Progesterone and progesterone receptor modulators in the management of symptomatic uterine fibroids. 2012

Vikram Sinai Talaulikar, and Isaac Manyonda
Department of Obstetrics & Gynaecology, St. George's Hospital and University of London, Cranmer Terrace, Tooting, London SW17 0RE, United Kingdom. vtalauli@sgul.ac.uk

The majority of symptomatic uterine fibroids are currently treated by surgical interventions (myomectomy or hysterectomy) or radiological treatments (uterine artery embolisation or focussed ultrasound surgery). None of these treatments is a panacea, and what is conspicuous is the lack of an effective long-term medical therapy for a disorder so common among women of reproductive age. It has been known for some time that progesterone and its receptors enhance proliferative activity in fibroids and this has raised the possibility that anti-progestins and (PRMs) could be useful in the medical management of fibroids. Some of the compounds which have produced promising results in recent clinical trials or research studies include mifepristone, CDB-4124 (telapristone), CP-8947, J-867 (asoprisnil) and CDB-2914 (ulipristal acetate or UA). UA has recently completed Phase III clinical trials with very encouraging results, and has now acquired a licence for clinical use in Europe. While considerable research has yet to be done on the long-term safety and efficacy of UA there is nevertheless good reason for optimism on the emergence of effective medical therapy in the form of UA and possibly other PRMs.

UI MeSH Term Description Entries
D006965 Hyperplasia An increase in the number of cells in a tissue or organ without tumor formation. It differs from HYPERTROPHY, which is an increase in bulk without an increase in the number of cells. Hyperplasias
D007436 Intrauterine Devices, Medicated Intrauterine devices that release contraceptive agents. Hormone-Releasing IUDs,IUD, Hormone Releasing,Intrauterine Devices, Hormone-Releasing,Intrauterine Devices, Progesterone-Releasing,Medicated Intrauterine Devices,Device, Hormone-Releasing Intrauterine,Device, Medicated Intrauterine,Device, Progesterone-Releasing Intrauterine,Devices, Hormone-Releasing Intrauterine,Devices, Medicated Intrauterine,Devices, Progesterone-Releasing Intrauterine,Hormone Releasing IUD,Hormone-Releasing IUD,Hormone-Releasing Intrauterine Device,Hormone-Releasing Intrauterine Devices,IUD, Hormone-Releasing,IUDs, Hormone-Releasing,Intrauterine Device, Hormone-Releasing,Intrauterine Device, Medicated,Intrauterine Device, Progesterone-Releasing,Intrauterine Devices, Hormone Releasing,Intrauterine Devices, Progesterone Releasing,Medicated Intrauterine Device,Progesterone-Releasing Intrauterine Device,Progesterone-Releasing Intrauterine Devices
D007889 Leiomyoma A benign tumor derived from smooth muscle tissue, also known as a fibroid tumor. They rarely occur outside of the UTERUS and the GASTROINTESTINAL TRACT but can occur in the SKIN and SUBCUTANEOUS TISSUE, probably arising from the smooth muscle of small blood vessels in these tissues. Fibroid,Fibroid Tumor,Fibroid Uterus,Fibroids, Uterine,Fibroma, Uterine,Fibromyoma,Leiomyoma, Uterine,Fibroid Tumors,Fibroid, Uterine,Fibroids,Fibromas, Uterine,Fibromyomas,Leiomyomas,Tumor, Fibroid,Tumors, Fibroid,Uterine Fibroid,Uterine Fibroids,Uterine Fibroma,Uterine Fibromas,Uterus, Fibroid
D009649 Norpregnadienes Pregnadienes which have undergone ring contractions or are lacking carbon-18 or carbon-19.
D010091 Oximes Compounds that contain the radical R2C Aldoximes,Hydroxyimino Compounds,Ketoxime,Ketoximes,Oxime,Compounds, Hydroxyimino
D011980 Receptors, Progesterone Specific proteins found in or on cells of progesterone target tissues that specifically combine with progesterone. The cytosol progesterone-receptor complex then associates with the nucleic acids to initiate protein synthesis. There are two kinds of progesterone receptors, A and B. Both are induced by estrogen and have short half-lives. Progesterone Receptors,Progestin Receptor,Progestin Receptors,Receptor, Progesterone,Receptors, Progestin,Progesterone Receptor,Receptor, Progestin
D004717 Endometrium The mucous membrane lining of the uterine cavity that is hormonally responsive during the MENSTRUAL CYCLE and PREGNANCY. The endometrium undergoes cyclic changes that characterize MENSTRUATION. After successful FERTILIZATION, it serves to sustain the developing embryo. Endometria
D004963 Estrenes Unsaturated derivatives of the ESTRANES with methyl groups at carbon-13, with no carbon at carbon-10, and with no more than one carbon at carbon-17. They must contain one or more double bonds. 19-Norandrostenes,19 Norandrostenes
D005260 Female Females
D006727 Hormone Antagonists Chemical substances which inhibit the function of the endocrine glands, the biosynthesis of their secreted hormones, or the action of hormones upon their specific sites. Antagonists, Hormone

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