EGFR antagonists(Epidermal growth factor receptor erbB1 antagonists), HER2 antagonists(Receptor tyrosine-protein kinase erbB-2 antagonists), HER4 antagonists(Receptor tyrosine-protein kinase erbB-4 antagonists)

Therapeutic Areas

NeoplasmsNervous System DiseasesEndocrinology and Metabolic Disease+ [2]

Active Indication

NeoplasmsAmyotrophic Lateral SclerosisHER2 Positive Breast Cancer

Inactive Indication-

Originator Organization

Shionogi & Co., Ltd.

Active Organization

Shionogi & Co., Ltd.Raya Therapeutic Inc.

Inactive Organization

EOC Pharma (Thaizhou) Co., Ltd.

License Organization

EOC Pharma (Thaizhou) Co., Ltd.

Shionogi & Co., Ltd.

Drug Highest PhasePhase 2

First Approval Date-

RegulationOrphan Drug (European Union)

Structure/Sequence

Molecular FormulaC30H27ClFN5O3

InChIKeyIBCIAMOTBDGBJN-NRLRZRKLSA-N

CAS Registry908305-13-5

100 Clinical Results associated with Epertinib

100 Translational Medicine associated with Epertinib

100 Patents (Medical) associated with Epertinib

Literatures (Medical) associated with Epertinib

01 May 2025·Journal of Mass Spectrometry

Development of High‐Throughput Quantitative Imaging Mass Spectrometry for Analysis of Drug Distribution in Tissues

Article

Author: Tanaka, Yukari

ABSTRACTMatrix‐assisted laser desorption/ionization–imaging mass spectrometry (MALDI–IMS) is applied in drug discovery and development. A high‐throughput quantitative MALDI–IMS methodology was developed to confirm whether epertinib is superior to lapatinib in penetrating brain metastases using intraventricular injection mouse models (IVMs) of human EGFR2 (HER2)‐positive breast or T790M–EGFR‐positive lung cancer cells. A simple calibration curve was prepared for each compound via spotting standard solutions without using blank tissue sections or blank tissues onto the same glass slide as the epertinib or lapatinib brain section samples. Quantitative MALDI–IMS was performed via coating a glass slide with a MALDI matrix solution containing each internal standard solution. The samples of calibration curve and brain section were analyzed using a linear ion trap mass spectrometer with a MALDI ion source. Epertinib and lapatinib responses were strongly linear, with a wide dynamic range and low variation (relative standard deviation [RSD] < 20%) among the individual concentrations. Epertinib and lapatinib were sufficiently extracted from brain sections after oral administration in a breast cancer IVM. The quantitative MALDI–IMS results revealed that the epertinib concentrations administered to the brain sections in the lung cancer IVM were similar to those measured using liquid chromatography–tandem mass spectrometry (LC–MS/MS). Quantitative MALDI–IMS, owing to its high reproducibility and throughput, is useful for selecting drug candidates in the early stages of discovery and development, enabling efficient and rapid screening of candidate compounds as well as an understanding of the mechanisms of drug efficacy, toxicity, and pharmacokinetics/pharmacodynamics.

01 Nov 2024·Biomedicine & Pharmacotherapy

Epertinib counteracts multidrug resistance in cancer cells by antagonizing the drug efflux function of ABCB1 and ABCG2

Article

Author: Li, Yen-Ching ; Ambudkar, Suresh V ; Lin, Bing-Huan ; Huang, Yang-Hui ; Wu, Yu-Shan ; Murakami, Megumi ; Wu, Chung-Pu ; Hung, Tai-Ho

A significant hurdle in cancer treatment arises from multidrug resistance (MDR), often due to overexpression of ATP-binding cassette (ABC) transporters like ABCB1 and/or ABCG2 in cancer cells. These transporters actively diminish the efficacy of cytotoxic drugs by facilitating ATP hydrolysis-dependent drug efflux and reducing intracellular drug accumulation in cancer cells. Addressing multidrug-resistant cancers poses a significant challenge due to the lack of approved treatments, prompting the exploration of alternative avenues like drug repurposing (also referred to as drug repositioning) of molecularly targeted agents to reverse MDR-mediated by ABCB1 and/or ABCG2 in multidrug-resistant cancer cells. Epertinib, a potent inhibitor of EGFR and HER2 currently in clinical trials for solid tumors, was investigated for its potential to resensitize ABCB1- and ABCG2-overexpressing multidrug-resistant cancer cells to chemotherapeutic agents. Our findings reveal that at sub-toxic, submicromolar concentrations, epertinib restores the sensitivity of multidrug-resistant cancer cells to cytotoxic drugs in a concentration-dependent manner. The results demonstrate that epertinib enhances drug-induced apoptosis in these cancer cells by impeding the drug-efflux function of ABCB1 and ABCG2 without altering their expression. ATPase activity and molecular docking were employed to reveal potential interaction sites between epertinib and the drug-binding pockets of ABCB1 and ABCG2. In summary, our study demonstrates an additional pharmacological capability of epertinib against the activity of ABCB1 and ABCG2. These findings suggest that incorporating epertinib into combination therapy could be advantageous for a specific patient subset with tumors exhibiting high levels of ABCB1 or ABCG2, warranting further exploration.

18 Jul 2023·Journal of molecular modeling

Identification of potential RapJ hits as sporulation pathway inducer candidates in Bacillus coagulans via structure-based virtual screening and molecular dynamics simulation studies.

Article

Author: Savardashtaki, Amir ; Mirmajidi, Seyedeh Habibeh ; Nezafat, Navid ; Ghasemi, Younes ; Negahdaripour, Manica ; Irajie, Cambyz

BACKGROUNDThe bacterium Bacillus coagulans has attracted interest because of its ability to produce spores and advantageous probiotic traits, such as facilitating food digestion in the intestine, managing some disorders, and controlling the symbiotic microbiota. Spore-forming probiotic bacteria are especially important in the probiotic industry compared to non-spore-forming bacteria due to their stability during production and high resistance to adverse factors such as stomach acid. When spore-forming bacteria are exposed to environmental stresses, they enter the sporulation pathway to survive. This pathway is activated by the final phosphorylation of the master regulator of spore response, Spo0A, and upon achieving the phosphorylation threshold. Spo0A is indirectly inhibited by some enzymes of the aspartate response regulator phosphatase (Rap) family, such as RapJ. RapJ is one of the most important Rap enzymes in the sporogenesis pathway, which is naturally inhibited by the pentapeptides.METHODSThis study used structure-based virtual screening and molecular dynamics (MD) simulation studies to find potential RapJ hits that could induce the sporulation pathway. The crystal structures of RapJ complexed with pentapeptide clearly elucidated their interactions with the enzyme active site.RESULTSBased on the binding compartment, through molecular docking, MD simulation, hydrogen bonds, and binding-free energy calculations, a series of novel hits against RapJ named tandutinib, infigratinib, sitravatinib, linifanib, epertinib, surufatinib, and acarbose were identified. Among these compounds, acarbose obtained the highest score, especially in terms of the number of hydrogen bonds, which plays a major role in stabilizing RapJ-ligand complexes, and also according to the occupancy percentages of hydrogen bonds, its hydrogen bonds were more stable during the simulation time. Consequently, acarbose is probably the most suitable hit for RapJ enzyme. Notably, experimental validation is crucial to confirm the effectiveness of the selected ligands.

100 Deals associated with Epertinib

R&D Status

10 top R&D records.

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Breast Cancer	Phase 2	France	Shionogi & Co., Ltd.	14 Nov 2017
Solid tumor	Phase 2	Europe	Shionogi & Co., Ltd.	19 Jan 2014
Neoplasms	Phase 2	-	Shionogi & Co., Ltd.	-
Amyotrophic Lateral Sclerosis	Preclinical	Canada	Raya Therapeutic Inc.	03 Mar 2025
HER2 Positive Breast Cancer	Preclinical	Japan	Shionogi & Co., Ltd.	01 Jul 2017

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


AACR2017	Phase 1	HER2 Positive Breast Cancer	-	S-222611	hmsndxhfpf(dyfpixgrmx) = wlcwbtzhpk obgagmeenf (wzmhqszthp ) View more	-	01 Jul 2017
ASCO2015	Phase 1	Brain metastases	76	S-222611 800mg	(jlagkhjffy) = cdixapicln jznvjghodj (uvaachpwvi ) View more	-	20 May 2015

Translational Medicine

Boost your research with our translational medicine data.

view full example data

Deal

Boost your decision using our deal data.

view full example data

Core Patent

Boost your research with our Core Patent data.

view full example data

Clinical Trial

Identify the latest clinical trials across global registries.

view full example data

Approval

Accelerate your research with the latest regulatory approval information.

view full example data

Regulation

Understand key drug designations in just a few clicks with Synapse.

view full example data

AI Agents Built for Biopharma Breakthroughs

Accelerate discovery. Empower decisions. Transform outcomes.

Get started for free today!

Accelerate Strategic R&D decision making with Synapse, PatSnap’s AI-powered Connected Innovation Intelligence Platform Built for Life Sciences Professionals.

Start your data trial now!

Synapse data is also accessible to external entities via APIs or data packages. Empower better decisions with the latest in pharmaceutical intelligence.

Bio

Bio Sequences Search & Analysis

Chemical

Chemical Structures Search & Analysis

Epertinib

Overview

Basic Info

Structure/Sequence

Related

R&D Status

Clinical Result

Translational Medicine

Deal

Core Patent

Clinical Trial

Approval

Regulation