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all-trans-[Pt(py)2(N3)2(biotin)(OH)]
- Development stage
- Preclinical
- Lead developer
- University of Warwick
- Modality
- Light/Condition-Responsive Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules
- Administration
- In Vitro (research), Potential For Intravenous Or Intratumoral If Clinically Translated
01
Overview
**all-trans-[Pt(py)2(N3)2(biotin)(OH)]** is a biotinylated, photoactive platinum(IV) anticancer prodrug designed to exploit both tumor-targeting by biotin conjugation and spatial activation via visible light irradiation. It features a platinum(IV) core coordinated with two pyridine (py) ligands, two azide (N3) ligands, one biotin moiety, and one hydroxide. The compound is highly stable in the dark; upon blue light irradiation (465 nm), it releases both cytotoxic Pt(II) species and azidyl radicals, promoting DNA binding (through inter- and intra-strand crosslinks) and inducing cell death. The biotin moiety enables potential targeting via avidin/streptavidin-based delivery systems. The drug demonstrates high photocytotoxicity in various cancer cell lines, including ovarian, lung, and prostate cancer. Developed and characterized by researchers at the University of Warwick, it is not currently developed by a commercial pharmaceutical company and is at the preclinical research stage[1][2].
- Other names
- trans,trans,trans-[Pt(py)2(N3)2(biotin)(OH)]
02
Targets
DNA
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