性别和体重对老年弥漫性大 B 细胞淋巴瘤患者利妥昔单抗清除率和血清消除半衰期的作用。
The role of sex and weight on rituximab clearance and serum elimination half-life in elderly patients with DLBCL.
机构信息
Institut für Pharmakologie der Uniklinik, Köln, Germany;
出版信息
Blood. 2012 Apr 5;119(14):3276-84. doi: 10.1182/blood-2011-09-380949. Epub 2012 Feb 15.
Pharmacokinetics of 8 doses of rituximab (375 mg/m(2)) given in combination with 2-week cyclophosphamide, hydroxydaunorubicin, vincristine, and prednisone/prednisolone (CHOP-14) was determined by ELISA in 20 elderly patients with diffuse large B-cell lymphoma (DLBCL) 10 minutes before and after each infusion and 1 week and 1, 2, 3, 6, and 9 months after the last infusion. Population pharmacokinetic modeling was performed with nonlinear mixed-effect modeling software (NONMEM VI). Concentration-time data were fitted into an open 2-compartment model and total clearance, central compartment volume, intercompartment clearance, and volume of distribution at steady-state (Vd(ss)) were investigated. Total clearance was 9.43 mL/h and Vd(ss) was 9.61 l. Rituximab clearance was reduced (8.21 mL/h vs 12.68 mL/h; P = .003) and elimination half-life was prolonged in women compared with men (t(1/2β) = 30.7 vs 24.7 days; P = .003). Body weight also affected Vd(ss) (0.1 l increase of Vd(ss) per kilogram above median of 75 kg). A sex-dependent effect and the higher weight of males contribute to their faster rituximab clearance, which might explain why elderly males benefit less from the addition of rituximab to CHOP than females. This trial was registered on www.clinicaltrials.gov as numbers NCT00052936, EU-20243 (RICOVER-60 Trial), EU-20534, and NCT00726700 (Pegfilgrastim Trial).
20 例老年弥漫性大 B 细胞淋巴瘤(DLBCL)患者在接受每周 2 次环磷酰胺、阿霉素、长春新碱和泼尼松/强的松(CHOP-14)治疗的第 14 天接受 8 剂利妥昔单抗(375mg/m2)治疗,用酶联免疫吸附法(ELISA)在每次输注前 10 分钟和输注后 1 周及 1、2、3、6 和 9 个月测定其药代动力学。采用非线性混合效应模型软件(NONMEM VI)进行群体药代动力学建模。将浓度-时间数据拟合到开放的 2 室模型中,并考察总清除率、中央室容积、分布容积和稳态分布容积(Vd(ss))。总清除率为 9.43ml/h,Vd(ss)为 9.61L。与男性相比,女性的利妥昔单抗清除率降低(8.21ml/h 比 12.68ml/h;P=0.003),消除半衰期延长(t1/2β=30.7 比 24.7 天;P=0.003)。体重也影响 Vd(ss)(体重每增加 75kg 中位数以上 0.1L)。性别依赖性效应和男性体重较高导致其利妥昔单抗清除率增加,这可能解释了为什么老年男性从利妥昔单抗联合 CHOP 治疗中获益不如女性。该试验在 www.clinicaltrials.gov 上注册,编号为 NCT00052936、EU-20243(RICOVER-60 试验)、EU-20534 和 NCT00726700(Pegfilgrastim 试验)。