Pt(II) Complex with FGFR4 Specificity as a Targeted Drug Conjugate for the Treatment of Hepatocellular Carcinoma. (PubMed, Inorg Chem)
Guided by the targeted drug conjugate (TDC) strategy, the pharmacophore of lenvatinib was modified by incorporating DN604 (C6H10N2O5Pt), a carboplatin analogue, to generate a Pt(II) complex Len-604 (C30H33ClN8O9Pt). It exhibited potent cytotoxicity against human hepatocellular carcinoma cell lines HUH-7 and SMMC-7721, with IC50 values of 5.62 and 5.64 μM, respectively. Significantly, in HUH-7 xenograft models, Len-604 exhibited stronger antitumor activity than lenvatinib, while showing lower toxicity than cisplatin and its physical mixture with lenvatinib.