FDA在4月11日称，已批准惠氏制药的Rapamune用于帮助改善肾移植患者植入肾脏的功能。药物的这项新适应症主要内容为患者在接受肾脏移植2-4个月后，具有轻中度器官排斥反应危险的患者可以停止应用环孢菌素。　为避免机体对移入肾脏的排斥，临床上通常要在肾脏移植术后给病人合并使用Rapamune和环孢菌素，但若长期应用，却会影响移入肾脏发挥正常功能，用高水平的Rapamune代替环孢菌素，有望能使肾功能得到进一步改善。　　
FDA称，所有最新进行肾脏移植术的患者，约有一半以上的人会从此适应症的批准中受益。　　
Rapamune(sirolimus)于1999年9月被FDA批准用于预防进行肾脏移植患者发生的器官排斥反应。推荐与环孢菌素与皮质甾类合用。它是由土壤放射菌链霉菌属hygroscopicus产生的大环内酯，分子量为914.2。
　　
在发挥免疫抑制作用方面，Sirolimus的作用机制与环孢菌素和免疫抑制剂不同，后面两者均是通过抑制钙调磷酸酶及减少白介素-2的表达来完成免疫抑制作用的。而sirolimus是通过抑制白介素-2介导的信号转导作用，但对钙调磷酸酶无抑制作用。

Rapamune (Sirolimus Tablets）

Rapamune is used for:

Rapamune is an immunosuppressant. It works by blocking the action of certain blood cells (eg, T lymphocytes) that can cause the body to reject the transplanted organ.

Do NOT use Rapamune if:

• you are allergic to any ingredient in Rapamune
• you are pregnant
• you have had a liver or lung transplant
• you are taking astemizole, itraconazole, ketoconazole, a macrolide antibiotic (eg, erythromycin), rifabutin, rifampin, tacrolimus, telithromycin, terfenadine, or voriconazole

Contact your doctor or health care provider right away if any of these apply to you.

Before using Rapamune:

Some medical conditions may interact with Rapamune. Tell your doctor or pharmacist if you have any medical conditions, especially if any of the following apply to you:

• if you are pregnant, planning to become pregnant, or are breast-feeding
• if you are of childbearing age
• if you are taking any prescription or nonprescription medicine, herbal preparation, or dietary supplement
• if you have allergies to medicines, foods, or other substances
• if you have liver problems, kidney problems, high cholesterol or triglycerides, low blood platelet levels, diabetes, or a history of lung or breathing problems
• if you are on dialysis, have recently received a vaccine, or have a history of tuberculosis (TB) or have ever had a positive TB skin test
• if you have had multiple organ transplants, an organ retransplanted, or a previous transplant that was rejected

Some MEDICINES MAY INTERACT with Rapamune. Tell your health care provider if you are taking any other medicines, especially any of the following:

• Angiotensin-converting enzyme (ACE) inhibitors (eg, lisinopril) because a serious side effect, involving swelling of the mouth, face, lips, tongue, throat, and hands; trouble swallowing or breathing; and unexplained hoarseness, may occur
• Aminoglycosides (eg, gentamicin), amiodarone, amphotericin B, azole antifungals (eg, fluconazole, itraconazole, ketoconazole, voriconazole), bromocriptine, cimetidine, cisapride, cyclosporine, danazol, diltiazem, HIV protease inhibitors (eg, ritonavir), macrolide antibiotics (eg, erythromycin), metoclopramide, mibefradil, nicardipine, streptogramins (eg, dalfopristin), tacrolimus, telithromycin, troleandomycin, or verapamil because they may increase the risk of Rapamune's side effects, including kidney problems
• Carbamazepine, phenobarbital, phenytoin, rifabutin, rifampin, rifapentine, or St. John's wort because they may decrease Rapamune's effectiveness
• Astemizole, calcineurin inhibitors (eg, tacrolimus), fibrates (eg, fenofibrate), HMG-CoA reductase inhibitors (eg, atorvastatin), mycophenolate, or terfenadine because the risk of their side effects may be increased by Rapamune

This may not be a complete list of all interactions that may occur. Ask your health care provider if Rapamune may interact with other medicines that you take. Check with your health care provider before you start, stop, or change the dose of any medicine.

How to use Rapamune:

Use Rapamune as directed by your doctor. Check the label on the medicine for exact dosing instructions.

• You may take Rapamune by mouth on an empty stomach or with food. However, you must take it the same way each time for it to work best. If you take Rapamune on an empty stomach, always take it on an empty stomach. If you take it with food, always take it with food.
• Swallow Rapamune whole. Do not break, crush, or chew before swallowing
• Wash your hands immediately after taking Rapamune.
• If you are also taking cyclosporine, take Rapamune 4 hours after your cyclosporine dose unless your doctor tells you otherwise.
• Grapefruit and grapefruit juice may increase the risk of side effects from Rapamune. Talk to your doctor before including grapefruit or grapefruit juice in your diet while taking Rapamune.
• Rapamune works best if it is taken at the same time each day. Continue to take Rapamune even if you feel well. Do not miss any doses.
• Do not stop taking Rapamune without first checking with your doctor.
• If you miss a dose of Rapamune, take it as soon as possible. If it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not take 2 doses at once.

Ask your health care provider any questions you may have about how to use Rapamune.

Important safety information:

• Do not change your dose of Rapamune without first checking with your doctor.
• Rapamune may lower the ability of your body to fight infection. Avoid contact with people who have colds or infections. Tell your doctor if you notice signs of infection like fever, sore throat, rash, or chills.
• Some patients treated with Rapamune have developed severe and sometimes fatal infections, such as progressive multifocal leukoencephalopathy (PML) or severe kidney problems associated with BK virus infection. In kidney transplant patients, BK virus infection may cause loss of the transplanted kidney. Tell your doctor right away if you notice symptoms of PML (eg, confusion; disorientation; depression; changes in thinking, strength, or vision; one-sided weakness; trouble walking or talking; loss of balance or coordination) or kidney problems (eg, change in the amount of urine, difficult or painful urination, blood in the urine). Discuss any questions or concerns with your doctor.
• Rapamune may increase your risk of developing skin cancer. Avoid using sunlamps or tanning booths. Limit your exposure to the sun. Use a sunscreen or wear protective clothing if you must be outside for more than a short time.
• Do not receive a live vaccine (eg, measles, mumps) while you are taking Rapamune. Talk with your doctor before you receive any vaccine.
• Rapamune may reduce the number of clot-forming cells (platelets) in your blood. Avoid activities that may cause bruising or injury. Tell your doctor if you have unusual bruising or bleeding. Tell your doctor if you have dark, tarry, or bloody stools.
• Do not switch between the tablet and solution forms of Rapamune without first checking with your doctor. The same doses may not be equally effective.
• Tell your doctor or dentist that you take Rapamune before you receive any medical or dental care, emergency care, or surgery.
• If you may become pregnant, you must use an effective form of birth control before you start taking Rapamune. You will need to continue to use birth control while you take Rapamune and for 12 weeks after you stop taking it. If you have questions about effective birth control, talk with your doctor.
• Decreased sperm production has occurred in some men taking Rapamune. Normal sperm production has usually returned when Rapamune was stopped. Discuss any questions or concerns with your doctor.
• Patients who take Rapamune after an organ transplant may have an increased risk of developing high blood sugar or diabetes. High blood sugar may make you feel confused, drowsy, or thirsty. It can also make you flush, breathe faster, or have a fruit-like breath odor. If these symptoms occur, tell your doctor right away.
• Lab tests, including complete blood cell counts, kidney function, urine protein, cholesterol levels, and sirolimus blood levels, may be performed while you use Rapamune. These tests may be used to monitor your condition or check for side effects. Be sure to keep all doctor and lab appointments.
• Rapamune should be used with extreme caution in CHILDREN younger than 13 years old; safety and effectiveness in these children have not been confirmed.
• Rapamune should be used with extreme caution in CHILDREN younger than 18 years old who are considered to be at high immunological risk; safety and effectiveness in these children have not been confirmed.
• PREGNANCY and BREAST-FEEDING: Rapamune may cause harm to the fetus. Do not become pregnant while you are using it. If you think you may be pregnant, contact your doctor. You will need to discuss the benefits and risks of using Rapamune while you are pregnant. It is not known if Rapamune is found in breast milk. Do not breast-feed while taking Rapamune.

Possible side effects of Rapamune:

All medicines may cause side effects, but many people have no, or minor, side effects. Check with your doctor if any of these most COMMON side effects persist or become bothersome:

Acne; back pain; constipation; diarrhea; headache; joint pain; nausea; stomach pain; trouble sleeping; vomiting; weakness.

Seek medical attention right away if any of these SEVERE side effects occur:

Severe allergic reactions (rash; hives; itching; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue; unusual hoarseness); calf pain or swelling; chest pain; dark urine; fast or irregular heartbeat; infection (chills, fever, frequent or painful urination, sore throat, unusual vaginal discharge or odor); mental or mood changes; muscle pain or tenderness; night sweats; red, swollen, blistered, or peeling skin; severe or persistent headache or dizziness; shortness of breath; skin growths or discoloration; swelling of the hands, ankles, feet, or stomach; swollen glands or veins; symptoms of kidney problems (eg, change in the amount of urine, difficult or painful urination, blood in the urine); symptoms of PML (eg, changes in thinking, strength, or vision; confusion; depression; disorientation; loss of balance or coordination; one-sided weakness; trouble walking or talking); tremor; unexplained dry cough; unusual bleeding or bruising; unusual lumps; unusual tiredness or weakness; unusual weight gain or loss; vision changes; wound healing problems; yellowing of the skin or eyes.