β3-adrenergic receptor

The asset is indicated for the treatment of overactive bladder syndrome symptoms in adult patients. Credit: New Africa / Shutterstock. The UK Medicines and Healthcare products Regulatory Agency (MHRA) has approved Pierre Fabre’s vibegron (Obgemsa) to treat overactive bladder (OAB) syndrome symptoms in adults. Symptoms include urgency, high urinary frequency and incontinence. A beta 3 adrenergic receptor agonist, vibegron functions as a bladder muscle relaxant to ease the bladder muscle activity. The recommended daily dose is a 75mg film-coated tablet. The approval is backed by data from the Phase III EMPOWUR clinical trial, which assessed it for 12 weeks in 1,515 OAB patients. See Also: Conflict means millions of children are missing vaccinations, UN says Moderna and Mitsubishi Tanabe link on mRNA vaccines in Japan Participants received a daily dose of either placebo, vibegron 75mg or an active control. Vibegron significantly reduced daily urination and incontinence episodes versus placebo, with improvements observed within two weeks and sustained over the treatment period. Patients on vibegron reported side effects such as headaches, diarrhoea, constipation, nausea, urinary tract infections and increased post-void residual urine volume. The MHRA assures ongoing monitoring of vibegron’s safety and efficacy and encourages reporting of any side effects through the Yellow Card scheme. The MHRA has also approved AstraZeneca ’s capivasertib (Truqap) for advanced HR-positive, HER2-negative breast cancer with specific genetic abnormalities unresponsive to other treatments. Capivasertib, an AKT inhibitor, impedes cancer cell proliferation and is administered orally alongside fulvestrant, a hormonal therapy. The approval was supported by a clinical trial involving 708 patients, with a subset of 289 patients exhibiting the targeted genetic mutations. In clinical studies, capivasertib-treated individuals had an average of 7.3 months during which their cancer did not progress, compared to 3.1 months for placebo-treated patients. High blood sugar, diarrhoea, rash and other skin drug responses, urinary tract infection, low blood haemoglobin levels, appetite loss, nausea, vomiting, mouth sores or ulcers with gum inflammation, itching and fatigue are possible side effects of the medication.

Researchers have figured out how to turn ordinary white fat cells, which store calories, into beige fat cells that burn calories to maintain body temperature. New UCSF study shows that suppressing a protein turns ordinary fat into a calorie burner and may explain why drug trials attempting the feat haven't been successful. Researchers at UC San Francisco have figured out how to turn ordinary white fat cells, which store calories, into beige fat cells that burn calories to maintain body temperature. The discovery could open the door to developing a new class of weight-loss drugs and may explain why clinical trials of related therapies have not been successful. Until now, researchers believed creating beige fat might require starting from stem cells. The new study published July 1 in the Journal of Clinical Investigation, showed that ordinary white fat cells can be converted into beige fat simply by limiting production of a protein. "A lot of people thought this wasn't feasible," said Brian Feldman, MD, PhD, the Walter L. Miller, MD Distinguished Professor in Pediatric Endocrinology and senior author of the study. "We showed not only that this approach works to turn these white fat cells into beige ones, but also that the bar to doing so isn't as high as we'd thought." A fat transformation Many mammals have three "shades" of fat cells: white, brown and beige. White fat serves as energy reserves for the body, while brown fat cells burn energy to release heat, which helps maintain body temperature. Beige fat cells combine these characteristics. They burn energy, and unlike brown fat cells, which grow in clusters, beige fat cells are embedded throughout white fat deposits. Humans and many other mammals are born with brown fat deposits that help them maintain body temperature after birth. But, while a human baby's brown fat disappears in the first year of life, beige fat persists. Humans can naturally turn white fat cells into beige ones in response to diet or a cold environment. Scientists tried to mimic this by coaxing stem cells into becoming mature beige fat cells. But stem cells are rare, and Feldman wanted to find a switch he could flip to turn white fat cells directly into beige ones. "For most of us, white fat cells are not rare and we're happy to part with some of them," he said. Of mice and humans Feldman knew from his earlier experiments that a protein called KLF-15 plays a role in metabolism and the function of fat cells. With postdoctoral scholar Liang Li, PhD, Feldman decided to investigate how the protein functioned in mice, which retain brown fat throughout their lives. They found that KLF-15 was much less abundant in white fat cells than in brown or beige fat cells. When they then bred mice with white fat cells that lacked KLF-15, the mice converted them from white to beige. Not only could the fat cells switch from one form into another, but without the protein, the default setting appeared to be beige. The researchers then looked at how KLF-15 exerts this influence. They cultured human fat cells and found that the protein controls the abundance of a receptor called Adrb1, which helps maintain energy balance. Scientists knew that stimulating a related receptor, Adrb3, caused mice to lose weight. But human trials of drugs that act on this receptor have had disappointing results. A different drug targeting the Adrb1 receptor in humans is more likely to work, according to Feldman, and it could have significant advantages over the new, injectable weight-loss drugs that are aimed at suppressing appetite and blood sugar. Feldman's approach might avoid side effects like nausea because its activity would be limited to fat deposits, rather than affecting the brain. And the effects would be long lasting, because fat cells are relatively long-lived. "We're certainly not at the finish line, but we're close enough that you can clearly see how these discoveries could have a big impact on treating obesity," he said. Liang Li is also an author of this study. This work was funded by NIH grant R01DK132404.

CASTRES, France, June 28, 2024 /PRNewswire/ -- The European Commission (EC) has authorized the marketing of OBGEMSA™ (vibegron) by Pierre Fabre Laboratories for the symptomatic treatment of overactive bladder syndrome in adults, a particularly debilitating condition affecting over 70 million patients* in Europe. In 2022, Pierre Fabre Laboratories acquired the exclusive license for vibegron from Urovant Sciences Gmbh for the registration and commercialization of this innovative treatment in the European Economic Area. The decision of the EC will be applicable to all EU member states as well as Iceland, Liechtenstein, and Norway. OBGEMSA™ is a trademark owned by Urovant Sciences. Continue Reading View PDF Pierre Fabre Laboratories announce granting of European marketing authorization for OBGEMSA™ (vibegron) in overactive bladder. "We are delighted with this development, which will allow European patients to benefit from a new therapeutic option for overactive bladder syndrome and further strengthen our expertise of over 40 years in urology. This decision confirms Pierre Fabre Laboratories' commitment to offering patients innovative therapies that provide better management of chronic debilitating diseases," said Eric Ducournau, CEO of Pierre Fabre Laboratories. The decision of the EC follows the favorable opinion issued on April 25 by the Committee for Medicinal Products for Human Use (CHMP) of the European Medicines Agency (EMA). It is based on the results of two pivotal, multicenter, double-blind, randomized phase 3 studies in adults with overactive bladder symptoms. Study RVT-901-3003 (EMPOWUR) evaluated the efficacy, tolerability, and safety of vibegron (at a dose of 75 mg per day) over 12 weeks compared to placebo and with tolterodine as a positive control. Its extension, study RVT-901-3004 (EMPOWUR Extension), double-blindly evaluated the long-term safety, tolerability, and efficacy of vibegron over 52 weeks, with tolterodine as an active comparator. In these studies, vibegron, as a new selective agonist of beta-3 adrenergic receptors (AR), demonstrated a favorable benefit-risk profile in the symptomatic treatment of urgency, increased frequency of urination, and urge urinary incontinence (UUI) that can occur in patients with overactive bladder syndrome. Contact: Laurence MARCHAL [email protected] PDF - Logo -