Development and evaluation of a theranostic probe with RGD peptide introduced platinum complex to enable tumor-specific accumulation

Cisplatin (CDDP) has been widely used for chemotherapy. However, it has several unfavorable side effects due to its low tumor selectivity. In this study, we designed, synthesized, and evaluated Pt(IV)-[c(RGDyK)]₂ (9), in which two molecules of an RGD peptide are introduced as a carrier molecule to cancer into oxoplatin, a Pt(IV) prodrug of CDDP, to enhance cancer selectivity. Furthermore, we prepared and evaluated Pt(IV)-[c(RGDyK)]{[¹²⁵I]c[RGDy(3-I)K]} ([¹²⁵I]10) for a preliminary step of nuclear medicine imaging and theranostics. Compound 9 inhibited cell growth in the cell viability assay and, [¹²⁵I]10 was highly accumulated in tumor tissues (1 h: 3.53 ± 0.53 %ID/g) in the biodistribution study. These results indicate that implementing RGD peptides into oxoplatin enabled tumor-specific accumulation, and combining [^123/124I]10 and 9 for diagnostic imaging and therapy could be useful for cancer theranostics.