See the DrugPatentWatch profile for lurbinectedin

Lurbinectedin is an antineoplastic agent, used in the treatment of various types of cancer. Its mechanism of action is primarily based on its interaction with DNA repair processes.

Lurbinectedin intercalates into DNA, causing a distortion in the double helix [1]. This distortion prevents the progression of RNA polymerase II, leading to the inhibition of transcription [1]. Furthermore, lurbinectedin has been found to trigger DNA double-strand breaks (DSBs) [1].

The drug's ability to induce DSBs is particularly significant because it activates the DNA damage response (DDR) pathway [1]. The DDR pathway is a complex network of proteins that detect and repair various types of DNA damage [1]. Lurbinectedin's interaction with the DDR pathway leads to the inhibition of DNA repair, which ultimately results in the death of cancer cells [1].

Moreover, lurbinectedin has been shown to inhibit the activity of PARP1, a key protein involved in the repair of single-strand breaks (SSBs) [1]. Inhibition of PARP1 leads to the accumulation of SSBs, which can subsequently lead to the formation of DSBs [1]. This further exacerbates the DNA damage response, contributing to the drug's anticancer effects.

In summary, lurbinectedin's mechanism of action involves the intercalation into DNA, leading to the inhibition of transcription and the induction of DNA double-strand breaks. The activation of the DNA damage response pathway and the inhibition of DNA repair processes contribute to the drug's anticancer effects.

Sources:
[1] DrugPatentWatch.com - Lurbinectedin - <https://www.drugpatentwatch.com/drugs/lurbinectedin>