Delving into the Latest Updates on Imexon with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Imexon (USAN/INN), AOP-990001, BM-06002

+ [2]

Target

RNRs

Action

inhibitors

Mechanism

RNR inhibitors(Ribonucleotide reductase inhibitors)

Therapeutic Areas

NeoplasmsDigestive System DisordersEndocrinology and Metabolic Disease+ [5]

Active Indication-

Inactive Indication

Advanced Pancreatic AdenocarcinomaBreast CancerCastration-Resistant Prostatic Cancer+ [4]

Originator Organization

AmpliMed Corp.

Active Organization-

Inactive Organization

AmpliMed Corp.

License Organization-

Drug Highest PhaseDiscontinuedPhase 2

First Approval Date-

RegulationOrphan Drug (United States), Orphan Drug (European Union)

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Structure/Sequence

Molecular FormulaC4H5N3O

InChIKeyBIXBBIPTYBJTRY-UHFFFAOYSA-N

CAS Registry59643-91-3

Protocol AMP-024 is a Phase 2 study of imexon plus docetaxel for patients with previously treated lung cancer that has spread in the body. Docetaxel is approved by the Food and Drug Administration (FDA) as a second line therapy for this cancer. The imexon is administered on days 1-5 and the docetaxel on day 1 of every 3 week cycle. The objective of the protocol is to determine if the combination of imexon plus docetaxel is safe and effective.

Start Date01 Aug 2010

Sponsor / Collaborator

AmpliMed Corp.

NCT00637247

/ CompletedPhase 2

A Phase 2 Randomized, Double-Blind, Multicenter Trial of Amplimexon® Plus Gemcitabine Versus Gemcitabine Plus Placebo in Patients With Metastatic Chemotherapy Naïve Pancreatic Adenocarcinoma (Stage IV)

The purpose of this study is to determine if imexon in combination with gemcitabine could improve overall survival as compared to gemcitabine alone in subjects with pancreatic cancer that has spread to other organs such as the liver or lungs. The study will also look at the safety of the combination as compared to gemcitabine alone. Participants in the study will be randomly assigned to either treatment and neither the participant or their doctors will know which treatment they will be receiving.

Start Date01 Apr 2008

Sponsor / Collaborator

AmpliMed Corp.

100 Clinical Results associated with Imexon

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100 Translational Medicine associated with Imexon

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100 Patents (Medical) associated with Imexon

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110

Literatures (Medical) associated with Imexon

01 Nov 2024·Translational Oncology

Disulfidptosis-related gene expression reflects the prognosis of drug-resistant cancer patients and inhibition of MYH9 reverses sorafenib resistance

Article

Author: Zhou, Jingyi ; Zhang, Kangnan ; Zhu, Zhenhua ; Wang, Na ; Xu, Ling ; Yu, Fudong ; Shi, Min

The onset of drug resistance in advanced cancer patients markedly diminishes their prognosis. Recently, disulfidptosis, a novel form of cell death, has been identified, triggered by excessive disulfide formation leading to cell shrinkage and F-actin contraction. Previous studies have identified 15 essential genes (FLNA, FLNB, MYH9, TLN1, ACTB, MYL6, MYH10, CAPZB, DSTN, IQGAP1, ACTN4, PDLIM1, CD2AP, INF2, SLC7A11) associated with disulfidptosis. This study sourced pan-cancer mRNA expression data from Xena to thoroughly evaluate the molecular and clinical characteristics of disulfidptosis-related genes. Through unsupervised clustering, mRNA expression data identified the expression levels of disulfidptosis-related genes and potential clusters related to this form of cell death. Kaplan-Meier survival curves illustrated the correlation between different clusters and overall survival. The findings reveal that high expression of disulfidptosis-related genes is linked to poor survival in liver cancer. The GDSC database was utilized to analyze the relationship between disulfidptosis-related genes and the AUC of 198 drugs. The results demonstrate that 12 disulfidptosis-related genes influence sorafenib resistance, as revealed by the intersection of differential genes related to sorafenib resistance from the GSE109211 dataset. Among them, the MYH9 gene was found to play a crucial role in both. Finally, experimental evidence confirmed that MYH9 mitigates sorafenib resistance in hepatocellular carcinoma through disulfidptosis-like changes. This study identifies disulfidptosis as a promising avenue for enhancing the sensitivity of tumor cells to drugs, offering new therapeutic perspectives for future research on disulfidptosis and drug resistance in cancer patients.

01 Aug 2024·CELL BIOLOGY INTERNATIONAL

Single‐cell and bulk RNA‐sequencing reveals mitosis‐involved gene HAUS1 is a promising indicator for predicting prognosis and immune responses in prostate adenocarcinoma (PRAD)

Article

Author: Yu, Yang ; Xu, Jie ; Wang, Yi ; Li, Deng ; Liu, Shiwei

Abstract:

It was imperative to identify latent biomarkers pertinent to malignancies, given the pivotal role targeted molecular therapies play in tumor treatment investigations. This study aimed to assess the validity of HAUS1 as an indicator for survival prognosis and immune responses in prostate adenocarcinoma (PRAD) via single‐cell and bulk RNA‐sequencing. Related data on HAUS1 expression in PRAD were obtained from online databases, followed by comprehensive analyses to delineate its associations with survival prognosis, implicated pathways, and immune responses. Besides, the expression pattern of HAUS1 in PRAD was also verified in vitro, by using qRT‐PCR, Western blot analysis, and immunohistochemistry. We found HAUS1 was downregulated in PRAD compared with normal tissues, as verified in vitro by qRT‐PCR, Western blot, and immunohistochemistry (p < 0.05). Single‐cell RNA‐sequencing analysis indicated that HAUS1 had relatively higher expressions in B cells, Mono/Macro cells, and Endothelial cells compared with other cell types. Cox regression analysis revealed HAUS1 could serve as an independent indicator for the overall survival prognosis of PRAD (p < 0.05). Spearman correlation analyses revealed HAUS1 was closely related to the tumor microenvironment, immune cell infiltration levels, immune checkpoints, and immune cell pathways (p < 0.05). Furthermore, HAUS1 expression was found to be closely related to the immunotherapeutic response of patients receiving clinical intervention (p < 0.05). Collectively, our findings underscored the significant role of HAUS1 in PRAD prognosis and immune response, thereby presenting a novel and promising avenue for investigating the clinical utility of immunotherapy in PRAD.

01 May 2023·JOURNAL OF MOLECULAR LIQUIDS

Adsorption of 40 low molecular weight drugs on pristine and fluorinated C60 fullerenes: Ab initio, statistical and neural networks analysis

Author: Kochaev, Alexey I. ; Maslov, Mikhail M. ; Grekova, Anastasiya A. ; Katin, Konstantin P. ; Bondarev, Nikolay V. ; Kaya, Savas ; Bauetdinov, Yusupbek A. ; Kalika, Elizaveta B.

Loading of 40 small drugs mols. with mol. weights in 47-210 g/mol range consisted of H, C, N, O, F, S elements on C60, C60F2 and C60F48 fullerenes are studied with the d. functional theory.Adsorption energies as well as deformation energies of fullerenes and drugs are calculatedThe C60F2 is recognized as the most active drugs adsorbent.Mean adsorption energies averaged over all considered drugs are 0.41, 0.59 and 0.54 eV with standard deviations of 0.10, 0.09 and 0.14 eV for C60, C60F2 and C60F48 fullerenes, resp.Mean energies of drug-induced deformations of C60, C60F2 and C60F48 are 8.6, 12.0 and 16.6 meV, resp.Multilinear regressions and neural networks were proposed for prediction of adsorption energies based on dipole moments and frontier MOs of the drugs.Achievable accuracy of such predictions is about 0.1 eV.Altretamine antibiotic is recognized as the notable drug possessing extremely high binding energies about 1 eV with fullerenes.IR spectral shifts due to its loading on fullerene carriers are calculated

100 Deals associated with Imexon

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External Link

KEGG	Wiki	ATC	Drug Bank
D08932	Imexon	-	DB05003

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
metastatic non-small cell lung cancer	Phase 2	United States	AmpliMed Corp.	01 Aug 2010
Pancreatic adenocarcinoma metastatic	Phase 2	United States	AmpliMed Corp.	01 Apr 2008
Multiple Myeloma	Phase 2	United States	AmpliMed Corp.	01 Oct 2005
Unresectable Melanoma	Phase 2	United States	AmpliMed Corp.	01 Jul 2005
Breast Cancer	Phase 1	United States	AmpliMed Corp.	01 Oct 2005
Castration-Resistant Prostatic Cancer	Phase 1	United States	AmpliMed Corp.	01 Oct 2005
Advanced Pancreatic Adenocarcinoma	Phase 1	United States	AmpliMed Corp.	01 Feb 2004

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT01314014 (Pubmed \| Blood)	Phase 2	B-Cell Lymphoma CD68 \| GPX1 \| SOD2	-	Imexon 1000 mg/m(2)	acvvpgjvpw(ekcstnpgut) = wxncknszmz tjmxyvcbrq (reqxnaidkh )	-	21 Aug 2014
NCT01314014 (ULYM11011, CTgov)	Phase 2	Lymphoplasmacytic Lymphoma \| Mantle-Cell Lymphoma \| Follicular Lymphoma ... View more	22	Imexon	vihabkwuly = nddsccnusk odbhzcnqru (qnastcfbng, vzwrwxajoz - qlvidgpwms) View more	-	01 Jul 2014
NCT00637247 (CTgov)	Phase 2	Pancreatic adenocarcinoma metastatic	142	gemcitabine+imexon (Imexon + Gemcitabine)	fcslxmdmwr = zbqoufajsg obpxcicijl (pblqijzuvw, hqyzdopdcm - ndjxrtviyq)	-	30 Nov 2010
NCT00637247 (CTgov)	Phase 2	Pancreatic adenocarcinoma metastatic	142	imexon placebo + gemcitabine (Placebo + Gemcitabine)	fcslxmdmwr = pihxwowypr obpxcicijl (pblqijzuvw, ymnzflitno - aeuvnyvjcl)	-	30 Nov 2010
NCT00327288 (Pubmed \| Invest New Drugs)	Phase 1	Prostatic Cancer	34	Docetaxel	wztgmautlj(ydckkxlsqo) = pbomhrhvde ymgupxkzlf (ctxzpfklee )	-	01 Oct 2010
NCT00327600 (Pubmed \| Cancer)	Phase 1/2	Unresectable Melanoma	68	Imexon plus dacarbazine	htoptgpoyn(ezjjdiljem) = rncecvfwvi xmmypmdcuk (spmlkjvafp ) View more	-	01 Aug 2010
NCT00327327 (Pubmed \| Cancer Chemother Pharmacol)	Phase 1	Pancreatic Cancer First line	105	Imexon	shefonnmpc(hfnpalkjih) = svsbdfonxi tnhtizpnyr (ivqkcqqskd )	-	01 Jul 2010
ASCO2008	Phase 1/2	Malignant melanoma, metastatic	68	Imexon (AMP) plus dacarbazine (DTIC)	nmgoslnsee(jfoxrmxvck) = Seven Pts had SAEs that were possibly or definitely related to treatment nalxsjnqsc (ynkgcgbwth ) View more	-	20 May 2008
ASCO2008	Phase 1	Prostatic Cancer	29	Imexon + Docetaxel	ptrodffyui(fewlvvozbx) = transient, grade 3–4 non cardiac chest pain (w/o enzyme elevations or EKG changes) in 3/3 pts with pulmonary metastases ejkxzuedmt (zimiztapms ) View more	-	20 May 2008
ASCO2005	Phase 1	HR-positive/HER2-low Solid Tumors	30	Imexon	vqgkyclslx(xbzbhfkjrs) = osiyrdqeqa lysltcoirb (ukzpqzkldf )	-	01 Jun 2005