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Current Developments in Pt(IV) Prodrugs Conjugated with Bioactive Ligands.
Xuejiao Li1, Yahong Liu2, Hongqi Tian1
1Tianjin Key Laboratory of Radiation Medicine and Molecular Nuclear Medicine, Institute of Radiation Medicine, Chinese Academy of Medical Sciences and Peking Union Medical College, Tianjin 300192, China.
Bioinorganic Chemistry and Applications
|November 8, 2018
Summary
Platinum(IV) (Pt(IV)) prodrugs conjugated with bioactive ligands show promise for enhanced cancer treatment by reducing side effects and overcoming resistance. Further research is needed for clinical approval.
Area of Science:
- Medicinal Chemistry
- Oncology
- Drug Delivery Systems
Background:
- Cisplatin, a widely used chemotherapy drug, faces challenges including significant side effects and acquired resistance.
- Platinum(IV) (Pt(IV)) prodrugs offer a promising strategy to overcome these limitations through modified structures.
- Conjugation with bioactive ligands aims to enhance targeting and introduce dual-function therapeutic effects.
Purpose of the Study:
- To review recent advancements in Pt(IV) prodrugs functionalized with bioactive-targeting ligands.
- To highlight the potential of these novel anticancer agents in preclinical settings.
- To identify future directions for the clinical development of Pt(IV) prodrugs.
Main Methods:
- Synthesis of Pt(IV) prodrugs incorporating modifications such as lipid chains, nanoparticles, and peptide chains.
- Conjugation of Pt(IV) complexes with various bioactive ligands, including histone deacetylase inhibitors, p53 agonists, alkylating agents, and nonsteroidal anti-inflammatory agents.
- Evaluation of anticancer efficacy and drug delivery improvements associated with these modified Pt(IV) complexes.
Main Results:
- Pt(IV) prodrugs conjugated with bioactive ligands demonstrate significant anticancer activity in preclinical studies.
- Modifications enhance hydrophobicity, improve drug delivery, and enable dual-action therapeutic strategies.
- Despite promising results, no Pt(IV) prodrugs conjugated with bioactive ligands have yet received clinical approval.
Conclusions:
- Pt(IV) prodrugs represent a valuable platform for developing next-generation cancer therapeutics.
- The conjugation of Pt(IV) complexes with bioactive ligands offers a rational approach to enhance efficacy and mitigate toxicity.
- Continued research and development are crucial to translate these promising preclinical findings into effective clinical treatments.
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