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PC-002
PC-002 is a novel small-molecule drug targeting the MYC gene mutation, which has been approved by the FDA for an MRCT phase 2 clinical study in high-grade B-cell lymphoma (HGBCL) and neuroendocrine prostate cancer (NEPC).
  • To develop a MYC targeting drug has been a challenge for many years
    • MYC acts as a transcription factor and transcription signal amplifier to regulate the expression of hundreds of other genes. Direct inhibition of MYC will affect many physiological processes.
    • MYC protein has a flexible structure. No active binding pocket of small molecules has been identified.
    • MYC binds to DNA as part of a protein complex. It can also bind to promoters/enhancers directly. It is difficult to develop small molecule drugs that directly target MYC protein-protein and protein-DNA interactions.
  • Novel targeting mechanism
    • The new direct target of PC-002 screened out by i-CR® platform is responsible for the selective degradation of MYC protein, thus turns Myc from “un-targetable” into “targetable”.
    • Inhibition of this target protein can efficiently induce apoptosis of cancer cells with deregulated Myc gene.
  • Specifically effective for cancers with Myc gene alteration
    • c-Myc amplification and translocation are correlated with PC-002 sensitivity. PC-002 displays strong inhibitory effects on diffused large B cell lymphomas (DLBCL) with c-Myc translocation.
    • N-Myc amplification is correlated with PC-002 sensitivity. PC-002 displays strong inhibitory effects on neuroblastomas with N-MYC amplification.
    • PC-002 demonstrates significant effect on various tumor models, in vitro and in vivo.
    • Eleven clinical trials with good safety results.
    • A phase II clinical trial is imminent. The application for the trial has been submitted to the FDA.
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