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Pt(II) Complex with FGFR4 Specificity as a Targeted Drug Conjugate for the Treatment of Hepatocellular Carcinoma

Libo Cai1, Gang Xu1, Shaohua Gou1

  • 1Pharmaceutical Research Center and School of Chemistry and Chemical Engineering, Southeast University, Nanjing 211189, China.

Inorganic Chemistry
|March 30, 2026
PubMed

Insights

A novel targeted drug conjugate, Len-604, combines lenvatinib with a carboplatin analogue to target hepatocellular carcinoma (HCC). This approach shows potent antitumor activity and reduced toxicity compared to existing treatments.

Area of Science:

  • Oncology
  • Medicinal Chemistry
  • Pharmacology

Background:

  • Hepatocellular carcinoma (HCC) is a challenging cancer with limited effective treatments.
  • Current therapies like targeted therapy and chemotherapy often have insufficient efficacy or severe side effects.

Purpose of the Study:

  • To develop a novel targeted drug conjugate (TDC) for HCC treatment.
  • To synthesize and evaluate a new platinum(II) complex, Len-604, by conjugating lenvatinib with a carboplatin analogue (DN604).

Main Methods:

  • Synthesized Len-604, a Pt(II) complex linking lenvatinib and DN604.
  • Assessed the binding affinity of Len-604 to fibroblast growth factor receptor 4 (FGFR4) protein.
  • Evaluated the in vitro cytotoxicity against HCC cell lines (HUH-7, SMMC-7721).
  • Tested the in vivo antitumor efficacy and toxicity in HUH-7 xenograft models.

Main Results:

  • Len-604 demonstrated specific binding to FGFR4 both in vitro and in vivo.
  • The compound exhibited potent cytotoxicity against HCC cell lines with low IC50 values.
  • In vivo studies showed Len-604 possessed superior antitumor activity compared to lenvatinib.
  • Len-604 displayed reduced toxicity relative to cisplatin and a lenvatinib-cisplatin physical mixture.

Conclusions:

  • Len-604 effectively targets HCC by leveraging the TDC strategy.
  • This novel conjugate offers a promising therapeutic approach for HCC with improved efficacy and safety profiles.

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