Delving into the Latest Updates on Golotimod with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Gamma-D-glutamyl-L-tryptophan, Golotimod (USAN/INN)

Target

STAT3

Mechanism

STAT3 inhibitors(Signal transducer and activator of transcription 3 inhibitors)

Therapeutic Areas

Infectious DiseasesDigestive System DisordersMouth and Tooth Diseases

Active Indication

TuberculosisHepatitis CMucositis

Inactive Indication

AsthmaChronic hepatitis C genotype 1Head and Neck Neoplasms+ [3]

Originator Organization

Verta, Inc.

Active Organization

Verta, Inc.

Inactive Organization

SciClone Pharmaceuticals LLC

Drug Highest PhaseApproved

First Approval Date

RU (01 Jan 2009),

Hepatitis CMucositis

Regulation-

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Structure

Molecular FormulaC16H19N3O5

InChIKeyCATMPQFFVNKDEY-YPMHNXCESA-N

CAS Registry229305-39-9

This is a phase 2b, double-blind, placebo-controlled, 4-arm, adaptive-design trial, initially stratified by cisplatin regimen, and then randomized 1:1:1:1. The study will be conducted in subjects receiving ChemoRT for the treatment of squamous cell carcinomas (SCCs) of the oral cavity, oropharynx, hypopharynx, or larynx. The study includes a treatment period of approximately 7 weeks, depending on the subject's prescribed radiation plan, and Week 1 and Week 4 post RT follow-up visits. It also includes a longer follow-up period of approximately 12 months to determine if there is an effect of SCV 07 on the tumor response to ChemoRT.

Start Date01 Dec 2010

Sponsor / Collaborator

SciClone Pharmaceuticals LLC

NCT01310205 / CompletedNot Applicable

An Extension of Study SCI-SCV-HCV-P2-001: Long-Term FU in Subj Who Opt for Retreatment With Pegylated Interferon and Ribavirin After Completing Treatment in a Phase 2 Study and Have Relapsed After at Least 44 Weeks Tx With Peg-IFN and RBV.

This is an extension of ongoing study SCI-SCV-HCV-P2-001 in which subjects will be invited to participate in this extension study if they complete treatment in study SCI-SCV-HCV-P2-001 and are eligible for retreatment with peg-IFN and RBV.

Start Date01 Aug 2010

Sponsor / Collaborator

SciClone Pharmaceuticals LLC

NCT00968357 / CompletedPhase 2

A Phase 2, Multicenter, Multidose, Open-Label Study to Evaluate the Safety and Immunomodulatory Effects of SCV-07 as Monotherapy or in Combination With Ribavirin in Noncirrhotic Subjects With Genotype 1 Chronic Hepatitis C Who Have Relapsed After a Response to a Course of at Least 44 Weeks Treatment With Pegylated Interferon and Ribavirin

SCV-07 (γ-D-glutamyl-L-tryptophan) is a new immunomodulatory compound that has been developed and patented both for composition and immunomodulatory use and is a synthetic dipeptide. The efficacy of SCV 07 in treating chronic hepatitis C virus (HCV) infection is expected to arise from the drug's ability to stimulate the T-helper 1 (Th1) type immune response and to block signal transducers and activator of transcription 3 (STAT3) mediated signaling. The purpose of this study is to determine if SCV-07 alone and/or SCV-07 in combination with ribavirin is safe and potentially effective for the treatment of genotype 1 compensated chronic hepatitis C in subjects who have relapsed after a response to a previous treatment course of at least 44 weeks with pegylated interferon and ribavirin. All subjects will receive 4 weeks of SCV-07 (Lead-in Phase), followed by 4 weeks of treatment with SCV-07 in combination with ribavirin (Combination Treatment).

Start Date01 Sep 2009

Sponsor / Collaborator

SciClone Pharmaceuticals LLC

100 Clinical Results associated with Golotimod

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100 Translational Medicine associated with Golotimod

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100 Patents (Medical) associated with Golotimod

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96

Literatures (Medical) associated with Golotimod

12 Aug 2020·Journal of Biomolecular Structure and Dynamics

Identification and evaluation of glutathione conjugate gamma-l-glutamyl-l-cysteine for improved drug delivery to the brain

Article

Author: Hassan, Md. Imtaiyaz ; Mohammad, Taj ; Alajmi, Mohammed F. ; Fatima, Saman ; Ahmad, Farhan Jalees ; Samim, Mohammed ; Jairajpuri, Deeba Shamim ; Rehman, Md Tabish ; Hussain, Afzal

Glutathione (GU), an endogenous antioxidant tripeptide, is frequently transferred in the human brain through N-methyl-d-aspartate receptor (NMDAR), profusely expressed at the blood-brain barrier (BBB) junction. GU, also modifies the characteristics of tight junction proteins (occludin and claudin) at the site of BBB by depolarizing the enzyme, protein tyrosine phosphatase that manifests its usefulness for passive delivery of nanocarriers to the brain. GU, thus, represents itself as an ideal ligand for the surface decoration of nanocarriers to successfully administer them across the brain via receptor-mediated drug delivery pathway. Hence, we have employed here, in-silico approaches to identify the potential GU-like molecules, as appropriate ligand(s) for surface engineering of nanoconstruct with the purpose of attaining targeted drug delivery to the brain. Structure-based virtual screening methods was used to filter PubChem database for the identification of bioactive compounds with >95% structure similarity with GU. We have further screened the compounds against NMDAR using molecular docking approach. Top hits were selected based on their high binding affinities and selectivity towards NMDAR, and their binding pattern was analysed in detail. Finally, all atom molecular dynamics simulation for 100 ns was carried out on free NMDAR and in-presence of the selected GU-like compound, gamma-l-glutamyl-l-cysteine to evaluate complex stability and structural dynamics. In conclusion, gamma-l-glutamyl-l-cysteine may act as potential binding partner of NMDAR which can further be evaluated in drug delivery system to brain across the BBB.Communicated by Ramaswamy H. Sarma.

01 Jan 2020·Zhurnal nevrologii i psikhiatrii im. S.S. Korsakova

Therapy optimization of asthenic disorders in remissions in patients with paroxysmal-progressive schizophrenia (a clinical and immunological analysis)

Article

Author: Klyushnik, T P ; Zozulya, S A ; Yakimets, A V ; Oleichik, I V

OBJECTIVETo study the efficacy of the immunomodulatory drug γ-D-glutamyl-L-tryptophan in complex therapy of asthenic disorders in remissions in patients with schizophrenia and to analyze clinical and immunological indicators.MATERIALS AND METHODSSixty-three male patients (aged 41.9±9.46 years) with paroxysmal-progressive schizophrenia in remission (ICD-10 F20.x1; F20.x2), including 24 patients with affective-asthenic and 39 with negative-asthenic types, were studied. The assessment of the patients' condition was carried out using PANSS, SANS, CDSS, MFI-20. The activity of inflammatory markers: leukocyte elastase (LE) and α1-proteinase inhibitor (a1-PI) was determined in blood serum. The clinical and immunological assessment was performed before, after therapy (in 5 days) and at the remote stage (in a month).RESULTSAugmentation of standard therapy with γ-D-glutamyl-L-tryptophan facilitated positive reduction in the main clinical manifestations of endogenous asthenia of both types in comparison with placebo (p<0.02). The features of the protease inhibitor system revealed in the patients confirm their clinical heterogeneity and also determine varying efficacy of augmentation by the immunotropic medicine. For patients with the low level of protease activity, which is characteristic of endogenous asthenia with prevalence of negative disorders in clinical picture, the augmentation by γ-D-glutamyl-L-tryptophan was more effective: the decrease in severity of asthenic symptoms was followed by the significant increase in the relatively reduced LE activity (p<0.01), which presumably, relates to the insufficiency of functional activity of neutrophils.CONCLUSIONAugmentation of complex therapy of asthenic disorders in schizophrenia by γ-D-glutamyl-L-tryptophan can be recommended.

26 Jul 2017·Journal of Agricultural and Food ChemistryQ1 · AGRICULTURAL & FORESTRY SCIENCE

Intervention of Dietary Dipeptide Gamma-l-Glutamyl-l-Valine (γ-EV) Ameliorates Inflammatory Response in a Mouse Model of LPS-Induced Sepsis

Q1 · AGRICULTURAL & FORESTRY SCIENCE

Article

Author: Majumder, Kaustav ; Chee, MacKenzie E. ; Mine, Yoshinori

Sepsis, the systemic inflammatory response syndrome (SIRS) with infection is one of the leading causes of death in critically ill patients in the developed world due to the lack of effective antisepsis treatments. This study examined the efficacy of dietary dipeptide gamma-l-glutamyl-l-valine (γ-EV), which was characterized previously as an anti-inflammatory peptide, in an LPS-induced mouse model of sepsis. BALB/c mice were administered γ-EV via oral gavage followed by an intraperitoneal injection of LPS to induce sepsis. The γ-EV exhibited antisepsis activity by reducing the expression of pro-inflammatory cytokines TNF-α, IL-6, and IL-1β in plasma and small intestine. γ-EV also reduced the phosphorylation of the signaling proteins JNK and IκBα. We concluded that γ-EV could possess an antisepsis effect against bacterial infection in intestine. This study proposes a signaling mechanism whereby the calcium-sensing receptor (CaSR) allosterically activated by γ-EV stimulates the interaction of β-arrestin2 with the TIR(TLR/IL-1R) signaling proteins TRAF6, TAB1, and IκBα to suppress inflammatory signaling.

100 Deals associated with Golotimod

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External Link

KEGG	Wiki	ATC	Drug Bank
D08928	-	A05A	DB05475

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Tuberculosis	RU	Verta, Inc.	13 Mar 2009
Hepatitis C	RU	-	01 Jan 2009
Mucositis	RU	-	01 Jan 2009

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Chronic hepatitis C genotype 1	Preclinical	US	SciClone Pharmaceuticals LLC	01 Sep 2009
Head and Neck Neoplasms	Preclinical	US	SciClone Pharmaceuticals LLC	01 Sep 2008
Stomatitis	Preclinical	US	SciClone Pharmaceuticals LLC	01 Sep 2008
Asthma	Preclinical	US	SciClone Pharmaceuticals LLC	-
Herpesviridae Infections	Preclinical	US	SciClone Pharmaceuticals LLC	-
Human Papillomavirus Infection	Preclinical	US	SciClone Pharmaceuticals LLC	-