Delving into the Latest Updates on E-7820 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

+ [1]

Target

CD49b

Mechanism

CD49b inhibitors(integrin subunit alpha 2 inhibitors)

Therapeutic Areas

NeoplasmsHemic and Lymphatic DiseasesOther Diseases+ [2]

Active Indication

Acute Myeloid LeukemiaChronic Myelomonocytic LeukemiaMyelodysplastic Syndromes+ [2]

Inactive Indication

Advanced Colorectal AdenocarcinomaAdvanced Malignant Solid NeoplasmColonic Cancer+ [4]

Originator Organization

Eisai Co., Ltd.

Active Organization

Eisai, Inc.

Cancer Therapy & Research Center Endowment

Memorial Sloan Kettering Cancer Center

Inactive Organization-

Drug Highest PhasePhase 2

First Approval Date-

Regulation-

Login to view timeline

Structure

Molecular FormulaC17H12N4O2S

InChIKeyLWGUASZLXHYWIV-UHFFFAOYSA-N

CAS Registry289483-69-8

The researchers are doing this study to find out whether E7820 is an effective treatment for people with relapsed/refractory myeloid cancers with mutations in splicing factor genes. Participants will have acute myeloid leukemia (AML), myelodysplastic syndromes (MDS), or chronic myelomonocytic leukemia (CMML).

Start Date13 Aug 2021

Sponsor / Collaborator

Memorial Sloan Kettering Cancer Center

[+1]

NCT01347645 / TerminatedPhase 1/2

An Open-Label, Multicenter, Randomized Phase Ib/II Study of Irinotecan Plus E7820 Versus FOLFIRI in Second-Line Therapy in Patients With Locally Advanced or Metastatic Colon or Rectal Cancer

The purpose of the Phase Ib portion is to find out the highest dose of study drug that can safely be given when tested in a small group of subjects.
The purpose of the Phase II portion is to find out how safe the study drug is when taken at the highest dose in a larger group of subjects.

Start Date30 Sep 2011

Sponsor / Collaborator

Eisai, Inc.

[+1]

NL-OMON36618 / CompletedNot Applicable

An Open-label, Dose Escalation, Pharmacodynamic, Pharmacokinetic, and Effect of Food Phase 1 Study of E7820, Administered as a Once Daily and Twice Daily Oral Dose to Determine the Maximum Tolerated Dose in Subjects with Unresectable Solid Tumors - Treatment of Unresectable Solid Tumors with E7820

Start Date18 Jul 2011

Sponsor / Collaborator

Eisai Co., Ltd.

100 Clinical Results associated with E-7820

Login to view more data

100 Translational Medicine associated with E-7820

Login to view more data

100 Patents (Medical) associated with E-7820

Login to view more data

23

Literatures (Medical) associated with E-7820

01 Dec 2023·Leukemia

E7820, an anti-cancer sulfonamide, degrades RBM39 in patients with splicing factor mutant myeloid malignancies: a phase II clinical trial

Article

Author: Hogg, Simon J ; Mi, Xiaoli ; Taylor, Justin ; Lu, Sydney X ; Bourcier, Jessie ; Wysocki, Mateusz ; Chaudhry, Sana ; Stahl, Maximilian ; Bewersdorf, Jan Philipp ; Rahman, Jahan ; Watts, Justin ; Stein, Eytan M ; Abdel-Wahab, Omar ; Chandhok, Namrata Sonia ; Totiger, Tulasigeri M ; Derkach, Andriy

06 Jan 2023·Japanese Journal of Clinical Oncology

Integrin alpha 2 is associated with tumor progression and postoperative recurrence in non-small cell lung cancer

Article

Author: Watanabe, Kousuke ; Kage, Hidenori ; Zokumasu, Koichi ; Nakajima, Jun ; Ando, Takahiro ; Kawakami, Masanori ; Nagase, Takahide ; Ushiku, Tetsuo ; Hinata, Munetoshi ; Matsumoto, Yoko ; Maemura, Keita ; Morota, Mizuki

AbstractBackgroundIntegrins are transmembrane proteins that mediate cell adhesion to extracellular matrix. Whereas expression of integrin alpha 2 is associated with motility, invasiveness and cellular differentiation in various tumors, the role of integrin alpha 2 in lung cancer has not been studied in detail. The aim of this study was to determine whether and how aberrant integrin alpha 2 expression in non-small cell lung cancer leads to different outcomes.MethodsWe measured expression of integrin alpha 2 by quantitative polymerase chain reaction in 100 samples collected from non-small cell lung cancer patients who had undergone surgical resection. We assigned patients to high and low expression groups and analyzed survival. Cellular morphology, adhesion, proliferation, migration and invasion were examined in human lung cancer cell lines.ResultsAmong 100 cases, 41 were female, with a median age of 71 years. High expression of integrin alpha 2 in non-small cell lung cancer was associated with lower recurrence-free survival (P = 0.004). Overexpression of integrin alpha 2 in cell lines had no effect on cell proliferation or invasion but resulted in increased cell size (1416 μm2 versus 470 μm2 in H522 cells, P < 0.001; 1822 μm2 versus 1029 μm2 in H661 cells, P = 0.02), adhesion (P < 0.001 in H522 and H661 cells) and migration (gap area filled was 71% versus 36% in H522 cells, P < 0.001; 57% versus 26% in H661 cells, P = 0.001). These changes were suppressed by E7820, an inhibitor of integrin alpha 2.ConclusionsIntegrin alpha 2 may play a significant role in lung cancer adhesion and migration, and may lead to a higher risk of recurrence.

01 Oct 2022·Toxicological Research

Role of integrin α2 in methotrexate-induced epithelial-mesenchymal transition in alveolar epithelial A549 cells

Article

Author: Takano, Mikihisa ; Ojima, Takamichi ; Yumoto, Ryoko ; Kawami, Masashi

Methotrexate (MTX) is widely used to treat various diseases. However, it induces adverse reactions like serious lung injury, including pulmonary fibrosis. Increasing evidence suggests that epithelial-mesenchymal transition (EMT) in injured alveolar epithelium contributes to the development of the pathophysiological state of the lung. We demonstrated that MTX induced EMT in cultured alveolar epithelial cell lines. Integrin-mediated signaling is considered a significant factor in recognizing the EMT process. However, the relationship between MTX-induced EMT and integrin family members is poorly understood. In the present study, we aimed to clarify the role of integrin in MTX-induced EMT in A549 and NCI-H1299 (H1299) cells by focusing on the integrin alpha 2 (ITGA2) subunit, selected based on our microarray analysis. MTX treatment for 72 h significantly increased the mRNA and cell surface expression of ITGA2 in both cell lines. However, this upregulation by MTX was suppressed by co-treatment with SB431542 and folic acid, which are inhibitors of MTX-induced EMT in A549 cells. The mRNA expression levels of EMT-related genes were more affected in the MTX-treated A549 cells with high ITGA2 expression than in those with low ITGA2 expression. Finally, E7820, an ITGA2 inhibitor, suppressed MTX-induced EMT-related phenotypic changes, such as morphology and mRNA and protein expression of α-smooth muscle actin, a representative EMT marker. These findings suggest that ITGA2 may play a key role in MTX-induced EMT in alveolar epithelial cells.

100 Deals associated with E-7820

Login to view more data

External Link

KEGG	Wiki	ATC	Drug Bank
-	-	-	DB12505

R&D Status

10 top R&D records.

Login

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Advanced Malignant Solid Neoplasm	Phase 1	CA	Eisai, Inc.	24 Sep 2007
Rectal Cancer	Preclinical	AU	Eisai, Inc.	30 Sep 2011
Rectal Cancer	Preclinical	BR	Eisai, Inc.	30 Sep 2011
Rectal Cancer	Preclinical	UA	Eisai, Inc.	30 Sep 2011
Rectal Cancer	Preclinical	US	Eisai, Inc.	30 Sep 2011
Rectal Cancer	Preclinical	AR	Eisai, Inc.	30 Sep 2011
Colorectal Cancer	Preclinical	IN	Eisai, Inc.	04 Mar 2010
Advanced Colorectal Adenocarcinoma	Discovery	CA	Eisai, Inc.	24 Sep 2007
Advanced Colorectal Adenocarcinoma	Discovery	US	Eisai, Inc.	24 Sep 2007
Advanced Malignant Solid Neoplasm	Discovery	US	Eisai, Inc.	24 Sep 2007

Login to view more data

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT01347645 (CTgov)	Phase 1/2	Rectal Cancer \| Colonic Cancer	82	E7820+irinotecan (Phase 1b, All Participants)	hrhywrlirv(xcjkhubrrt) = gmymizerpu tmlrpdiyns (hqwjdkdsze, wjlztdjwft - urenlruopo)	-	25 Nov 2022
NCT01347645 (CTgov)	Phase 1/2	Rectal Cancer \| Colonic Cancer	82	E7820+Irinotecan (Phase 2: E7820 70 mg + Irinotecan)	(vjrihagajl) = vrdxzxnzhq rhvwshjpvc (fvjdamqawu, vtwknotimf - vjhhouirhv) View more	-	25 Nov 2022
NCT05024994 (ASH2022) Manual	Phase 2	Myeloid Tumor	12	E7820	(rdpxwnndre) = bmgvfcwyeq xlblvwzxur (ggghyzvkmn, 1.5 - NR) View more	Positive	15 Nov 2022
NCT01773421 (CTgov)	Phase 1	Advanced Malignant Solid Neoplasm \| Unresectable Solid Neoplasm	45	E7820 (Treatment Phase Part A: E7820 50 mg Fed)	pynydvqada(jsclqhycka) = kgrzbddynm hlexbvmebo (zenjtepmoa, tsjmpzvpna - xfehjsblvj) View more	-	18 Jan 2020
NCT01773421 (CTgov)	Phase 1		45	E7820 (Treatment Phase Part A: E7820 50 mg Fasted)	pynydvqada(jsclqhycka) = zfldjrcnre hlexbvmebo (zenjtepmoa, cbtflwrtsd - qsbmmuymog) View more	-	18 Jan 2020
ASCO2010	Phase 2	Refractory Colorectal Carcinoma \| Metastatic Colorectal Carcinoma	28	E7820	gxwfmbysxe(aebydwqhji) = E7820 related-grade 3 toxicities included increased AST (3/28, 11%), increased ALT (2/28, 7%), and diarrhea, hypomagnesemia, decreased glomerular filtration rate and elevated creatinine (1/28, 3% in each) xhrtfdkcqa (wewhvkloaw ) View more	Negative	20 May 2010
ASCO2008	Phase 1	HR-positive/HER2-low Solid Tumors	17	E7820	(wbrhzuwiyg) = wacuxvjduc ilkhfvvrsd (ovhovezlfa ) View more	-	20 May 2008
ASCO2006	Phase 1	Solid tumor	30	E7820	(gcndpmvrhm) = iagiwzgqot ytbcguxpgk (guaaiwfree )	-	20 Jun 2006