Cinrebafusp alfa (PRS 343) 是一种高亲和力的CD137/HER2双特异性抗钙蛋白药物。Cinrebafusp alfa 结合重组人 HER2 (Kd=0.3 nM) 和人单体 CD137 (4-1BB;Kd=5 nM)。Cinrebafusp alfa 通过肿瘤定位的 HER2 依赖性 4-1BB 聚集和激活促进 T 细胞共刺激，进一步增强 T 细胞受体介导的活性并导致肿瘤破坏。Cinrebafusp alfa 具有用于 HER2+ 实体瘤研究的潜力。
| 生物活性 | Cinrebafusp alfa (PRS 343) is a high affinityCD137/HER2bispecfic anticalin-based drug. Cinrebafusp alfa binds to recombinant human HER2 (Kd=0.3 nM) and human monomeric CD137 (4-1BB;Kd=5 nM). Cinrebafusp alfa facilitates T-cell costimulation by tumor-localized, HER2-dependent4-1BBclustering and activation, further enhancing T-cell receptor-mediated activity and leading to tumor destruction. Cinrebafusp alfa has the potential for HER2+ solid tumors research[1][2]. |
| IC50& Target[1] | 4-1BB 5 nM (Kd) | HER2 0.3 nM (Kd) |
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体外研究
(In Vitro) | Cinrebafusp alfa (PRS 343) 结合表达 HER2 的 MCF-7 细胞和转染人 4-1BB 的 CHO 细胞，在 FACS 测定中 EC50分别为 7.4 nmol/L，6.2 nmol/L[1]。
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体内研究
(In Vivo) | Cinrebafusp alfa (PRS 343; 0.2-10 mg/kg; 静脉给药; 每周一次; 持续 20 天) 在移植有 HER2 阳性 SK-OV-3 肿瘤细胞的人源化小鼠模型中导致肿瘤生长抑制并且肿瘤浸润淋巴细胞呈剂量依赖性增加[1]。
Cinrebafusp alfa (10 mg/kg; 静脉给药; 单剂量) 在雄性 CD-1 小鼠中的终末消除半衰期为 >14 天。Cinrebafusp alfa (3 mg/kg; 静脉注射; 单剂量) 在雄性食蟹猴中的终末消除半衰期约为 4 天[1]。
| Animal Model: | SK-OV-3 ovarian cancer model in human PBMC-reconstituted NOG female mice, ages 5-7 weeks[1] | | Dosage: | 0.2, 1, 5, 10 mg/kg | | Administration: | IV; once weekly; for 20 day | | Result: | Displayed dose-dependent antitumor efficacy with doses ranging from 4 μg to 100 μg (approximately 0.2 mg/kg to 5 mg/kg), while the 200-μg dose (approximately 10 mg/kg) did not further enhance tumor regression.
Led to a significant increase in human CD45+ lymphocytes in tumor tissue. |
| Animal Model: | Male CD-1 mice[1] | | Dosage: | 10 mg/kg (Pharmacokinetic Analysis) | | Administration: | IV; single dose | | Result: | Had the terminal elimination half-life of >14 days. |
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| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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