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Drug intelligence / Profile preview
melphalan-benzylguanidine hybrid
- Development stage
- Preclinical
- Lead developer
- University Hospital Tübingen
- Modality
- Small Molecules
01
Overview
Melphalan-benzylguanidine hybrids (MBGs) are novel targeted alkylating agents developed for the treatment of neuroblastoma. These hybrid molecules combine a norepinephrine transporter (NET)-targeting benzylguanidine moiety (inspired by meta-iodobenzylguanidine, or mIBG) with the cytotoxic alkylating functionality of melphalan. By leveraging the selective uptake of benzylguanidine via the norepinephrine transporter (also known as noradrenaline transporter, NAT) which is frequently overexpressed in neuroblastoma, these hybrids aim to deliver potent DNA-alkylating cytotoxicity directly to tumor cells while minimizing the systemic toxicities associated with conventional melphalan. Preclinical studies have demonstrated that certain monoalkylating and dialkylating hybrids (such as pM*BG and pMBG) exhibit selective NET-mediated uptake and enhanced in vitro cytotoxicity compared to melphalan.
- Other names
- MBGsmelphalan benzylguanidine hybridsmelphalan-benzylguanidine hybridsmM*BGmMBGpM*BGpMBG
02
Targets
DNANET (Norepinephrine Transporter)OCT (Organic cation transporter family)
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