VP-128

VP-128 is a **novel hybrid molecule** that links **17β-oestradiol (E2)** to a **platinum(II) complex**. It was developed to selectively target **estrogen receptor alpha (ERα)-positive cancers**, especially breast cancer cells. Compared to cisplatin, VP-128 shows markedly improved anti-tumor activity towards ERα-positive MCF-7 breast cancer cells both in vitro and in vivo, without increasing systemic toxicity. VP-128’s mechanism involves selective binding to ERα, induction of apoptosis in ERα-positive cells, and modulation of ER-regulated gene expression. In ERα-negative cells, it induces apoptosis via mitochondrial pathways. This dual targeting makes VP-128 a promising candidate for hormone-dependent cancer therapy[1][5]. Developed originally as an E-CDDP derivative (estradiol-cisplatin conjugate), VP-128 retains high affinity for estrogen receptors and incorporates platinum-based cytotoxicity[1][5].

Other names

17beta-oestradiol-platinum(II) hybridE(2)-linked platinum(II) hybridestradiol-linked platinum(II) complex