Delving into the Latest Updates on Cizolirtine Citrate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

+ [2]

Target

CGRP

Mechanism

CGRP antagonists(Calcitonin gene-related peptide antagonists)

Therapeutic Areas

Nervous System DiseasesUrogenital Diseases

Active Indication-

Inactive Indication

PainUrinary Bladder, OveractiveUrinary Incontinence+ [1]

Originator Organization

Esteve Pharmaceuticals S.A.

Active Organization-

Inactive Organization

Esteve Pharmaceuticals S.A.

Drug Highest PhaseDiscontinuedPhase 3

First Approval Date-

Regulation-

Structure

Molecular FormulaC21H29N3O8

InChIKeyJLKUMSHHQYQLSG-UHFFFAOYSA-N

CAS Registry251375-82-3

View All Structures (2)

A 12-week multicentre, randomised, double-blind, parallel group, Phase IIpilot study to evaluate the efficacy and safety of cizolirtine citrate 200 mgbid (400 mg/d), cizolirtine citrate 300 mg bid (600 mg/d) and cizolirtinecitrate 400 mg bid (800 mg/d) versus placebo in the treatment of patientswith Stress Urinary Incontinence (SUI)

Start Date20 Oct 2005

Sponsor / Collaborator-

EUCTR2004-001119-69-CZ / Unknown statusNot Applicable

An evaluation of the dose-response relationship of Cizolirtine citrate 300 mg, twice daily, and 400 mg, twice daily, versus placebo in subjects with urge urinary incontinence.A 12-week, randomised, double-blind, placebo-controlled, multicentre study, parallel-group, Phase III clinical study with a 12 months safety follow-up period.

Start Date03 Nov 2004

Sponsor / Collaborator-

100 Clinical Results associated with Cizolirtine Citrate

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100 Translational Medicine associated with Cizolirtine Citrate

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100 Patents (Medical) associated with Cizolirtine Citrate

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28

Literatures (Medical) associated with Cizolirtine Citrate

01 Jul 2022·Regulatory Toxicology and PharmacologyQ4 · MEDICINE

Results from two-year rodent oral carcinogenicity studies of cizolirtine, a substance-P and calcitonin gene-related peptide release modulator

Q4 · MEDICINE

Article

Author: Guzmán, Antonio ; Vila, Cristina ; Encina, Gregorio ; Marín, Ana-Paz ; Tortajada, Araceli

Cizolirtine is a substance-P and calcitonin gene-related peptide release modulator developed for the treatment of pain and urinary incontinence. To assess its carcinogenic potential, cizolirtine was administered by oral route once daily for up to 104 weeks to CD-1 mice at doses of 40, 90, or 200 mg/kg/day, and to Han Wistar rats at doses of 40, 90 or 200 mg/kg/day to males and 40, 110 or 160 mg/kg/day to females. There were treatment-related neoplastic findings both in mice and rats. In mice, administration of cizolirtine was associated to an increase in skin fibrosarcomas and sarcomas among high-dose males, considered secondary to increased aggression and specific to the animal model. In rats, there was an increased incidence of liver adenomas in males and females, and carcinomas in males, in association with an increased incidence of hepatocyte hypertrophy, vacuolation and clear cell foci, and considered related to sustained long-term enzyme induction resulting in increased liver metabolism and associated hypertrophic changes. The observed neoplastic findings in mouse skin and rat liver after life-time oral administration of cizolirtine are considered related to rodent-specific non-genotoxic mechanisms of questionable relevance to man.

03 Apr 2022·Cutaneous and Ocular Toxicology

Ocular adverse effects of bladder medication: a systematic review

Review

Author: Chifor, Anthony ; Bassi, Arshpreet ; Malvankar-Mehta, Monali S. ; Pur, Daiana Roxana

BACKGROUNDWith the ageing population, lower urinary tract symptoms are becoming more prevalent with an estimate that by 2025, 52 million adults in the USA will be affected. After lifestyle modifications fail to resolve symptoms, second-line therapy with medications is often recommended by both the European Association of Urology and the American Urological Association. Considering the vulnerability of older patients to co-morbidities, physicians must be more aware of adverse side effects. This study aims to identify a linkage between common overactive bladder and interstitial cystitis medication and adverse ocular symptoms.METHODSA comprehensive literature search was conducted in MEDLINE, EMBASE, CINAHL, PsycInfo, and HealthSTAR alongside a grey literature search in clinicaltrials.gov to include all articles relating to bladder medication and vision-threatening loss. Covidence review software was utilised to conduct the systematic review.RESULTSIn total, 222 articles were screened, and 23 articles met the inclusion criteria. Comprehensive coverage of 10 available medications was analysed. All medications reported adverse vision effects stratified over 15 categories. The most common adverse effect was reported to be blurred vision (n = 12 studies). Mirabegron had the most number of adverse types of ocular symptoms that covered 6 categories. Cizolirthine Citrate and Elocatitol had the least amount of ocular side effects reported. From the total of 8459 patients that were treated for either overactive bladder syndrome or interstitial cystitis with oral medications, 422 reported adverse vision effects.CONCLUSIONSThis review suggests that ocular safety should be assessed in patients requiring systematic drug therapy in order to guide future research, focussing on long-term tolerability.

01 Jun 2021·Regulatory Toxicology and PharmacologyQ4 · MEDICINE

Twenty six-week repeat dose oral rat toxicity study of cizolirtine, a substance-P and calcitonin gene-related peptide release modulator

Q4 · MEDICINE

Article

Author: Vila, Cristina ; Tortajada, Araceli ; Guzmán, Antonio ; Marín, Ana-Paz ; Encina, Gregorio ; Fernández de Henestrosa, Antonio R

Cizolirtine, a substance-P and calcitonin gene-related peptide release modulator developed for the treatment of pain and urinary incontinence, was orally administered for 26-weeks to rats at dosages of 20, 60 and 200 mg/kg/day. Clinical signs were limited to post-dosing salivation and brown staining on head and muzzle. There were slight decreases in bodyweight gain and slight increases in water consumption among cizolirtine-treated animals. Slight increases in plasma alkaline phosphatase activity, and cholesterol and phospholipid concentrations were observed in mid- and/or high-dose animals. Low urinary volume, pH and sodium and potassium outputs were observed after 12-weeks, and low urinary pH, low sodium and high potassium outputs at end of treatment. Increased relative (to bodyweight) liver weight was observed in high-dose animals. Treated males and high-dose females showed a dose-related increase in the incidence and severity of periacinar hepatocytic hypertrophy and midzonal/periacinar hepatocytic fat vacuolization. Increased incidences of hepatic clear cell foci were observed in all cizolirtine-treated male groups and, to a lesser extent, in treated females. Ovaries of treated females showed a dose-dependent increased incidence of absent corpora lutea and, occasionally, follicular cysts. The dosages of 20 and 60 mg/kg/day were considered as the No-Observed-Adverse-Effect Levels for males and females, respectively.

100 Deals associated with Cizolirtine Citrate

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Pain	Phase 3	-	Esteve Pharmaceuticals S.A.	-
Urinary Bladder, Overactive	Phase 3	-	Esteve Pharmaceuticals S.A.	-
Urinary Bladder, Overactive	Phase 3	-	Esteve Pharmaceuticals S.A.	-
Urinary Incontinence	Phase 3	-	Esteve Pharmaceuticals S.A.	-
Urinary Incontinence	Phase 3	-	Esteve Pharmaceuticals S.A.	-
Urinary Incontinence, Stress	Phase 3	-	-	-
Pain	Discovery	-	Esteve Pharmaceuticals S.A.	-