Delving into the Latest Updates on Clemastine Fumarate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

(+)-(2R)-2-(2-(((R)-p-chloro-α-methyl-α-phenylbenzyl)oxy)ethyl)-1-methylpyrrolidine, (+)-(2R)-2-[2-[[(R)-p-chloro-α-methyl-α-phenylbenzyl]oxy]ethyl]-1-methylpyrrolidine, Clemastine

+ [9]

Target

H1 receptor

Mechanism

H1 receptor antagonists(Histamine H1 receptor antagonists)

Therapeutic Areas

Immune System DiseasesInfectious DiseasesEye Diseases+ [3]

Active Indication

Conjunctivitis, AllergicCommon ColdEczema+ [3]

Inactive Indication

Rhinitis, Allergic, Seasonal

Originator Organization

Novartis Pharma AG

Active Organization

NISSIN Pharmaceutical Co., Ltd.

Shandong Keyuan Pharmaceutical Co., Ltd.

Shandong Linuo Pharmaceutical Co. Ltd.

Inactive Organization

Novartis Pharmaceuticals Corp.

NovaDel Pharma, Inc.

Drug Highest PhaseApproved

First Approval Date

JP (17 Jan 1970),

Common ColdEczemaPruritus+ [2]

Regulation-

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Structure

Molecular FormulaC25H30ClNO5

InChIKeyPMGQWSIVQFOFOQ-YKVZVUFRSA-N

CAS Registry14976-57-9

View All Structures (2)

The goal of this study is to find out if the antihistamine, clemastine, can make the white matter in the brain better in older adults with depression. The study will also determine whether this improvement can make antidepressant treatment work better, reduce depressive symptoms, and improve memory and thinking.

Start Date01 Oct 2024

Sponsor / Collaborator

University of Illinois

[+1]

NCT06065670 / Not yet recruitingPhase 1/2IIT

A Randomized, Double-Blind, Delayed Treatment, Placebo-Controlled Trial to Assess the Changes in Multi-parametric MRI in Patients With Acute Demyelinating Lesions Taking Clemastine Fumarate as a Myelin Repair Therapy

The clinical trial is intended to assess for clinical evidence of Clemastine Fumarate as a myelin repair therapy in patients with acute inflammatory injury-causing demyelination as measured by multi-parametric MRI assessments.
No reparative therapies exist for the treatment of acute demyelinating lesions. Clemastine fumarate was identified along with a series of other antimuscarinic medications as a potential remyelinating agent using the micropillar screen (BIMA) developed at the University of California, San Francisco (UCSF). Following in vivo validation, an FDA IND exemption was granted to investigate clemastine for the treatment of multiple sclerosis in the context of chronic optic neuropathy. That pilot study was recently completed and is the first randomized control trial documenting efficacy for a putative remyelinating agent for the treatment of MS. The preselected primary efficacy endpoint (visual evoked potential) was met and a strong trend to benefit was seen for the principal secondary endpoint assessing function (low contrast visual acuity). That trial number was 13-11577.
This study seeks to follow up on that study and examine clemastine fumarate's protective and reparative effects in the context of acute demyelinating brain lesions as imaged by multi-parametric MRI assessments. The investigators will be assessing the effects of clemastine fumarate as a remyelinating therapy and assessing its effect on MRI metrics of lesions found in patients with a confirmed diagnosis of acute inflammatory injury-causing demyelination.
In addition to using conventional multi-parametric MRI assessments, this study will also evaluate a new MRI technique called Ultrashort Echo Time (UTE) MRI to assess the effects of clemastine fumarate as a remyelinating therapy of acute lesions found in patients with a confirmed diagnosis of acute inflammatory injury-causing demyelination and compare it to the other assessments.

Start Date15 Sep 2024

Sponsor / Collaborator

The University of California, San Francisco

NCT06087757 / RecruitingPhase 3IIT

Clemastine Treatment in Individuals With Williams Syndrome- a Double-blind Placebo Control to Assess the Safety and Efficacy

This study explores the neurobiological etiology of Williams syndrome and potential therapeutic targets for associated social, motor, and cognitive abnormalities. The main translational objective will be to test the effectiveness of Clemasntine on neurocognitive and other associated abnormalities in individuals with Williams syndrome.

Start Date01 Apr 2024

Sponsor / Collaborator

Sheba Medical Center

[+1]

100 Clinical Results associated with Clemastine Fumarate

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100 Translational Medicine associated with Clemastine Fumarate

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100 Patents (Medical) associated with Clemastine Fumarate

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489

Literatures (Medical) associated with Clemastine Fumarate

01 Jan 2025·Brain Research

Clemastine enhances exercise-induced motor improvement in hypoxic ischemic rats

Article

Author: Komaki, Yuji ; Iwaki, Sunao ; Tsurugizawa, Tomokazu ; Goto, Taichi ; Takashima, Ichiro ; Kunori, Nobuo

Neonatal hypoxic ischemia (HI) occurs owing to reduced cerebral oxygen levels and perfusion during the perinatal period. Brain injury after HI triggers neurological manifestations such as motor impairment, and the improvement of impaired brain function remains challenging. Recent studies suggest that cortical myelination plays a role in motor learning, but its involvement in motor improvement after HI injury is not well understood. This study aimed to investigate the impact of myelination on motor improvement following neonatal HI injury. We employed a modified Rice-Vannucci model; the right common carotid artery of postnatal day 7 (P7) Wistar rats was isolated and divided, and the rats were then exposed to hypoxic condition (90 min, 8 % O2). A total of 101 rats (66 males) were divided into four groups: trained-HI (n = 38), trained-Sham (n = 16), untrained-HI (n = 31), and untrained-Sham (n = 16). The trained groups underwent rotarod-based exercise training from P22 to P41 (3 days per week). Structural analysis using magnetic resonance imaging and immunohistochemistry (n = 6 per group) revealed increased fractional anisotropy and myelin density in the primary somatosensory cortex of the trained-HI group. We further evaluated the effect of myelination promotion on rotarod performance by administering clemastine, a myelination-promoting drug, via daily intraperitoneal injections. Clemastine did not enhance motor improvement in untrained-HI rats. However, clemastine-administered trained-HI rats (n = 7) exhibited significantly improved motor performance compared to both saline-administered trained-HI rats (n = 11) and clemastine-administered untrained-HI rats (n = 7). These findings suggest that myelination may be a key mechanism in motor improvement after HI injury and that combining exercise training with clemastine administration could be an effective therapeutic strategy for motor improvement following HI injury.

31 Dec 2024·Molecular & Cellular Oncology

Clemastine and hyperthermia enhance sensitization of osteosarcoma cells for apoptosis

Article

Author: He, Yiping ; Kumar, Deepak ; Niture, Suryakant ; Vandana ; Gadi, Sashi ; Hoang, Hieu ; Obu, Somtochukwu

Clemastine is an antagonist of histamine H1 receptor may provide benefits in the treatment of osteosarcoma (OS). In the current study, we used hyperthermia approach to sensitize OS cells to clemastine-mediated cell death. Osteosarcoma U-2 OS and Saos-2 cells were treated with clemastine at 37°C, followed by 42°C for 2 h, and released at 37°C for 6 h. The impact of clemastine and hyperthermia on OS cell survival and autophagy-mediated cell death was investigated. Exposure of U-2 OS and Saos-2 cells to clemastine and hyperthermia (42°C) inhibited dose-dependent clemastine-mediated cell survival by increasing cell apoptosis. Hyperthermia and clemastine exposure modulated inflammatory and unfolded protein response (UPR) signaling differentially in U-2 OS and Saos-2 cells. Exposure of U-2 OS and Saos-2 cells to hyperthermia and clemastine inhibited AKT/mTOR and induced expression of the autophagy biomarkers LC3B II and LC3-positive puncta formation. The inhibition of autophagy by 3-methyladenine blocked hyperthermia and clemastine-mediated induction of LC3B II, LC3-positive puncta formation, and OS cell apoptosis. These results indicate that clemastine and hyperthermia sensitize OS cell lines by inducing increased autophagic cell death. Collectively, our data suggest that hyperthermia along with antihistamine therapy may provide an improved approach for the treatment of OS.

18 Oct 2024·Annals of neurology

Clemastine Induces Oligodendrocyte Progenitor Pool Exhaustion and Senescence in the Context of Chronic Demyelination in a Rabbit Model.

Article

Author: Gadelkarim, Farah ; Buck, Gregory T ; Raymond, Faye D ; Cooper, James J M ; Muthaiah, Rupadevi ; Sim, Fraser J ; Ravichandar, Roopa ; Frost, Jon R

OBJECTIVESClemastine has emerged as a promising therapy for the restoration of neurologic function in patients with multiple sclerosis (MS). However, clemastine and other agents with prodifferentiative effects on oligodendrocyte progenitor cells (OPCs) in rodent models have underperformed in clinical trials. We hypothesized that the preclinical studies showed more robust effects because of the abundance of OPCs in rodent models. To better examine the therapeutic potential of clemastine, we examined its effect on demyelinated white matter lesions in rabbits, which exhibit progenitor densities and limited remyelination more closely matching those found in tissues from patients with MS.METHODSWe used lysolecithin to induce demyelination in white matter of New Zealand rabbits and then administered oral clemastine (10mg/kg/day) for various periods before assessing the OPC and oligodendrocyte (OL) populations in these lesions.RESULTSDaily administration of clemastine for the full study period (56 days) increased oligodendrogenesis in white matter lesions. However, shorter durations of treatment failed to increase overall OL density despite enhancing OPC-to-OL differentiation. This effect was due to exhaustion of the OPC pool, as the differentiating progenitors were not replaced because of reduced OPC proliferation. Notably, delayed administration of clemastine led to an accumulation of activated OPCs expressing markers of senescence.INTERPRETATIONAlthough capable of driving OL differentiation, clemastine treatment in rabbits hampered progenitor pool replenishment, induced senescence, and promoted conversion of microglia/macrophages to a proinflammatory phenotype. Whether these effects would also occur in humans or with other prodifferentiative therapies should be studied further, but our data suggest the need to carefully consider progenitor dynamics in the treatment of MS. ANN NEUROL 2024.

100 Deals associated with Clemastine Fumarate

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External Link

KEGG	Wiki	ATC	Drug Bank
D00666	Clemastine Fumarate	R06AA04 D04AA14	DB00283

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Conjunctivitis, Allergic	CN	Shandong Linuo Pharmaceutical Co. Ltd.	01 Jan 1991
Conjunctivitis, Allergic	CN	Shandong Keyuan Pharmaceutical Co., Ltd.	01 Jan 1991
Common Cold	JP	NISSIN Pharmaceutical Co., Ltd.	17 Jan 1970
Eczema	JP	NISSIN Pharmaceutical Co., Ltd.	17 Jan 1970
Pruritus	JP	NISSIN Pharmaceutical Co., Ltd.	17 Jan 1970
Rhinitis, Allergic	JP	NISSIN Pharmaceutical Co., Ltd.	17 Jan 1970
Urticaria	JP	NISSIN Pharmaceutical Co., Ltd.	17 Jan 1970

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Rhinitis, Allergic, Seasonal	Phase 2	US	NovaDel Pharma, Inc.	-

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT06039137 (H1-Switch Study, Pubmed)	Not Applicable	-	-	Intravenous Clemastine	ehitzsngmd(opmevqdufs) = rwvxvbyluq asjqklfnru (cibmzgespd, -3.4 to 1.1)	Positive	07 Jun 2024
				Oral Cetirizine	ehitzsngmd(opmevqdufs) = umnuwqdtzp asjqklfnru (cibmzgespd, -3.4 to 1.1)
TRAP-MS (ACTRIMS2024)	Not Applicable	Multiple Sclerosis, Chronic Progressive	9	Clemastine Fumarate	rfhhqdlenf(hjwwogetye) = zeyywqrrpn ickzmrhnep (hkegfmjkis )	Negative	29 Feb 2024
NCT02040298 (ReBUILD, CTgov)	Phase 2	Multiple Sclerosis, Relapsing-Remitting	50	Clemastine (Clemastine)	xulgkfqcjc(qqvngoywbz) = adpfpxnmim akzofofxir (trhhkgjwcg, kxvdkzcuvt - esllatoaau) View more	-	15 Jul 2021
				Placebo+clemastine (Placebo)	xulgkfqcjc(qqvngoywbz) = frbjxlkeog akzofofxir (trhhkgjwcg, zpjadbvbwq - sdprruptvf) View more