TH-302
| TH-302 | |
|---|---|
| [[File:|frameless|220px|alt=|]] | |
| INN | |
| Drug class | |
| Routes of administration | Intravenous |
| Pregnancy category | |
| Bioavailability | |
| Metabolism | |
| Elimination half-life | |
| Excretion | |
| Legal status | |
| CAS Number | 918633-87-1 |
| PubChem | 16054624 |
| DrugBank | |
| ChemSpider | 17286447 |
| KEGG | |
TH-302, also known as Evofosfamide, is a hypoxia-activated prodrug that has been investigated for its potential use in cancer therapy. It is designed to target the hypoxic regions of tumors, which are often resistant to conventional therapies.
Mechanism of Action[edit | edit source]
TH-302 is a prodrug that is activated under low oxygen conditions, which are commonly found in solid tumors. The drug is composed of a 2-nitroimidazole moiety linked to a bromo-isophosphoramide mustard (Br-IPM) moiety. Under hypoxic conditions, the 2-nitroimidazole is reduced, releasing the active cytotoxic agent, Br-IPM, which can then alkylate DNA and induce cell death.
Clinical Development[edit | edit source]
TH-302 has been evaluated in several clinical trials for the treatment of various cancers, including pancreatic cancer, soft tissue sarcoma, and non-small cell lung cancer. In these trials, TH-302 was often used in combination with other chemotherapeutic agents such as doxorubicin and gemcitabine.
Pancreatic Cancer[edit | edit source]
In a phase III clinical trial, TH-302 was combined with gemcitabine for the treatment of advanced pancreatic cancer. The trial aimed to assess the efficacy and safety of the combination compared to gemcitabine alone.
Soft Tissue Sarcoma[edit | edit source]
TH-302 was also studied in combination with doxorubicin in a phase III trial for patients with advanced soft tissue sarcoma. The trial evaluated the overall survival and progression-free survival of patients receiving the combination therapy.
Challenges and Future Directions[edit | edit source]
Despite promising preclinical data, the clinical development of TH-302 has faced challenges. Some trials did not meet their primary endpoints, leading to questions about the drug's efficacy in certain cancer types. However, research continues to explore the potential of TH-302 in combination with other therapies and in different cancer settings.
Also see[edit | edit source]
Alphabetic list of antineoplastic agents - 0-9 - A1 - A2 - A3 - A4 - A5 -A6 - B - C - D - E - F - G - H - I - JK - L - M - NO - PQ - R - S - T - UVW - XYZ
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