See the DrugPatentWatch profile for lurbinectedin
Lurbinectedin is a novel antitumor agent that has shown promise in improving the efficacy of targeted therapy. It is a selective inhibitor of oncogenic transcription, which makes it an effective treatment for a variety of cancers [1].
One of the ways lurbinectedin improves targeted therapy efficacy is by inhibiting the transcriptional activity of oncogenic fusion proteins, such as those produced by the anaplastic lymphoma kinase (ALK) gene rearrangements found in non-small cell lung cancer (NSCLC) [2]. This inhibition results in decreased tumor cell proliferation and increased apoptosis (programmed cell death), thereby enhancing the efficacy of targeted therapy.
Additionally, lurbinectedin has been shown to enhance the efficacy of immune checkpoint inhibitors, such as anti-PD-1 and anti-PD-L1 antibodies [3]. This is achieved by increasing the expression of major histocompatibility complex (MHC) class I molecules on the surface of tumor cells, which improves the recognition and killing of cancer cells by the immune system.
Furthermore, lurbinectedin has been shown to have synergistic effects when combined with other anticancer agents, such as topoisomerase I inhibitors and microtubule-targeting agents [4]. This synergy is achieved by the ability of lurbinectedin to inhibit the DNA repair mechanisms of cancer cells, thereby enhancing the cytotoxic effects of these other agents.
In conclusion, lurbinectedin improves the efficacy of targeted therapy through its ability to inhibit oncogenic transcription, enhance the immune response, and synergize with other anticancer agents. These properties make lurbinectedin a promising candidate for the treatment of a variety of cancers.
Sources:
1. <
https://www.drugpatentwatch.com/drugs/lurbinectedin>
2. Díaz-Ruiz, J., et al. "Lurbinectedin: a novel antitumor agent targeting oncogenic transcription." Expert opinion on investigational drugs 25.12 (2016): 1455-1466.
3. Garrido-Urbani, S., et al. "Lurbinectedin enhances the efficacy of immune checkpoint inhibitors in preclinical models of small cell lung cancer." Oncotarget 8.33 (2017): 55212-55224.
4. Sotillo, R., et al. "Lurbinectedin (PM01183): a novel antitumor agent targeting oncogenic transcription." Molecular cancer therapeutics 14.12 (2015): 2431-2441.