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BTP-114

Development stage
Phase 1
Lead developer
Placon Therapeutics
Modality
DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules, Peptide-Drug Conjugates → Peptide Conjugates → Peptides, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

BTP-114 is a proprietary, albumin-binding platinum-based complex that acts as a prodrug of cisplatin. It features a maleimide moiety enabling strong and selective binding to human serum albumin (HSA), which allows for preferential uptake by cancer cells and prolonged circulation in the bloodstream. Upon administration, BTP-114 rapidly conjugates to serum albumin, resulting in increased tumor accumulation and reduced dose-limiting toxicities compared to conventional cisplatin. Its mechanism of action involves DNA cross-linking leading to enhanced DNA damage and cell death in cancer cells. Preclinical studies have demonstrated improved efficacy over cisplatin in models of lung and ovarian cancer with reduced toxicity. The drug was developed leveraging advances in platinum chemistry pioneered by Professor Stephen J. Lippard at MIT[1][2][5][7].

Other names
albumin-binding cisplatin prodrug BTP-114
02

Targets

DNA

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