Table 1.

Bioreductive prodrugs of DNA-reactive cytotoxins recently or currently in clinical development (modified from Wilson & Hay, 2011)

Prodrug	Current clinical status	Company or institution	Chemical class	Mechanism of cytotoxicity
Tirapazamine (SR 4233)	Phase III, cervix (closed)	SRI International/NCI	Aromatic N-oxide	Complex DNA damage
Apaziquone (E09)	Phase III, bladder (closed)	Spectrum	Quinone	ICL
TH-302	Phase I/II, multiple (active)	Threshold	Nitro	ICL
PR-104	Phase I/II, leukaemia (active)	Proacta and University of Auckland	Nitro	ICL
Banoxantrone (AQ4N)	Recent Phase I/II	Novacea	Aliphatic N-oxide	TOPOII
Caricotamide (EP-0152R) plus tretazicar (CB1954)	Phase II, HCC (discontinued)	BTG	Nitro	ICL
RH1	Recent Phase I	CRUK	Quinone	ICL
NLCQ-1	Preclinical	Evanston Hospital	Nitro	TOPOII or multiple?
SN30000 (CEN-209)	Preclinical	Centella and University of Auckland	Aromatic N-oxide	Complex DNA damage
SN29730	Preclinical	University of Auckland	Nitro	Adenine N3 alkylation
KS119W	Preclinical	Yale University	Nitro	Guanine O6 ICL

CRUK, Cancer Research UK; HCC, hepatocellular carcinoma; ICL, DNA interstrand crosslink; NCI, US National Cancer Institute; TOPOII, topoisomerase II

Used with permission from Wilson et al (2011) Targeting hypoxia in cancer therapy. Nature Reviews. Cancer, 11, 393–410.