Hyponatremia is a common electrolyte imbalance which often results from hormonal disregulation. The study aims to investigate whether the apelin hormone, which plays a role in regulating salt and water balance in the body, can be used to treat hyponatremia.
The study will involve healthy volunteers who will be given a medication that causes their bodies to retain water, thus inducing a temporary hyponatremia state. The researchers will measure the volunteers' blood and urine electrolyte levels to see how these are influenced by apelin administration. As comparison, the same measurements will be done in volunteers dosed with placebo instead of apelin.
The researchers believe that apelin may be able to help to correct hyponatremia by increasing urine output. If the study focused in the healthy volunteers population is successful, the investigators will assess the effect of apelin administration in patients with chronic hyponatremia.
The study's hypothesis is that intravenous apelin will increase urinary excretion and sodium levels in healthy participants with artificially induced hyponatremia.

Start Date01 Mar 2024

Sponsor / Collaborator

Universitätsspital Basel

NCT03449251 / Active, not recruitingPhase 2IIT

A Series of Pilot Studies to Evaluate the Haemodynamic and Metabolic Effects of Apelin and Relaxin in Healthy Humans, Subjects With Increased Weight and Patients With Type 2 Diabetes Mellitus

Type two diabetes mellitus (T2DM) is a common, long term metabolic disorder characterised by hyperglycaemia (high blood glucose) resulting from insulin resistance and relative insulin insufficiency. The risk of developing insulin resistance and subsequently T2DM is increased by being overweight and also through a sedentary lifestyle. As the onset can be gradual, physiological damage may have occurred prior to diagnosis. Diabetes is associated with the development of microvascular complications (diabetic nephropathy, neuropathy, and retinopathy), and macrovascular complications (coronary artery disease, peripheral arterial disease, and stroke). While there are many treatments available for T2DM, these complications may still arise, leading to significant morbidity and mortality. There is therefore an urgent need to identify novel signalling pathways that may contribute to the development of diabetes related complications. The identification of these pathways may ultimately lead to the development of new therapies targeting better blood glucose control and preventing these subsequent complications.
Both animal and human studies have indicated that two endogenous peptides, apelin and relaxin both act as vasodilators in the human cardiovascular system and could also have beneficial action in T2DM. Therefore, we aim to carry out experimental medicine studies to test this hypothesis, and explore the signalling pathway in the human vascular system.

Start Date28 Mar 2018

Sponsor / Collaborator

Cambridge University Hospitals NHS Foundation Trust

[+3]

NCT02724566 / CompletedPhase 1IIT

Influence of Apelin on Insulin Sensitivity in Type 2 Diabetic Volunteers

Preclinical studies have demonstrated in mouse models that (PYR1)-apelin-13 exerts a glucose-regulating action in vivo. The (PYR1)-apelin-13 effect on insulin sensitivity in healthy overweighed volunteers has been previously assessed in a phase I clinical trial (APELINS study; NCT02033473). The APELINS-2 clinical trial aims to expand the initial proof of concept to the population targeted by future innovative insulin-sensitizing therapies: patients living with type 2 diabetes.

Start Date01 May 2016

Sponsor / Collaborator

Société Francophone Du Diabete

100 Clinical Results associated with Apelin

100 Translational Medicine associated with Apelin

100 Patents (Medical) associated with Apelin

957

Literatures (Medical) associated with Apelin

01 Dec 2024·Molecular Biology Reports

Quercetin prevents kidney against diabetes mellitus (type 1) in rats by inhibiting TGF-β/apelin gene expression

Article

Author: Firouzeh, Gholampour ; Zeinab, Karimi ; Gholamreza, Daryabor ; Hossein, Ashraf

BACKGROUNDOne of the main causes of diabetic nephropathy is oxidative stress induced by hyperglycemia. Apelin inhibits insulin secretion. Besides, renal expression of TGF-β is increased in diabetes mellitus (DM). The preventive effect of quercetin (Q) against renal functional disorders and tissue damage developed by DM in rats was assessed.METHODSForty male Wistar rats were grouped into normal control (NC), normal + quercetin (NQ: quercetin, 50 mg/kg/day by gavage), diabetic control (DC: streptozotocin, 65 mg/kg, i.p.), diabetic + quercetin pretreatment (D + Qpre), and diabetic + quercetin post-treatment (D + Qpost). All samples (24-hour urine, plasma, pancreatic, and renal tissues) were obtained at the terminal of the experiment.RESULTSCompared to NC and NQ groups, DM ended in elevated plasma and glucose levels, decreased plasma insulin level, kidney dysfunction, augmented levels of malondialdehyde, decreased level of reduced glutathione, reduced enzymatic activities of superoxide dismutase and catalase, elevated gene expression levels of apelin and TGF-β, also renal and pancreatic histological damages. Quercetin administration diminished entire the changes. However, the measure of improvement in the D + Qpre group was higher than that of the D + Qpost group.CONCLUSIONQuercetin prevents renal dysfunction induced by DM, which might be related to the diminution of lipid peroxidation, strengthening of antioxidant systems, and prevention of the apelin/ TGF-β signaling pathway.

01 Nov 2024·Life Sciences

Apelinergic system in acute kidney injury: Mechanistic insights and therapeutic potential

Review

Author: Gaikwad, Anil Bhanudas ; Shelke, Vishwadeep ; Patil, Niraj Sunil

Acute kidney injury (AKI) has emerged as a global health crisis, surpassing mortality rates associated with several cancers and heart failure. The lack of effective therapies, coupled with challenges in diagnosis and the high cost of kidney transplantation, underscores the urgent need to explore novel therapeutic targets and strategies for AKI. Understanding the intricate pathophysiology of AKI is paramount in this endeavor. The components of the apelinergic system-namely, apelin and elabela/toddler, along with their receptor-are prominently expressed in various kidney cells and have garnered significant attention in renal research. Recent studies have highlighted the renoprotective role of the apelinergic system in AKI. This system exerts its protective effects by modulating several pathophysiological processes, including reducing endoplasmic reticulum (ER) stress, improving mitochondrial dynamics, inhibiting inflammation and apoptosis, promoting diuresis through vasodilation of renal vasculature, and counteracting the effects of reactive oxygen species (ROS). Despite these advancements, the precise involvement of the apelinergic system in the progression of AKI remains unclear. Furthermore, the therapeutic potential of apelin-13 in AKI is not fully understood. This review aims to elucidate the role of the apelinergic system in AKI and its interactions with key pathomechanisms involved in the progression of AKI. Additionally, we discuss the current clinical status of exogenous apelin-13 therapy, providing insights that will guide future research on apelin against AKI.

01 Aug 2024·Neurobiology of Disease

Fluorinated apelin-13 mediates neuroprotective effects in multiple sclerosis models

Article

Author: Bagnard, Dominique ; Charmarké-Askar, Imane ; Spenlé, Caroline ; Kuntzel, Thomas ; Riou, Aurélien ; Riché, Stéphanie ; Bonnet, Dominique ; Birmpili, Dafni ; Pham-Van, Lucas Dinh ; Xhurxhi, Thanos

Multiple sclerosis (MS) is an autoimmune and neurodegenerative disease leading to demyelination and axonal loss. Current treatments are immunomodulatory or immunosuppressive drugs acting on the inflammatory component. However, these treatments do not adequately address the crucial aspect of neuroprotection. Recently, an association between an altered balance of adipokines and MS has been proposed as both a risk factor for developing MS and a chronic disease aggravating factor. Specifically, a decrease of apelin plasma levels in MS patients compared to controls correlates with the number of relapses and disease severity. Here we report a dramatic downregulation of apelin levels in the CNS of EAE mice which is also detected in MS patients brain samples compared to controls. Exploiting innovative design and synthesis techniques, we engineered a novel fluorinated apelin-13 peptide characterized by enhanced plasmatic stability compared to its native counterpart. With this peptide, we assessed the potential therapeutic benefits of apelin preventive supplementation in the EAE mouse model. We show that the fluorinated Apelin-13 peptide ameliorates EAE clinical score and preserves myelin content in the EAE MOG model recapitulating the progressive form of disease. These results combined with ex-vivo experiments in brain organotypic slices and in vitro studies in neurons and primary microglia and macrophages suggest that apelin has neuroprotective effects and influences the microglia/macrophages function.

News (Medical) associated with Apelin

04 Sep 2024

·www.biospace.com

Lilly Partner BioAge Files for IPO to Advance Obesity Candidate

iStock, JHVEPhoto BioAge will use the proceeds from the initial public offering to move its oral apelin receptor agonist azelaprag past its Phase III STRIDES study and into a registrational Phase III trial. BioAge Labs revealed its plans for an initial public offering on Tuesday, as it looks to capitalize on the red-hot obesity medication market. The California-based biotech has not yet announced how much it expects to raise, nor has it set a completion date for the initial public offering (IPO). Once completed, BioAge will trade on the Nasdaq Global Market under the ticker symbol BIOA. The biotech is also offering its underwriters—Goldman Sachs, Citi, Jefferies and Morgan Stanley—a 30-day option to purchase additional shares of its common stock at the IPO price, minus discounts and commissions. According to BioAge, the primary objective of its IPO is to increase the company’s “financial flexibility” as well as to provide additional capital for its operations. The biotech will use the proceeds to advance its lead candidate azelaprag past its Phase III STRIDES study and into a registrational Phase III trial. Designed to be orally available, azelaprag is a small molecule activator of the apelin receptor which could help “recapitulate many of the benefits of exercise,” according BioAge. Azelaprag works by mimicking apeline, a protein that the body secretes in response to exercise, helping to potentially boost patients’ basal metabolic rate and insulin sensitivity while also inhibiting inflammation and muscle atrophy. Currently, the biotech is running a Phase II study assessing azelaprag with Eli Lilly’s blockbuster incretin therapy tirzepatide to help lower body weight, while also improving body composition. Topline data from the study are expected in the third quarter of 2025. BioAge also has plans to launch a Phase II study of azelaprag with Novo Nordisk’s semaglutide next year. BioAge will use the IPO funds to start a proof-of-concept study of azelaprag in insulin sensitivity, with an eye toward expanding its indication. A chunk of the IPO raise will also go toward developing its NLRP3 blocker for neuroinflammation. Tuesday’s IPO announcement comes after BioAge in February 2024 announced that it raised $170 million in an oversubscribed Series D funding round. Lilly Ventures, the venture capital arm of Eli Lilly, participated in the financing round. Lilly is also partnered with BioAge for the biotech’s Phase II trial of azelaprag. With its IPO, BioAge joins three other biotechs that have recently announced plans to go public. Last month, MBX Biosciences revealed its Nasdaq bid , the proceeds from which will help support its chronic hypoparathyroidism program. Cancer-focused Bicara Therapeutics and immunology player Zenas Biopharma also revealed IPO plans.

Phase 2IPOPhase 3

03 Sep 2024

·www.prnewswire.com

Vasa Therapeutics Announces Initiation of Phase 1 First-in-Human Clinical Trial of VS-041 for the Treatment of Heart Failure with Preserved Ejection Fraction

Vasa Therapeutics granted MHRA Clinical Trial Authorization (CTA) for VS-041 for the treatment of heart failure with preserved ejection fraction (HFpEF) Company's seed funding extended to $11M ENCINITAS, Calif. and WROCLAW, Poland, Sept. 3, 2024 /PRNewswire/ -- Vasa Therapeutics ("Vasa"), a clinical stage biopharmaceutical company developing novel therapies for cardiovascular and metabolic aging, announced today that the U.K. Medicines and Healthcare products Regulatory Agency (MHRA) has granted clinical trial authorization (CTA) for Vasa to commence a Phase 1 first-in-human clinical trial to evaluate the safety, tolerability, and pharmacokinetics of its investigational drug VS-041 in healthy adult participants. VS-041 is an oral compound with a novel mechanism of action for the potential treatment of heart failure with preserved ejection fraction (HFpEF). "The MHRA's authorization marks a major step forward in our mission to develop VS-041 as a disease-modifying therapy for HFpEF," said Artur Plonowski, MD, PhD, Chief Executive Officer, Vasa Therapeutics. "There are currently no approved HFpEF treatments that improve structural properties of myocardium and provide durable clinical benefit. By inhibiting the release of endotrophin, a biomarker and mediator of fibrotic and inflammatory responses, VS-041 has the potential to become the first personalized approach in HFpEF management that could be used in patients with elevated levels of endotrophin who have a high risk of an unfavorable prognosis." The commencement of the Phase 1 trial of VS-041 coincides with an extension of the Company's seed funding, bringing the total round to $11 million. The financing was led by Orphinic Scientific SA with participation from i&i Biotech Fund I SCSp. Proceeds will support the clinical development of VS-041 and advancement of Vasa's preclinical programs. About HFpEF and endotrophin Heart failure is a serious condition that affects more than 64 million people worldwide.1 Approximately 6.7 million Americans have heart failure, which is expected to increase to over 8.5 million Americans by 2030.2 Nearly half of patients with heart failure have heart failure with preserved ejection fraction (HFpEF)3, and the prevalence of HFpEF is increasing.2,4 Approximately 75% of patients with HFpEF will die within five years of initial hospitalization, and 84% will be rehospitalized.2 Currently approved therapies for HFpEF provide clinical improvement but do not result in disease modification and durable improvement upon discontinuation of the treatment.5 Endotrophin, a collagen type VI–derived signaling peptide, has been linked to cardiac metabolic dysregulation, inflammation, and fibrosis. Baseline plasma endotrophin levels HFpEF patients were shown to be strongly and independently associated with increased risk of poor outcomes (deaths or heart failure rehospitalizations).6 About VS-041 VS-041 is an oral compound that was discovered and developed by Vasa for the potential treatment of HFpEF. VS-041 robustly reduces cardiac fibrosis and significantly improves diastolic heart functions in a preclinical HFpEF model. The compound also inhibits the release of endotrophin from primary human cardiac fibroblasts. In GLP toxicology studies, VS-041 demonstrated a highly favorable safety and tolerability profile. Preclinical development of VS-041 was co-funded by the European Regional Development Fund and the Polish National Centre for Research and Development (POIR.01.01.01-00-1210/19-01). About Vasa Therapeutics Vasa is a privately held biopharmaceutical company developing therapeutics that target pathophysiologies of cardiovascular and metabolic aging. In addition to VS-041, Vasa developed a cutting-edge platform for long-acting apelin for combination treatment with incretins in obesity, especially for patients at risk for skeletal muscle loss or cardiovascular disease. As a monotherapy, long-acting apelin agonists could also be beneficial in treating muscle atrophy, heart failure, chronic kidney disease, or peripheral artery disease. Vasa's preclinical pipeline also includes a best-in-class inhibitor of CamKIId for heart failure and life-threatening arrhythmias. For more information, please visit References: James et al. GBD 2017 Disease and Injury Incidence and Prevalence Collaborators. Lancet 2018; 392: 1789–858. Bozkurt B, Ahmad T, Alexander KM, Baker WL, Bosak K, Breathett K, Fonarow GC, Heidenreich P, Ho JE, Hsich E, Ibrahim NE, Jones LM, Khan SS, Khazanie P, Koelling T, Krumholz HM, Khush KK, Lee C, Morris AA, Page RL 2nd, Pandey A, Piano MR, Stehlik J, Stevenson LW, Teerlink JR, Vaduganathan M, Ziaeian B; Writing Committee Members. Heart Failure Epidemiology and Outcomes Statistics: A Report of the Heart Failure Society of America. J Card Fail. 2023 Oct;29(10):1412-1451. doi: 10.1016/j.cardfail.2023.07.006. Epub 2023 Sep 26. PMID: 37797885; PMCID: PMC10864030. Dunlay SM, Roger VL, Weston SA, Jiang R, Redfield MM. Longitudinal changes in ejection fraction in heart failure patients with preserved and reduced ejection fraction. Circ Heart Fail. 2012 Nov;5(6):720-6. doi: 10.1161/CIRCHEARTFAILURE.111.966366. Epub 2012 Aug 30. PMID: 22936826; PMCID: PMC3661289. Yancy CW, Jessup M, Bozkurt B, et al. 2013 ACCF/AHA Guideline for the Management of Heart failure: A Report of the American College of Cardiology Foundation/American Heart Association Task Force on Practice Guidelines. Circulation. 2013;128:e240-e327. Packer M, Butler J, Zeller C, Pocock SJ, Brueckmann M, Ferreira JP, Filippatos G, Usman MS, Zannad F, Anker SD. Blinded Withdrawal of Long-Term Randomized Treatment With Empagliflozin or Placebo in Patients With Heart Failure. Circulation. 2023 Sep 26;148(13):1011-1022. Chirinos JA, Zhao L, Reese-Petersen AL, Cohen JB, Genovese F, Richards AM, Doughty RN, Díez J, González A, Querejeta R, Zamani P, Nuñez J, Wang Z, Ebert C, Kammerhoff K, Maranville J, Basso M, Qian C, Rasmussen DGK, Schafer PH, SeifFert D, Karsdal MA, Gordon DA, Ramirez-Valle F, Cappola TP. Endotrophin, a Collagen VI Formation-Derived Peptide, in Heart Failure. NEJM Evid. 2022 Oct;1(10):10.1056 SOURCE Vasa Therapeutics

INDPhase 1

22 Aug 2024

·www.fiercebiotech.com

Ex-GSK CEO takes up board post at aging and obesity biotech BioAge

BioAge put itself on the map in 2020 by raising $90 million to treat aging and age-related diseases. BioAge Labs has appointed former GSK CEO Jean-Pierre Garnier as chair of its board of directors, bringing the pharma veteran back into the anti-aging space 16 years after he made a big bet on the sector.Garnier worked as CEO of GSK, then called GlaxoSmithKline, from 2000 to 2008. Toward the end of his time heading up the company, Garnier oversaw the $720 million acquisition of Sirtris Pharmaceuticals. The biotech landed the buyout on the basis of evidence that resveratrol, a molecule in red wine, and other sirtuin-targeted drugs could extend healthy life spans.Sirtris ran into problems in the years after the buyout, with programs failing and researchers at Amgen and Pfizer questioning the validity of the science underpinning the biotech. GSK shuttered Sirtris in 2013. Garnier worked as CEO of Pierre Fabre for two years after departing GSK. Since leaving the CEO life behind, Garnier has held a series of board positions at biotechs including Actelion, Cellectis and Idorsia. BioAge sees benefits to being the latest biotech to bring Garnier onto its board. “His extensive experience in leading biotech and pharmaceutical companies through critical growth phases will be invaluable as we progress our lead compound, azelaprag, through clinical development for obesity and advance our pipeline of metabolic aging therapies,” BioAge CEO Kristen Fortney, Ph.D., said in a statement.BioAge put itself on the map in 2020 by raising $90 million to treat aging and age-related diseases. This year, BioAge raised a further $170 million to capitalize on the potential for its apelin receptor agonist azelaprag to combine well with GLP-1 drugs, boosting weight loss while preserving muscle mass. BioAge picked up the asset from Amgen.Garnier's reemergence on the anti-aging scene comes about two years after Hal Barron, M.D., stepped down as chief scientific officer of GSK to take the CEO post at another biotech with a longevity angle, Altos Labs.

Executive ChangeAcquisition

100 Deals associated with Apelin

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Cardiovascular Diseases	Phase 2	GB	AstraZeneca PLC	28 Mar 2018
Diabetes Mellitus, Type 2	Phase 2	GB	AstraZeneca PLC	28 Mar 2018

Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ERA2023	Not Applicable	Chronic Kidney Diseases	24	apelin (Healthy volunteers)	gmjaunyxgb(tavrageavx) = bwkxfsrung feqazbamah (kqxovtqkjr ) View more	-	15 Jun 2023
				apelin (Chronic kidney disease)	gmjaunyxgb(tavrageavx) = tjlifnsebz feqazbamah (kqxovtqkjr ) View more
ERA2023	Not Applicable	Chronic Kidney Diseases	30	Apelin (Patients with CKD)	(auatmtabgh) = mgdmyvfuyy vgbtmypldm (elnsstxfkw ) View more	-	15 Jun 2023
				Apelin (Healthy volunteers)	(auatmtabgh) = aeyszforvl vgbtmypldm (elnsstxfkw ) View more
EASD2015	Not Applicable	-	-	Apelin	usomvqhfyl(xdtjcffkpa) = Average frequency of NO hypothalamic release is significantly reduced following infusion of low-doses of apelin in the digestive tract (0,11 ± 0,003 Hz vs 0,12 ± 0,002 for control; P<0.001) kytpmrapnz (uojpjqychg ) View more	-	16 Sep 2015
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