Drug intelligence / Profile preview

Fostroxacitabine bralpamide

Development stage
Phase 2
Lead developer
Medivir
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Oral
01

Overview

Fostroxacitabine bralpamide is a liver-targeting nucleotide phosphoramidate prodrug of troxacitabine monophosphate, designed to deliver the active cytotoxic agent selectively to the liver. Upon oral administration, it is rapidly hydrolyzed in hepatocytes by carboxylesterase 1, generating high levels of troxacitabine triphosphate in the liver. This metabolite is incorporated into tumor cell DNA, leading to chain termination and inhibition of DNA synthesis, resulting in antitumor activity. The drug aims to maximize exposure within the liver while minimizing systemic toxicity and adverse effects on other organs. It is under development primarily for hepatocellular carcinoma (HCC) and other primary or secondary tumors affecting the liver[1][2][4][5][6].

Brand names
fostrox
Other names
Fostroxacitabine bralpamide [USAN]UNII-Q1I6YZ0NGFUNII-Q-1I6YZ0NGFUNII-Q 1I6YZ0NGFQ1I6YZ0NGFQ-1I6YZ0NGFQ 1I6YZ0NGF
02

Targets

DNA polymerase family

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