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lurbinectedin
- Development stage
- Approved
- Lead developer
- PharmaMar
- Modality
- DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
- Administration
- Intravenous
01
Overview
Lurbinectedin is a synthetic alkaloid and chemotherapeutic agent used primarily for the treatment of metastatic small cell lung cancer (SCLC) in adults who have experienced disease progression after platinum-based chemotherapy. It is structurally related to trabectedin, with enhanced antitumor activity due to a specific chemical modification. Lurbinectedin acts as a DNA alkylating agent, binding covalently to guanine residues in the minor groove of DNA, which leads to DNA bending, disruption of transcription factor activity, impairment of DNA repair pathways, and ultimately double-strand breaks and cell death. Additionally, it inhibits RNA polymerase II-dependent transcription and modulates the tumor microenvironment by reducing monocyte/macrophage activity and infiltration into tumors[3][4][5][6][8]. The drug was developed from marine-derived compounds originally isolated from Ecteinascidia turbinata.
- Brand names
- Zepzelca
- Other names
- lurbinectedinum
02
Targets
TAM (TAM receptor tyrosine kinases)DNA minor groovePol II EC (RNA polymerase II elongation factor ELL)
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