Triapine® is designed to prevent the replication of tumor cells by blocking an enzyme necessary for DNA synthesis and repair. Triapine® is being evaluated in clinical trials sponsored by the National Cancer Institute.
A: Triapine® is a small molecule that inhibits an enzyme, ribonucleotide reductase, important to the synthesis of DNA. DNA synthesis is necessary for cancer cells to replicate; therefore inhibition of the ribonucleotide reductase enzyme can prevent cancer cells from dividing in the body. Disruption of DNA synthesis in some cancer cells will also cause their death.
DNA synthesis is also involved in repairing damage to cancer cells that have been treated with many standard cancer chemotherapy agents. The ability of cancer cells to rapidly repair DNA damage caused by chemotherapy is one reason that cancer cells become resistant to standard anticancer agents. Because Triapine® inhibits DNA synthesis, it can inhibit DNA repair.
Preclinical experiments conducted by Vion have shown that Triapine® can increase the antitumor effects of standard cancer agents such as cisplatin, cyclophosphamide, and etoposide in mouse tumor models.
A: Triapine® is being evaluated in clinical trials sponsored by the National Cancer Institute. Search “Triapine” at clinicaltrials.gov for a list of trials.
Vion has previously conducted several clinical trials of Triapine®.