lurbinectedin acts as a selective inhibitor of RNA polymerase II, an enzyme involved in transcription. By inhibiting RNA polymerase II, lurbinectedin disrupts the transcription of genes critical for tumor cell survival and proliferation. lurbinectedin causes DNA damage by forming covalent adducts with DNA.
This leads to the formation of DNA-protein cross-links and DNA strand breaks, resulting in DNA damage within tumor cells. The inhibition of transcription and induction of DNA damage by lurbinectedin collectively contribute to its antiproliferative effects. It intrudes with the ability of cancer cells to replicate and divide, ultimately inhibiting tumor growth.
lurbinectedin has shown efficacy in treating relapsed or refractory small-cell lung cancer, a highly aggressive and often challenging-to-treat form of lung cancer.
lurbinectedin has also demonstrated activity in metastatic triple-negative breast cancer, a subtype lacking estrogen receptors, progesterone receptors, and HER2/neu amplification. TNBC is often associated with a poorer prognosis and limited treatment options.