TH-302 is a novel cancer therapeutic specifically activated under the low oxygen or "hypoxic" conditions typical of solid tumor cancer cells. TH-302 is a nitroimidazole-linked prodrug of a brominated derivative... TH-302 is a nitroimidazole-linked prodrug of a brominated derivative of an isophosphoramide mustard previously used in cancer drugs such as ifosfamide, cyclophosphamide, and glufosfamide.
- Mechanism
- Curator reviewed
TH-302 combines a 2-nitroimidazole oxygen-sensing trigger with a masked DNA crosslinker. Upon activation in oxygen deficient zones, TH-302 is converted selectively to the drug's active form, dibromo isophosphoramide mustard, a potent alkylator. TH-302 targets levels of severe hypoxia that are found in tumors but are rare in normal tissues - this is how selective targeting of the tumor occurs. After conversion to the active form of the drug, the hypoxic cells are exposed to high concentrations of released cytotoxic agent, which can also diffuse into the adjacent regions of the tumor.
- Primary indication
- Investigated for use/treatment in solid tumors.Curator reviewed
- Formula / weight
- C9H16Br2N5O4P · 449.04 g/mol (avg)
- Also known as
- (1-methyl-2-nitro-1H-imidazol-5-YL)methyl N,N'-bis(2-bromoethyl)diamidophosphate · (1-methyl-2-nitro-1H-imidazole-5-yl)methyl N,N'-bis(2-bromoethyl) diamidophosphate
- Code names
- HAP-302 · TH-302
Resolves to
UGJWRPJDTDGERK-UHFFFAOYSA-NSMILESCN1C(COP(=O)(NCCBr)NCCBr)=CN=C1[N+]([O-])=OWhat you can answer from here — as of July 03, 2026
Which companies are running trials of Evofosfamide, in which indications and phases, and which of those programs are still active?
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