Delving into the Latest Updates on Imidafenacin with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Imidafenacin (JAN/INN)

+ [9]

Target

M1 receptor x M3 receptor

Action

antagonists

Mechanism

M1 receptor antagonists(Muscarinic acetylcholine receptor M1 antagonists), M3 receptor antagonists(Muscarinic acetylcholine receptor M3 antagonists)

Therapeutic Areas

Urogenital Diseases

Active Indication

Urinary Bladder, OveractivePollakisuriaUrinary Incontinence, Urge

Inactive Indication-

Originator Organization

KYORIN Pharmaceutical Co., Ltd.

Active Organization

R-Pharm Overseas, Inc.

Tianjin Hankang Pharmaceutical Biotechnology Co. Ltd.

Eisai Co., Ltd.

+ [3]

Inactive Organization

R-Pharm JSC

Drug Highest PhaseApproved

First Approval Date

Japan (18 Apr 2007),

Urinary Bladder, Overactive

Regulation-

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Structure/Sequence

Molecular FormulaC20H21N3O

InChIKeySQKXYSGRELMAAU-UHFFFAOYSA-N

CAS Registry170105-16-5

主要目的：在空腹及餐后给药条件下，比较江苏联环药业股份有限公司提供的咪达那新片（规格：0.1 mg）与杏林製薬株式会社生产的咪达那新片（规格：0.1 mg，商品名：Uritos®）在健康成年人群中吸收程度和速度的差异，评价其生物等效性。次要目的：在空腹及餐后给药条件下，评价江苏联环药业股份有限公司提供的咪达那新片（规格：0.1 mg）的安全性。

[Translation]

Main purpose: To compare imidanacin tablets (specification: 0.1 mg) provided by Jiangsu Lihuan Pharmaceutical Co., Ltd. and imidanacin tablets (specification: 0.1 mg) produced by Xinglin Pharmaceutical Co., Ltd. under fasting and postprandial administration conditions. mg, trade name: Uritos®) in healthy adult populations to evaluate its bioequivalence. Secondary purpose: To evaluate the safety of midanacin tablets (specification: 0.1 mg) provided by Jiangsu Lihuan Pharmaceutical Co., Ltd. under fasting and postprandial administration conditions.

Start Date08 Aug 2024

Sponsor / Collaborator

Jiangsu Lianhuan Pharmaceutical Co., Ltd.

ChiCTR2300070562

/ SuspendedNot ApplicableIIT

A randomized, open-label, two-formulation, two-period, crossover study of the bioequivalence of a single oral dose of Imidafenacin tablets in fasted and fed healthy Chinese subjects

Start Date17 Apr 2023

Sponsor / Collaborator-

CTR20202404

/ CompletedNot Applicable

咪达那新片（0.1mg）在中国健康人群中空腹和餐后状态下单次给药的人体生物等效性临床试验

[Translation] A human bioequivalence clinical trial of imidacin tablets (0.1 mg) in Chinese healthy subjects after single administration in fasting and fed state

1. 以杏林制药株式会社生产的咪达那新片（0.1mg，商品名为URITOS）为参比制剂，以南京制药厂有限公司生产的咪达那新片（0.1mg）为受试制剂，通过单中心、随机、开放、单次给药、两制剂、两周期、两序列、交叉设计的临床试验来评价两种制剂在中国健康受试者中空腹和餐后状态下的生物等效性。 2. 观察受试制剂和参比制剂在中国健康受试者中的安全性。

[Translation]

1. Using imidafenacin tablets (0.1 mg, trade name Uritos) produced by Kyorin Pharmaceutical Co., Ltd. as the reference preparation and imidafenacin tablets (0.1 mg) produced by Nanjing Pharmaceutical Factory Co., Ltd. as the test preparation, a single-center, randomized, open, single-dose, two-preparation, two-cycle, two-sequence, crossover clinical trial was conducted to evaluate the bioequivalence of the two preparations in fasting and fed states in healthy Chinese subjects. 2. Observe the safety of the test preparation and the reference preparation in healthy Chinese subjects.

Start Date03 Dec 2020

Sponsor / Collaborator

Nanjing Pharmaceutical Factory

100 Clinical Results associated with Imidafenacin

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100 Translational Medicine associated with Imidafenacin

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100 Patents (Medical) associated with Imidafenacin

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158

Literatures (Medical) associated with Imidafenacin

01 Jun 2024·Journal of Inclusion Phenomena and Macrocyclic Chemistry

Predictors for symptom improvement in overactive bladder patients treated with imidafenacin

Author: Kim, Hyeon Woo ; Seong, Wooseop ; Kim, Tae Nam ; Lee, Jeong Zoo ; Shin, Dong Gil ; Kim, Seunghyeon ; Park, Yangkyu ; Jang, Kyoungha

The objective of this investigation is to ascertain the determinants associated with the amelioration of symptoms in female patients suffering from overactive bladder (OAB) following treatment with 0.2 mg of imidafenacin.The study included 66 female OAB patients who had been prescribed a daily dose of 0.2 mg imidafenacin for a min. of 3 mo, spanning from March 2018 to June 2020.Various clin. parameters including age, coexistence of addnl. voiding symptoms, prior history of urol. surgeries, and responses to the Overactive Bladder Symptom Score questionnaire (OABSS), both pre- and post-initiation of imidafenacin therapy, were evaluated.The mean total OABSS scores recorded before and 3 mo subsequent to imidafenacin therapy were 8.36 ± 3.65 and 5.15 ± 3.22, resp.Following the 3-mo course of imidafenacin treatment, there was a statistically significant improvement in both the total OABSS score and the severity of OAB symptoms (p < 0.001 for both).Prior to treatment initiation, Group B (n = 38) exhibited significantly higher total OABSS scores and subscores compared to Group A (n = 28) (p < 0.05).Multivariable anal. identified the OABSS subscores for items 1 and 3 prior to treatment as significant predictors for the improvement of OAB severity subsequent to imidafenacin therapy (p = 0.046, OR 3.10, 95% CI 1.019-9.440 and p < 0.001, OR 2.77, 95% CI 1.671-4.587, resp.).Consequently, imidafenacin emerges as an efficacious therapeutic agent for alleviating OAB severity in female patients, with the OABSS subscores for items 1 and 3 prior to treatment initiation holding potential utility in predicting the efficacy of imidafenacin in managing OAB.

01 Jun 2024·Drug Metabolism and Pharmacokinetics

Predicting muscarinic receptor occupancy in human bladder mucosa from urinary concentrations of antimuscarinic agents for overactive bladder

Article

Author: Okura, Takashi ; Shiho, Mizuki ; Yamada, Shizuo ; Tanaka, Shimako ; Akashita, Gaku ; Nakatani, Eriko

To assess the pharmacologically relevant and selective muscarinic receptor occupancy in the bladder mucosa, we considered not only plasma drug concentrations but also urinary drug concentrations. The purpose of this study was to predict muscarinic receptor occupancy in the human bladder mucosa based on urinary concentrations in response to clinical dosages of antimuscarinic agents used to treat overactive bladder. The calculated mean plasma or serum unbound steady state concentrations were 0.06-11 nM in clinical dosages of five antimuscarinic agents. Urinary concentrations calculated from the mean plasma or serum and renal clearance ranged between 19 nM and 2 μM, which were >10-fold higher than the K_i values for bladder muscarinic receptors excluding propiverine. Bladder mucosal muscarinic receptor occupancy estimated from the urinary concentrations and the K_i values was >90 % at a steady state in clinical dosages of five antimuscarinic agents. The bladder muscarinic receptor occupancy was higher than that in the parotid gland calculated based on the mean plasma or serum unbound concentrations and K_i values for muscarinic receptors in the parotid gland. These results suggest that sufficient and selective muscarinic receptor occupancy by antimuscarinic agents, to exert pharmacological effects, in the bladder mucosa can be predicted using urinary concentrations.

19 Apr 2024·ACS Chemical Biology

Characterization of Chemical Interactions between Clinical Drugs and the Oral Bacterium, Corynebacterium matruchotii, via Bioactivity-HiTES

Article

Author: Park, Sehwan ; Kim, Ki Hyun ; Song, Jeongwon ; Lee, Da Yeong ; Lee, Gyu Sung ; Lee, Bum Soo ; Kim, Jonghwan ; Lee, Seoung Rak ; Kim, Chung Sub

In the field of natural product research, the rediscovery of already-known compounds is one of the significant issues hindering new drug development. Recently, an innovative approach called bioactivity-HiTES has been developed to overcome this limitation, and several new bioactive metabolites have been successfully characterized by this method. In this study, we applied bioactivity-HiTES to Corynebacterium matruchotii, the human oral bacterium, with 3120 clinical drugs as potential elicitors. As a result, we identified two cryptic metabolites, methylindole-3-acetate (MIAA) and indole-3-acetic acid (IAA), elicited by imidafenacin, a urinary antispasmodic drug approved by the Japanese Pharmaceuticals and Medical Devices Agency (PMDA). MIAA showed weak antibacterial activity against a pulmonary disease-causing Mycobacterium conceptionense with an IC₅₀ value of 185.7 μM. Unexpectedly, we also found that C. matruchotii metabolized fludarabine phosphate, a USFDA-approved anticancer drug, to 2-fluoroadenine which displayed moderate antibacterial activity against both Bacillus subtilis and Escherichia coli, with IC₅₀ values of 8.9 and 20.1 μM, respectively. Finally, acelarin, a prodrug of the anticancer drug gemcitabine, was found to exhibit unreported antibacterial activity against B. subtilis with an IC₅₀ value of 33.6 μM through the bioactivity-HiTES method as well. These results indicate that bioactivity-HiTES can also be applied to discover biotransformed products in addition to finding cryptic metabolites in microbes.

100 Deals associated with Imidafenacin

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External Link

KEGG	Wiki	ATC	Drug Bank
D06273	Imidafenacin	G04BD	DB09262

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Urinary Bladder, Overactive	Japan	KYORIN Pharmaceutical Co., Ltd.	18 Apr 2007
Urinary Bladder, Overactive	Japan	Ono Pharmaceutical Co., Ltd.	18 Apr 2007

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Pollakisuria	NDA/BLA	Russia	R-Pharm Overseas, Inc.	30 Jan 2022
Urinary Incontinence, Urge	Phase 1	China	Tianjin Hankang Pharmaceutical Biotechnology Co. Ltd.	17 Jun 2015
Urinary Bladder, Overactive	Discovery	-	Ono Pharmaceutical Co., Ltd.	01 Oct 2003

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT03575702 (Pubmed) Manual	Phase 3	Urinary Bladder, Overactive	300	imidafenacin	(agrcnoznjr) = kpqbcwgtrz dewlhgbojp (qouoeodxkb, 2.2) View more	Non-inferior	01 Jun 2019
				tolterodine	(agrcnoznjr) = rqefqmtlmn dewlhgbojp (qouoeodxkb, 1.8) View more
NCT03575702 (CTgov)	Phase 3	Urinary Bladder, Overactive	300	Uritos® (Uritos®)	eiowdafver(qtnlhmemyt) = dcakxfqcxf mxfnlafixq (umpqoouqvw, xjumhlcdwv - yoepoyykpv) View more	-	21 May 2019
				Urotol® (Urotol®)	eiowdafver(qtnlhmemyt) = aftlsuczlp mxfnlafixq (umpqoouqvw, drybvwpobe - xxxktddvlk) View more
NCT02294396 (CTgov)	Phase 4	Urinary Bladder, Overactive	649	Mirabegron tablet+Solifenacin tablet (Mirabegron + Solifenacin)	qklmfptkne(uzwlwkvrmf) = zuvccifoxb vqinnupdte (adqugcynax, dojsqfxtiv - cgoobufpjs) View more	-	24 Dec 2018
				Mirabegron tablet+Propiverine tablet (Mirabegron + Propiverine)	qklmfptkne(uzwlwkvrmf) = bgjrjfobri vqinnupdte (adqugcynax, qhddwvkppz - wltavtybxm) View more
ADDITION STUDY (Pubmed \| Urology)	Not Applicable	Prostatic Hyperplasia \| Overactive bladder syndrome Add-on	308	Tamsulosin + Imidafenacin	ayofdgcrch(bevsniqwyu) = paxgnewpkr afuzupidfo (xbdquysjwf, 1.47 - 2.74) View more	Positive	01 Oct 2013