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

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

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Gene Sequence

Sequence Code 29236244

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Sequence Code 29273623

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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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11

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 Dec 2023·Cancer Biotherapy and Radiopharmaceuticals

Screening and Preclinical Evaluation of Novel Radiolabeled Anti-Fibroblast Activation Protein-α Recombinant Antibodies

Article

Author: Dai, Juan ; Xu, Shasha ; Li, Shenghua ; Tang, Xiaobin ; Wang, Zheng ; Cai, Fei ; Luo, Zhigang ; Geng, Changran ; Cui, Jingjing ; Xu, Jianfeng

Background: Fibroblast activation protein-α (FAPα) is selectively overexpressed in tumor-associated fibroblasts in more than 90% of epithelial tumors, and may be a good target for anticancer treatment, for example, using an anti-FAPα recombinant antibody (rAb) labeled with radionuclides. In the present report, the radiolabeling and preclinical evaluation of novel anti-FAPα rAbs were investigated. Materials and Methods: Two novel anti-FAPα VHHs (AMS002-1 and AMS002-2) with high binding affinity to FAPα were selected from an antibody phage library. The anti-FAPα VHHs were then fused with the Fc fragment of human IgG4 to create two VHH-Fc rAbs. The VHH-Fc rAbs were radiolabeled with ⁸⁹Zr and ¹⁷⁷Lu. The radiolabeled products were evaluated by radioligand-binding assays using FAPα-expressing cells. The biodistribution and tumor-targeting properties were investigated by small-animal PET/CT. AMS002-1-Fc, which showed promising tumor-targeting properties in ⁸⁹Zr-microPET imaging, was radiolabeled with ¹⁷⁷Lu for efficacy study on HT1080 tumor-bearing mice and monitored with SPECT/CT imaging. Results: The two VHH-Fc rAbs with good affinity with K_D values in low nanomolar range were identified. Both PET/CT imaging with ⁸⁹Zr-AMS002-1-Fc rAb and SPECT/CT imaging with ¹⁷⁷Lu-AMS002-1-Fc rAb demonstrated highest tumor uptakes at 72 h p.i. and long tumor retention in the preclinical models. Furthermore, ex vivo biodistribution analysis revealed high tumor uptake of ⁸⁹Zr-AMS002-1-Fc at 48 h p.i. with the value of 6.91% ± 2.08% ID/g. Finally, radioimmunotherapy with ¹⁷⁷Lu-AMS002-1-Fc rAb delayed the tumor growth without significant weight loss in mice with HT1080 xenografts. The tumor size of untreated control group was 2.59 times larger compared with the treatment group with ¹⁷⁷Lu-AMS002-1-Fc at day 29. Conclusion: ⁸⁹Zr/¹⁷⁷Lu-AMS002-1-Fc represent a pair of promising radiopharmaceuticals for theranostics on FAPα-expressing tumors.

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 ; Liu, Fusheng ; Sun, Fengqiao

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

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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	-	AnGes, Inc.	-
Dermatitis, Atopic	Phase 3	-	Osaka University	-
Dermatitis, Atopic	Phase 3	-	Nippon Zoki Pharmaceutical Co. Ltd.	-
Dermatitis, Atopic	Phase 3	-	Shionogi & Co., Ltd.	-
Low Back Pain	Phase 1	US	AnGes, Inc.	26 Feb 2018
Intervertebral Disc Degeneration	Discovery	US	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)	yziutjfjkb(bnctcciegd) = tvpdahwqhr ikqttfnldj (ajbnayzbiz, urqkzukqnh - difcmjjepx) View more	-	23 Aug 2024
				placebo+etoposide+carboplatin+cisplatin (Phase 2 Placebo)	yziutjfjkb(bnctcciegd) = eqquqoyfyd ikqttfnldj (ajbnayzbiz, ixaonbicla - gcczdlvrwv) View more