Delving into the Latest Updates on Imexon with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Imexon (USAN/INN)

+ [2]

Target

Ribonucleotide reductase

Mechanism

RNR inhibitors(Ribonucleotide reductase inhibitors)

Therapeutic Areas

NeoplasmsImmune System DiseasesCardiovascular Diseases+ [6]

Active Indication-

Inactive Indication

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

Originator Organization

AmpliMed Corp.

Active Organization-

Inactive Organization

AmpliMed Corp.

Drug Highest PhaseDiscontinuedPhase 2

First Approval Date-

RegulationOrphan Drug (EU)

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Structure

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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57

Literatures (Medical) associated with Imexon

01 Jul 2022·The FASEB Journal

A pan‐cancer analysis identifies HDAC11 as an immunological and prognostic biomarker

Article

Author: Xue, Kai ; Li, Ran ; Wu, Xiaolu ; Zhao, Ping ; Li, Junmin

AbstractHistone deacetylase 11 (HDAC11) is aberrantly expressed in many types of cancer, and such abnormalities are associated with tumor immunity and heterogeneous clinical outcomes. Here, we explore the prognostic value and immunological function of HDAC11 across 33 cancer types. We observe HDAC11 is aberrantly expressed in 25 cancer types and positively or negatively associated with prognosis in different cancers. HDAC11 played a protective prognostic role in KIRP, KIRC, LGG, PCPG, READ, and UVM, which was contrary to the conventional opinion that HDAC11 was an oncogenic gene. Moreover, HDAC11 is negatively associated with tumor immune components, most immune checkpoint genes, and key cytokine expression. HDAC11 is correlated with tumor mutational burden in 11 cancer types and with microsatellite instability in 9 cancer types, suggesting HDAC11 may affect a patient's response to immune checkpoint inhibitor (ICI) therapy. In addition, HDAC11 is negatively correlated with the drug sensitivity of oxaliplatin, carmustine, ifosfamide, imexon, lomustine, and BN‐2629, indicating the potential synergy between HDAC11 inhibitors and these anti‐tumor drugs. In vitro assays indicate that HDAC11 inhibitor SIS17 combined with oxaliplatin shows a synergistic cytotoxic role in K562 cells while SIS17 has an antagonistic effect on the cytotoxic role of oxaliplatin in 769P cells. HDAC11 is also associated with hallmark pathways, including epithelial mesenchymal transition, IL‑6/JAK/STAT3, and allograft rejection pathways. Overall, we provide clues regarding the key role of HDAC11 in multiple cancers.

01 Jan 2022·American journal of translational research

Identification of differentially expressed autophagy genes associated with osteogenic differentiation in human bone marrow mesenchymal stem cells.

Article

Author: Liu, Hongliang ; Li, Ming ; Li, Zhong ; Zhang, Kun ; Huang, Qiang ; Ma, Teng ; Wang, Qian ; Wang, Zhimeng ; Wang, Yakang ; Ren, Cheng ; Lu, Yao ; Sun, Liang ; Xu, Yibo

BACKGROUNDMesenchymal stem cells derived from human tissues have been widely used for tissue regeneration because of their strong self-renewal capacity and multi-potential properties. Autophagy plays a vital role in maintaining bone homeostasis. However, the mechanism underlying this role for autophagy in the osteogenic differentiation of mesenchymal stem cells remains to be elucidated.METHODSTwo microarray datasets were downloaded from the GEO database. Fourteen bone marrow mesenchymal stem cell samples comprising control and induction groups were selected to identify differentially expressed autophagy-related genes via multiple bioinformatics approaches, followed by functional analysis. Interactions among differentially expressed autophagy genes, miRNAs, and transcription factors were analyzed and visualized using Cytoscape software. The association between hub differentially expressed genes and autophagy was validated by qRT-PCR.RESULTSTen autophagy-related genes (including VPS8, NDRG4, and CYBB) were identified as osteogenic hub genes. Correlation analysis revealed that CYBB was highly correlated with the sensitivity to multiple drugs, such as imexon, megestrol acetate, and isotretinoin. The regulatory network displayed a complex connection among miRNAs, transcription factors, and differentially expressed autophagy genes. Friends' analysis showed that NDRG4 was highly closely related to other hub genes (P < 0.05). Furthermore, NDRG4 expression was downregulated in the induction group (P < 0.01). NDRG4 was significantly correlated with infiltrating immune cells, including monocytes, eosinophils, type 17 T helper cells, neutrophils, activated CD8 T cells, and immature B cells. Levels of the 10 autophagy-related genes (including VPS8, NDRG4, and CYBB) were successfully validated based on in vitro experiments.CONCLUSIONWe identified candidate molecules to further investigate their functions in osteogenesis, providing novel insights into the role of autophagy in mesenchymal stem cell differentiation.

01 May 2021·Life SciencesQ3 · MEDICINE

A pan-cancer analysis of the HER family gene and their association with prognosis, tumor microenvironment, and therapeutic targets

Q3 · MEDICINE

Article

Author: Mi, Denghai ; Miao, Yandong ; Wang, Jiangtao ; Yang, Xiaolong

AIMSThe human epidermal growth factor receptor (HER) family gene is involved in a wide range of biological functions in human cancers. Nevertheless, there is little research that comprehensively analysis the correlation between HER family members and prognosis, tumor microenvironment (TME) in different cancers.MATERIALS AND METHODSBased on updated public databases and integrated several bioinformatics analysis methods, we evaluated expression level, prognostic values of HER family gene and explore the association between expression of HER family gene and TME, Stemness score, immune subtype, drug sensitivity in pan-cancer.KEY FINDINGSEGFR, ERBB2, ERBB3, and ERBB4 were higher expressed in four cancers, five cancers, ten cancers, and two cancers, respectively. HER family gene expression is related to the prognosis in several cancers from TCGA and has a significant correlation with stromal and immune scores in pan-cancer also has a significant correlation with RNA stemness score and DNA stemness score in pan-cancer. Expression level of HER family gene is associated with immune subtype in head and neck squamous cell carcinoma and kidney renal clear cell carcinoma. EGFR expression was negatively associated with drug sensitivity of Pipamperone, Tamoxifen, Bafetinib and positively related to drug sensitivity of Dasatinib and Staurosporine. ERBB2 expression was negatively related to drug sensitivity of Ifosfamide, Imexon, and Oxaliplatin. ERBB4 expression was positively related to drug sensitivity of E-7820.SIGNIFICANCEThese findings may elucidate the roles played by HER family gene in cancer progression and providing insights for further investigation of the HER family gene as potential targets in pan-cancer.

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	US	AmpliMed Corp.	01 Aug 2010
Multiple Myeloma	Phase 2	US	AmpliMed Corp.	01 Oct 2005
Unresectable Melanoma	Phase 2	US	AmpliMed Corp.	01 Jul 2005
Breast Cancer	Phase 1	US	AmpliMed Corp.	01 Oct 2005
Castration-Resistant Prostatic Cancer	Phase 1	US	AmpliMed Corp.	01 Oct 2005
Advanced Pancreatic Adenocarcinoma	Phase 1	US	AmpliMed Corp.	01 Feb 2004
Pancreatic adenocarcinoma	Phase 1	US	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 \| Circulation)	Phase 2	B-cell lymphoma refractory	22	Imexon 1000 mg/m(2)	(ubxxifcwof) = qahkfmaysh vfnsexggpw (mypxqexcts )	-	21 Aug 2014
NCT01314014 (ULYM11011, CTgov)	Phase 2	Lymphoplasmacytic Lymphoma \| Follicular Lymphoma \| Mantle-Cell Lymphoma \| Burkitt Lymphoma \| Diffuse Large B-Cell Lymphoma \| Small Lymphocytic Lymphoma \| Marginal Zone B-Cell Lymphoma	22	Imexon	qiqlemjsun(oyjbklzajn) = sfbxwdcedx kmvflzhkmv (tkahevovgc, jtlhpopsfw - greisiacib) View more	-	01 Jul 2014
NCT00637247 (CTgov)	Phase 2	Pancreatic adenocarcinoma metastatic	142	imexon in combination+gemcitabine (Imexon + Gemcitabine)	gwgorhazbs(qspfgvkkjo) = uxjovsohmp ujknkvvrki (dtibphipbn, qdazuccftn - raeiogewzt)	-	30 Nov 2010
NCT00637247 (CTgov)	Phase 2	Pancreatic adenocarcinoma metastatic	142	imexon placebo + gemcitabine (Placebo + Gemcitabine)	gwgorhazbs(qspfgvkkjo) = hnvykyxinr ujknkvvrki (dtibphipbn, gfggzdhwcp - waslfhoxtu)	-	30 Nov 2010
NCT00327600 (Pubmed \| Cancer)	Phase 1/2	Unresectable Melanoma	68	Imexon plus dacarbazineImexon plus dacarbazine	(zbvrfbwxzx) = lkytdvhofk gwkckppfcf (uioxpjixkr ) View more	-	01 Aug 2010
NCT00327327 (Pubmed \| Cancer Chemother Pharmacol)	Phase 1	Pancreatic Cancer First line	105	Imexon	(rscjgzosit) = betbphknmk sokuwbchta (dimpptfghi )	-	01 Jul 2010
ASCO2008	Phase 1/2	Malignant melanoma, metastatic	68	Imexon (AMP) plus dacarbazine (DTIC)	(xsxkdcfaql) = Seven Pts had SAEs that were possibly or definitely related to treatment wjuzovjbpj (wnipatyyac ) View more	-	20 May 2008
ASCO2008	Phase 1	Prostatic Cancer	29	Imexon + Docetaxel	(kajxsuqqbc) = transient, grade 3–4 non cardiac chest pain (w/o enzyme elevations or EKG changes) in 3/3 pts with pulmonary metastases gfmcjidfxa (oexjephimc ) View more	-	20 May 2008
ASCO2005	Phase 1	HR-positive/HER2-low Solid Tumors	30	Imexon	foanvpooav(ozixcjksbg) = bvgkbpphnj tmgtohlmgt (qynxpfoiuy )	-	01 Jun 2005