Department of Biomedical Engineering, Johns Hopkins University School of Medicine, Baltimore, MD, USA.
Department of Biomedical Engineering, Johns Hopkins University School of Medicine, Baltimore, MD, USA; AsclepiX Therapeutics, Inc., Baltimore, MD, USA.
Peptides. 2023 Nov;169:171075. doi: 10.1016/j.peptides.2023.171075. Epub 2023 Aug 15.
Triple-negative breast cancer (TNBC) is a particularly aggressive and invasive subtype of breast cancer that represents a major cause of death of women worldwide. Here we describe the efficacy of an integrin-binding antiangiogenic peptide in a variety of delivery methods and dosing conditions. This peptide, AXT201, demonstrated consistent anti-tumor efficacy when administered intraperitoneally, subcutaneously, and intratumorally, and retained this activity even when dosing frequency was reduced to once every two weeks. Finally, in vivo imaging and biodistribution studies of AXT201 showed a long-term persistence of at least 10 days at the site of injection and a stable detectable signal in the blood over 48 h, indicating a sustained release profile. Taken together, these findings indicate AXT201 exhibits favorable pharmacokinetic properties for a 20-mer peptide.
三阴性乳腺癌（TNBC）是一种侵袭性和侵略性特别强的乳腺癌亚型，是全球女性死亡的主要原因之一。在这里，我们描述了整联蛋白结合抗血管生成肽在多种给药方法和剂量条件下的疗效。这种名为 AXT201 的肽在腹腔内、皮下和肿瘤内给药时均表现出一致的抗肿瘤疗效，即使将给药频率降低至每两周一次，其活性仍得以保留。最后，AXT201 的体内成像和生物分布研究表明，在注射部位至少有 10 天的长期持久性，并且在 48 小时内血液中可稳定检测到信号，表明其具有持续释放的特征。综上所述，这些发现表明 AXT201 对 20 肽具有良好的药代动力学特性。
