Delving into the Latest Updates on Verubulin with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Azixa, Veribulin, Verubulin (USAN/INN)

+ [6]

Target

Tubulin

Action

inhibitors

Mechanism

Tubulin inhibitors

Therapeutic Areas

NeoplasmsNervous System Diseases

Active Indication

Brain Cancer

Inactive Indication

Brain metastasesColorectal CancerGlioblastoma+ [5]

Originator Organization

Immune Pharmaceuticals, Inc.

Active Organization

Immune Pharmaceuticals, Inc.

Inactive Organization

Myrexis, Inc.

License Organization

Immune Pharmaceuticals, Inc.

Myrexis, Inc.

Drug Highest PhasePhase 2

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC17H17N3O

InChIKeySNHCRNMVYDHVDT-UHFFFAOYSA-N

CAS Registry827031-83-4

This is a phase 0 study that will enable an assessment of biodistribution and estimation of absorbed dose in humans based on data collected from five healthy volunteers, which is typically the minimum number required by the FDA for first-in-human studies to assess dosimetry of a new tracer. The evaluation of the brain imaging of thirty additional subjects in the 2nd part of the study will lead to a descriptive assessment of the targeting and pharmacokinetics of MPC6827 in the brain and between normal and diseased brain.

Start Date08 Jan 2021

Sponsor / Collaborator

Columbia University

NCT01285414

/ CompletedPhase 2

A Phase 2 Study of Verubulin With Radiation Therapy and Temozolomide in Subjects Newly Diagnosed With Glioblastoma Multiforme

This, international, multi-center, Phase 2 study of verubulin will be conducted in patients with newly diagnosed Glioblastoma Multiforme (GBM). The study will be conducted in two parts. Part A is an open-label dose finding study that will determine the safety and tolerability of verubulin in combination with standard treatment. Part B is a randomized open-label study that will investigate progression-free survival and overall survival of patients receiving verubulin, at the dose determined in Part A, in combination with standard treatment versus standard treatment alone.

Start Date01 Dec 2010

Sponsor / Collaborator

Myrexis, Inc.

NCT00892931

/ CompletedPhase 2

Phase 2 Study of Azixa (MPC-6827) for the Treatment of Patients With Recurrent Glioblastoma Multiforme

The purpose of this study is to determine the safety and effectiveness of Azixa in patients with recurrent glioblastoma multiforme

Start Date01 Apr 2009

Sponsor / Collaborator

Myrexis, Inc.

100 Clinical Results associated with Verubulin

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100 Translational Medicine associated with Verubulin

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100 Patents (Medical) associated with Verubulin

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48

Literatures (Medical) associated with Verubulin

16 Dec 2024·Chemical Research in Toxicology

Quantitative Structure–Activity Relationship Models to Predict Cardiac Adverse Effects

Article

Author: Stavitskaya, Lidiya ; Racz, Rebecca ; Volarath, Patra ; Mou, Zhongyu ; Girireddy, Mounika ; Chakravarti, Suman ; Cross, Kevin P.

Drug-induced cardiotoxicity represents one of the most common causes of attrition of drug candidates in preclinical and clinical development. For this reason, the evaluation of cardiac toxicity is essential during drug development and regulatory review. In the present study, drug-induced postmarket adverse event combinations from the FDA Adverse Event Reporting System were extracted for 2002 drugs using 243 cardiac toxicity-related preferred terms (PTs). These PTs were combined into 12 groups based on their clinical relevance to serve as training sets. The optimal classification scheme was determined using a combination of data sources that included drug labeling information, published literature, clinical study data, and postmarket surveillance data. Two commercial QSAR platforms were used to construct 12 models, including general cardiac toxicity, cardiac ischemia, heart failure, cardiac valve disease, myocardial disease, pericardial disease, structural heart disease, cardiac arrhythmia, Torsades de Pointes, long QT syndrome, atrial fibrillation and ventricular arrhythmia, and cardiac arrest. The cross-validated performance for the new models reached a sensitivity of up to 80% and negative predictivity of up to 80%. These new models covering a wide range of cardiac endpoints will provide fast, reliable, and comprehensive predictions of potential cardiotoxic compounds in drug discovery and regulatory safety assessment.

01 Nov 2024·European Journal of Medicinal Chemistry

Discovery of novel thiophene[3,2-d]pyrimidine-based tubulin inhibitors with enhanced antitumor efficacy for combined use with anti-pd-l1 immunotherapy in melanoma

Article

Author: Wang, Yuxi ; Chen, Jianjun ; Peng, Xiaopeng ; Zhao, Huiting ; Li, Ling ; Liu, Jin ; Wu, Chengyong ; Xu, Chenglong

Herein, we designed and synthesized a series of novel 2-methylthieno [3,2-d]pyrimidine analogues as tubulin inhibitors with antiproliferative activities at low nanomolar levels. Among them, compound DPP-21 displayed the most potent anti-proliferative activity against six cancer cell lines with an average IC₅₀ of ∼6.23 nM, better than that of colchicine (IC₅₀ = 9.26 nM). DPP-21 exerted its anti-cancer activity by suppressing the polymerization of tubulin with an IC₅₀ of 2.4 μM. Furthermore, the crystal structure of DPP-21 in complex with tubulin was solved by X-ray crystallography to 2.94 Å resolution, confirming the direct binding of DPP-21 to the colchicine site. Moreover, DPP-21 arrested the cell cycle in the G2/M phase of mitosis, subsequently inducing tumor cell apoptosis. Additionally, DPP-21 was able to effectively inhibit the migration of cancer cells. Besides, DPP-21 exhibited significant in vivo anti-tumor efficacy in a B16-F10 melanoma tumor model with a TGI of 63.3 % (7 mg/kg) by intraperitoneal (i.p.) injection. Notably, the combination of DPP-21 with NP-19 (a PD-L1-targeting small molecule inhibitor reported by our group before) demonstrated enhanced anti-cancer efficacy in vivo. These results suggest that DPP-21 is a promising lead compound deserving further investigation as a potential anti-cancer agent.

01 May 2024·Journal of Cellular and Molecular Medicine

Prognostic and immunotherapeutic implications of bilirubin metabolism‐associated genes in lung adenocarcinoma

Article

Author: Li, Zeyao ; Ling, Xiean ; Huang, Tonghai ; Ren, Kangqi ; Chen, Lin

AbstractLung adenocarcinoma (LUAD) is a major subtype of non‐small‐cell lung cancer and accompanies high mortality rates. While the role of bilirubin metabolism in cancer is recognized, its specific impact on LUAD and patient response to immunotherapy needs to be elucidated. This study aimed to develop a prognostic signature of bilirubin metabolism‐associated genes (BMAGs) to predict outcomes and efficacy of immunotherapy in LUAD. We analysed gene expression data from The Cancer Genome Atlas (TCGA) to identify survival‐related BMAGs and construct a prognostic model in LUAD. The prognostic efficacy of our model was corroborated by employing TCGA‐LUAD and five Gene Expression Omnibus datasets, effectively stratifying patients into risk‐defined cohorts with marked disparities in survival. The BMAG signature was indeed an independent prognostic determinant, outperforming established clinical parameters. The low‐risk group exhibited a more favourable response to immunotherapy, highlighted by increased immune checkpoint expression and immune cell infiltration. Further, somatic mutation profiling differentiated the molecular landscapes of the risk categories. Our screening further identified potential drug candidates preferentially targeting the high‐risk group. Our analysis of critical BMAGs showed the tumour‐suppressive role of FBP1, highlighting its suppression in LUAD and its inhibitory effects on tumour proliferation, migration and invasion, in addition to its involvement in cell cycle and apoptosis regulation. These findings introduce a potent BMAG‐based prognostic indicator and offer valuable insights for prognostication and tailored immunotherapy in LUAD.

100 Deals associated with Verubulin

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External Link

KEGG	Wiki	ATC	Drug Bank
D10029	-	-	DB05585

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Neurodegenerative Diseases	Phase 2	United States	Myrexis, Inc.	25 Sep 2020
Brain metastases	Phase 2	United States	Immune Pharmaceuticals, Inc.	03 Jan 2016
Melanoma	Phase 2	United States	Immune Pharmaceuticals, Inc.	29 Dec 2015
Glioblastoma	Phase 2	United States	Immune Pharmaceuticals, Inc.	19 Dec 2015
Glioblastoma Multiforme	Phase 2	United States	Myrexis, Inc.	01 Apr 2009
Recurrent Glioblastoma	Phase 2	United States	Myrexis, Inc.	01 Apr 2009
Refractory Malignant Solid Neoplasm	Phase 2	United States	Myrexis, Inc.	01 Mar 2005
Brain Cancer	Phase 2	-	Immune Pharmaceuticals, Inc.	-
Colorectal Cancer	Phase 2	United States	Immune Pharmaceuticals, Inc.	-

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ASCO2011	Phase 2	Recurrent Glioblastoma	31	Verubulin	pezwxncvdo(vrombwfihg) = iknzxdpmfy fuptaxramx (bvlaopzbzt, 3% - 25%) View more	Positive	20 May 2011
ASCO2010	Not Applicable	Recurrent Glioblastoma	19	MPC-6827	(wxvxvtvjra) = eapvmbfurm zecnvlycrz (hnvxesckxn, [1.3 - 7.1]) View more	-	20 May 2010
ASCO2010	Not Applicable	Metastatic melanoma	22	MPC-6827	(pxkattarvq) = lzgpamcfed rxnxeqwbwm (dkuyucvaxz, [1.7 - 5.5])	-	20 May 2010
AACR2009	Phase 1	Solid tumor	48	Azixa	(jxrdaccitk) = faaodbxzqq oqevzolvmr (bgyjjyomfx )	-	01 May 2009
ASCO2007	Phase 1	HR-positive/HER2-low Solid Tumors \| Brain metastases	-	MPC-6827	(btidrqkcti) = rtyfdqyfbj ihnfintsiz (impmahmybd )	-	20 Jun 2007