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药品详细

Mycophenolic acid (霉酚酸 )

化学结构式图
中文名
霉酚酸
英文名
Mycophenolic acid
分子式
Not Available
化学名
(4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enoic acid
分子量
Average: 320.3371
Monoisotopic: 320.125988372
CAS号
24280-93-1
ATC分类
L04A 未知
药物类型
small molecule
阶段
商品名
Melbex;Myfortic;
同义名
Mycophenoic acid;
基本介绍

Mycophenolic acid is an an immunosuppresant drug and potent anti-proliferative, and can be used in place of the older anti-proliferative azathioprine. It is usually used as part of triple therapy including a calcineurin inhibitor (ciclosporin or tacrolimus) and prednisolone. It is also useful in research for the selection of animal cells that express the E. coli gene coding for XGPRT (xanthine guanine phosphoribosyltransferase).

生产厂家
  • Novartis pharmaceuticals corp
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Woodroffe R, Yao GL, Meads C, Bayliss S, Ready A, Raftery J, Taylor RS: Clinical and cost-effectiveness of newer immunosuppressive regimens in renal transplantation: a systematic review and modelling study. Health Technol Assess. 2005 May;9(21):1-179, iii-iv. Pubmed
剂型
Form Route Strength
Tablet, coated Oral
规格
Unit description Cost Unit
Myfortic 360 mg Enteric Coated Tabs 8.0 USD tab
Myfortic 360 mg tablet 7.69 USD tablet
Myfortic 180 mg tablet 3.85 USD tablet
化合物类型
Type small molecule
Classes
  • Salicylates and Derivatives
  • Benzene and Derivatives
  • Benzyl Esters
  • Benzylacetates
  • Methoxyphenols
Substructures
  • Carboxylic Acids and Derivatives
  • Benzofurans
  • Hydroxy Compounds
  • Alkanes and Alkenes
  • Benzyl Alcohols and Derivatives
  • Acetates
  • Benzoates
  • Salicylates and Derivatives
  • Phenols and Derivatives
  • Lactones
  • Ethers
  • Benzene and Derivatives
  • Benzyl Esters
  • Benzylacetates
  • Methoxyphenols
  • Heterocyclic compounds
  • Aromatic compounds
  • Anisoles
  • Benzoyl Derivatives
  • Phenyl Esters
适应症
IMMUNOSUPPRESSIVE 免疫抑制;
药理
Indication For the prophylaxis of organ rejection in patients receiving allogeneic renal transplants, administered in combination with cyclosporine and corticosteroids.
Pharmacodynamics Mycophenolic acid is an antibiotic substance derived from Penicillium stoloniferum. It blocks de novo biosynthesis of purine nucleotides by inhibition of the enzyme inosine monophosphate dehydrogenase. Mycophenolic acid is important because of its selective effects on the immune system. It prevents the proliferation of T-cells, lymphocytes, and the formation of antibodies from B-cells. It also may inhibit recruitment of leukocytes to inflammatory sites.
Mechanism of action Mycophenolic acid is a potent, selective, uncompetitive, and reversible inhibitor of inosine monophosphate dehydrogenase (IMPDH), and therefore inhibits the de novo pathway of guanosine nucleotide synthesis without incorporation into DNA. Because T- and B-lymphocytes are critically dependent for their proliferation on de novo synthesis of purines, whereas other cell types can utilize salvage pathways, mycophenolic acid has potent cytostatic effects on lymphocytes. Mycophenolic acid inhibits proliferative responses of T- and B-lymphocytes to both mitogenic and allospecific stimulation. Addition of guanosine or deoxyguanosine reverses the cytostatic effects of mycophenolic acid on lymphocytes. Mycophenolic acid also suppresses antibody formation by B-lymphocytes. Mycophenolic acid prevents the glycosylation of lymphocyte and monocyte glycoproteins that are involved in intercellular adhesion to endothelial cells and may inhibit recruitment of leukocytes into sites of inflammation and graft rejection.
Absorption Bioavailability following oral administration of Myfortic delayed-release tablet ranges from 70-95%
Volume of distribution
  • 54 卤 25 L
Protein binding >98%
Metabolism

Mycophenolic acid is metabolized mainly by glucuronyl transferase to glucuronidated metabolites, predominantly the phenolic glucuronide, mycophenolic acid glucuronide (MPAG). MPAG does not manifest pharmacological activity. The acyl glucuronide minor metabolite has pharmacological activity similar to mycophenolic acid. The AUC ratio of Mycophenolic acid:MPAG:acyl glucuronide is approximately 1:24:0.28 at steady state.
Route of elimination Not Available
Half life The mean elimination half-life for mycophenolic acid ranges from 8-16 hours, while that of the MPAG metabolite ranges from 13-17 hours.
Clearance
  • 140 +/- 30 mL/min [Stable renal transplant patients]
Toxicity Oral (LD50): Acute: 352 mg/kg [Rat], 1000 mg/kg [Mouse], and >6000 mg/kg [Rabbit]. Possible signs and symptoms of acute overdose could include the following: hematological abnormalities such as leukopenia and neutropenia, and gastrointestinal symptoms such as abdominal pain, diarrhea, nausea and vomiting, and dyspepsia.
Affected organisms
  • Humans and other mammals
Pathways Not Available
理化性质
Properties
State solid
Melting point 141 oC
Experimental Properties
Property Value Source
water solubility Insoluble PhysProp
logP 2.8 PhysProp
Predicted Properties
Property Value Source
water solubility 3.55e-02 g/l ALOGPS
logP 2.36 ALOGPS
logP 3.53 ChemAxon Molconvert
logS -3.96 ALOGPS
pKa 9.76 ChemAxon Molconvert
hydrogen acceptor count 5 ChemAxon Molconvert
hydrogen donor count 2 ChemAxon Molconvert
polar surface area 93.06 ChemAxon Molconvert
rotatable bond count 6 ChemAxon Molconvert
refractivity 85.23 ChemAxon Molconvert
polarizability 32.95 ChemAxon Molconvert
药物相互作用
Drug Interaction
Trastuzumab Trastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events.
Valganciclovir The excretion rates of Valganciclovir and/or Mycophenolic acid may decrease. Monitor for increased serum concentrations and toxicity of both agents.
食物相互作用
Not Available

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