2013年7月20日,安斯泰来（Astellas）美国子公司今天宣布，ASTAGRAF XL（他克莫司缓释胶囊，tacrolimus extended release capsules）获FDA批准，与霉酚酸酯（MMF）及皮质类醇联用、结合或无巴利昔单抗（basiliximab）诱导，用于预防成人肾移植受者中的器官排斥。安斯泰来于2012年9月提交了该药的新药申请（NDA）。
在美国，ASTAGRAF XL是首个每日一次的他克莫司制剂，该药作为免疫抑制组合方案中的核心组成部分，为肾移植受者预防器官排斥反应提供了一个很有潜力的疗法。
该药的获批，是基于2项主要的、随机、比较III期临床研究，涉及美国、欧洲、加拿大、南美、澳大利亚、南非等国的1093例患者（545例他克莫司缓释胶囊治疗）。
在2007年，他克莫司缓释胶囊在欧洲获批以商品名Advagraf销售；2008年，该药在日本获批以商品名Graceptor销售。总体而言，他克莫司缓释胶囊已获得了全球73个国家的监管批准，每年经该药治疗的患者数超过14万人。
药品完整说明书附件：http://www.medicationdaily.com/astagraf-xl/info/adverse-reactions
IMPORTANT SAFETY INFORMATION
What is the most important information I should know about ASTAGRAF XL?
ASTAGRAF XL can cause serious side effects, including:
1.Increased risk of cancer. People who take ASTAGRAF XL have an increased risk of getting some kinds of cancer, including skin and lymph gland cancer (lymphoma).
2.Increased risk of infection. ASTAGRAF XL is a medicine that affects your immune system and can lower the ability of your immune system to fight infections. Serious infections can happen in people receiving ASTAGRAF XL that can cause death. Call your doctor right away if you have symptoms of an infection such as: fever, sweats or chills, cough or flu-like symptoms, muscle aches, or warm, red or painful areas on your skin.
3.Increased risk of death in females who have had a liver transplant. You should not take ASTAGRAF XL without talking to your doctor if you have had a liver transplant.
What should I tell my doctor before taking ASTAGRAF XL?
Before you take ASTAGRAF XL tell your doctor if you: plan to receive any live vaccines, have or have had liver, kidney or heart problems, or have any other medical conditions. Talk to your doctor if you are pregnant or plan to become pregnant. Tell your doctor if you are breastfeeding or plan to breastfeed. ASTAGRAF XL can pass into your breast milk. You and your doctor should decide if you will take ASTAGRAF XL or breastfeed. You should not do both.
Tell your doctor about all the medicines you take, including prescription and over-the-counter medicines, vitamins and herbal supplements. ASTAGRAF XL may affect the way other medicines work and other medicines may affect how ASTAGRAF XL works. Know the medicines you take. Keep a list of them and show it to your doctor and pharmacist when you get a new medicine. Tell your doctor or pharmacist if there are any changes to the list of medicines you take.
How should I take ASTAGRAF XL?
•Take ASTAGRAF XL exactly as your doctor tells you to take it.
•Your doctor will tell you how much ASTAGRAF XL to take and when to take it.
•Your doctor may change your dose of ASTAGRAF XL if needed. Do not stop taking or change your dose of ASTAGRAF XL without talking to your doctor.
•Take ASTAGRAF XL capsules whole. Do not break, crush, chew or dissolve before swallowing. If you cannot swallow ASTAGRAF XL capsules whole, tell your doctor.
•Take ASTAGRAF XL at the same time each morning, preferably on an empty stomach at least one hour before, or at least two hours after, you have eaten a meal.
•If you miss your dose of ASTAGRAF XL, it should be taken as soon as possible, but no longer than 14 hours after your regularly scheduled time. If longer than 14 hours, the missed dose should be skipped and the next dose should be taken the following morning at your regularly scheduled time. Do not take two doses at the same time.
•If you take too much ASTAGRAF XL , call your doctor or go to the nearest hospital emergency room right away.
What should I avoid while taking ASTAGRAF XL?
While you take ASTAGRAF XL you should not receive any live vaccinations such as flu vaccine through your nose, measles, mumps, rubella, polio by mouth, TB vaccine, yellow fever, chicken pox or typhoid.
Avoid exposure to sunlight and UV light such as tanning machines. Wear protective clothing and use a sunscreen.
You should not eat grapefruit or drink grapefruit juice while taking ASTAGRAF XL.
You should not drink an alcoholic beverage when taking ASTAGRAF XL. It can increase your chances of getting serious side effects.
What are the possible side effects of ASTAGRAF XL?
•See “What is the most important information I should know about ASTAGRAF XL?”
•Medication errors: People who take ASTAGRAF XL have sometimes been given the wrong medicine, because some medicines have the same ingredient as ASTAGRAF XL. You should check your ASTAGRAF XL when you get a new prescription medicine to make sure you have received the right medicine. Call your doctor right away if you think you were given the wrong medicine. Ask your doctor or pharmacist if you are not sure what ASTAGRAF XL should look like.
ASTAGRAF XL may cause serious side effects, including: high blood sugar (diabetes), kidney problems, nervous system problems, high levels of potassium in your blood, high blood pressure, or heart problems such as changes in the electrical activity of your heart (QT prolongation). Call your doctor right away if you have any of these symptoms: frequent urination, increased thirst or hunger, blurred vision, confusion, drowsiness, loss of appetite, fruity smell on your breath, nausea, vomiting or stomach pain, coma, muscle tremors, numbness and tingling, headache, seizures or vision changes.
The most common side effects of ASTAGRAF XL in people receiving kidney transplant are: diarrhea, constipation, nausea, swelling of the hands, ankles or legs, tremors (shaking of the body) or low red blood cell count (anemia).
Tell your doctor if you have any side effect that bothers you or that does not go away. These are not all the possible side effects of ASTAGRAF XL. For more information, ask your doctor or pharmacist. Call your doctor for medical advice about side effects.