Cao Zhihai, Li Yao, Hou Denny, Wang Shufang, Yao Wei, Zhang Gaochong, Chen Jianmin, Tang Zhengwei, Song Linda, Zhao Xingna, Chu Xiaoxiang, Wang Xiaoyan, Li Renshu, Hu Wei
School of Pharmacy, Anhui Medical University, Hefei, 230032, China.
Department of Clinical Pharmacology, The Second Affiliated Hospital of Anhui Medical University, Hefei, 230601, China.
Clin Drug Investig. 2025 Nov;45(11):855-863. doi: 10.1007/s40261-025-01488-x. Epub 2025 Sep 28.
In clinical practice, granulocyte colony-stimulating factor (G-CSF) is often used to lower infection risk and avoid poor outcomes from chemotherapy dose reduction or delay. Efbemalenograstim alfa (also known as F-627) is a non-pegylated but long-acting (once-per-cycle) recombinant human granulocyte colony-stimulating factor (rhG-CSF) compared with pegfilgrastim. This study was designed to obtain pharmacokinetic (PK)/pharmacodynamic (PD), safety, and tolerability data for F-627 in healthy Chinese participants.
This was a single-center, open-label phase I clinical study involving 24 healthy Chinese volunteers (sex ratio = 1:1). All the participants were administered a single subcutaneous injection of 20 mg F-627 into the abdomen.
In this study, 15 (62.5%) participants reported 28 treatment-related adverse events. PK/PD data showed that after a single 20 mg subcutaneous (SC) F-627 abdominal injection in healthy Chinese participants, serum concentrations peaked at 36 h post dose, while the absolute neutrophil count (ANC) peaked at 96 h. After peaking, F-627 serum levels decreased rapidly to low concentrations by 120 h, while ANC declined gradually to near baseline by day 15. Similar trends in serum concentration and ANC kinetics were seen between sex.
This phase I study showed that 20 mg F-627 was well tolerated and exhibited a favorable safety profile in a healthy Chinese population. The PK and PD data correlated well and were consistent across sex.
This trial was registered at the Chinese Clinical Trial Registry (chictr.org.cn) on 10 September 2024 (registration ID: ChiCTR2400089548).
在临床实践中，粒细胞集落刺激因子（G-CSF）常用于降低感染风险，避免因化疗剂量减少或延迟导致的不良后果。与培非格司亭相比，艾贝格司亭α（也称为F-627）是一种非聚乙二醇化但长效（每周期一次）的重组人粒细胞集落刺激因子（rhG-CSF）。本研究旨在获取F-627在健康中国受试者中的药代动力学（PK）/药效学（PD）、安全性和耐受性数据。
这是一项单中心、开放标签的I期临床研究，涉及24名健康中国志愿者（性别比例=1:1）。所有受试者均在腹部皮下注射一次20mg F-627。
在本研究中，15名（62.5%）受试者报告了28例与治疗相关的不良事件。PK/PD数据显示，在健康中国受试者中单次腹部皮下注射20mg F-627后，血清浓度在给药后36小时达到峰值，而绝对中性粒细胞计数（ANC）在96小时达到峰值。达到峰值后，F-627血清水平在120小时迅速降至低浓度，而ANC在第15天逐渐降至接近基线水平。性别之间血清浓度和ANC动力学呈现相似趋势。
这项I期研究表明，20mg F-627在健康中国人群中耐受性良好，安全性良好。PK和PD数据相关性良好，且在性别间一致。
本试验于2024年9月10日在中国临床试验注册中心（chictr.org.cn）注册（注册号：ChiCTR2400089548）。
