Vipivotide tetraxetan (PSMA-617) 是前列腺特异性膜抗原 (PSMA) 的强有效抑制剂，其 K_i 值为 0.37 nM。Vipivotide tetraxetan (PSMA-617)由三种成分组成:药效基团Glutamate-urea-Lysine，螯合剂DOTA（能够结合68Ga或177Lu），以及连接这两个实体的linker。Glutamate-urea-Lysine 可以与前列腺特异性膜抗原 (PSMA) 选择性结合。

Vipivotide tetraxetan (PSMA-617) is a high potent prostate-specific membrane antigen (PSMA) inhibitor, with a K i of 0.37 nM. Vipivotide tetraxetan (PSMA-617) is designed consisting of three components: the pharmacophore Glutamate-urea-Lysine, the chelator DOTA able to complex both 68Ga or 177Lu, and a linker connecting these two entities. Glutamate-urea-Lysine is the selective pharmacophore to bind to prostate specific membrane antigen.

Solid

Traditional Cytotoxic Agents

Vipivotide tetraxetan (PSMA-617) demonstrates high radiolytic stability for at least 72 h. A high inhibition potency (equilibrium dissociation constant Ki=2.34±2.94 nM on LNCaP; Ki=0.37±0.21 nM enzymatically determined) and highly efficient internalization into LNCaP cells are demonstrated. has not independently confirmed the accuracy of these methods. They are for reference only.

Organ distribution with 68Ga-labeled Vipivotide tetraxetan (PSMA-617) after 1 h (n=3) reveals a high specific uptake in LNCaP tumors and in the kidneys. The high uptake in the kidneys is nearly completely blocked by coinjection of 2 mg of 2-PMPA per kilogram. Other organs such as the liver, lung, and spleen show rather low uptake and no blocking effect, with the exception of the spleen. Tumor-to-background ratios are 7.8 (tumor to blood) and 17.1 (tumor to muscle) at 1 h after injection. As compared with the 68Ga-labeled version, the organ distribution with 177Lu-labeled Vipivotide tetraxetan (PSMA-617) (n=3) show a similar uptake in the LNCaP tumors and in the kidneys. The liver uptake is found to be statistically different. Tumor-to-background ratios determined 1 h after injection show slightly higher values (tumor to blood, 22.1; tumor to muscle, 25.6) than previous organ d

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[1]. Bene?ová M, et al. Preclinical Evaluation of a Tailor-Made DOTA-Conjugated PSMA Inhibitor with Optimized Linker Moiety for Imaging and Endoradiotherapy of Prostate Cancer. J Nucl Med. 2015 Jun;56(6):914-20.

In Vitro: DMSO : 125 mg/mL (119.95 mM; Need ultrasonic)H₂O : ≥ 100 mg/mL (95.96 mM)