Delving into the Latest Updates on Irinotecan-eluting beads with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

DEBIRI, Irinotecan bead, PARAGON Bead

+ [2]

Target

Top I

Action

inhibitors

Mechanism

TOP1 inhibitors(DNA topoisomerase I inhibitors)

Therapeutic Areas

NeoplasmsNervous System DiseasesDigestive System Disorders+ [1]

Active Indication

Bile Duct NeoplasmsColorectal CancerGlioma+ [1]

Inactive Indication-

Originator Organization

Singapore General Hospital Pte Ltd.

Active Organization

Singapore General Hospital Pte Ltd.

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC33H38N4O6

InChIKeyUWKQSNNFCGGAFS-XIFFEERXSA-N

CAS Registry97682-44-5

In order to extract the profiles of patients receiving DEBIRI treatment at best, the investigators proposed the establishment of a national prospective cohort to collect information on the greatest number of patients treated with DEBIRI. This cohort will allow a better understanding of the effectiveness, tolerance, feasibility and differences of practices at national level for this approach. These data will assist in the development of clinical trials in situations that appear to be most promising in clinical practice.

Start Date03 Feb 2016

Sponsor / Collaborator

Fédération Francophone de la Cancérologie Digestive

NCT02110953

/ TerminatedPhase 1IIT

Phase I Study of Drug-Eluting Irinotecan Beads (DEBIRI) in Refractory Metastatic Colorectal Cancer With Liver-Only or Liver-Predominant Disease

This phase I trial studies the side effects and best dose of irinotecan-eluting beads in treating patients with colon or rectal cancer that has spread to the liver and does not respond to treatment with standard therapy. Irinotecan-eluting beads are tiny beads that have been loaded with irinotecan hydrochloride, a chemotherapy drug. Drugs used in chemotherapy, such as irinotecan hydrochloride, work in different ways to stop the growth of tumor cells, either by killing the cells or stopping them from dividing. This treatment delivers the chemotherapy directly to the tumor area inside the liver instead of to the whole body as with systemic delivery of the drug. Irinotecan-eluting beads may work better that standard chemotherapy in treating patients with colon or rectal cancer that has spread to the liver.

Start Date29 Jan 2016

Sponsor / Collaborator

The Fox Chase Cancer Center

[+1]

100 Clinical Results associated with Irinotecan-eluting beads

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100 Translational Medicine associated with Irinotecan-eluting beads

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100 Patents (Medical) associated with Irinotecan-eluting beads

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9,022

Literatures (Medical) associated with Irinotecan-eluting beads

03 May 2025·Journal of Biomolecular Structure and Dynamics

Synergy between human DNA ligase I and topoisomerase 1 unveils new therapeutic strategy for the management of colorectal cancer

Article

Author: Rawat, Rohit Singh ; Maurya, Pooja ; Banerjee, Dibyendu ; Siddiqi, Mohammad Imran ; Gupta, Sampa ; Krishna, Shagun ; Sashidhara, Koneni V.

DNA topoisomerase 1 (Topo 1) is a pivotal player in various DNA processes, including replication, repair, and transcription. It serves as a target for anticancer drugs like camptothecin and its derivatives (Topotecan and SN-38/Irinotecan). However, the emergence of drug resistance and the associated adverse effects, such as alopecia, anemia, dyspnea, fever, chills, and painful or difficult urination, pose significant challenges in Topo 1-targeted therapy, necessitating urgent attention. Human DNA Ligase 1 (hLig I), recognized primarily for its role in DNA replication and repair of DNA breaks, intriguingly exhibits a DNA relaxation activity akin to Topo 1. This raised the hypothesis that hLig I might compensate for Topo 1 inhibition, contributing to resistance against Topo 1 inhibitors. To explore this hypothesis, we assessed the efficacy of hLig I inhibition alone and in combination with Topo 1 in cancer cells. As anticipated, the overexpression of hLig I was observed after Topo 1 inhibition in colorectal cancer cells, affirming our hypothesis. Previously identified as an inhibitor of hLig I's DNA relaxation activity, compound 27 (C 27), when combined with Topotecan, demonstrated a synergistic antiproliferative effect on colorectal cancer cells. Notably, cells with downregulated hLig I (via siRNA, inhibitors, or genetic manipulation) exhibited significantly heightened sensitivity to Topotecan. This observation strongly supports the concept that hLig I contribute to resistance against clinically relevant Topo 1 inhibitors in colorectal cancers. In conclusion, our findings offer evidence for the synergistic impact of combining hLig I inhibitors with Topotecan in the treatment of colorectal cancers, providing a promising strategy to overcome resistance to Topo 1 inhibitors.Communicated by Ramaswamy H. Sarma.

01 Mar 2025·Macromolecular Bioscience

Sustained Drug Release from Dual‐Responsive Hydrogels for Local Cancer Chemo–Photothermal Therapy

Article

Author: Dao, Anh Thi Ngoc ; Suzuki, Ryuju ; Koseki, Yoshitaka ; Liu, Zhixiang ; Kasai, Hitoshi

AbstractAs an exceptional carrier for localized drug delivery to tumors, hydrogels can achieve prolonged drug release through careful design and adjustments, effectively targeting cancer cells and minimizing side effects. This study investigates a novel dual‐responsive hydrogel system designed for the delivery of nanomedicines, focusing on drug release and the local antitumor efficacy of SN‐38‐cholesterol nanoparticles (SN‐38‐chol NPs) and polydopamine NPs (PDA NPs)/poly(n‐isopropylacrylamide) (pNIPAM) hydrogels. By combining the thermosensitive properties of pNIPAM with the near‐infrared (NIR) responsiveness of PDA NPs, the hydrogel aims to enhance on‐demand drug release. SN‐38‐chol NPs, known for their stability and small size, are incorporated into the hydrogel to improve drug release dynamics. The investigation reveals a drug release cycle of over three weeks, maintaining sensitivity to both temperature and NIR light for controlled drug release. In vivo studies demonstrate the high tumor growth inhibition performance of the system after photothermal treatment induced by 808 nm NIR light. These results suggest that the drug‐carrying hydrogel system holds promise for diverse applications in chemical and physical therapies, including the treatment of malignant wounds, post‐surgery wound healing, and direct tumor treatment. This study establishes the potential of SN‐38‐chol NPs and PDA NPs/pNIPAM hydrogels as effective platforms for chemo‐phototherapy.

01 Mar 2025·European Journal of Medicinal Chemistry

Repurposing FDA-approved drugs to target G-quadruplexes in breast cancer

Article

Author: Marzano, Simona ; Randazzo, Antonio ; Landolfi, Laura ; Catalanotti, Bruno ; Malfitano, Anna Maria ; Pagano, Bruno ; Moraca, Federica ; Castellano, Giuliano ; Napolitano, Fabiana ; Arciuolo, Valentina ; Di Porzio, Anna ; D'Aria, Federica ; Amato, Jussara

Breast cancer, a leading cause of cancer-related mortality in women, is characterized by genomic instability and aberrant gene expression, often influenced by noncanonical nucleic acid structures such as G-quadruplexes (G4s). These structures, commonly found in the promoter regions and 5'-untranslated RNA sequences of several oncogenes, play crucial roles in regulating transcription and translation. Stabilizing these G4 structures offers a promising therapeutic strategy for targeting key oncogenic pathways. In this study, we employed a drug repurposing approach to identify FDA-approved drugs capable of binding and stabilizing G4s in breast cancer-related genes. Using ligand-based virtual screening and biophysical methods, we identified several promising compounds, such as azelastine, belotecan, and irinotecan, as effective G4 binders, with significant antiproliferative effects in breast cancer cell lines. Notably, belotecan and irinotecan exhibited a synergistic mechanism, combining G4 stabilization with their established topoisomerase I inhibition activity to enhance cytotoxicity in cancer cells. Our findings support the therapeutic potential of G4 stabilization in breast cancer, validate drug repurposing as an efficient strategy to identify G4-targeting drugs, and highlight how combining G4 stabilization with other established drug activities may improve anticancer efficacy.

100 Deals associated with Irinotecan-eluting beads

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External Link

KEGG	Wiki	ATC	Drug Bank
-	-	L01XX19	-

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Bile Duct Neoplasms	-	Singapore General Hospital Pte Ltd.	-
Colorectal Cancer	-	Singapore General Hospital Pte Ltd.	-
Glioma	-	Singapore General Hospital Pte Ltd.	-
Liver Cancer	-	Singapore General Hospital Pte Ltd.	-

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT01839877 (FFCD-1201 \| FFCD 1201, CTgov)	Phase 2	colon cancer liver metastasis	58	systemic FOLFOX+DEBIRI	(fiukjdqwtr) = qgjdojffux uglzkkvtqz (hnjusaacvb, mvvvxfnaia - nwqimbrlwq) View more	-	08 Oct 2024
ASCO2023	Not Applicable	Colorectal Liver Metastases	101	Irinotecan-eluting HepaSphere chemoembolization plus HAIC	(gkrcteajot) = 27.7% kclfkbvztk (vdjhmjrkck ) View more	Positive	31 May 2023
NCT01839877 (FFCD-1201, Pubmed \| Br J Cancer)	Phase 2	Colorectal Liver Metastases First line	-	DEBIRI plus mFOLFOX6	(nrtkcmslvm) = zetwjrknsv lvochyhkjo (ybknfjpjcq ) View more	-	18 Aug 2020
NCT02015754 (CTgov)	Phase 2	Colorectal Liver Metastases	14	TACE+DEBIRI	iwnvohkhlr(iikamtbrmf) = vwpkrqbbgw odbhwridgp (rirneskxbx, rkidrxrnlz - iujjjgxfua) View more	-	22 Mar 2018
ASCO_GI2015	Phase 2	Colorectal Liver Metastases	-	DEBIRI	(divdlazgnu) = nweoxvoyuk pjajhoyvob (eclqptakdz ) View more	Positive	20 Jan 2015
ASCO_GI2013	Not Applicable	Colorectal Liver Metastases Neoadjuvant	10	DEBIRI	bqqzdcabkl(sxjoodpuxs) = hzzmjgzoct aowubxhsoe (fujsjsdwtc ) View more	-	01 Feb 2013
ASCO_GI2012	Phase 3	Colorectal Liver Metastases	74	Polyvinyl alcohol microspheres loaded with irinotecan	pebjqgfqaz(ebpuyixcyz) = dfaupabxar dcslaxslma (sqctkexkms ) View more	Positive	01 Feb 2012
ASCO_GI2012	Phase 3	Colorectal Liver Metastases	74	Systemic chemotherapy	pebjqgfqaz(ebpuyixcyz) = hbxeifmzbv dcslaxslma (sqctkexkms ) View more	Positive	01 Feb 2012
ASCO2011	Not Applicable	Lung Cancer	16	drug-eluting beads (Segmental pulmonary arterial chemoembolization (SPACE) + RFA)	kdjexaphov(lhornbrgwa) = 1 bronco-pleural fistula (5%) oaldthqkdp (nmatukrpmg ) View more	-	20 May 2011
PRECISION V (ASCO2010)	Not Applicable	Hepatocellular Carcinoma	212	PRECISION TACE with drug-eluting beads (DC Beads)	(tsxaosctaz) = mgfqlflksq eitrfvccmv (mqpwtmlwny )	-	20 May 2010
PRECISION V (ASCO2010)	Not Applicable	Hepatocellular Carcinoma	212	PRECISION TACE with drug-eluting beads (conventional transarterial chemoembolization (cTACE))	(tsxaosctaz) = nrcyefjpyx eitrfvccmv (mqpwtmlwny )	-	20 May 2010
ASCO2010	Not Applicable	Hepatocellular Carcinoma	56	DEB-TACE with epirubicin drug-eluting beads	(mniyofibue) = mjwgojivmc oxpzigbcty (byigwuzlgn ) View more	-	20 May 2010