西羅莫司

Sirolimus (INN/USAN), also known as rapamycin, is an immunosuppressant drug used to prevent rejection in organ transplantation;西羅莫司（INN / USAN），也稱為雷帕黴素，是一種免疫抑製劑，用於預防器官移植中的排斥反應。 it is especially useful in kidney transplants.它在腎臟移植中特別有用。 A macrolide, sirolimus was first discovered as a product of the bacterium Streptomyces hygroscopicus in a soil sample from Easter Island - an island also known as "Rapa Nui", hence the name.大環內酯類西羅莫司是作為吸水鏈黴菌的產物在復活節島的一個土壤樣品中發現的，該島也被稱為“ Rapa Nui”，因此得名。 It is marketed under the trade name Rapamune by Wyeth.它由惠氏以商品名Rapamune銷售。
Sirolimus was originally developed as an antifungal agent.西羅莫司最初是作為抗真菌劑開發的。 However, this was abandoned when it was discovered that it had potent immunosuppressive and antiproliferative properties.然而，當發現它具有有效的免疫抑制和抗增殖特性時，它被放棄了。
The anti-proliferative effects of sirolimus may have a role in treating cancer.西羅莫司的抗增殖作用可能在治療癌症中起作用。 Recently, it was shown that sirolimus inhibited the progression of dermal Kaposi's sarcoma in patients with renal transplants.最近，顯示西羅莫司抑制腎移植患者皮膚卡波西氏肉瘤的進展。 Other mTOR inhibitors such as temsirolimus (CCI-779) or everolimus (RAD001) are being tested for use in cancers such as glioblastoma multiforme and mantle cell lymphoma.正在測試其他mTOR抑製劑，例如替西羅莫司（CCI-XNUMX）或依維莫司（RADXNUMX）在多形性膠質母細胞瘤和套細胞淋巴瘤等癌症中的使用。
Akt信號傳導可促進Akt陽性淋巴瘤中的細胞存活，並起到防止化學藥物如阿黴素或環磷酰胺的細胞毒性作用的作用。 Bcl-2陽性淋巴瘤對治療完全耐藥； nor are eIF4E expressing lymphomas sensitive to sirolimus.表達eIFXNUMXE的淋巴瘤對西羅莫司也不敏感。 Rapamycin showed no effect on its own.雷帕黴素本身沒有作用。