Delving into the Latest Updates on Afacifenacin Fumarate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Afacifenacin

Target

ENaC x mAChRs

Action

modulators, antagonists

Mechanism

ENaC modulators(Epithelial sodium channel modulators), mAChRs antagonists(Muscarinic acetylcholine receptor antagonists)

Therapeutic Areas

Other Diseases

Active Indication

Nocturia

Inactive Indication

Overactive bladder syndromeUrinary Bladder, Overactive

Originator Organization

Sumitomo Pharma Co., Ltd.

Active Organization

Sumitomo Pharma Co., Ltd.

Inactive Organization

Sumitomo Pharma America, Inc.Sumitomo Dainippon Pharma America, Inc.

Nippon Shinyaku Co., Ltd.

Drug Highest PhasePhase 2

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC27H26F3N3O2

InChIKeyIJUMFEAYOMCXAQ-VWLOTQADSA-N

CAS Registry877606-63-8

View All Structures (2)

SMP-986 is a compound being developed for the treatment of overactive bladder syndrome (OABS). This clinical study is designed to test the hypothesis that SMP-986 at doses of 20mg, 40mg, 80mg or 120mg provides greater symptom relief in OABS compared to placebo. The hypothesis will be tested by measuring the change in mean voids/24 hrs after treatment with SMP-986 compared to placebo, as well comparing the change in: the severity of urgency episodes, mean number of urgency episodes/24 hr, mean number of incontinence episodes/24 hr and the mean void volume/void between SMP-986 and placebo.

Start Date01 Dec 2006

Sponsor / Collaborator

Sumitomo Pharma America, Inc.

[+5]

100 Clinical Results associated with Afacifenacin Fumarate

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100 Translational Medicine associated with Afacifenacin Fumarate

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100 Patents (Medical) associated with Afacifenacin Fumarate

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3

Literatures (Medical) associated with Afacifenacin Fumarate

01 Jan 2022·Current Therapeutic Research

Drugs Currently Undergoing Preclinical or Clinical Trials for the Treatment of Overactive Bladder: A Review

Review

Author: Joseph, Silvia ; Peedicayil, Jacob ; Maria, Steffi A

BackgroundOveractive bladder (OAB) is a common clinical condition for which current drug treatment comprises drugs blocking the cholinergic nerve supply, or augmenting the adrenergic nerve supply, to the detrusor muscle of the urinary bladder. Current treatments have drawbacks, including lack of efficacy and the development of adverse effects in some patients. Hence, new and better drugs for treating OAB will be clinically useful.ObjectiveThis review is meant to provide information on drugs currently undergoing preclinical or clinical trials for the treatment of OAB published in journal articles or elsewhere.MethodsThe cited articles were retrieved from PubMed and Google Scholar from January 1, 1990, to December 31, 2021. The search terms used were contraction or contractility, detrusor, inhibition, isolated or in vitro, in vivo, overactive bladder, and relaxant effect or relaxation.ResultsThere are 4 classes of new drugs under various stages of development for the treatment of OAB. These are drugs acting on the autonomic nerve supply to the detrusor muscle of the urinary bladder that include the anticholinergics tarafenacin and afacifenacin and the β₃ adrenoceptor agonists solabegron and ritobegron; drugs acting on ion channels in the detrusor muscle (eg, potassium channel openers and calcium channel blockers), drugs acting on cellular enzymes like phosphodiesterase-5 inhibitors and Rho kinase inhibitors, and drugs acting on miscellaneous targets (eg, pregabalin and trimetazidine).ConclusionsDrugs currently used to treat OAB target only the cholinergic and adrenergic cellular signalling pathways. There are many other drugs under trial targeting other cellular pathways that may be useful for treating OAB. Their approval for clinical use might improve the treatment of patients with OAB. (Curr Ther Res Clin Exp. 2022; 83:XXX-XXX).

01 Oct 2014·Expert Opinion on Investigational DrugsQ2 · MEDICINE

Phase II drugs that target cholinergic receptors for the treatment of overactive bladder

Q2 · MEDICINE

Review

Author: Ilias Giarenis ; Martino Maria Zacche ; Linda Cardozo

INTRODUCTIONOveractive bladder (OAB) is a term used to describe the symptom syndrome of urgency, with or without urgency incontinence, usually associated with frequency and nocturia. Antimuscarinics are the most widely prescribed class of drugs for OAB, although their systemic adverse effects limit their use in clinical practice as compliance. This has led to developments in the field.AREAS COVEREDIn this review, the authors describe Phase II drugs that target cholinergic receptors. First, the authors present the new antimuscarinics (tarafenacin and afacifenacin). This is followed by reports on a combination drug (tolenix) containing a muscarinic antagonist (tolterodine) associated with a muscarinic agonist (pilocarpine). Further, the authors discuss the trials of well-known drugs in either new combination therapy (solifenacin and mirabegron) or with new routes of delivery (oxybutynin vaginal ring). Finally, the authors examine the option of targeting nicotinic acetylcholine receptors (dexmecamylamine).EXPERT OPINIONDifferent strategies have been adopted to improve the efficacy and tolerability of therapeutics for OAB. Nicotinic receptors represent a novel therapeutic target; however, it is unlikely that antimuscarinic agents will be replaced as standard first-line therapy in the near future.

BMC Genomics

Identification of antiparasitic drug targets using a multi-omics workflow in the acanthocephalan model

Article

Author: Glaser, Manuel ; Hellmann, Sören Lukas ; Hankeln, Thomas ; Silva Gomes, Ana Lúcia ; Dezfuli, Bahram Sayyaf ; Herlyn, Holger ; Schmidt, Hanno ; Wade, Rebecca C ; Mauer, Katharina ; Butter, Falk

AbstractBackgroundWith the expansion of animal production, parasitic helminths are gaining increasing economic importance. However, application of several established deworming agents can harm treated hosts and environment due to their low specificity. Furthermore, the number of parasite strains showing resistance is growing, while hardly any new anthelminthics are being developed. Here, we present a bioinformatics workflow designed to reduce the time and cost in the development of new strategies against parasites. The workflow includes quantitative transcriptomics and proteomics, 3D structure modeling, binding site prediction, and virtual ligand screening. Its use is demonstrated for Acanthocephala (thorny-headed worms) which are an emerging pest in fish aquaculture. We included three acanthocephalans (Pomphorhynchus laevis, Neoechinorhynchus agilis,Neoechinorhynchus buttnerae) from four fish species (common barbel, European eel, thinlip mullet, tambaqui).ResultsThe workflow led to eleven highly specific candidate targets in acanthocephalans. The candidate targets showed constant and elevated transcript abundances across definitive and accidental hosts, suggestive of constitutive expression and functional importance. Hence, the impairment of the corresponding proteins should enable specific and effective killing of acanthocephalans. Candidate targets were also highly abundant in the acanthocephalan body wall, through which these gutless parasites take up nutrients. Thus, the candidate targets are likely to be accessible to compounds that are orally administered to fish. Virtual ligand screening led to ten compounds, of which five appeared to be especially promising according to ADMET, GHS, and RO5 criteria: tadalafil, pranazepide, piketoprofen, heliomycin, and the nematicide derquantel.ConclusionsThe combination of genomics, transcriptomics, and proteomics led to a broadly applicable procedure for the cost- and time-saving identification of candidate target proteins in parasites. The ligands predicted to bind can now be further evaluated for their suitability in the control of acanthocephalans. The workflow has been deposited at the Galaxy workflow server under the URLtinyurl.com/yx72rda7.

100 Deals associated with Afacifenacin Fumarate

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Nocturia	Phase 2	-	Sumitomo Pharma Co., Ltd.	-
Nocturia	Phase 1	Japan	Nippon Shinyaku Co., Ltd.	-
Urinary Bladder, Overactive	Phase 1	European Union	Sumitomo Pharma Co., Ltd.	-
Urinary Bladder, Overactive	Phase 1	Japan	Sumitomo Pharma Co., Ltd.	-
Overactive bladder syndrome	Preclinical	Spain	Sumitomo Dainippon Pharma America, Inc.	01 Dec 2006
Overactive bladder syndrome	Preclinical	Germany	Sumitomo Dainippon Pharma America, Inc.	01 Dec 2006
Overactive bladder syndrome	Preclinical	Estonia	Sumitomo Pharma America, Inc.	01 Dec 2006
Overactive bladder syndrome	Preclinical	Poland	Sumitomo Pharma America, Inc.	01 Dec 2006
Overactive bladder syndrome	Preclinical	Lithuania	Sumitomo Pharma America, Inc.	01 Dec 2006
Overactive bladder syndrome	Preclinical	France	Sumitomo Dainippon Pharma America, Inc.	01 Dec 2006

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT00409539 (CTgov)	Phase 2	Overactive bladder syndrome	550	Placebo (Placebo)	fkjjghdelm(zpvyucqueg) = cvgtftivgl nuqnznhxlb (jbpbtuhhvy, rbvmyrqbow - rnknavfaph) View more	-	10 Dec 2014
				SMP-986 (20mg Dose of SMP-986)	fkjjghdelm(zpvyucqueg) = lexkfnndfi nuqnznhxlb (jbpbtuhhvy, plbukjfpvr - qxpbxxkpbp) View more