480448-29-1

Basic information

• Product Name: Edoxaban hydrochloride
• Synonyms: Edoxaban hydrochloride;N1-(5-Chloro-2-pyridinyl)-N2-[(1S,2R,4S)-4-[(dimethylamino)carbonyl]-2-[[(4,5,6,7-tetrahydro-5-methylthiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]cyclohexyl]ethanediamide hydrochloride;Edoxaban (HCl salt);Edoxaban Monohydrochloride;Edoxaban Hcl;N'-(5-chloropyridin-2-yl)-N-[(1S,2R,4S)-4-(dimethylcarbamoyl)-2-[(5-methyl-6,7-dihydro-4H-[1,3]thiazolo[5,4-c]pyridine-2-carbonyl)amino]cyclohexyl]oxamide:hydrochloride
• CAS NO: 480448-29-1
• Molecular Formula: C24H31Cl2N7O4S
• Molecular Weight: 584.51844
• Mol File: 480448-29-1.mol
• Article Data: 3

Chemical Properties

• Appearance: /
• CAS DataBase Reference: Edoxaban hydrochloride(CAS DataBase Reference)
• NIST Chemistry Reference: Edoxaban hydrochloride(480448-29-1)
• EPA Substance Registry System: Edoxaban hydrochloride(480448-29-1)

Safety Data

• Hazardous Substances Data: 480448-29-1(Hazardous Substances Data)

Usage

Description

Edoxaban hydrochloride, also known as Lixiana, is a direct inhibitor of Factor Xa (FXa) that was approved by the Minister of Health, Labor, and Welfare in Japan in April 2011. It is primarily used for the prevention of venous thromboembolism (VTE) after major orthopedic surgery. Edoxaban exhibits a high degree of selectivity for FXa, with a Ki value of 0.56 nM, and is a weak inhibitor of thrombin with a Ki value of 6000 nM. It also demonstrates selectivity over other serine proteases in the coagulation cascade and over trypsin and chymotrypsin. The synthesis of this class of FXa inhibitors starts with the assembly of the diaminocyclohexane scaffold, followed by the coupling of the P1 and P4 groups.

Uses

Used in Pharmaceutical Industry:
Edoxaban hydrochloride is used as an anticoagulant for the prevention of venous thromboembolism (VTE) after major orthopedic surgery. It functions by directly inhibiting Factor Xa (FXa), a key enzyme in the coagulation cascade, with high selectivity and potency. This selective inhibition helps to reduce the risk of blood clot formation without significantly affecting other serine proteases or trypsin and chymotrypsin, thus minimizing the risk of bleeding complications.
Used in Research and Development:
Edoxaban hydrochloride is also utilized in the research and development of novel anticoagulant therapies. Its high selectivity for FXa makes it a valuable compound for studying the role of FXa in various coagulation-related disorders and for developing new drugs with improved safety and efficacy profiles.

Originator

Daiichi Pharmaceutical (Japan)

Relevant articles and documents

SUSTAINED-RELEASE SOLID PREPARATION FOR ORAL USE

It is intended to avoid dose dumping of a drug and improve the dissolution properties of the drug in the lower gastrointestinal tract, and thereby provide a sustained-release matrix preparation for oral administration that reliably exhibits its main pharmacological effect when orally administered once or twice a day. The present invention provides a sustained-release preparation obtained by mixing of (A) a pharmacologically active drug, (B) hydroxypropyl methylcellulose acetate succinate having a median size (D50) of 40 μm or smaller, (C) a cellulose derivative, and (D) a saccharide or a nonionic water-soluble polymer followed by molding.

SUSTAINED-RELEASE SOLID PREPARATION FOR ORAL USE

It is intended to avoid dose dumping of a drug and improve the dissolution properties of the drug in the lower gastrointestinal tract, and thereby provide a sustained-release pellet preparation for oral administration that reliably exhibits its main pharmacological effect when orally administered once or twice a day. The present invention provides a sustained-release preparation obtained by mixing of (A) a pharmacologically active drug, (B) hydroxypropyl methylcellulose acetate succinate, (C) a plasticizer, and (D) polyethylene glycol followed by extrusion granulation.