- |||||||||| Esmya (ulipristal acetate) / ASKA Pharma, Gedeon Richter, AbbVie, Perrigo Company, Mifeprex (mifepristone) / Danco Laboratories
Journal: Is there still a place for progesterone receptor modulators in chronic use ? (Pubmed Central) - Sep 12, 2024
Despite certain concerns, SPRMs offer promising prospects in gynecological pathologies, opening up new therapeutic avenues to improve women's health and quality of life. This article describes the case of a patient with peritoneal leiomyomatosis for whom UPA significantly alleviated symptoms, reduced disease progression and improved quality of life, even allowing a pregnancy.
- |||||||||| Esmya (ulipristal acetate) / ASKA Pharma, Gedeon Richter, AbbVie, Perrigo Company
Journal: Functional evidence for two distinct mechanisms of action of progesterone and selective progesterone receptor modulator on uterine leiomyomas. (Pubmed Central) - Jul 28, 2024
and SMAD3 (SMAD3, TGF-? receptor types 1 and II, Ras homolog A, vascular endothelial growth factor, collagen, type I, ?-1) signaling pathways could therefore be a treatment option for uterine leiomyomas.
- |||||||||| tranexamic acid oral / Generic mfg.
Review, Journal: The modern management of uterine fibroids-related abnormal uterine bleeding. (Pubmed Central) - Jun 19, 2024
Medical treatments used for UFs-related abnormal uterine bleeding include symptomatic agents, such as nonsteroidal antiinflammatory drugs and tranexamic acid, and hormonal therapies, including combined oral contraceptives, gonadotropin-releasing hormone agonists or antagonists, levonorgestrel intrauterine systems, selective progesterone receptor modulators, and aromatase inhibitors...Furthermore, the management of ID and IDA, as a consequence of acute and chronic bleeding, should be taken into account by using iron replacement therapy both during medical treatment and before and after a surgical procedure. In case of symptomatic UFs, the location, size, multiple UFs or coexistent adenomyosis should guide the choice with a shared decision-making, considering long- and short-term treatment goals expected by the patient, including pregnancy desire or wish to preserve the uterus independently of reproductive goals.
- |||||||||| Review, Journal: Experimental and new investigational drugs for the treatment of uterine fibroids. (Pubmed Central) - Jun 7, 2024
Ongoing research on natural compounds, such as vitamin D and epigallocatechin gallate (EGCG), presents emerging options for treating uterine fibroids. This evolving landscape reflects the ongoing efforts to improve therapeutic outcomes for individuals with symptomatic uterine fibroids.
- |||||||||| Esmya (ulipristal acetate) / ASKA Pharma, Gedeon Richter, AbbVie, Perrigo Company
Preclinical, Journal: Ulipristal (UPA) Effects on Rat Ovaries: Unraveling Follicle Dynamics, Ovulation Inhibition, and Safety Implications for prolonged use. (Pubmed Central) - Apr 16, 2024
These results suggest that UPA treatment promotes follicle development at each stage but inhibits ovulation by suppressing the LH surge, resulting in an increase in atretic follicles or unruptured luteinized cysts. These results suggest that UPA may not have both toxic effects on the ovary and a direct local effect on ovarian follicles, but we should be careful about the effects of prolonged UPA treatment in patients with uterine fibroids on their future fecundity.
- |||||||||| tranexamic acid oral / Generic mfg.
Review, Journal: The efficacy of medical management of leiomyoma-associated heavy menstrual bleeding: a mini review. (Pubmed Central) - Mar 25, 2024
Medical management of HMB is the preferred first-line treatment and includes nonsteroidal anti-inflammatory drugs, contraceptive hormones, tranexamic acid, levonorgestrel intrauterine system, gonadotropin-releasing hormone (GnRH) antagonists and antagonists, selective progesterone receptor modulators, selective estrogen receptor modulators, and aromatase inhibitors...Patients may also face financial barriers to GnRH analog therapy. Future studies are required to delineate the nonhormonal treatment options and the long-term management of leiomyoma-associated HMB.
- |||||||||| progesterone / Generic mfg.
Journal: White matter volume and treatment with selective progesterone receptor modulator in patients with premenstrual dysphoric disorder. (Pubmed Central) - Mar 18, 2024
No treatment effect was observed on WMV in any region, including the anterior thalamic radiations, cingulum, forceps minor, fornix, inferior fronto-occipital fasciculus, superior cerebellar peduncle, superior longitudinal fasciculus, and uncinate fasciculus. This is the first finding to indicate that no white matter volume alterations follow three-month progesterone antagonism, suggesting that white matter volume does not participate in symptom relief upon SPRM treatment for PMDD.
- |||||||||| Esmya (ulipristal acetate) / ASKA Pharma, Gedeon Richter, AbbVie, Perrigo Company, Mifeprex (mifepristone) / Danco Laboratories
Journal: Structural analysis and ensemble docking revealed the binding modes of selected progesterone receptor modulators. (Pubmed Central) - Dec 5, 2023
Our ensemble docking and MD simulation revealed that studied ligands have preferential selectivity toward the specific conformation of PR. It is anticipated that our study will be a useful resource to all the drug discovery scientists who are engaged in the identification of lead molecules against UF.
- |||||||||| progesterone / Generic mfg.
Journal: Progesterone Control of Myometrial Contractility. (Pubmed Central) - Nov 6, 2023
Yet, our knowledge of the complex and redundant hormonal pathways controlling uterine contractile activity leading to delivery of the neonate remains incomplete. Finally, we introduce recent animal studies using a novel class of drugs, Selective Progesterone Receptor Modulators, targeting progesterone signalling to prevent premature myometrial contractions.
- |||||||||| EC313 / Evestra, mesoprogestin (EVE104) / Evestra
Preclinical, Journal: Next step in the development of mesoprogestins: the preclinical profile of EC313. (Pubmed Central) - Oct 2, 2023
For an explanation of these findings, the possibility is discussed that the mixed agonistic/antagonistic feature of EC313 is tissue target-specific based on its super-additive synergism characteristic for active bifunctional agents. In conclusion, the specific pharmacodynamic profile of this compound opens the possibility for the development of a drug with a distinct pharmaco-endocrinological profile against uterine fibroids, endometriosis, and other PR-dependent gynecological diseases.
- |||||||||| Esmya (ulipristal acetate) / ASKA Pharma, HRA Pharma, Gedeon Richter, AbbVie, sepranolone (UC1010) / Asarina Pharma
Review, Journal: GABA-ergic Modulators: New Therapeutic Approaches to Premenstrual Dysphoric Disorder. (Pubmed Central) - Aug 21, 2023
We then reflect on the implications of these therapeutic advances, including how they may promote our knowledge of affective regulation more generally. We conclude that these and other studies of PMDD may yield critical insight into the etiopathogenesis of affective disorders, considering that (1) symptoms in PMDD have a predictable onset and offset, allowing for examination of affective state kinetics, and (2) GABAergic interventions in PMDD can be used to better understand the relationship between mood states, network regulation, and the balance between excitatory and inhibitory signaling in the brain.
- |||||||||| Esmya (ulipristal acetate) / ASKA Pharma, HRA Pharma, Gedeon Richter, AbbVie
Journal: Measurement of changes in uterine and fibroid volume during treatment of heavy menstrual bleeding (HMB). (Pubmed Central) - Jun 12, 2023
In the present study, SPRM-UPA failed to produce a significant reduction in the volume of the uterus or the total volume of fibroids (which were present in approximately half of the patients) after either two or three 12-week courses of treatment. This finding represents a new insight in respect of the management of HMB using treatment strategies that target hormone-dependence.
- |||||||||| Esmya (ulipristal acetate) / ASKA Pharma, HRA Pharma, Gedeon Richter, AbbVie
Journal: New Pharmacological Approaches to the Management of Premenstrual Dysphoric Disorder. (Pubmed Central) - May 29, 2023
Recently, a clinically significant reduction in the severity of the mental symptoms of PMDD was observed upon treatment with a selective progesterone receptor modulator (SPRM), as demonstrated when comparing ulipristal acetate with placebo in a randomised controlled trial...They also call for studies on the long-term efficacy, safety, and viability of SPRMs in female individuals during their fertile age to further support the development of targeted management of female's mental ill-health in relation to the menstrual cycle. The present overview thus seeks to inform about current and new pharmacological approaches to the management of premenstrual dysphoric disorder.
- |||||||||| Esmya (ulipristal acetate) / ASKA Pharma, HRA Pharma, Gedeon Richter, AbbVie, Apristor (onapristone XR) / Context Therap
Preclinical, Journal: Z-Endoxifen prevents aggressive mammary cancers in mice by inhibiting cell proliferation and creating a tumor suppressive microenvironment. (Pubmed Central) - May 3, 2023
The expression of genes associated with cell cycle, cell proliferation and extracellular matrix remodeling was similarly repressed by endoxifen and UPA however only endoxifen significantly downregulated prominent genes associated with poor prognosis (Col11a1, Il17b, Pdgfa, Tnfrsf11a). Our results indicate that endoxifen can prevent breast cancers, even when tamoxifen-resistant, through its role in favorable tissue remodeling and immunomodulation.
- |||||||||| Esmya (ulipristal acetate) / ASKA Pharma, HRA Pharma, Gedeon Richter, AbbVie
Clinical, Review, Journal: Ulipristal Acetate in Adenomyosis. (Pubmed Central) - Jan 21, 2023
It seems that ulipristal acetate induces partial or complete remission of AUB caused by adenomyosis, but the evidence concerning its effect on pelvic pain and the radiologic findings of the disease is conflicting. Nevertheless, given the paucity of data, it is still preliminary to draw any conclusion about the subject.
- |||||||||| Esmya (ulipristal acetate) / ASKA Pharma, HRA Pharma, Gedeon Richter, AbbVie, Mifeprex (mifepristone) / Danco Laboratories
Journal: Second-trimester abortion care for those with complex medical conditions. (Pubmed Central) - Nov 9, 2022
Pregnant people presenting for care in the second trimester may have conditions that make an abortion more technically or medically complex. Clinicians can mitigate much of this increased risk with preprocedural planning, and appropriate intra-operative preparedness.
- |||||||||| Journal: Loss of the repressor REST affects progesterone receptor function and promotes uterine leiomyoma pathogenesis. (Pubmed Central) - Nov 1, 2022
Crucially, we identify an interaction between REST and PGR in healthy myometrium and present a putative mechanism for the dysregulation of progesterone-responsive genes in UL ensuing in the loss of REST. Using three Rest conditional knockout mouse lines, we provide a comprehensive picture of the impact loss of REST has in UL pathogenesis and in altering the response of UL to steroid hormones.
- |||||||||| Apristor (onapristone XR) / Context Therap
The SMILE Study: A phase II trial of onapristone in combination with fulvestrant for patients with ER-positive and HER2-negative metastatic breast cancer after progression on endocrine therapy and CDK 4/6 inhibitors (Hall 1) - Oct 10, 2022 - Abstract #SABCS2022SABCS_1690;
The primary objective is to evaluate the objective response rate; secondary objectives include safety and tolerability, progression-free survival, disease control rate, and duration of response. Other correlates include optional functional imaging of PgR binding with 18F-FFNP PET/CT and biomarker analysis (ER, total PgR, HER2, Ki67, CD24, CD44, LDH1, KLF4, CK 5/6, PhosphoSer294-PgR on tissue samples, ESR1 mutations, and circulating tumor DNA analysis).
- |||||||||| Orgovyx (relugolix) / Intas, Gedeon Richter, Takeda, ASKA Pharma, Sumitomo Pharma, Yselty (linzagolix) / Kissei, Theramex, Syneos Health, Orilissa (elagolix) / AbbVie
Journal: Novel pharmacological therapies for the treatment of endometriosis. (Pubmed Central) - Sep 24, 2022
Most studies have focused on the evaluation of the efficacy and safety of GnRH antagonists (plus add-back therapy in cases of prolonged treatment), which should be used as second-line treatment options in selected cases (i.e. non-responders to first-line treatments). Further studies are needed to identify the ideal treatment for women with endometriosis.
- |||||||||| Esmya (ulipristal acetate) / ASKA Pharma, HRA Pharma, Gedeon Richter, AbbVie, Mifeprex (mifepristone) / Danco Laboratories
Journal: Selective progesterone receptor modulators and reproductive health. (Pubmed Central) - Jul 13, 2022
SPRMs and progesterone antagonists have great therapeutic promise for use in other reproductive disorders, including breast cancer, endometriosis, adenomyosis, estrogen-free contraception and cervical ripening but require additional study. Alternative formulations, whether local (topical breast or intrauterine) or extended-release may reduce the incidence of liver function abnormalities and should be explored.
- |||||||||| Visanne (dienogest) / Mochida, Bayer
Review, Journal: Hormonal treatments for endometriosis: The endocrine background. (Pubmed Central) - Jun 4, 2022
Estrogen-dependency and progesterone-resistance are the key events which cause the ectopic implantation of endometrial cells, decreasing apoptosis and increasing oxidative stress, inflammation and neuroangiogenesis...Progestins are mostly used for long term treatments (dienogest, NETA, MPA) and act on multiple sites of action...Nowadays, all these hormonal drugs are considered the first-line treatment for women with endometriosis to improve their symptoms, to postpone surgery or to prevent post-surgical disease recurrence. This review aims to provide a comprehensive state-of-the-art on the current and future hormonal treatments for endometriosis, exploring the endocrine background of the disease.
- |||||||||| progesterone / Generic mfg.
Promegestone Regulates Local Metabolism of Progesterone, Cervical Remodelling and Timing of Labour Onset in Mice. () - Apr 6, 2022 - Abstract #SRI2022SRI_575;
These data suggest that in addition to suppression of myometrial inflammation, R5020 is able to significantly inhibit local P4 metabolism, reduce premature cervical inflammation, supress cervical ripening, and prevent PTB. This discovery is a gateway into a novel therapeutic approach for preterm birth prevention in women at high risk for PTL using drug Promegestone.
- |||||||||| progesterone / Generic mfg.
Progesterone-Responsive Expression of ANKRD1 in Human Myometrial Cells. () - Apr 6, 2022 - Abstract #SRI2022SRI_356;
These results demonstrate that expression of ANKRD1 is modulated by manipulation of progesterone receptor activity via progesterone, mifepristone, and promegestone. The encoded protein has plausible functions in myocyte contractile behavior, regulation of NF-kappa B signaling, and regulation of gene expression, which will be explored in future studies.
- |||||||||| tranexamic acid oral / Generic mfg.
Review, Journal: THE USE OF ULTRASOUND GUIDED HIGH INTENSITY FOCUSED ULTRASOUND (HIFU) IN THE TREATMENT OF UTERINE FIBROIDS: AN OVERVIEW. (Pubmed Central) - Mar 23, 2022
Medical therapy includes hormonal contraceptives, tranexamic acid, and nonsteroidal anti-inflammatory drugs (reduce heavy menstrual bleeding)...Surgical treatment includes hysterectomy, myomectomy - invasive and minimally invasive. Non-surgical management include uterine artery embolization, and focused ultrasound surgery.This review aims to present the role of High-Intensity Focused Ultrasound in the treatment of uterine fibroids.
|
