Drug intelligence / Profile preview

triapine

Development stage
Phase 3
Lead developer
Nanopharmaceutics
Modality
Small Molecules
Administration
Intravenous
01

Overview

Triapine is a synthetic heterocyclic carboxaldehyde thiosemicarbazone and a potent inhibitor of ribonucleotide reductase, an enzyme essential for the conversion of ribonucleoside diphosphates to deoxyribonucleotides required for DNA synthesis. By chelating iron and inhibiting this enzyme, triapine depletes the pool of deoxynucleotides necessary for DNA replication and repair, selectively targeting rapidly dividing cancer cells. The active species is believed to be its iron chelate form. Triapine has been investigated primarily as an antitumor agent in various cancers including leukemia, lung cancer, kidney cancer, prostate cancer, and pancreatic cancer. It was initially developed by Vion Pharmaceuticals; after their bankruptcy in 2009 it was acquired by Nanotherapeutics and later transferred to Nanoshift LLC/Nanopharmaceutics[1][5][7].

Brand names
Triapine
Other names
3-Aminopyridine-2-carboxaldehyde thiosemicarbazone2-((3-Aminopyridin-2-yl)methylene)hydrazinecarbothioamide[(E)-(3-Aminopyridin‑2‑yl)methylideneamino]thioureaHydrazinecarbothioamide, 2‑((3-amino‑2-pyridinyl)methylene)-Hydrazinecarbothioamide, 2‑[(3-amino‑2-pyridinyl)methylene]-, (E)-
02

Targets

RRM2

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