Expert opinion on investigational drugs

INTRODUCTION: Endometriosis is a chronic, estrogen-dependent inflammatory disease affecting up to 10% of reproductive-aged women. Current therapies are predominantly hormone-based and offer symptomatic relief without correcting the immune d…

INTRODUCTION: Dysmenorrhea is the most common cause of gynecological pain among women that has considerable impact on quality of life and psychosocial wellbeing. Non-steroidal anti-inflammatory drugs (NSAIDs) and hormonal therapies are most…

INTRODUCTION: Endometriosis is an estrogen-dependent disease on the background of progesterone resistance. Increased estrogen production, low estrogen metabolization, and altered estrogen receptors (ERs) expression contribute to the hyperes…

INTRODUCTION: Uterine myomas and endometriosis are benign hormone-dependent diseases affecting women of reproductive age. Substantial efforts have been made to develop innovative medical options for treating these gynecologic diseases. Elag…

IntroductionVon Hippel-Lindau (VHL) disease is an inherited autosomal dominant syndrome caused by a germline mutation and/or deletion of the VHL gene. Inappropriate hypoxia-inducible factor (HIF)-mediated transcription of proangiogenic and …

INTRODUCTION: Pharmacotherapy has a key role in endometriosis treatment and management, however, a significant proportion of patients have only intermittent or limited benefits with current treatment options. Therefore, novel therapeutic ap…

KEYWORDS: Endometriosisestrogen biosynthesisAKR1C3steroid sulphatase17β-hydroxysteroid dehydrogenase 1aromatase inhibitors

INTRODUCTION: Endometriosis is a hormone-dependent benign chronic disease that requires a chronic medical therapy. Although currently available drugs are efficacious in treating endometriosis-related pain, some women experience partial or n…

INTRODUCTION: The GnRH agonistic analogs enable for desensitizing the hypothalamo-pituitary-gonadal axis in malignant and benign conditions where minimizing the production of sex hormones, or blocking ovulation is necessary. The possible in…

INTRODUCTION: Endometriosis is an estrogen-dependent chronic disease of women of fertile age requiring chronic therapy. Although available drugs have good efficacy and safety profiles, some patients experience partial or no improvement of p…

INTRODUCTION: Endometriosis is a benign sex hormone-dependent gynecological disease, characterized by the presence and growth of endometrial tissue outside the uterus; it affects 10% of women of reproductive age and is associated with infer…

INTRODUCTION: Current therapies for endometriosis cannot completely cure the disease, and patients present with high recurrence rates. Novel medical approaches are, therefore, needed. AREAS COVERED: In endometriosis, aromatase was long thou…

BACKGROUND: Clinical evidence has shown that conditions such as uterine fibroids, endometriosis and breast cancer are progesterone-dependent diseases. Therefore, progesterone receptor (PR) antagonists and selective PR modulators (SPRMs) are…

Endometriosis is a common and enigmatic disease causing pelvic pain and infertility. Current treatment is mainly based on the use of surgery and ovarian suppressive agents. There is in particular the need for new therapeutic options able to…

Leuprolide acetate is a synthetic nonapeptide that is a potent gonadotropin-releasing hormone receptor (GnRHR) agonist used for diverse clinical applications, including the treatment of prostate cancer, endometriosis, uterine fibroids, cent…

Endometriosis is an enigmatic disease found in as many as 30% of reproductive age women. The symptoms for women who suffer from this malady vary but may include subfertility or chronic pelvic pain. Because endometriosis lesions rely on estr…

Gonadotropin-releasing hormone (GnRH) stimulates the pituitary secretion of both luteinising hormone (LH) and follicle-stimulating hormone (FSH), and thus controls the hormonal and reproductive functions of the gonads. The blockade of the e…

Since the discovery of the antiprogestin RU 486 (mifepristone), other compounds have been synthesised that function as pure progesterone antagonists or progesterone receptor modulators. The latter are mixed agonists-antagonists. Mifepriston…

The third generation aromatase inhibitors are both remarkably potent and specific endocrine agents inhibiting aromatase activity and reducing circulating oestrogen levels in postmenopausal women to levels never previously seen. Their therap…