Effects of the Novel Orally Active Antiestrogen TZE-5323 on Experimental Endometriosis
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The novel anti-estrogen TZE-5323 effectively reduced endometriosis lesion volume in rats without adverse effects on bone density or estradiol levels.
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Abstract
Danazol and gonadotropin-releasing hormone agonists which are used as therapeutic drugs for endometriosis, develop adverse reactions in association with their long-term use. The efficacy of anti-estrogens for endometriosis, an estrogen-dependent disorder, has not been demonstrated. A novel, orally active anti-estrogen, TZE-5323 ((2-cyclohexy-6-hydroxybenzo[b]thien-3-yl)[4-[2-(1- piperidinyl)ethoxy]phenyl] methanone hydrochloride, CAS 150797-71-0; free salt formula) was developed. TZE-5323 showed strong affinity for human estrogen receptor alpha (hER alpha) and beta (hER beta), and dose-dependently inhibited estradiol-stimulated transcriptional activation via hER alpha and hER beta. Furthermore, TZE-5323 dose-dependently reduced estrogen-increased uterine weight in ovariectomized rats. Tamoxifen showed agonistic activity on hER alpha, while TZE-5323 did not show such activity. In the experimental endometriosis model in rats in which endometrial tissue is autotransplanted into the renal subcapsular space, TZE-5323 dose-dependently reduced the volume of the endometrial implant as did danazol and leuprorelin acetate. Furthermore, the long-term administration of TZE-5323 neither showed a decrease in bone mineral density nor did it affect serum estradiol concentrations in intact rats. Therefore, TZE-5323 suggested its potential as a novel therapeutic drug for endometriosis which is effective also in long-term use.
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Cited by (12)
- Experimental Animal Models in Obstetrics and Gynecology 2024
- New insights into the efficacy of <scp>SR</scp>‐16234, a selective estrogen receptor modulator, on the growth of murine endometriosis‐like lesions 2018
- SR-16234, a Novel Selective Estrogen Receptor Modulator for Pain Symptoms with Endometriosis: An Open-label Clinical Trial 2017
- SR-16234, a Novel Selective Estrogen Receptor Modulator for Pain Symptoms with Endometriosis: An Open-label Clinical Trial. 2017
- Experimental Treatments of Endometriosis 2015
- Innovations in classical hormonal targets for endometriosis 2015
- New trends for the medical treatment of endometriosis 2012
- Management of Endometriosis-associated Pain 2010
- Benign Gynecological Diseases and SERMs 2006
- Subcutaneous Depot Medroxyprogesterone Acetate versus Leuprolide Acetate in the Treatment of Endometriosis-Associated Pain 2006
- Subcutaneous depot medroxyprogesterone acetate versus leuprolide acetate in the treatment of endometriosis-associated pain 2005
- Advances in the management of endometriosis: an update for clinicians 2005
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- openalex
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