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药品详细

Caspofungin(卡泊芬净)

化学结构式图
中文名
卡泊芬净
英文名
Caspofungin
分子式
C52H88N10O15
化学名
N-[(3S,6S,9S,11R,15S,18S,20R,21S,24S,25S)-3-[(1R)-3-amino-1-hydroxypropyl]-21-[(2-aminoethyl)amino]-6-[(1S,2S)-1,2-dihydroxy-2-(4-hydroxyphenyl)ethyl]-11,20,25-trihydroxy-15-[(1R)-1-hydroxyethyl]-2,5,8,14,17,23-hexaoxo-1,4,7,13,16,22-hexaazatricyclo[22.3.0.0^{9,13}]heptacosan-18-yl]-10,12-dimethyltetradecanamide
分子量
Average: 1093.3131
Monoisotopic: 1092.643062196
CAS号
179463-17-3
ATC分类
J02A Antimycotics for Systemic Use
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

Caspofungin (brand name Cancidas worldwide) is an antifungal drug, the first of a new class termed the echinocandins from Merck & Co., Inc. It shows activity against infections with Aspergillus and Candida, and works by inhibiting β(1,3)-D-Glucan of the fungal cell wall. Caspofungin is administered intravenously.

生产厂家
  • Merck and co inc
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Letscher-Bru, Valérie, and Raoul Herbrecht. 2003. Caspofungin: the first representative of a new antifungal class. Journal of Antimicrobial Chemotherapy 51, no. 3 (March 1): 513 -521. doi:10.1093/jac/dkg117.
  2. Sucher AJ, Chahine EB, Balcer HE: Echinocandins: the newest class of antifungals. Ann Pharmacother. 2009 Oct;43(10):1647-57. Epub 2009 Sep 1. Pubmed
  3. Morrison VA: Caspofungin: an overview. Expert Rev Anti Infect Ther. 2005 Oct;3(5):697-705. Pubmed
  4. McCormack PL, Perry CM: Caspofungin: a review of its use in the treatment of fungal infections. Drugs. 2005;65(14):2049-68. Pubmed
  5. Morris MI, Villmann M: Echinocandins in the management of invasive fungal infections, part 1. Am J Health Syst Pharm. 2006 Sep 15;63(18):1693-703. Pubmed
  6. Morris MI, Villmann M: Echinocandins in the management of invasive fungal infections, Part 2. Am J Health Syst Pharm. 2006 Oct 1;63(19):1813-20. Pubmed
剂型
规格
化合物类型
Type small molecule
Classes
  • Echinocandins
  • Lactams
Substructures
  • Echinocandins
  • Hydroxy Compounds
  • Benzyl Alcohols and Derivatives
  • Phenols and Derivatives
  • Amino Ketones
  • Aliphatic and Aryl Amines
  • Pyrrolidines
  • Benzene and Derivatives
  • Carboxylic Acids and Derivatives
  • Aminals and Derivatives
  • Alcohols and Polyols
  • Heterocyclic compounds
  • Aromatic compounds
  • Carboxamides and Derivatives
  • Phenylpropylamines
  • Lactams
  • Tyrosols
  • Phenyl Esters
适应症
药理
Indication For the treatment of esophageal candidiasis and invasive aspergillosis in patients who are refractory to or intolerant of other therapies.
Pharmacodynamics Caspofungin is an antifungal drug, and belongs to a new class termed the echinocandins. It is used to treat Aspergillus and Candida infection, and works by inhibiting cell wall synthesis. Antifungals in the echinocandin class inhibit the synthesis of glucan in the cell wall, probably via the enzyme 1,3-beta glucan synthase. There is a potential for resistance development to occur, however in vitro resistance development to Caspofungin by Aspergillus species has not been studied.
Mechanism of action Caspofungin inhibits the synthesis of beta-(1,3)-D-glucan, an essential component of the cell wall of Aspergillus species and Candida species. beta-(1,3)-D-glucan is not present in mammalian cells. The primary target is beta-(1,3)-glucan synthase.
Absorption 92% tissue distribution within 36-48 hours after intravenous infusion
Volume of distribution Not Available
Protein binding 97%
Metabolism
Metabolized slowly by hydrolysis and N-acetylation
Route of elimination After single intravenous administration of [3H] caspofungin acetate, excretion of caspofungin and its metabolites in humans was 35% of dose in feces and 41% of dose in urine.
Half life 9-11 hours
Clearance
  • 12 mL/min [After single IV administration]
Toxicity Side effects include rash, swelling, and nausea (rare)
Affected organisms
  • Aspergillis, Candida and other fungi
Pathways Not Available
理化性质
Properties
State solid
Experimental Properties
Property Value Source
logP 0 Not Available
Predicted Properties
Property Value Source
water solubility 3.67e-01 g/l ALOGPS
logP 0.17 ALOGPS
logP -4.8 ChemAxon
logS -3.5 ALOGPS
pKa (strongest acidic) 8.75 ChemAxon
pKa (strongest basic) 9.76 ChemAxon
physiological charge 2 ChemAxon
hydrogen acceptor count 18 ChemAxon
hydrogen donor count 16 ChemAxon
polar surface area 412.03 ChemAxon
rotatable bond count 23 ChemAxon
refractivity 278.78 ChemAxon
polarizability 117.52 ChemAxon
药物相互作用
Drug Interaction
Cyclosporine Cyclosporine increases the effect and toxicity of caspofungin
Rifampin Decreased levels/effects of caspofungin
Tacrolimus Caspofungin may decrease the blood concentration of Tacrolimus. Monitor for changes in the therapeutic/toxic effects of Tacrolimus if Caspofungin therapy is initiated, discontinued or altered.
食物相互作用
Not Available

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