Delving into the Latest Updates on Ebastine with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Bactil, Bromselon, Ebastine (JP17/USAN/INN)

+ [20]

Target

H1 receptor

Mechanism

H1 receptor antagonists(Histamine H1 receptor antagonists)

Therapeutic Areas

Immune System DiseasesInfectious DiseasesEye Diseases+ [3]

Active Indication

Conjunctivitis, AllergicDermatitisEczema+ [5]

Inactive Indication-

Originator Organization

Almirall SA

Active Organization

Almirall SA

Sanofi

Sumitomo Pharma Co., Ltd.

Inactive Organization

Hoechst Pakistan Ltd.

Drug Highest PhaseApproved

First Approval Date

ES (01 Jan 1990),

Chronic UrticariaRhinitis, Allergic

Regulation-

Login to view timeline

Structure/Sequence

Molecular FormulaC32H39NO2

InChIKeyMJJALKDDGIKVBE-UHFFFAOYSA-N

CAS Registry90729-43-4

This is an open-label phase I/II study evaluating the addition of ebastine to docetaxel in the treatment for metastatic castration resistant prostate cancer.
Patients will be randomized in a 2:1 fashion to receive ebastine daily during and after treatment with a maximum of 10 courses of docetaxel.
The primary endpoint is change in the profile of urinary and blood lipids to indicate absorption and possible efficacy of ebastine.
Secondary endpoints include PSA response and radiologic progression free survival.

Start Date20 Jun 2024

Sponsor / Collaborator

Rigshospitalet

[+1]

CTR20234125

/ CompletedNot Applicable

依巴斯汀片人体生物等效性研究

[Translation] Study on the bioequivalence of Ebastine tablets in human body

采用单中心、随机、开放、两周期、单剂量、空腹及餐后给药设计，比较北京四环科宝制药股份有限公司提供的依巴斯汀片（规格：10 mg）与ALMIRALL,S.A.持证的原研进口药品依巴斯汀片（商品名：开思亭®/Kestine®，规格：10 mg）在健康人群中吸收程度和速度的差异。

[Translation]

A single-center, randomized, open, two-period, single-dose, fasting and postprandial administration design was used to compare the differences in absorption extent and speed between Ebastine Tablets (10 mg) provided by Beijing Sihuan Kebao Pharmaceutical Co., Ltd. and Ebastine Tablets (Kestine®, 10 mg), an original imported drug licensed by ALMIRALL, S.A., in healthy people.

Start Date13 Jan 2024

Sponsor / Collaborator

Beijing Sihuan Kebao Pharmaceutical Co., Ltd.

100 Clinical Results associated with Ebastine

Login to view more data

100 Translational Medicine associated with Ebastine

Login to view more data

100 Patents (Medical) associated with Ebastine

Login to view more data

351

Literatures (Medical) associated with Ebastine

01 Jan 2025·International Journal of Biological Sciences

S6K1 is a Targetable Vulnerability in Tumors Exhibiting Plasticity and Therapy Resistance

Article

Author: Ganguly, Saptadwipa ; Jiang, Jieyun ; Orren, David ; Burikhanov, Ravshan ; D'Orazio, John ; Rao, Mahadev ; Goellner, Eva M ; Watt, David S ; Sviripa, Vitaliy M ; Spielmann, Peter H ; Zhan, Chang-Guo ; Brainson, Christine F ; Ellingson, Sally ; Shenoy, Gautham G ; Rangnekar, Vivek M ; Gosser, Christian M

Background: Most tumors initially respond to treatment, yet refractory clones subsequently develop owing to resistance mechanisms associated with cancer cell plasticity and heterogeneity. Methods: We used a chemical biology approach to identify protein targets in cancer cells exhibiting diverse driver mutations and representing models of tumor lineage plasticity and therapy resistance. An unbiased screen of a drug library was performed against cancer cells followed by synthesis of chemical analogs of the most effective drug. The cancer subtype target range of the leading drug was determined by PRISM analysis of over 900 cancer cell lines at the Broad Institute, MA. RNA-sequencing and enrichment analysis of differentially expressed genes, as well as computational molecular modeling and pull-down with biotinylated small molecules were used to identify and validate RPS6KB1 (p70S6K or S6K1) as an essential target. Genetic restoration was used to test the functional role of S6K1 in cell culture and xenograft models. Results: We identified a novel derivative of the antihistamine drug ebastine, designated Super-ebastine (Super-EBS), that inhibited the viability of cancer cells representing diverse KRAS and EGFR driver mutations and models of plasticity and treatment resistance. Interestingly, PRISM analysis indicated that over 95% of the diverse cancer cell lines tested were sensitive to Super-EBS and the predicted target was the serine/threonine kinase S6K1. S6K1 is upregulated in various cancers relative to counterpart normal/benign tissues and phosphorylated-S6K1 predicts poor prognosis for cancer patients. We noted that inhibition of S6K1 phosphorylation was necessary for tumor cell growth inhibition, and restoration of phospho-S6K1 rendered tumor cells resistant to Super-EBS. Inhibition of S6K1 phosphorylation by Super-EBS induced caspase-2 dependent apoptosis via inhibition of the Cdc42/Rac-1/p-PAK1 pathway that led to actin depolymerization and caspase-2 activation. The essential role of S6K1 in the action of Super-EBS was recapitulated in xenografts, and knockout of S6K1 abrogated tumor growth in mice. Conclusion: S6K1 is a therapeutic vulnerability in tumors exhibiting intrinsic and/or acquired resistance to treatment.

01 Jan 2025·Clinical and Translational Allergy

Prednisolone versus antihistamine for allergic rhinitis: No significant difference found in randomized trial

Article

Author: Bjermer, Leif ; Karlsson, Agneta ; Hellkvist, Laila ; Sahlstrand‐Johnsson, Pernilla ; Westin, Ulla ; Hansson, Kerstin ; Skröder, Carl ; Cardell, Lars Olaf ; Dahl, Åslög

AbstractBackgroundSeasonal allergic rhinitis (AR) impacts public health by affecting work productivity and quality of life. The Swedish tree pollen season starts in February with alder and hazel pollination, followed by birch and ends with oak in May. Systemic corticosteroids are often prescribed when topical treatments fail, despite limited evidence supporting their efficacy.ObjectiveTo compare the effectiveness of prednisolone tablets versus antihistamine tablets in reducing symptoms and medication usage in patients with moderate to severe tree pollen‐induced AR.MethodsThis interventional single‐center, double‐blinded randomized trial included 34 patients. Treatment was initiated, and symptoms were registered during the tree pollen season. The two groups received either prednisolone tablets (20 mg) or ebastine tablets (20 mg) for 7 days. Treatment effects were evaluated by comparing daily symptom scores, use of topical medication, and a combined symptom‐medical score between the groups. Quality of life was recorded at the start and after 3 weeks.ResultsBoth interventions demonstrated efficacy in enhancing quality of life metrics. The area under the curve (AUC) for the combined symptom severity and medication usage score averaged 34.0 (SD = 19.1, 95% CI = 24.5–43.4) in the group treated with prednisolone. This was marginally lower than the control group, with an AUC of 32.6 (SD = 13.2, 95% CI = 25.6–39.7). The difference was not statistically significant (p = 0.80). Both groups exhibited only mild adverse events, which were statistically comparable in frequency and severity.ConclusionsPrednisolone tablets did not show superior efficacy over antihistamine tablets in reducing symptoms or medication usage in tree pollen‐induced AR. These results suggest that systemic corticosteroids may not provide additional benefits over antihistamines, and clinicians should prioritize individualized treatment based on patient preferences and tolerability.

01 Dec 2024·Computational and Structural Biotechnology Journal

Acidic sphingomyelinase interactions with lysosomal membranes and cation amphiphilic drugs: A molecular dynamics investigation

Article

Author: Papaleo, Elena ; Favaro, Lorenzo ; Maeda, Kenji ; Lambrughi, Matteo ; Scrima, Simone ; Jäättelä, Marja

Lysosomes are pivotal in cellular functions and disease, influencing cancer progression and therapy resistance with Acid Sphingomyelinase (ASM) governing their membrane integrity. Moreover, cation amphiphilic drugs (CADs) are known as ASM inhibitors and have anti-cancer activity, but the structural mechanisms of their interactions with the lysosomal membrane and ASM are poorly explored. Our study, leveraging all-atom explicit solvent molecular dynamics simulations, delves into the interaction of glycosylated ASM with the lysosomal membrane and the effects of CAD representatives, i.e., ebastine, hydroxyebastine and loratadine, on the membrane and ASM. Our results confirm the ASM association to the membrane through the saposin domain, previously only shown with coarse-grained models. Furthermore, we elucidated the role of specific residues and ASM-induced membrane curvature in lipid recruitment and orientation. CADs also interfere with the association of ASM with the membrane at the level of a loop in the catalytic domain engaging in membrane interactions. Our computational approach, applicable to various CADs or membrane compositions, provides insights into ASM and CAD interaction with the membrane, offering a valuable tool for future studies.

100 Deals associated with Ebastine

Login to view more data

External Link

KEGG	Wiki	ATC	Drug Bank
D01478	Ebastine	R06AX22	DB11742

R&D Status

Approved

10 top approved records.

Login

to view more data

Indication	Country/Location	Organization	Date
Conjunctivitis, Allergic	CN	-	16 May 2000
Dermatitis	JP	Sumitomo Pharma Co., Ltd.	16 Apr 1996
Eczema	JP	Sumitomo Pharma Co., Ltd.	16 Apr 1996
Prurigo	JP	Sumitomo Pharma Co., Ltd.	16 Apr 1996
Pruritus	JP	Sumitomo Pharma Co., Ltd.	16 Apr 1996
Urticaria	JP	Sumitomo Pharma Co., Ltd.	16 Apr 1996
Chronic Urticaria	ES	-	01 Jan 1990
Rhinitis, Allergic	ES	-	01 Jan 1990

Developing

10 top R&D records.

Login

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Rhinitis, Allergic	Preclinical	US	Hoechst Pakistan Ltd.	-

Login to view more data

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ASCO2009	Not Applicable	Metastatic breast cancer	1,411	ESAs	njxvrnloxr(llzvgpguda) = nonpljdcjc izphxsedby (nmbyfpigku ) View more	-	20 May 2009
				No ESAs	njxvrnloxr(llzvgpguda) = zjsooddxxk izphxsedby (nmbyfpigku ) View more