Potential of Mirabegron and its Extended-release Formulations for the Treatment of Overactive Bladder Syndrome.

Abstract:

BACKGROUND:Overactive bladder syndrome is a broadly occurring urological disorder with a distressing impact on the quality of life. The commonly used antimuscarinic drugs show poor patient compliance because of unsatisfactory potency, tolerability and high occurrence of adverse effects such as dry mouth, blurred vision, constipation, dizziness etc. Mirabegron is the first approved β3-adrenoreceptor agonist, used as mono or in combination therapies for overactive bladder syndrome. OBJECTIVE:The present review provides an insight into the mechanism, pharmacokinetics, toxicokinetics, clinical trials and the development of various conventional and modified-release dosage forms of mirabegron for the treatment of overactive bladder syndrome. RESULTS:The clinical trials of phase II and phase III of mirabegron demonstrated symptomatic relief from the overactive bladder without disturbing the micturition cycle. To date, mirabegron showed promising results for safety, tolerability and efficacy in patients with overactive bladder syndrome. The modified-release tablet dosage form of mirabegron appear to be a proficient and suitable replacement for antimuscarinics and revealed the tremendous potential to overcome the adverse effects of conventional antimuscarinic drugs like Oxybutyline chloride ER, Detrol LA, VESIcare, etc. Conclusion: Mirabegron shows a distinct mode of action, i.e., targeting β3-adrenoreceptors and improving bladder storage without altering void contractions. The limited side effects, high safety, efficacy and tolerability of mirabegron present an adequate substitute to antimuscarinics. However, long-term analysis and clinical studies are prerequisites for assessing the safety, tolerability and efficacy profile of mirabegron.

journal_name

Curr Drug Metab

journal_title

Current drug metabolism

authors

Mandpe P,Prabhakar B,Shende P

doi

10.2174/1389200221666200425211139

subject

Has Abstract

pub_date

2020-01-01 00:00:00

pages

79-88

issue

2

eissn

1389-2002

issn

1875-5453

pii

CDM-EPUB-106115

journal_volume

21

pub_type

杂志文章,评审
  • Nanotechnologies: a strategy to overcome blood-brain barrier.

    abstract::The possibility to treat central nervous system (CNS) disorders is strongly limited by the poor access of many therapeutic agent to the target tissues. This is mainly due to the presence of the blood-brain barrier (BBB), formed by a complex interplay of endothelial cells, astrocyte and pericytes, through which only se...

    journal_title:Current drug metabolism

    pub_type: 杂志文章,评审

    doi:10.2174/138920012798356943

    authors: De Rosa G,Salzano G,Caraglia M,Abbruzzese A

    更新日期:2012-01-01 00:00:00

  • Curcumin - A Novel Therapeutic Agent in the Prevention of Colorectal Cancer.

    abstract:BACKGROUND:Colorectal cancer is the third important cause of cancer-associated deaths across the world. Hence, there is an urgent need for understanding the complete mechanism associated with colorectal cancer, which in turn can be utilized toward early detection as well as the treatment of colorectal cancer in humans....

    journal_title:Current drug metabolism

    pub_type: 杂志文章,评审

    doi:10.2174/1389200220666191007153238

    authors: Gupta MK,Vadde R,Sarojamma V

    更新日期:2019-01-01 00:00:00

  • The impact of in vitro binding on in vitro-in vivo extrapolations, projections of metabolic clearance and clinical drug-drug interactions.

    abstract::This review provides a vista of the current opportunities and remaining challenges in the area of in vitro-in vivo extrapolation, with particular emphasis on drug binding terms in predictive models, which has been the source of much controversy. Although the importance of fu(inc) (fraction unbound in in vitro incubati...

    journal_title:Current drug metabolism

    pub_type: 杂志文章,评审

    doi:10.2174/138920006776359266

    authors: Grime K,Riley RJ

    更新日期:2006-04-01 00:00:00

  • Psychedelic 5-methoxy-N,N-dimethyltryptamine: metabolism, pharmacokinetics, drug interactions, and pharmacological actions.

    abstract::5-methoxy-N,N-dimethyltryptamine (5-MeO-DMT) belongs to a group of naturally-occurring psychoactive indolealkylamine drugs. It acts as a nonselective serotonin (5-HT) agonist and causes many physiological and behavioral changes. 5-MeO-DMT is O-demethylated by polymorphic cytochrome P450 2D6 (CYP2D6) to an active metab...

    journal_title:Current drug metabolism

    pub_type: 杂志文章,评审

    doi:10.2174/138920010794233495

    authors: Shen HW,Jiang XL,Winter JC,Yu AM

    更新日期:2010-10-01 00:00:00

  • Gender differences in p-glycoprotein expression and function: effects on drug disposition and outcome.

    abstract::Gender differences in drug concentrations, drug response and toxicity have been attributed to various distinct yet interrelated physiological and molecular mechanisms. Drug transporters and metabolising enzymes play an important role in the xenobiotic cascade and are important regulators of drug disposition at the mol...

    journal_title:Current drug metabolism

    pub_type: 杂志文章,评审

    doi:10.2174/138920009788498996

    authors: Bebawy M,Chetty M

    更新日期:2009-05-01 00:00:00

  • Physiologically-Based Pharmacokinetic (PBPK) Modelling of Transporter Mediated Drug Absorption, Clearance and Drug-Drug Interactions.

    abstract::Membrane transporters play an important role in intestinal absorption, distribution and clearance of drugs. Additionally transporters along with enzymes regulate tissue exposures (e.g. liver, kidney and brain), which are important for safety and efficacy considerations. Early identification of transporters involved gu...

    journal_title:Current drug metabolism

    pub_type: 杂志文章

    doi:10.2174/1389200221999210101233340

    authors: Taskar KS,Harada I,Alluri RV

    更新日期:2021-01-01 00:00:00

  • Talin: A Potential Drug Target for Cancer Therapy.

    abstract::Talin is an intracellular cytoskeletal protein and one of the major components of the focal adhesion complex. It mainly acts as an interlink between transmembrane integrin receptors and cytosolic F-actin. Apart from integrins and actin, it also interacts with various other proteins in the adhesion complex to regulate ...

    journal_title:Current drug metabolism

    pub_type: 杂志文章

    doi:10.2174/1389200221666200214114018

    authors: Malla RR,Vempati RK

    更新日期:2020-01-01 00:00:00

  • Pharmacokinetics, Metabolism, Distribution and Permeability of Nanomedicine.

    abstract:BACKGROUND:Medical application of nanotechnology is termed as Nanomedicine and is widely used in healthcare industries. Nanotechnology has helped Physicians, Scientists and Technologists to understand the changes in cellular levels to develop nanomedicines and address the challenges faced by the healthcare sectors. Nan...

    journal_title:Current drug metabolism

    pub_type: 杂志文章,评审

    doi:10.2174/1389200219666180305154119

    authors: Ravindran S,Suthar JK,Rokade R,Deshpande P,Singh P,Pratinidhi A,Khambadkhar R,Utekar S

    更新日期:2018-01-01 00:00:00

  • Emerging technologies, recent developments, and novel applications for drug metabolite identification.

    abstract::Drug metabolite identification and metabolic characteristics analysis play a crucial role in new drug research and development, because they can lead to varied efficacy, severe adverse reactions, and even toxicity. Classical methodologies for metabolite identification have mainly been based on mass spectrometry (MS) c...

    journal_title:Current drug metabolism

    pub_type: 杂志文章,评审

    doi:10.2174/1389200216666141230105649

    authors: Lu W,Xu Y,Zhao Y,Cen X

    更新日期:2014-01-01 00:00:00

  • Decreasing systemic toxicity via transdermal delivery of anticancer drugs.

    abstract::When used at a high dose, many anticancer drugs produce undesirable side effects including hepatotoxicity. Transdermal delivery bypasses first-pass metabolism, allowing the use of a lower dose of drug while decreasing systemic toxicity. In this review, we summarize various advanced technologies for improving anticance...

    journal_title:Current drug metabolism

    pub_type: 杂志文章,评审

    doi:10.2174/138920008785821693

    authors: Fang JY,Liu PF,Huang CM

    更新日期:2008-09-01 00:00:00

  • Quantitative in vivo microdialysis in pharmacokinetic studies: some reminders.

    abstract::This paper reviews the empirical methods of quantitative microdialysis that have been used to interpret the results obtained from pharmacokinetic studies. The concept of extraction efficiency or recovery and the properties of recovery in vivo (variation with flow rate, time dependency and influence of the mode of admi...

    journal_title:Current drug metabolism

    pub_type: 杂志文章,评审

    doi:10.2174/1389200053586109

    authors: Cano-Cebrián MJ,Zornoza T,Polache A,Granero L

    更新日期:2005-04-01 00:00:00

  • Stem Cells, a New Generation Model for Predictive Nano Toxicological Assessment.

    abstract::With the recent advancement in nanoscience and nanotechnology, there is a growing demand for assessment of the toxicological effects of nano materials to humans and other biological systems. And a predictive toxicology approach that uses in vitro screening assays in conjunction with in vivo study results are widely em...

    journal_title:Current drug metabolism

    pub_type: 杂志文章,评审

    doi:10.2174/1389200216666151015113720

    authors: Suma RN,Mohanan PV

    更新日期:2015-01-01 00:00:00

  • Helix-Coil Transition Signatures B-Raf V600E Mutation and Virtual Screening for Inhibitors Directed Against Mutant B-Raf.

    abstract:BACKGROUND:Mutation in the B RAF at V600E has been well implicated in the carcinogenesis that makes it as an attractive therapeutictarget. In the present study, we sought to identify the basis of V600E mutation at functional and structural grounds. The study also endeavors in identification of small molecule as a poten...

    journal_title:Current drug metabolism

    pub_type: 杂志文章

    doi:10.2174/1389200218666170503114611

    authors: Bandaru S,Sumithnath TG,Sharda S,Lakhotia S,Sharma A,Jain A,Hussain T,Nayarisseri A,Singh SK

    更新日期:2017-07-21 00:00:00

  • Pharmacological Effects of RAAS Blockade in Ischemic Nephropathy.

    abstract:BACKGROUND:The management of ischemic nephropathy due to atherosclerotic renal artery stenosis has become increasingly conservative in the modern era, with current guidelines recommending optimized medical therapy as the initial step. The doubts raised by the recently published trials of revascularization strategies ha...

    journal_title:Current drug metabolism

    pub_type: 杂志文章,评审

    doi:10.2174/1389200217666160219114443

    authors: Rivoli L,Di Mario F,Coppolino G,Gigante A,Barbano B,Farrah TE,Rosato E,Fuiano G,Cianci R

    更新日期:2016-01-01 00:00:00

  • Effects of Montmorillonite on Growth Performance, Serum Biochemistry and Oxidative Stress of Red-Crowned Crane (Grus japonensis) Fed Mycotoxin-Contaminated Feed.

    abstract:BACKGROUND:The red-crowned crane (Grus japonensis) is one of the most vulnerable bird species in the world. Mycotoxins are toxic secondary metabolites produced by fungi and considered naturally unavoidable contaminants in animal feed. Our recent survey indicated that the mycotoxins had the potential to contaminate redc...

    journal_title:Current drug metabolism

    pub_type: 杂志文章

    doi:10.2174/1389200221666200726221126

    authors: Liu D,Wu Q,Liu H,Lu C,Gu C,Kuca K,Wu W

    更新日期:2020-01-01 00:00:00

  • Current Treatment Options for HCC: From Pharmacokinetics to Efficacy and Adverse Events in Liver Cirrhosis.

    abstract:BACKGROUND:Hepatocellular carcinoma (HCC) is among the world's most common cancers. For over ten years, the only medical treatment for it has been the multikinase inhibitor Sorafenib. Currently, however, other first or second-line therapeutic options have also shown efficacy against HCC, such as multikinase inhibitors ...

    journal_title:Current drug metabolism

    pub_type: 杂志文章

    doi:10.2174/1389200221999200918141239

    authors: Galati G,Massimo Vainieri AF,Maria Fulgenzi CA,Di Donato S,Silletta M,Gallo P,Onorato A,Vespasiani-Gentilucci U,Picardi A

    更新日期:2020-01-01 00:00:00

  • Effect of environmental substances on the activity of arylamine N-acetyltransferases.

    abstract::Arylamine N-acetyltransferases (NAT) are xenobiotic-metabolizing enzymes responsible for the acetylation of many aromatic arylamine and heterocyclic amines, thereby playing an important role in both detoxification and activation of numerous drugs and carcinogens. Two closely related isoforms (NAT1 and NAT2) have been ...

    journal_title:Current drug metabolism

    pub_type: 杂志文章,评审

    doi:10.2174/138920008784892092

    authors: Rodrigues-Lima F,Dairou J,Dupret JM

    更新日期:2008-07-01 00:00:00

  • A comprehensive listing of bioactivation pathways of organic functional groups.

    abstract::The occurrence of idiosyncratic adverse drug reactions during late clinical trials or after a drug has been released can lead to a severe restriction in its use and even in its withdrawal. Metabolic activation of relatively inert functional groups to reactive electrophilic intermediates is considered to be an obligato...

    journal_title:Current drug metabolism

    pub_type: 杂志文章,评审

    doi:10.2174/1389200054021799

    authors: Kalgutkar AS,Gardner I,Obach RS,Shaffer CL,Callegari E,Henne KR,Mutlib AE,Dalvie DK,Lee JS,Nakai Y,O'Donnell JP,Boer J,Harriman SP

    更新日期:2005-06-01 00:00:00

  • Oxidative and Non-Oxidative Metabolomics of Ethanol.

    abstract:BACKGROUND:It is well known that ethanol can cause significant morbidity and mortality, and much of the related toxic effects can be explained by its metabolic profile. OBJECTIVE:This work performs a complete review of the metabolism of ethanol focusing on both major and minor metabolites. METHOD:An exhaustive litera...

    journal_title:Current drug metabolism

    pub_type: 杂志文章,评审

    doi:10.2174/1389200217666160125113806

    authors: Dinis-Oliveira RJ

    更新日期:2016-01-01 00:00:00

  • Role of Graphene Nano-Composites in Cancer Therapy: Theranostic Applications, Metabolic Fate and Toxicity Issues.

    abstract::Graphene and its modified nano-composites have gained much attention in recent times in cancer therapy as nanotheranostics due to low production cost, ease in synthesis and physicochemical properties (ultra-large surface area with planar structure and π-π conjugation with the unsaturated and aromatic drugs/biomolecule...

    journal_title:Current drug metabolism

    pub_type: 杂志文章,评审

    doi:10.2174/1389200215666141125120633

    authors: Rahman M,Ahmad MZ,Ahmad J,Firdous J,Ahmad FJ,Mushtaq G,Kamal MA,Akhter S

    更新日期:2015-01-01 00:00:00

  • Electroporation in DNA vaccination protocols against cancer.

    abstract::Since conventional therapeutic approaches in cancer are highly invasive they hardly prolong patient survival for more than few months. Having the ability to stimulate both cellular and humoural immune responses, immunisation with naked plasmid DNA encoding tumour-associated antigens or tumour-specific antigens has rec...

    journal_title:Current drug metabolism

    pub_type: 杂志文章,评审

    doi:10.2174/1389200211314030004

    authors: Chiarella P,Fazio VM,Signori E

    更新日期:2013-03-01 00:00:00

  • Comparison of Bromhexine and its Active Metabolite - Ambroxol as Potential Analgesics Reducing Oxaliplatin-induced Neuropathic Pain - Pharmacodynamic and Molecular Docking Studies.

    abstract:BACKGROUND:Painful peripheral neuropathy is a dose-limiting adverse effect of the antitumor drug oxaliplatin. The main symptoms of neuropathy: tactile allodynia and cold hyperalgesia, appear in more than 80% of patients on oxaliplatin therapy and are due to the overexpression of neuronal sodium channels (Navs) and neur...

    journal_title:Current drug metabolism

    pub_type: 杂志文章

    doi:10.2174/1389200221666200711155632

    authors: Furgała-Wojas A,Kowalska M,Nowaczyk A,Fijałkowski Ł,Sałat K

    更新日期:2020-01-01 00:00:00

  • Pharmacokinetics and pharmacodynamics of endoperoxide antimalarials.

    abstract::There are several clinically useful endoperoxides, mainly artemisinin derivatives available in market for the treatment of malaria. These are highly potent drugs, with fastest parasite reduction ratio, broadest parasite stage specificity and effectiveness against all species of plasmodium in human. Endoperoxides are c...

    journal_title:Current drug metabolism

    pub_type: 杂志文章,评审

    doi:10.2174/138920009787846323

    authors: Gautam A,Ahmed T,Batra V,Paliwal J

    更新日期:2009-03-01 00:00:00

  • Review of and perspectives on the toxicology of graphene-based materials.

    abstract::Graphene possesses a wide range of potential biomedical applications because of the unique physical and chemical properties. However, the side effects of grapheme and its derivatives on a number of biological models even on human body are still not very clear. Therefore, to properly assess the potential risk of graphe...

    journal_title:Current drug metabolism

    pub_type: 杂志文章,评审

    doi:10.2174/138920021131400108

    authors: Xu C,Wang J,Xu Y,Shang G,Wang R,Lin Y

    更新日期:2013-10-01 00:00:00

  • Age-related changes in pharmacokinetics.

    abstract::Ageing is characterized by a progressive decline in the functional reserve of multiple organs and systems, which can influence drug disposition. In addition, comorbidity and polypharmacy are highly prevalent in the elderly. As ageing is associated with some reduction in first-pass metabolism, bioavailability of a few ...

    journal_title:Current drug metabolism

    pub_type: 杂志文章,评审

    doi:10.2174/138920011796504527

    authors: Shi S,Klotz U

    更新日期:2011-09-01 00:00:00

  • Heterotropic cooperativity in oxidation mediated by cytochrome p450.

    abstract::Cytochrome P450s (P450 or CYPs) comprise a superfamily of enzymes that catalyze the oxidation of a wide variety of xenobiotic chemicals. Although most of P450 inhibitors decrease the metabolic activities mediated by the corresponding P450 forms, unexpected phenomena, which are called as activation or heterotropic coop...

    journal_title:Current drug metabolism

    pub_type: 杂志文章,评审

    doi:10.2174/138920008784746364

    authors: Niwa T,Murayama N,Yamazaki H

    更新日期:2008-06-01 00:00:00

  • Total Sleep Duration and Risk of Type 2 Diabetes: Evidence-Based On Clinical and Epidemiological Studies.

    abstract:BACKGROUND:Increasing incidences of type 2 diabetes make it necessary to have a better understanding of the risk factors for its prediction. Taking a note of resilience in risk factors, dynamics of the emerging factors other than traditional ones are showing a great interest in recent years which imprints a significant...

    journal_title:Current drug metabolism

    pub_type: 杂志文章,评审

    doi:10.2174/1389200219666180628170431

    authors: Yadav D,Cho KH

    更新日期:2018-01-01 00:00:00

  • LC/MS based tools and strategies on qualitative and quantitative analysis of herbal components in complex matrixes.

    abstract::Accompanying with hot discussions on developing multi-target drugs for the therapy of multi-gene diseases, herbal medicines are receiving more and more attention worldwide in both academic and industrial fields. Pharmacokinetic and metabolic research is one of the important issues for intensive understanding of therap...

    journal_title:Current drug metabolism

    pub_type: 杂志文章,评审

    doi:10.2174/138920012803341285

    authors: Wu L,Hao H,Wang G

    更新日期:2012-11-01 00:00:00

  • Drug-induced Cholestasis: Mechanisms, Models, and Markers.

    abstract:BACKGROUND:Drug-induced cholestasis is a risk factor in the progression of drug candidates, and poses a serious health hazard if not detected before going into a human. Intrahepatic accumulation of Bile Acids (BAs) represents a characteristic phenomenon associated with drug-induced cholestasis. METHODS:This review wil...

    journal_title:Current drug metabolism

    pub_type: 杂志文章,评审

    doi:10.2174/1389200219666180427165035

    authors: Chatterjee S,Annaert P

    更新日期:2018-01-01 00:00:00

  • Prediction of human drug metabolizing enzyme induction.

    abstract::New chemical entities are routinely screened in vitro and in vivo for their ability to induce cytochrome P450s (CYP), other drug-metabolizing enzymes and possibly transporters in an attempt to more accurately predict clinical parameters such as drug-drug interactions and clearance in humans. Some of these potential th...

    journal_title:Current drug metabolism

    pub_type: 杂志文章,评审

    doi:10.2174/1389200033489352

    authors: Mankowski DC,Ekins S

    更新日期:2003-10-01 00:00:00