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Efalizumab

发布日期:2010-02-26 12:27:18  作者:  来源:互联网  浏览次数:0  文字大小:【】【】【
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单克隆抗体药物Efalizumab(商品名Raptiva,Genentech/Xoma)治疗银屑病(牛皮癣)新药

银屑病是一种常见的皮肤病,以红色或粉红色且带有白色或银色鳞片的增长性皮肤损伤为特征。现有资料表明,白细胞(主要是T细胞)在表皮部分的渗入活动是引起和维持银屑病症状存在的主要驱动力,而在此过程中涉及许多细胞间的黏附分子,其中包括属于整合素(integrin)家族的淋巴细胞功能相关抗原-1(LFA-1)。LFA-1通过其a亚基的I domain与它的最重要的配体——细胞间黏附分子-1(ICAM-1)的domain 1结合,参与介导许多免疫过程。

  Efalizumab是一种针对LFA-1的a亚基的人源化单克隆抗体药物,可以通过阻止LFA-1与ICAM-1的结合进而抑制白细胞的活动。该抗体药物于2002年通过FDA批准,是目前治疗牛皮癣的最有效的药物之一。丁建平课题组的李胜同学等运用结构生物学和生物化学的方法,研究了Efalizumab的Fab片断和该片断与LFA-1的a亚基的I domain的复合物的晶体结构以及抗原—抗体相互作用的性质。通过对复合物的结构分析以及与文献中生化数据的比较,鉴定了Efalizumab的抗原决定表位(epitope)。

  结构分析显示,在复合物结构中I domain处于非激活状态,Efalizumab在I domain上的抗原决定表位不同于ICAM-1的结合位点。进一步通过与已报道的LFA-1 I domain/ICAM-1复合物的结构比较,发现Efalizumab与LFA-1 I domain的结合,会导致Fab的轻链与ICAM-1的domain 2产生空间位置的重叠,从而阻碍了ICAM-1与LFA-1的结合,并进一步抑制了LFA-1的活性。这些结果在分子水平上揭示了Efalizumab对LFA-1的活性产生抑制作用的分子机制,并合理解释了已有的生物化学和免疫学数据。基于该研究结果,研究人员提出了通过对Efalizumab进行定点突变、研发具有更高特异性和更强亲和力的抗体药物的策略,同时依据该抗体药物与小分子药物具有不同作用位点的结果,提出了将Efalizumab与其他小分子药物联合应用以达到更佳治疗效果的方案。这些研究结果对于抗牛皮癣的抗体药物的研发和临床治疗具有重要的指导意义。

RAPTIVA

Raptiva Information

 

Raptiva is a popular immunosuppressant that is more commonly known under the generic name of Efalizumab. Similar medicines are known to act on the patient’s organism’s immune system.

Raptiva Indications

Raptiva is a well known medicine that is generally prescribed to patients who are suffering from psoriasis. However, this drug is known to sometimes serve some other medical purposes that have not been listed in this guide. Ask your personal health care specialist for more information about this medicine.

Raptiva Warnings

Before you start taking Raptiva, you should alert your personal physician if you are suffering from any other medical condition, especially the following:

  • chronic or active bacterial, viral, or fungal infection;
  • are currently receiving phototherapy;
  • are suffering from a suppressed immune system.

If you are suffering from any of the medical conditions that have been listed here, you might not be allowed to start taking this product.

Raptiva Intake Guidelines

You should ask your personal physician how and when to take each of your doses of Raptiva. Do not disobey any of your doctor’s instructions. If you fail to understand some of them, you should ask a pharmacist, a nurse or a physician for more information. Store this medicine in a place that is away from heat and moisture (do not keep it in the bathroom or anywhere near the kitchen sink).

This medicine is generally administered in the form of a sub dermal injection. Your personal physician should give you a set of detailed instructions regarding the proper administration and preparation of this medicine. You will probably receive your injection of Raptiva every 7 days. Do not stop your treatment with this medical product without your personal physician’s consent, as this could have severe consequences.

Raptiva Dosage

Your personal healthcare provider will calculate the correct dose of Raptiva that you should take in, in order to get the proper effects from your treatment with it. Do not make any alterations to the dose that your physician has prescribed you without his or her consent. Remember that the correct dose of Raptiva can (and usually does) vary from one patient to another, as it depends on the severity of the disorder, the patient’s general health condition, sex, age, etc.

Raptiva Overdose

If you suspect that you might be suffering from an overdose with this medicine, you should seek emergency medical attention. Contact your local poison control centre at once. Inform your personal physician as soon as possible if necessary, go to the nearest emergency room. If you are suffering from an overdose with Raptiva you will probably experience vomiting and / or nausea.

Raptiva Missed Dose

In order to get the maximum benefit from your treatment with this medicine (Raptiva) you ought to make sure that you use each and every one of your prescribed doses of this medical product at their due time. However, if you happen to miss using a dose of this medicine, we strongly recommend you to contact your personal health care specialist and ask him or her for further instructions (advice). You must not use double doses of this drug without your personal physician’s consent, as this is known to increase your risk of developing overdose with Raptiva.

Raptiva Side Effects

Patients who develop any symptoms of an infection (such as chills, fever, coughing, congestion, sore throat) or if they experience pain, redness, or swelling of a wound, difficult urination or burning during urination should alert their personal health care speicalist at once. Patients who are using Raptiva are known to be more prone to develop some types of cancer (for example lymphoma). Ask your personal physician about the risks that are known to be involved by a prolonged treatment with Raptiva.

Taking Raptiva will severely decrease your normal number of blood platelets, triggering bleeding or easy bruising. If you happen to experience severe bruising or bleeding, pinpoint sub dermal red spots, nosebleeds, easy gum bleeding, or bloody, black, or tarry stools you should stop using this medicine and alert your personal physician at once. Patients who are suffering from psoriasis should not be allowed to start to follow a treatment with Raptiva, as their initial psoriasis severity could worsen.

Patients who are using this medicine and who develop symptoms of a highly severe allergic reaction to this drug (closing of the throat; hives; difficulty breathing; swelling of the tongue, lips, or face) should seek immediate medical care. A treatment with Raptiva normally triggers symptoms such as nausea, headache, fever, chills, and muscle aches, joint pain, back pain and or swelling.

Raptiva Drug Reactions

A patient who is currently following a treatment with Raptiva should not be allowed to receive any type of vaccines without first consulting it with his or her personal health care specialist. Intake of this medical product could make vaccines less effective, and sometimes even harmful. Patients who are using this medicine on a regular basis should avoid coming into direct contact with other patients who have recently received "live" vaccines (such as nasal influenza vaccine, oral polio vaccine) because the virus could be easily transmitted through air. During your intake of this medicine you should avoid using any of these:

  • medications that are supposed to prevent your organism from rejecting a transplant;
  • some types of cancer drugs;
  • medicines that are supposed to treat some other types of immune system medical disorders.

Buy Raptiva

Buy Raptiva through our Online Pharmacy Escrow Service or at any Canada Pharmacy where it is sold. In some countries RAPTIVA may also be known as: Efalizumab

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