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Saxagliptin hydrate

Saxagliptin hydrate structure

CAS No:
945667-22-1
Formula:
C18H27N3O3
Chemical Name:
Saxagliptin hydrate
Synonyms:
2-Azabicyclo[3.1.0]hexane-3-carbonitrile, 2-[(2S)-2-amino-2-(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)acetyl]-, hydrate (1:1), (1S,3S,5S)-;Saxagliptin hydrate;Saxagliptin hydrate Unii-9gb927lajw;(1S,3S,5S)-2-[(2S)-2-Amino-2-(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile hydrate;Saxagliptin hydrate (1S,3S,5S)-2-[(2S)-2-Amino-2-(3-hydroxytricyclo[3.3.1.1(3,7)]dec-1-yl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile hydrate;CS-1180;BMS 477118 hydrate;BMS477118 hydrate
Categories:
Active Pharmaceutical Ingredients > Other Chemical Drugs

Description

Saxagliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor which is used in combination with diet and exercise in the therapy of type 2 diabetes, either alone or in combination with other oral hypoglycemic agents. Saxagliptin is a relatively new medication and has yet to be implicated in causing clinically apparent liver injury.

While liraglutide targets the incretin system as a GLP-1 analog for therapeutic intervention in T2DM, saxagliptin enhances GLP-1 plasma concentrations by inhibiting the DPP-4 enzyme responsible for degradation of GLP-1 by cleavage of the two N-terminal amino acids adjacent to alanine (or proline), thereby rendering the hormone inactive. Similarto vildagliptin, saxagliptin is a cyanopyrrolidine substrate-based inhibitor. The proline mimetic occupies the small S1-pocket while the nitrile’s trajectory aligns with the scissile bond of the substrate. The slow dissociation kinetics of saxagliptin is attributed to a reversible, covalent reaction between the nitrile and the catalytically active serine hydroxyl (Ser630). The steric bulk provided by the adamantyl moiety and the constrained cyclopropyl ring stabilizes the trans-rotamer of the amide, thereby preventing the problematic intramolecular cyclization, via the amino group attacking the nitrile, which is favored in the cis-conformation.Since metabolism of saxagliptin is primarily mediated by CYP3A4/5, there is a potential for drug interactions with concomitant administration of strong inducers or inhibitors of these cytochrome P450 enzymes. The most common adverse events (>5% of patients) included upper respiratory tract infection, urinary tract infection, and headache.

ChEBI: Saxagliptin hydrate is a hydrate that is the monohydrate form of anhydrous saxagliptin. Used for the treatment of Type II diabetes. It has a role as a hypoglycemic agent and an EC 3.4.14.5 (dipeptidyl-peptidase IV) inhibitor. It contains a saxagliptin.

Saxagliptin hydrate Basic Attributes

Molecular Weight：

333.43

Exact Mass：

333.20524173

EC Number：

641-082-3

Color/Form：

White to Off-White

Characteristics

Melting Point：

106-108°C

Critical Temperature & Pressure：

-20°C Freezer

Safety Information

wgk germany：

WGK 3

GHS Classification：

|Danger|H317 (88.89%): May cause an allergic skin reaction [Warning Sensitization, Skin]|P201, P202, P260, P261, P264, P270, P272, P280, P281, P285, P302+P352, P304+P341, P308+P313, P314, P321, P333+P313, P342+P311, P363, P405, and P501|Aggregated GHS information provided by 9 companies from 2 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Toxicity

Hepatotoxicity：

In large clinical trials, rates of serum enzyme elevations were similar with saxagliptin therapy (

Drug Information

LiverTox Summary：

Drug Classes：

Antidiabetic Agents

Saxagliptin hydrate Use and Manufacturing

Saxagliptin Hydrate is a selective and reversible dipeptidyl peptidase-4 (DPP4) inhibitor that may be used to develop treatment for type 2 diabetes.

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