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Lurbinectedin is a marine-derived chemotherapeutic agent classified as a DNA alkylating agent, primarily used for the treatment of metastatic small-cell lung cancer (SCLC) in adults who have progressed after platinum-based chemotherapy. It acts by binding to the minor groove of DNA, inhibiting transcription and leading to apoptosis in cancer cells. Lurbinectedin also exhibits immune-modulatory effects by activating the Stimulator of interferon genes (STING) protein pathway, promoting anti-tumor immune responses[2][3][5][8]. Itraconazole is an oral triazole antifungal that inhibits fungal lanosterol 14α-demethylase, disrupting ergosterol synthesis and compromising fungal cell membrane integrity[4][7]. When co-administered, itraconazole—a strong Cytochrome P450 3A4 (CYP3A4) inhibitor—significantly increases systemic exposure to lurbinectedin by reducing its clearance and prolonging its half-life; this necessitates dose adjustments of lurbinectedin to avoid toxicity[1][6].
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