Home Proteases PSMA inhibitor Vipivotide tetraxetan (PSMA-617)

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Vipivotide tetraxetan (PSMA-617) PSMA inhibitor

Cat.No.S8670

Vipivotide tetraxetan (PSMA-617) is a chemically modified PSMA(prostate-specific membrane antigen) inhibitor with a Ki of 0.37 nM.
Vipivotide tetraxetan (PSMA-617) PSMA inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 1042.14

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Quality Control

Batch: S867001 Water]100 mg/mL]false]]]false]]]false Purity: 99.73%
99.73

Solubility

In vitro
Batch:

Water : 100 mg/mL

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Chemical Information, Storage & Stability

Molecular Weight 1042.14 Formula

C49H71N9O16

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1702967-37-0 -- Storage of Stock Solutions

Synonyms N/A SMILES C1CC(CCC1CNC(=O)CN2CCN(CCN(CCN(CC2)CC(=O)O)CC(=O)O)CC(=O)O)C(=O)NC(CC3=CC4=CC=CC=C4C=C3)C(=O)NCCCCC(C(=O)O)NC(=O)NC(CCC(=O)O)C(=O)O

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Mechanism of Action

Targets/IC50/Ki
PSMA
(Cell-free assay)
0.37 nM(Ki)
In vitro

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.
In vivo

The small-animal PET measurements show high tumor-to-background contrasts as early as 1 h after injection. In vivo distribution reveals specific uptake in LNCaP tumors and in the kidneys 1 h after injection. With regard to therapeutic use, PSMA-617 exhibits a rapid clearance from the kidneys from 113.3 ± 24.4 at 1 h to 2.13 ± 1.36 percentage injected dose per gram at 24 h. The favorable pharmacokinetics of the molecule leads to tumor-to-background ratios of 1,058 (tumor to blood) and 529 (tumor to muscle), respectively,24 h after injection.
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-09-02)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT07200830 RECRUITING
Metastatic Castration-Resistant Prostate Carcinoma; Metastatic Prostate Adenocarcinoma; Stage IVB Prostate Cancer AJCC v8
Alliance for Clinical Trials in Oncology
 2026-03-31 PHASE3
NCT06600802 RECRUITING
Castration-resistant Metastatic Prostate Cancer; Treated by 177Lutetium-PSMA-617 (Lu-PSMA)
Centre Jean Perrin
 2024-10-08
NCT05803941 RECRUITING
Prostate Cancer
Novartis Pharmaceuticals
 2023-08-14 PHASE4
NCT06496581 RECRUITING
Prostate Cancer Metastatic
UNICANCER
 2024-09-12 PHASE3
NCT07550517 NOT_YET_RECRUITING
High-Risk Localized Prostate Cancer
Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins
 2026-08 PHASE2
NCT06320067 RECRUITING
Prostate Cancer Metastatic
University College, London
 2024-06-11 PHASE3

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