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药品详细

Amlexanox(氨来呫诺)

化学结构式图
中文名
氨来呫诺
英文名
Amlexanox
分子式
C16H14N2O4
化学名
2-amino-5-oxo-7-(propan-2-yl)-5H-chromeno[2,3-b]pyridine-3-carboxylic acid
分子量
Average: 298.2934
Monoisotopic: 298.095356946
CAS号
68302-57-8
ATC分类
A01A 未知;R03D 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

Amlexanox is an antiallergic drug, clinically effective for atopic diseases, especially allergic asthma and rhinitis. Amlexanox as a topical paste is a well tolerated treatment of recurrent aphthous ulcers. Recurrent aphthous ulcer (RAU) is the most prevalent oral mucosal disease in humans, estimated to affect between 5% and 50% of the general population.

生产厂家
  • Uluru inc
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Bell J: Amlexanox for the treatment of recurrent aphthous ulcers. Clin Drug Investig. 2005;25(9):555-66. Pubmed
剂型
规格
化合物类型
Type small molecule
Classes
  • Chromones
Substructures
  • Hydroxy Compounds
  • Acetates
  • Pyridines and Derivatives
  • Aliphatic and Aryl Amines
  • Benzene and Derivatives
  • Chromones
  • Carboxylic Acids and Derivatives
  • Aminopyridines and Derivatives
  • Heterocyclic compounds
  • Aromatic compounds
适应症
药理
Indication Used as a paste in the mouth to treat aphthous ulcers (canker sores).
Pharmacodynamics Amlexanox is a mucoadhesive oral paste which has been clinically proven to abort the onset, accelerate healing and resolve the pain of aphthous ulcers (canker sores). It decreases the time ulcers take to heal. Because amlexanox decreases the healing time, it also decreases the pain you feel. Recent studies have also shown that the majority of ulcers can be prevented by application of the paste during the prodromal (pre-ulcerative) phase of the disease. Recurrent Aphthous Ulcers (RAU) also known as Recurrent Aphthous Stomatitis (RAS) is recognized as the most common oral mucosal disease known to man. Estimates suggest that 20% - 25% of the general population suffer at least one incidence of aphthous ulcers each year. Amlexanox is also being investigated for its anti-allergenic and anti-inflammatory properties.
Mechanism of action As a benzopyrano-bipyridine carboxylic acid derivative, amlexanox has anti-inflammatory and antiallergic properties. It inhibits chemical mediatory release of the slow-reacting substance of anaphylaxis (SRS-A) and may have antagonistic effects on interleukin-3. When cells are under stress, they release an inactive form of human fibroblast growth factor 1 (FGF-1), a potent mitogen (entity that causes mitosis). Amlexanox binds to FGF1, increasing its conformational stability, sterically blocking Cu(2+) induced oxidation which normally leads to activation of FGF-1.
Absorption No significant absorption directly through the active ulcer. Most of the systemic absorption is via the gastrointestinal tract.
Volume of distribution Not Available
Protein binding Not Available
Metabolism
Metabolized to hydroxylated and conjugated metabolites.
Route of elimination Not Available
Half life Elimination half-life is 3.5 ± 1.1 hours.
Clearance Not Available
Toxicity Not Available
Affected organisms
  • Humans and other mammals
Pathways Not Available
理化性质
Properties
State solid
Experimental Properties
Property Value Source
logP 4.1 Not Available
Predicted Properties
Property Value Source
water solubility 1.46e-01 g/l ALOGPS
logP 2.76 ALOGPS
logP 3.65 ChemAxon
logS -3.3 ALOGPS
pKa (strongest acidic) 4.3 ChemAxon
pKa (strongest basic) 0.87 ChemAxon
physiological charge -1 ChemAxon
hydrogen acceptor count 5 ChemAxon
hydrogen donor count 2 ChemAxon
polar surface area 102.51 ChemAxon
rotatable bond count 2 ChemAxon
refractivity 81.43 ChemAxon
polarizability 30.82 ChemAxon
药物相互作用
食物相互作用
Not Available

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