Sheikh Saira Z, Hammer Anne E, Fox Norma Lynn, Groark James, Struemper Herbert, Roth David, Gordon David
Int J Clin Pharmacol Ther. 2016 Nov;54(11):914-922. doi: 10.5414/CP202623.
To study self-administration and pharmacokinetics (PK) of subcutaneous (SC) belimumab in patients with systemic lupus erythematosus (SLE).
Patients previously treated with belimumab self-administered belimumab 200 mg SC weekly for 8 weeks using an autoinjector. The primary endpoint was the proportion of patients able to self-administer their first and second dose (weeks 1 and 2) in the clinic. The proportion able to self-administer at weeks 4 and 8 (clinic) and weeks 3, 5, 6, and 7 (home) were secondary endpoints. Belimumab PK, safety, and injection-site pain were assessed.
91/95 patients completed the study (withdrawals: adverse events (AEs): 3; lost to follow-up: 1). 93% were female, and mean (SD) age was 44.8 (12.50) years. The majority (99%, 89/90; no attempt, n = 5) successfully self-administered belimumab SC at weeks 1 and 2 (5 had clinic staff assistance), and 98% (85/87) successfully self-administered at weeks 4 and 8. Home-administration success rates were high (93%, (81/87) at weeks 3, 5, 6, and 7). Week 8 median trough concentration was 113 µg/mL. For patients with a ≤ 1.5-week interval between IV SC administration, week-1 concentrations were higher vs. week 8 (+ 51% median) but within a range observed with IV dosing; those with a ≥ 2.5-week interval had median differences close to 0. AEs and serious AEs were low, with no deaths; pain levels were low and decreased with subsequent injections.
CONCLUSION: Patients with SLE successfully self-administered belimumab SC using a novel autoinjector; the PK profile was stable following a switch from IV with acceptable AE and pain levels. The recommended dosing interval between IV to SC dosing is 1 - 4 weeks. .
研究皮下注射贝利尤单抗在系统性红斑狼疮（SLE）患者中的自我给药情况及药代动力学（PK）。
曾接受贝利尤单抗治疗的患者使用自动注射器，每周皮下注射200mg贝利尤单抗，共8周。主要终点是患者在诊所能够自行注射第一剂和第二剂（第1周和第2周）的比例。能够在第4周和第8周（诊所）以及第3、5、6和7周（家中）自行给药的比例为次要终点。评估贝利尤单抗的PK、安全性和注射部位疼痛情况。
91/95例患者完成了研究（退出：不良事件（AE）：3例；失访：1例）。93%为女性，平均（标准差）年龄为44.8（12.50）岁。大多数患者（99%，89/90；未尝试，n = 5）在第1周和第2周成功自行皮下注射贝利尤单抗（5例有诊所工作人员协助），98%（85/87）在第4周和第8周成功自行给药。在家给药成功率较高（第3、5、6和7周为93%，（81/87））。第8周的中位谷浓度为每毫升113微克。对于静脉注射与皮下注射间隔≤1.5周的患者，第1周的浓度高于第8周（中位值增加51%），但在静脉给药观察到的范围内；间隔≥2.5周的患者中位差异接近0。AE和严重AE发生率较低，无死亡；疼痛程度较低且随着后续注射而减轻。
SLE患者使用新型自动注射器成功自行皮下注射贝利尤单抗；从静脉注射转换为皮下注射后，PK特征稳定，AE和疼痛程度可接受。静脉注射至皮下注射的推荐给药间隔为1 - 4周。
