatography, liquid chromatography/mass spectrometry and gas chromatography/mass spectrometry

Kim

Lee

Kim

et al. 2000

Rapid Commun. Mass Spectrom.

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Clinical evaluation of an oral progestin contraceptive, R-2323, 5mg, administered at weekly intervals

Cited by 35 publications

References 1 publication

Effects of gestrinone on uterine leiomyoma and expression of c-Src in a guinea pig model

Effects of gestrinone on uterine leiomyoma and expression of c-Src in a guinea pig model

Determination and excretion study of gestrinone in human urine by high performance liquid chromatography and gas chromatography/mass spectrometry

Determination of the metabolites of gestrinone in human urine by high performance liquid chromatography, liquid chromatography/mass spectrometry and gas chromatography/mass spectrometry

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