Drug intelligence / Profile preview

evofosfamide + gemcitabine

Development stage
Unknown
Lead developer
Merck KGaA
Modality
Small Molecules
Administration
Intravenous
01

Overview

Evofosfamide + gemcitabine is a combination of a hypoxia-activated prodrug (evofosfamide, also known as TH-302) and the nucleoside analog chemotherapeutic gemcitabine. Evofosfamide is designed to be selectively activated under the hypoxic conditions commonly found in solid tumors, releasing an alkylating agent (bromo-isophosphoramide mustard) that induces DNA cross-linking and cell death. Gemcitabine is a cytidine analog that inhibits DNA synthesis through incorporation into DNA and inhibition of ribonucleotide reductase. This combination was investigated mainly in metastatic or locally advanced unresectable pancreatic ductal adenocarcinoma and soft tissue sarcoma. Although early studies suggested potential synergistic activity—gemcitabine may increase tumor hypoxia, further activating evofosfamide—large clinical trials did not demonstrate a statistically significant improvement in overall survival over gemcitabine alone[1][2][3][5].

Brand names
Gemzar
Other names
evofosfamide plus gemcitabineTH-302 plus gemcitabineTH302 plus gemcitabineTH 302 plus gemcitabine
02

Targets

DNARNR (Ribonucleotide reductase)

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