Delving into the Latest Updates on Cupabimod with Synapse

Overview

Basic Info

Drug Type

TF Decoy

Synonyms

NDON, NF-kD-transcription-factor, NF-kappa-B decoy oligonucleotide

+ [19]

Target

NF-κB

Action

inhibitors

Mechanism

NF-κB inhibitors(Nuclear factor NF-kappa-B complex inhibitors)

Therapeutic Areas

Immune System DiseasesCongenital DisordersSkin and Musculoskeletal Diseases

Active Indication

Dermatitis, Atopic

Inactive Indication

Intervertebral Disc DegenerationLow Back Pain

Originator Organization

AnGes, Inc.

Active Organization

Nippon Zoki Pharmaceutical Co. Ltd.

Shionogi & Co., Ltd.

AnGes, Inc.

+ [1]

Inactive Organization-

Drug Highest PhasePhase 3

First Approval Date-

Regulation-

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Structure/Sequence

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Sequence Code 29236244

Source: *****

Sequence Code 29273623

Source: *****

A Phase 1b, Multicenter, Double-blind, Randomized, Placebo-controlled, Single Ascending-Dose, Clinical Study Evaluating the Safety, Tolerability and Exploratory Efficacy of a Targeted Single Injection of an Intradiscal Nuclear Factor-κB Decoy Oligodeoxynucleotide (AMG0103) in Subjects With Chronic Discogenic Lumbar Back Pain

This clinical trial evaluate the safety, tolerability and exploratory efficacy of targeted single injection of AMG0103 in subject with chronic discogenic lumbar back pain

Start Date26 Feb 2018

Sponsor / Collaborator

AnGes, Inc.

NCT01443065

/ CompletedPhase 2IIT

MEGA (Met or EGFR Inhibition in Gastroesophageal Adenocarcinoma): FOLFOX Alone or in Combination With AMG 102 or Panitumumab as First-line Treatment in Patients With Advanced Gastroesophageal Adenocarcinoma FNCLCC-FFCD-AGEO PRODIGE 17-ACCORD 20 Randomized Phase II Trial

This multicentre, open-label, randomized phase II trial is ongoing in 30 centres in France. Main eligibility criteria include: histologically proven adenocarcinoma of the stomach, esophagus or gastroesophageal junction; locally advanced or metastatic disease; measurable disease (RECIST 1.1); no known HER2 overexpression; no prior palliative chemotherapy.

Start Date01 Jan 2011

Sponsor / Collaborator

UNICANCER

100 Clinical Results associated with Cupabimod

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100 Translational Medicine associated with Cupabimod

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100 Patents (Medical) associated with Cupabimod

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9

Literatures (Medical) associated with Cupabimod

01 Feb 2024·Bioorganic Chemistry

Design, synthesis and evaluation of quinazoline derivatives as Gαq/11 proteins inhibitors against uveal melanoma

Article

Author: Xiao, Wei ; Xiong, Xiao-Feng ; Fan, Guangjin ; Liu, Lu ; Ye, Jia

Uveal melanoma (UM) represents the predominant ocular malignancy among adults, exhibiting high malignancy and proclivity for liver metastasis. GNAQ and GNA11 encoding Gαq and Gα11 proteins are key genes to drive UM, making the selective inhibition of Gαq/11 proteins to be a potential therapeutic approach for combating UM. In this study, forty-six quinazoline derivatives were designed, synthesized, and assessed for their ability to inhibit Gαq/11 proteins and UM cells. Compound F33 emerged as the most favorable candidate, and displayed moderate inhibitory activity against Gαq/11 proteins (IC₅₀ = 9.4 μM) and two UM cell lines MP41 (IC₅₀ = 6.7 μM) and 92.1 (IC₅₀ = 3.7 μM). Being a small molecule inhibitor of Gαq/11 proteins, F33 could effectively suppress the activation of downstream signaling pathways in a dose-dependent manner, and significantly inhibits UM in vitro.F33 represents a promising lead compound for developing therapeutics for UM by targeting Gαq/11 proteins.

01 Feb 2023·Melanoma Research

Orthotopic murine xenograft model of uveal melanoma with spontaneous liver metastasis

Article

Author: Fabra, Àngels ; Gutierrez, Cristina ; Ramos, Raquel ; Varela, Mar ; Caminal, José M. ; Lorenzo, Daniel ; Paules, Maria José ; Piulats, Josep M. ; Vinyals, Antònia ; Cabré, Eduard ; Ferreres, Josep R. ; Gomá, Montse

Uveal melanoma is the most common intraocular malignancy in adults. Despite the effective primary treatment, up to 50% of patients with uveal melanoma will develop metastatic lesions mainly in the liver, which are resistant to conventional chemotherapy and lead to patient’s death. To date, no orthotopic murine models of uveal melanoma which can develop spontaneous metastasis are available for preclinical studies. Here, we describe a spontaneous metastatic model of uveal melanoma based on the orthotopic injection of human uveal melanoma cells into the suprachoroidal space of immunodeficient NSG mice. All mice injected with bioluminescent OMM2.5 (n = 23) or MP41 (n = 19) cells developed a primary tumor. After eye enucleation, additional bioluminescence signals were detected in the lungs and in the liver. At necropsy, histopathological studies confirmed the presence of lung metastases in 100% of the mice. Liver metastases were assessed in 87 and in 100% of the mice that received OMM2.5 or MP41 cells, respectively. All tumors and metastatic lesions expressed melanoma markers and the signaling molecules insulin-like growth factor type I receptor and myristoylated alanine-rich C-kinase substrate, commonly activated in uveal melanoma. The novelty of this orthotopic mouse xenograft model is the development of spontaneous metastases in the liver from the primary site, reproducing the organoespecificity of metastasis observed in uveal melanoma patients. The faster growth and the high metastatic incidence may be attributed at least in part, to the severe immunodeficiency of NSG mice. This model may be useful for preclinical testing of targeted therapies with potential uveal melanoma antimetastatic activity and to study the mechanisms involved in liver metastasis.

01 Feb 2023·Journal of Cancer Research and Clinical Oncology

Enhancing the immune effect of oHSV-1 therapy through TLR3 signaling in uveal melanoma

Article

Author: Zhang, Junwen ; Li, Mingxin ; Liu, Sisi ; Sun, Fengqiao ; Liu, Fusheng

PURPOSEUveal melanoma (UM) is the most common primary intraocular malignant tumor in adults, with patients having a low overall survival rate. Oncolytic viruses (OVs) have been shown effective as monotherapy or combined with immunotherapy in the treatment of UM. Oncolytic herpes simplex type I virus (oHSV-1) was found to alter gene expression and immune function in UMs. We investigated whether a combination treatment would be more effective in treating UM and reactive immune cells.METHODSRNA sequencing analysis were used to identify the effect of oHSV-1 infection in UM cells and protein changes were validated by western blot. Cell viability assays were performed through UM cell lines (MUM2B, 92.1, and MP41) and retinal pigment epithelial cell line (ARPE-19) to identify the efficacy and safety of the combination treatment. Western blot, qRT-PCR, cell viability assay and immunocytochemistry were performed to discover the reactivation of immune cells (U937 and HMC3).RESULTSThrough RNA sequencing analysis and in vitro molecular biology assays, this study tested the ability of oHSV-1 combined with the TLR3 agonist poly(I:C) to re-activate the TLR3 meditated NF-ƙB signaling pathway and further increase the anti-tumor activity of UM cells and macrophages, including the stimulation of macrophage polarization and proliferation.CONCLUSIONSThese findings indicate that the treatment of UM with a combination of oHSV-1 and poly(I:C) generates immune responses and enhances anti-tumoral activity, suggesting the need for further investigations and clinical trials of this combination.

100 Deals associated with Cupabimod

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External Link

KEGG	Wiki	ATC	Drug Bank
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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Dermatitis, Atopic	Phase 3	-	Osaka University	-
Dermatitis, Atopic	Phase 3	-	AnGes, Inc.	-
Dermatitis, Atopic	Phase 3	-	Nippon Zoki Pharmaceutical Co. Ltd.	-
Dermatitis, Atopic	Phase 3	-	Shionogi & Co., Ltd.	-
Intervertebral Disc Degeneration	Discovery	United States	AnGes, Inc.	26 Feb 2018
Low Back Pain	Discovery	United States	AnGes, Inc.	26 Feb 2018

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT00791154 (SCLC, CTgov)	Phase 1/2	Extensive stage Small Cell Lung Cancer	213	Ganitumab (Phase 2 Ganitumab)	wwwoeuefql(dckzobxidp) = qwlnseyjcj gtfjabxwnr (sxazfnvnqs, iqndaqpkbu - ynpjknqpjf) View more	-	23 Aug 2024
				placebo+etoposide+carboplatin+cisplatin (Phase 2 Placebo)	wwwoeuefql(dckzobxidp) = ijkcgowngi gtfjabxwnr (sxazfnvnqs, rgjdwweixs - fchoqciokm) View more