2. Academic Validation
  3. Lipophilic Group-Modified Gd-PCTA as a High-Performance MRI Contrast Agent Featuring Kinetic Inertness, Protein Binding, and Enhanced T1 Relaxivity

Lipophilic Group-Modified Gd-PCTA as a High-Performance MRI Contrast Agent Featuring Kinetic Inertness, Protein Binding, and Enhanced T1 Relaxivity

  • J Med Chem. 2026 Mar 26;69(6):6976-6990. doi: 10.1021/acs.jmedchem.5c03268.
Sangyun Lee 1,  Ah Rum Baek 2,  Bokyung Sung 2,  Byeong Woo Yang 3,  Sohyeon Yang 3,  Soyeon Kim 4,  Ji-Ung Yang 4,  In Ok Ko 4,  Gang Ho Lee 5,  Ji-Ae Park 4,  Yongmin Chang 1 2 6 7
Affiliations

Affiliations

  • 1 Department of Medical & Biological Engineering, Kyungpook National University, Daegu 419944, Korea.
  • 2 Institute of Biomedical Engineering Research, Kyungpook National University, Daegu 419944, Korea.
  • 3 Theranocure Co., Ltd., Daegu 41405, Korea.
  • 4 Division of Applied RI, Korea Institute of Radiological and Medical Sciences, Seoul 139-706, Korea.
  • 5 Department of Chemistry, Kyungpook National University, Daegu 419944, Korea.
  • 6 Department of Radiology, Kyungpook National University Hospital, Daegu 41944, Korea.
  • 7 Department of Molecular Medicine, School of Medicine, Kyungpook National University, Daegu 41944, Korea.
PMID: 41801798 DOI: 10.1021/acs.jmedchem.5c03268
Abstract

To address the demands for safer and more effective gadolinium-based contrast agents (GBCAs) for magnetic resonance imaging (MRI), we developed Gd-PCTA-Ach, a novel macrocyclic complex featuring a lipophilic cyclohexanol pendant arm. Gd-PCTA-Ach exhibited superior relaxivity (r1 = 13.6 ± 0.2 and r2 = 15.8 ± 0.2 mM-1s-1 at 37 °C, 3.0 T) and kinetic inertness compared to clinically approved agents. Attributed to its enhanced lipophilicity, Gd-PCTA-Ach exhibits moderate albumin affinity (34.8%), resulting in prolonged blood circulation compared to standard extracellular fluid MRI agents. In vivo T1-weighted imaging demonstrated that Gd-PCTA-Ach is primarily cleared via the renal pathway but also exhibits partial hepatobiliary excretion, accounting for approximately 10% of the total elimination. Consequently, Gd-PCTA-Ach successfully visualized tumor lesions in both brain and liver tumor mouse models. These findings position Gd-PCTA-Ach as a highly potent, multipurpose contrast agent with an improved stability profile and broad diagnostic utility.

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