Ceberio I, Dai K, Devlin S M, Barker J N, Castro-Malaspina H, Goldberg J D, Giralt S, Adel N G, Perales M-A
1] Adult Bone Marrow Transplantation Service, Department of Medicine, Memorial Sloan Kettering Cancer Center, New York, NY, USA [2] Department of Hematology, Hospital Universitario Donostia, Donostia, Spain.
Pharmacy Service, Memorial Sloan Kettering Cancer Center, New York, NY, USA.
Bone Marrow Transplant. 2015 Mar;50(3):438-43. doi: 10.1038/bmt.2014.286. Epub 2015 Jan 19.
Antifungal prophylaxis with azoles is considered standard in allogeneic hematopoietic SCT (allo-HSCT). Although sirolimus is being used increasingly for the prevention of GVHD, it is a substrate of CYP3A4, which is inhibited by voriconazole, and concurrent administration can lead to significantly increased exposure to sirolimus. We identified 67 patients with hematologic malignancies who underwent allo-HSCT with sirolimus, tacrolimus and low-dose MTX and received concomitant voriconazole prophylaxis from April 2008 to June 2011. All patients underwent a non-myeloablative or reduced-intensity conditioned allo-HSCT. Patients received sirolimus and voriconazole concurrently for a median of 113 days. The median daily dose reduction of sirolimus at the start of coadministration was 90%. The median serum sirolimus trough levels before and at steady state of coadministration were 5.8 ng/mL (range: 0-47.6) and 6.1 ng/mL (range: 1-14.2) (P=0.45), respectively. One patient with an average sirolimus level of 6 ng/mL developed sirolimus-related thrombotic microangiopathy that resolved after sirolimus discontinuation. No sinusoidal obstructive syndrome was reported. Seventeen patients (25%) prematurely discontinued voriconazole because of the adverse events. Only two patients (3%) presented with possible invasive fungal infections at day 100. We demonstrate that sirolimus and voriconazole coadministration with an empiric 90% sirolimus dose reduction and close monitoring of sirolimus trough levels is safe and well tolerated.
在异基因造血干细胞移植(allo-HSCT)中,使用唑类进行抗真菌预防被视为标准做法。尽管西罗莫司越来越多地用于预防移植物抗宿主病(GVHD),但它是细胞色素P450 3A4(CYP3A4)的底物,而伏立康唑会抑制CYP3A4,同时使用会导致西罗莫司的暴露量显著增加。我们确定了67例血液系统恶性肿瘤患者,这些患者在2008年4月至2011年6月期间接受了allo-HSCT,使用了西罗莫司、他克莫司和低剂量甲氨蝶呤,并同时接受了伏立康唑预防。所有患者均接受了非清髓性或降低强度预处理的allo-HSCT。患者同时接受西罗莫司和伏立康唑的中位时间为113天。联合用药开始时,西罗莫司的中位每日剂量减少了90%。联合用药前和稳态时,西罗莫司的中位血清谷浓度分别为5.8 ng/mL(范围:0 - 47.6)和6.1 ng/mL(范围:1 - 14.2)(P = 0.45)。一名平均西罗莫司水平为6 ng/mL的患者发生了与西罗莫司相关的血栓性微血管病,在停用西罗莫司后病情缓解。未报告有肝窦阻塞综合征。17例患者(25%)因不良事件提前停用了伏立康唑。只有2例患者(3%)在第100天时出现了可能的侵袭性真菌感染。我们证明,西罗莫司和伏立康唑联合使用时,经验性地将西罗莫司剂量减少90%并密切监测西罗莫司谷浓度是安全的,且耐受性良好。