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ANTAGONIST - ClinicalTrials.gov

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Last Updated: 10 May 2022

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Myomectomy vs Uterine Artery Embolization vs GnRh Antagonist for AUB-L

Although many women with fibroids are symptomatic, 20-50% of women may have bulk signs such as pelvic pressure, urinary, or gastrointestinal problems, as well as heavy menstrual bleeding. Heavy menstrual bleeding can lead to severe anemia that needs medical and economic implications. Fibroids are also linked to infertility and recurrent pregnancy loss in fetility and recurrent pregnancy loss. tranexamic acid, an antifibrinolytic agent that decreases menstrual blood loss, and nonsteroidal anti-inflammatory drugs that decrease blood loss and improve pain relief are among nonhormonal medical treatments that can reduce blood loss and pain relief. The most common surgical treatment of fibroids is hysterectomy, but other surgical options are also available to women who want to preserve the uterus. Urine fibroid or uterine artery embolization is another option for fibroid management. Patient satisfaction is high in both myomectomy and UAE. Patients who receive UAE medical treatment have a marginally higher risk of further intervention compared to myomectomy. A new type of medical therapy has become available to women who do not want any type of surgical intervention or the UAE procedure. With add-back therapy in the morning and 300 mg elagolix alone at night, it is administered at a total daily dose of 600 mg: 300 mg elagolix with add-back therapy in the morning and 300 mg elagolix alone at night. According to a placebo with a promising safety record, the Oriahnn dose and formulation resulted in a significant decrease in menstrual blood loss compared to placebo, but it has never been compared to any other fibroids therapy.

Source link: https://clinicaltrials.gov/ct2/show/NCT04856306


An Investigation of the Antidepressant Effects of the mGlu2/3 Receptor Antagonist TS-161 in Treatment-Resistant Depression

OBJECTIVE MODULE Modulation of glutamatergic signaling has been implicated in the development of depressive symptoms and related constructs/dimensions of observable behavior and neurobiological measures with therapy. During acute major depressive episodes, current standard monoaminergic pharmacological treatments for major depressive disorder have only been marginally helpful. In order to produce more effective therapeutics, we've systematically tested various glutamatergic modulators in patients with mood disorders. The antidepressant properties of mGlu2/3 receptor antagonists in preclinical assays, as well as the functional/neural cellular and molecular pathways involved in their actions, are worthy of investigating, but without the side effects and abuse potential of ketamine. The present Phase 2 proof-of-concept study will examine in patients with MDD, the antidepressant effects of TS-161, the burgeoning and selective mGlu2/3 receptor antagonist TP0178894 that crosses the blood brain barrier, is intended to evaluate in subjects with MDD. TS-161 produced acute and prolonged antidepressant-like results in animal model assays of antidepressant effectiveness, but not with ketamine-like side effects, as determined by a lack of rise in locomotion activity or abuse potential. The finding that an mGlu2/3 receptor antagonist has antidepressant effects without psychotomimetic side effects could increase the clinical relevance of the mGlu2/3 receptor antagonist and may lead to the development of novel drug targets for depression treatment. Twenty-five people with a treatment-resistant major depressive disorder will be accepted, according to a study by POPULATION. The investigation will determine the success of improving overall depressive symptomatology and tolerability of TS-161 in treatment-resistant MDD.

Source link: https://clinicaltrials.gov/ct2/show/NCT04821271


Effect of a Dual Orexin Receptor Antagonist, Lemborexant, on Total Sleep Time in Shift Workers: a Randomized Controlled Trial

According to a meta-analysis of sleep in shift workers, fixed night shift workers sleep on average, 0. 4 hours less than fixed day shift workers, and rotating shift workers sleep on average 1 hour less than fixed day shift workers. Although sleep difficulties and sleep loss among shift workers may be multiple reasons, shift workers may have sleep difficulties, and sleep loss is expected to be a key factor, according to the misalignment of one's sleep preference and one's circadian rhythm. Sleep deficiency among night shift and rotating shift workers has been shown to have significant health risks, including elevated risk of cardiovascular disease and cancer. Effective sleep systems in shift workers are lacking. Since Lemborexant is also a hypocretin/orexin antagonist, it is also predicted to improve daytime sleep in shift workers, but it will have the advantage over Suvorexant in the dosages available for clinical use.

Source link: https://clinicaltrials.gov/ct2/show/NCT05344443


Phase IIa Trial of a Selective Glucocorticoid Receptor Antagonist in the Treatment of Veterans With Posttraumatic Stress Disorder (PTSD)

Posttraumatic stress disorder is a common psychiatric disorder that is associated with significant morbidity and mortality around the world. Both PTSD and Major Depression have been shown to be promising with glucocorticoid receptor antagonists. Hypothesized Glucocorticoid receptor antagonists such as mifepristone are hypothesized to realibrate the HPA axis by blockade of peripheral and central GR and improve central glucocorticoid signaling and heighten central glucocorticoid receptor antagonists. Increased central glucocorticoid signaling and normalization of HPA axis control could restrict stress responsive mechanisms, such as the sympathetic nervous system, which are linked to clinical development in PTSD. At 4 weeks in a subgroup of Veterans with PTSD without a history of traumatic brain injury, a recently completed trial of mifepristone, a GR antagonist that can modulate dysregulation of the HPA axis, demonstrated clinical benefits. CORT108297, a second-generation glucocorticoid receptor antagonist with no affinity for the PR, and has been ordered for a Phase IIa clinical trial in veterans with PTSD. Veterans' symptoms of PTSD, and placebo-controlled Phase IIa clinical trial by the investigators would evaluate the efficacy and safety of CORT108297-180 million mg daily for 7 days. Each of the two sites will welcome 44 medically fit male and female veterans of chronic PTSD with randomized CORT108297 or b placebo n=22 per site, resulting in a final sample size of 88 participants over a 26-month enrollment window.

Source link: https://clinicaltrials.gov/ct2/show/NCT04452500


An Investigation of the Antidepressant Effects of the Glycine Receptor Antagonist AV 101 (4-chlorokynurenine) in Major Depressive Disorder

Objective Modulation of the NMDA receptor complex or other aspects of glutamatergic signaling is likely to be involved in the improvement of depressive symptoms and related constructs/dimensions of observable behavior and neurobiological measurements. During acute depressive episodes, the most common monoaminergic pharmacological treatments for major depressive disorder have only been modestly helpful. In order to create improved therapeutics, we've routinely tested various glutamatergic modulators in patients with mood disorders in order to find novel therapeutics. Targeting the receptor's glycine co-agonist site of the receptor may minimize the receptor's adverse effects that occur with ketamine without affecting the receptor's robust efficacy, according to the investigator. The demonstration that a glycine-antagonist has antidepressant activity without psychotomimetic side effects may help the NMDAR's therapeutic value and may encourage the development of new drug targets for depression therapy. In treatment-resistant MDD, the study will determine the eficacy of AV 101 in improving overall depressive symptomatology and tolerability. In patients with treatment-resistant MDD patients with asymptomatic disorder, the score decrease in Hamilton Depression Rating Scale total scores to AV 101 correlates with antidepressant response decrease, while two others investigate other potential response biomarkers. Subjects receiving a remission HDRS total score of less than or equal to 50 percent; change from baseline in Hamilton Anxiety Rating Scale HAM-A, Montgomery-Asberg's Depression Rating Scale MADRS, and the Columbia Suicide Severity Rating Scale C-SSRS total scores.

Source link: https://clinicaltrials.gov/ct2/show/NCT02484456


Combined Beta- Plus Auger Electron Therapy Using a Novel Somatostatin Receptor Subtype 2 Antagonist Labelled With Terbium-161 (161Tb-DOTA-LM3): Beta Plus Study

Neuroendocrine neoplastic neoplasia is a group of neoplasms that arise from neuroendocrine cells and are most common in the intestine, pancreas, and lung. Peptide receptor radionuclide therapy in the SST2 is aimed at the SST2 by the administration of radiolabelled SST2 agonists such as 177Lu-DOTATOC and 177Lu-DOTATATE. terbium-161 has been found to be more effective than 177Lu not only in conjunction with SST2 agonists but also with SST2 antagonists, but especially with SST2 antagonists. Comparing to 177Lu-DOTATOC and 177Lu-DOTATATE, 1 SST2-block antagonists bind to many more SST2-binding locations and accumulate mainly on the cellular membrane, with the exceptions of the cellular membrane. When compared to 177Lu-DOTA-LM3, a 3 -fold higher dose to single cancer cells can be delivered not only by radiation, but also by the release of conversion and Auger electrons, leading to a 3 - 4 fold rise in single cancer cells.

Source link: https://clinicaltrials.gov/ct2/show/NCT05359146


Phase 2 Study of Systemic IL-6 Receptor Antagonist ACTEMRA® (Tocilizumab) for the Treatment of Progressive/Recurrent Pediatric Adamantinomatous Craniopharyngioma

We suspect that the IL6-receptor antagonist ACTEMRA will be safe and effective in inducing tumor formation in children with residual ACP. Up to 38 patients will be receiving tocilizumab at the dose indicated for pediatric Systemic Juvenile Arthritis in this review. It will be a multi-center Phase 2 trial with two strata for patients aged > 1 year and 25 years with unresectable ACP who may have been treated with radiation or without radiation therapy in the past.

Source link: https://clinicaltrials.gov/ct2/show/NCT05233397

* Please keep in mind that all text is summarized by machine, we do not bear any responsibility, and you should always check original source before taking any actions

* Please keep in mind that all text is summarized by machine, we do not bear any responsibility, and you should always check original source before taking any actions