Chemical Information

Biological Activity of TH-302

TH-302 is selective hypoxia-activated prodrug targeting hypoxic regions of solid tumors with IC50 of 19 nM, demonstrates 270-fold enhanced cytotoxicity under hypoxia versus their potency under aerobic conditions, stable to cytochrome P450 metabolism.
IC50 value:
Target:
TH-302 is a newly developed antineoplastic drug which represents a potential new class of tumor selective hypoxia-activated prodrugs (HAPs).

Clinical Information of TH-302

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References on TH-302

[1]. Inhibition of Both Thioredoxin Reductase and Glutathione Reductase may Contribute to the Anticancer Mechanism of TH-302 Full Text By Li, Shengrong; Zhang, Jinsong; Li, Jun; Chen, Dongming; Matteucci, Mark; Curd, John; Duan, Jian-Xin From Biological Trace Element Research (2010), 136(3), 294-301.

[2]. Phase 1 Study of the Safety, Tolerability, and Pharmacokinetics of TH-302, a Hypoxia-Activated Prodrug, in Patients with Advanced Solid Malignancies Full Text By Weiss, Glen J.; Infante, Jeffrey R.; Chiorean

[3]. Liu Q, et al. TH-302, a hypoxia-activated prodrug with broad in vivo preclinical combination therapy efficacy: optimization of dosing regimens and schedules. Cancer Chemother Pharmacol. 2012 Jun;69(6):1487-98.

[4]. Jung D, et al. Metabolism and excretion of TH-302 in dogs. Xenobiotica. 2012 Jul;42(7):687-700.

[5]. Sun JD, et al. Selective tumor hypoxia targeting by hypoxia-activated prodrug TH-302 inhibits tumor growth in preclinical models of cancer. Clin Cancer Res. 2012 Feb 1;18(3):758-70.