Disease relevance of Enclomiphene

• The antitumor activity of three enclomiphene (trans-1- (p-beta-diethylaminoethoxyphenyl)1,2-diphenyl-2-chloroethylene) analogs and the cis isomer zuclomiphene was investigated in MCF 7 human mammary carcinoma cells in culture [1].
• Infertility can be treated with clomifene (clomiphene citrate), metformin, gonadotropins or surgery to the ovaries [2].
• OBJECTIVE: An attempt was made to induce ovulation with low-dose follicle-stimulating hormone (FSH) in clomifene-resistant women with anovulatory polycystic ovarian disease (PCOD) [3].
• Use of clomifene during early pregnancy and risk of hypospadias: population based case-control study [4].
• Secondary outcome measures were ongoing pregnancy, spontaneous abortion, and clomifene resistance [5].

High impact information on Enclomiphene

• However, studies with zuclomiphene and estrogen-irreversible doses of enclomiphene and 6866 indicate that these antiestrogens also influence cell proliferation in vitro by mechanisms that probably do not involve RE [1].
• Studies of protein binding to nonpolar solutes by using zonal elution and high-performance affinity chromatography: interactions of cis- and trans-clomiphene with human serum albumin in the presence of beta-cyclodextrin [6].
• When clomifene fails to induce ovulation, menotropins (human menopausal gonadotrophin) or gonadotrophin-releasing hormone (GnRH) are effective, most notably in WHO group 1 [7].
• The reduction in uterine estrogen and progesterone receptor levels was also counteracted by the concomitant injection of flutamide, but not by enclomiphene [8].
• Clomifene has been associated with hot flushes, multiple gestation, visual disturbances, cervical mucus abnormalities and luteal phase deficiency [9].

Chemical compound and disease context of Enclomiphene

• Population A total of 335 women with WHO group II anovulatory infertility failing to ovulate or conceive on clomifene citrate [10].

Biological context of Enclomiphene

• The displacement of [3H]estradiol with unlabeled hormone or with the antiestrogens, nafoxidine, enclomiphene and tamoxifen (TAM) exhibits identical IC50 values either in the cytosol or in the microsomal membranes [11].
• To assess the potential effects of these isomers on fertilization and early embryogenesis, 3200 embryos were obtained from mouse oocytes fertilized in vivo and in vitro and exposed to increasing concentrations of zuclomiphene, enclomiphene, and clomiphene citrate in culture [12].
• Group 1 cows (n = 24) received three silastic implants, each containing 150 mg of enclomiphene, on d 20 postpartum [13].
• Does previous response to clomifene citrate influence the selection of gonadotropin dosage given in subsequent superovulation treatment cycles [14]?
• Days to first estrus did not differ (P greater than .05) between enclomiphene-treated (57 +/- 6; n = 24) and control (56 +/- 4; n = 28) cows [13].

Anatomical context of Enclomiphene

• Both tamoxifen and clomifene competed with [3H]-QNB and [3H]-nitrendipine for their binding to the receptor in the membrane fractions from the urinary bladder and myometrium [15].
• We examined the effects of enclomiphene and zuclomiphene, alone and in combination with oestradiol, on basal and gonadotrophin-stimulated progesterone secretion by isolated subpopulations of both large (granulosa-lutein) and small (theca-lutein) ovine luteal cells [16].
• Effect of clomifene on thyroid function in normal men [17].
• The luteolytic effect of enclomiphene was mediated by the uterus, as has been shown for estradiol [18].

Associations of Enclomiphene with other chemical compounds

• However, CLO is a mixture of two stereoisomers, enclomiphene (ENC) and zuclomiphene (ZUC), which have distinctly different activities on reproductive tissues and tumor cells [19].
• A single peak of [3H]E2 binding occurred in the 5.2 S region after glycerol density gradient centrifugation, which was competed for by DES, E2, and enclomiphene [20].
• However, even higher ovulation frequencies have been observed when metformin has been adjuvant to clomifene therapy [21].
• Plackett-Burman (P-B) experimental design has been used to optimize the factors affecting separation of Z and E isomers of clomiphene (zuclomiphene and enclomiphene respectively) using capillary electrophoresis [22].
• In both groups serum concentrations of TSH, thyroxine, triiodothyronine, T3 resin uptake test and thyroid hormone binding proteins were measured before, during and after oral administration of clomifene [17].

Gene context of Enclomiphene

• Methods: Forty three anovular women who had received clomifene for ovulation induction followed by gonadotropins for IUI or IVF superovulation were reviewed retrospectively [14].
• MDL 103,323, an enclomiphene analog, was tested for binding to the estrogen receptor, inhibition of human tumor xenografts and prevention of carcinogen-induced mammary tumors [23].
• CONCLUSION: Ultrasound-guided, transvaginal, ovarian, interstitial laser treatment appears effective in improving hormonal profiles and inducing ovulation and successful pregnancy in women with clomifene-resistant PCOS [24].
• Rats were injected s.c. with clomiphene (CL), zuclomiphene (ZUC) or enclomiphene (ENC) on days 1,3, and 5 of life and the stimulation of the reproductive tract and estrogen receptor binding was observed [25].
• In Group 2 the response of TSH to TRH showed a non-significant increase after 5 days and a significant increase (P less than 0.01) after 12 days of clomifene [17].

Analytical, diagnostic and therapeutic context of Enclomiphene

• In Exp. II, 17 suckled cows were randomly assigned to three treatment groups: 1) control group (n = 6) receiving one empty implant, 2) 10-cm enclomiphene implant group (n = 5) and 3) 30-cm enclomiphene implant group (n = 6) [26].
• MAIN RESULTS: Meta-analysis showed that metformin is effective in achieving ovulation in women with PCOS with odds ratios of 3.88 (CI 2.25 to 6.69) for metformin versus placebo and 4.41 (CI 2.37 to 8.22) for metformin and clomifene versus clomifene alone [27].

References