Abstract: Provided herein is a combination of agents for reducing cell viability and/or cell proliferation. The combination comprises an FGFR4 inhibitor and an EGFR inhibitor.
Abstract: Linker-drug compounds and antibody-drug conjugates that bind to human oncology targets are disclosed. The linker-drug compounds and antibody-drug conjugates comprise a splicing modulator drug moiety. The disclosure further relates to methods and compositions for use in the treatment of neoplastic disorders by administering the antibody-drug conjugates provided herein. In an embodiment, the splicing modulator comprises a pladienolide or a pladienolide derivative.
Type:
Grant
Filed:
November 30, 2020
Date of Patent:
June 7, 2022
Assignee:
EISAI R&D MANAGEMENT CO., LTD.
Inventors:
Ermira Pazolli, Silvia Buonamici, Thiwanka Samarakoon, Sudeep Prajapati, Nathan Fishkin, James Palacino, Michael Seiler, Ping Zhu, Andrew Cook, Peter Smith, Xiang Liu, Shelby Ellery, Dominic Reynolds, Lihua Yu, Zhenhua Wu, Shouyong Peng, Nicholas Calandra, Megan Sheehan, Yonghong Xiao
Abstract: The present invention provides a method for producing active hepatocyte growth factor activator (HGFA) and active hepatocyte growth factor (HGF) without using animal serum. The present invention relates to a method for producing active HGFA without using animal serum. The method is characterized in that it comprises a step of obtaining a culture supernatant comprising pro-HGFA by culturing mammalian cells expressing inactive hepatocyte growth factor activator (pro-HGFA) in a medium without serum, and a step of adjusting the culture supernatant comprising pro-HGFA obtained in the above step to weakly acidic to convert pro-HGFA into active HGFA. The present invention also relates to a method for producing active HGF with HGFA produced by said method.
Abstract: The present invention provides an anti-APOA4 monoclonal antibody or an antibody fragment thereof capable of accurately measuring apolipoprotein A-IV (APOA4) in a specimen, a measurement method for immunologically measuring APOA4 using the antibody or the antibody fragment thereof, and a kit for measuring APOA4 containing the antibody or the antibody fragment thereof.
Abstract: An object of the present invention is to provide a lyophilized formulation having improved storage stability of hepatic growth factor compared to conventional lyophilized formulations. The present invention provides a lyophilized formulation comprising (1) a hepatic growth factor, (2) trehalose and (3) one or more compounds selected from the group consisting of arginine, histidine, lysine, meglumine, glutamic acid, aspartic acid, proline, creatine, creatinine, tris(hydroxymethyl)aminomethane, and pharmaceutically acceptable salts thereof.
Abstract: A salt of the compound represented by formula (1) and crystals thereof having the potential to be used as drug substances for pharmaceutical products.
Abstract: Provided is a therapeutic agent for Lewy body disease comprising (S)-7-(2-methoxy-3,5-dimethylpyridin-4-yl)-1-(tetrahydrofuran-3-yl)-1H-pyrazolo[4,3-c]quinolin-4(5H)-one represented by formula (I) or a pharmaceutically acceptable salt thereof.
Abstract: A combined administration of a liposomal composition comprising Eribulin or a pharmaceutically acceptable salt thereof and a PD-1 antagonist exhibits unexpected antitumor effect.
Type:
Application
Filed:
December 28, 2021
Publication date:
April 21, 2022
Applicants:
Eisai R&D Management Co., Ltd., Ono Pharmaceutical Co., Ltd.
Abstract: A method for the synthesis of diazabicyclo[6.2.0]decane compounds is provided. The synthesis proceeds by stereoselective synthesis of a chiral lactone followed by azetidine formation via a series of chemoselective reactions. Bicyclization results with the formation of diazobicyclo[6.2.0]decane related compounds.
Type:
Application
Filed:
January 9, 2020
Publication date:
April 14, 2022
Applicant:
Eisai R&D Management Co., Ltd.
Inventors:
Francis G. FANG, Branko MITASEV, Jiong YANG
Abstract: Antibodies, antigen-binding fragments, and conjugates (e.g., antibody-drug conjugates (ADCs) such as those comprising a splicing modulator) that bind to BCMA are disclosed. The disclosure further relates to methods and compositions for use in the treatment of cancer by administering a composition provided herein.
Type:
Application
Filed:
June 4, 2021
Publication date:
March 17, 2022
Applicant:
Eisai R&D Management Co., Ltd.
Inventors:
Ryan Henry, Thiwanka Samarakoon, Nathan Fishkin, Ping Zhu, Ermira Pazolli, James Palacino, Juan C. Almagro
Abstract: Provided is a compound represented by formula (IV) or a salt thereof, wherein the content of the compound represented by formula (I) is 350 ppm by mass or less.
Abstract: This disclosure provides methods for treating a hepatocellular carcinoma (e.g., unresectable HCC) with lenvatinib or a pharmaceutically acceptable salt thereof. Also encompassed by the disclosure are dosage regimens described herein of lenvatinib or a pharmaceutically acceptable salt thereof for use in treating hepatocellular carcinoma (e.g., unresectable hepatocellular carcinoma) according to any of the methods described herein. Particularly useful dosages and dose modifications upon the occurrence of an adverse event or events are also disclosed.
Abstract: The present disclosure describes combination therapies comprising an antagonist of Programmed Death 1 receptor (PD-1) and a multi-RTK inhibitor, and the use of the combination therapies for the treatment of cancer. The multi-RTK inhibitor may be represented by Formula (I): wherein R1 is C1-6 alkyl or C3-8 cycloalkyl, R2 is a hydrogen atom or C1-6 alkoxy, and R3 is a hydrogen atom or a halogen atom. A tumor therapeutic agent is disclosed that combines a compound or pharmaceutically acceptable salt thereof represented by Formula I and an anti-PD-1 antibody.
Abstract: An aqueous pharmaceutical formulation of a solubilizing agent with a pyridone compound that is useful as an inhibitor to non-NMDA receptors, particularly to the AMPA receptor is disclosed herein. In some embodiments the pyridone compound is supersaturated in aqueous solution at pH between 6 and 8. The formulations are particularly useful as intravenous injections.
Type:
Application
Filed:
December 16, 2019
Publication date:
January 27, 2022
Applicant:
Eisai R&D Management Co., Ltd.
Inventors:
Geoffrey S. HIRD, Ganesh S.P. BOMMAREDDY, Anjali JOSHI, Ph.D., James MCSHANE
Abstract: Provided are compounds represented by the following formulas (I), (II), (III) and (IV) having orexin type 2 receptor-activating activity, or their pharmaceutically acceptable salts.
Abstract: Disclosed is a therapeutic agent for hepatocellular carcinoma, comprising 5-((2-(4-(2-hydroxyethyl)piperidin-4-yl)benzamide)pyridin-4-yl)oxy)-6-(2-methoxyethoxy)-N-methyl-1H-indole-1-carboxamide or a pharmacologically acceptable salt thereof.
Abstract: The present invention provides a modified nucleic acid monomer compound having a specific backbone such as 2-ethylglycerol or methoxymethyl-1,3-propanediol backbone instead of a ribose or deoxyribose backbone of a nucleoside, and an oligonucleic acid analogue containing the monomer compound as at least one of building blocks. The oligonucleic acid analogue containing the nucleic acid monomer compound of the present invention allows provision of an oligonucleic acid analogue having excellent biological stability and/or target gene silencing activity.