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MP-16

Development stage: Preclinical
Modality: MicroRNA (miRNA) → Small RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics, Antisense Oligonucleotides (ASOs) → Long RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics, PROTACs (E3 ligase recruitment) → Targeted Protein Degraders (TPDs) → Small Molecules, Antisense DNA → DNA Therapeutics → Nucleic Acid Therapeutics, Small Interfering RNA (siRNA) → Small RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics, Bivalent/Multivalent Binders → Multivalent & Scaffold-Based Small Molecules → Small Molecules
Administration: Oral

Overview

MP-16 is an oligonucleotide-based proteolysis-targeting chimera (PROTAC) designed for the treatment of hepatocellular carcinoma (HCC). It functions by conjugating the VHL E3 ligase ligand VH032 with an optimized DNA sequence that specifically recognizes the oncogenic transcriptional factor c-Myc. This conjugation leads to the formation of a VHL/PROTAC/c-Myc ternary complex, which subsequently triggers the degradation of c-Myc via the ubiquitin-proteasome system. Preclinical studies in mice models have shown that MP-16 significantly inhibits HCC tumor growth and demonstrates promising drug safety.

Targets

VHL (Von Hippel–Lindau tumor suppressor protein)MYC (MYC proto-oncogene protein)

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