Delving into the Latest Updates on Amcasertib with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Amcasertib (USAN/INN)

+ [3]

Target

NANOG

Mechanism

NANOG modulators(Nanog homeobox modulators)

Therapeutic Areas

NeoplasmsDigestive System DisordersEndocrinology and Metabolic Disease+ [3]

Active Indication-

Inactive Indication

Advanced cancerAdvanced Hepatocellular CarcinomaAdvanced Malignant Solid Neoplasm+ [7]

Originator Organization

Avania LLC

Active Organization-

Inactive Organization

Sumitomo Pharma America, Inc.

Avania LLC

1Globe Biomedical Co Ltd

+ [1]

Drug Highest PhaseDiscontinuedPhase 2

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC31H33N5O2S

InChIKeyQDWKGEFGLQMDAM-UHFFFAOYSA-N

CAS Registry1129403-56-0

This is an open label, multi-center, phase II study of BBI503 administered to adult patients with advanced gastrointestinal stromal tumor who have exhausted all currently approved standard anti-cancer treatment options. BBI503 will be administered orally, daily, in continuous 28-day cycles at a dose of 300 mg once daily. Cycles will be repeated until patients are no longer clinically benefiting from therapy due to disease progression, adverse events, or another discontinuation criterion.
Safety, tolerability and efficacy of BBI503 will be assessed for the duration of study treatment.

Start Date13 Mar 2017

Sponsor / Collaborator

Sumitomo Pharma America, Inc.

NCT02232646

/ WithdrawnPhase 2

A Phase II Clinical Study of BBI503 in Adult Patients With Advanced Urologic Malignancies

This is an open label, multi-center, Phase II study of BBI503 administered to adult patients with selected advanced urologic malignancies. The primary objective of this study is to evaluate the disease control rate of patients with renal cell cancer and urothelial carcinoma treated with BBI503.

Start Date01 Jan 2017

Sponsor / Collaborator

Sumitomo Pharma America, Inc.

NCT02483247

/ CompletedPhase 1

A Phase Ib/II Clinical Study of BBI503 in Combination With Selected Anti-Cancer Therapeutics in Adult Patients With Advanced Cancer

This is an open label, multi-center, Phase 1/2 study of BBI503 administered in combination with selected anti-cancer therapeutics in adult patients with advanced cancer. The goal of the study is to determine the safety, tolerability, and RP2D of BBI503 in combination with each of the selected anti-cancer agents.

Start Date01 Sep 2015

Sponsor / Collaborator

Sumitomo Pharma America, Inc.

100 Clinical Results associated with Amcasertib

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100 Translational Medicine associated with Amcasertib

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100 Patents (Medical) associated with Amcasertib

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1

Literatures (Medical) associated with Amcasertib

Medical Oncology

Cancer stemness kinase inhibitor amcasertib: a promising therapeutic agent in ovarian cancer stem and cancer cell models with different genetic profiles

Article

Author: Asik, Aycan ; Guler Kara, Hale ; Gunduz, Cumhur ; Ozates, Neslihan Pinar

Ovarian cancer, often referred to as the 'silent killer,' is a significant contributor to mortality rates. Emerging evidence implicates Nanog as a potential therapeutic target in ovarian cancer. Amcasertib (BBI-503) is an orally administered primary class stemness kinase inhibitor that effectively targets NANOG and various cancer stem cell pathways by specifically inhibiting serine-threonine stemness kinases. This study aimed to evaluate the antineoplastic effects of Nanog inhibition, a critical transcription factor associated with pluripotency and its role in ovarian cancer tumorigenesis, using the novel therapeutic agent Amcasertib in ovarian cancer cells characterized by distinct genetic profiles. The cytotoxicity of Amcasertib was assessed in both ovarian cancer and cancer stem cell models utilizing the Xelligence-RTCA system. The impact of the determined IC50 dose on apoptosis, invasion, migration, epithelial-mesenchymal transition (EMT), cell cycle progression, colony formation, and spheroid growth was evaluated using appropriate analytical techniques. Our findings revealed that Amcasertib exhibited significant antiproliferative effects and induced apoptosis in ovarian cancer and cancer stem cells. Moreover, Amcasertib caused G1 phase arrest and impeded colony formation in MDAH-2774 cells. Additionally, Amcasertib effectively inhibited spheroid growth in OVCAR-3 and OCSC cells. Notably, it demonstrated the ability to suppress invasion and migration in MDAH-2774 and OCSC cells. Furthermore, the suppression of Nanog-mediated stem cell-like features by Amcasertib was particularly pronounced in ER-negative ovarian cancer and cancer stem cells, highlighting its high anticancer efficacy in this subgroup. These results suggest that Amcasertib holds promise as a potential standalone or combination therapy agent for the treatment of ER-negative ovarian cancer.

100 Deals associated with Amcasertib

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External Link

KEGG	Wiki	ATC	Drug Bank
D10903	-	-	DB14866

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Bile Duct Neoplasms	Phase 3	-	1Globe Biomedical Co Ltd	-
Hepatobiliary cancer	Phase 2	CA	Sumitomo Pharma America, Inc.	01 Feb 2015
Advanced Hepatocellular Carcinoma	Phase 2	US	Sumitomo Pharma America, Inc.	01 Dec 2014
Bile Duct Neoplasms	Phase 2	-	Avania LLC	-
Bile Duct Neoplasms	Phase 2	-	1Globe Biomedical Co Ltd	-
Bile Duct Neoplasms	Phase 2	-	Avania LLC	-
Hepatocellular Carcinoma	Phase 2	-	Avania LLC	-
Hepatocellular Carcinoma	Phase 2	-	Avania LLC	-
Hepatocellular Carcinoma	Phase 2	-	1Globe Biomedical Co Ltd	-
Hepatocellular Carcinoma	Phase 1	-	1Globe Biomedical Co Ltd	-

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT02432690 (CTgov)	Phase 2	Recurrent ovarian cancer	13	BBI503	djtvhnusbu(mozuxgboqh) = azdcjcgrmc bibaobbyyh (xdpmnvwgss, yxcahhqpbw - gfhyqworei) View more	-	29 Aug 2022
NCT01781455 (ASCO2017)	Phase 1/2	Adenoid Cystic Carcinoma	14	Amcasertib	(autofxeljz) = jblfgtspqv pyvfdqdpgh (xkzocnqrup ) View more	-	30 May 2017
NCT01781455 (ASCO2017)	Phase 1/2	Advanced Head and Neck Carcinoma	21	Amcasertib	(dnmlnjhscf) = uulmzqtoko zbmztzsgui (trbweflvlr ) View more	-	30 May 2017
NCT01781455 (ASCO2016)	Phase 1	Advanced Head and Neck Carcinoma	33	BB503	(gbzhfianxe) = Grade 3 AE included rapidly reversible diarrhea (n = 5) and nausea/vomiting (n = 1) rcgkrhtfnl (fjktqvuzgy )	Positive	20 May 2016
NCT01781455 (ASCO2015)	Phase 1	Advanced Colorectal Adenocarcinoma	47	BBI503 monotherapy	(wsyogfemta) = idlcjweeuc uufglrfdmd (jgotrfxwry )	-	20 May 2015
NCT01781455 (ASCO2014)	Phase 1	HR-positive/HER2-low Solid Tumors	26	BBI503	(rrdfrlsmmk) = oqfllgcfai pkiniwluyi (aawgcaedzt ) View more	-	20 May 2014