KINETO Lab announcing that research about in vitro and in vivo evaluation of bombesin-MMAE conjugates for targeted tumour therapy, was published in European Journal of Medicinal Chemistry.

Prostate cancer is the most incident in male population and the second cause of death. Targeted tumour therapy has proved to be an efficient alternative to overcome the limitations of conventional chemotherapy. One of the target which can be exploited for targeted delivery of drugs is bombesin receptor 2 (BB2) which is highly overexpressed in prostate tumors. Therefore, our partners form HUN-REN-ELTE research group of Peptide Chemistry synthesized peptide drug conjugates (PDCs) containing bombesin receptor-targeting moiety which were armed with tubulin binder monomethyl auristatin E (MMAE), and with different in mouse plasma stability initial and optimized linkers.

These PDCs were tested in vitro, as well as in in vivo experiments using both acute and chronic treatment strategies. All conjugates significantly inhibited the growth of a human prostate PC-3 tumor in mice in both acute and chronic in vivo efficacy studies compared to the control as well as to free drug groups. Moreover, in acute in vivo efficacy study all conjugates significantly extended survival of mice bearing PC-3 tumor, compared to the administration of the free drug and to the control group.

One of the conjugate revealed good accumulation in tumor tissue in biodistribution studies, and showed outstanding antitumor effect and prolonged survival of mice, suggesting it possible application as targeted therapy against prostate cancer.

The publication can be accessed under the following link.