ミコフェノール酸モフェチル 化學(xué)特性,用途語,生産方法
外観
白色～ほとんど白色粉末～結(jié)晶
用途
免疫抑制薬核酸合成阻害作用による免疫抑制薬
効能
免疫抑制薬, イノシン一リン酸脫水素酵素阻害薬
商品名
セルセプト (中外製薬)
説明
Mycophenolate mofetil was launched in 1995 in the U.S.A., its first market
worldwide, for the prevention of acute kidney transplant rejection in conjunction with
other immunosuppressive therapy and to treat refractory acute kidney graft rejection.
With improved oral absorption and bioavailability, mycophenolate mofetil is a prodrug of
mycophenolic acid (MPA), a fermentation product of several Penicillium species. MPA
is a selective, reversible, non-competitive inhibitor of inosinate dehydrogenase and
guanylate synthetase. It inhibits the de now pathway of purine biosynthesis. MPA
was found to have more potent antiproliferative effects on T and B lymphocytes than
other cell types. Compared with other immunosuppressants, mycophenolate mofetil is
reportedly superior due to its unique mechanism of action and excellent safety profile
for long term use. Mycophenolate mofetil is being investigated clinically in the
treatment of heart and liver transplantation rejection, asthma, in preventing coronary
artery restenosis, and in treating rheumatoid arthritis.
化學(xué)的特性
White Powder
使用
For the prophylaxis of organ rejection in patients receiving allogeneic renal, cardiac or hepatic transplants. Mycophenolate mofetil should be used concomitantly with cyclosporine and corticosteroids.
定義
ChEBI: A carboxylic ester resulting from the formal condensation between the carboxylic acid group of mycophenolic acid and the hydroxy group of 2-(morpholin-4-yl)ethanol. In the liver, it is metabolised to mycophenolic acid, an immunosuppressant for which it is
prodrug. It is widely used to prevent tissue rejection following organ transplants as well as for the treatment of certain autoimmune diseases.
適応癥
Mycophenolate mofetil (MMF, CellCept) is an ester
prodrug of mycophenolic acid (MPA), a Penicillium-derived
immunosuppressive agent that
blocks de novo purine synthesis by noncompetitively inhibiting
the enzyme inosine monophosphate dehydrogenase.
MPA preferentially suppresses the proliferation
of cells, such as T and B lymphocytes, that lack the
purine salvage pathway and must synthesize de novo the guanosine nucleotides required for DNA and RNA
synthesis.MPA has been used for decades as a systemic
treatment for moderate to severe psoriasis. MMF was
developed to increase the bioavailability of MPA.
作用機序
the guanosine nucleotides required for DNA and RNA
synthesis.MPA has been used for decades as a systemic
treatment for moderate to severe psoriasis. MMF was
developed to increase the bioavailability of MPA.
臨床応用
MMF is indicated for the prophylaxis of organ rejection
in patients receiving renal, hepatic, and cardiac
transplants; it is often used in combination with other
immunosuppressive agents for this indication. In dermatology,
MMF is particularly useful as monotherapy, or as
a steroid-sparing agent, for treatment of autoimmune
blistering diseases (bullous pemphigoid and pemphigus).
It may also be useful for the treatment of inflammatory
skin diseases mediated by neutrophilic infiltration,
such as pyoderma gangrenosum, and psoriasis.
副作用
Adverse effects produced by MMF most
commonly include nausea, abdominal cramps, diarrhea,
and possibly an increased incidence of viral and bacterial
infections. Whether MMF may be associated with
an increased long-term risk of lymphoma or other malignancies
is controversial; however, any such risk is
likely to be lower in patients treated for skin disease
with MMF monotherapy than in transplant patients
treated with combination immunosuppressive therapy.
ミコフェノール酸モフェチル 上流と下流の製品情報
原材料
準(zhǔn)備製品