A Phase 1/2, Open-label Study Evaluating the Safety, Tolerability, Pharmacokinetics, Pharmacodynamics, and Efficacy of Chaperone-mediated Protein Degrader RNK05047 in Subjects with Advanced Solid Tumors (CHAMP-1)
DISEASE:
SOLID TUMOR CANCERS
SUMMARY:
RNK05047 is a chaperone-mediated degrader (CHAMP), a hetero-bifunctional small molecule that binds to both BRD4 and members of the heat-shock protein, 90KD (HSP90) chaperone protein family. Chemically induced proximity between BRD4 and HSP90 in cells results in degradation of BRD4 via the ubiquitin-proteasome system and downregulation of BRD4-regulated gene expressions.
RNK05047 accumulates in tumors relative to plasma and nontumor tissues and induces degradation of BRD4 protein, but not related members of the bromodomain and extraterminal (BET) protein family, BRD2 and BRD3.
In lay terms, people with amplified BRD4 have a higher expression of oncogenes which promote increased tumor cells, increased instability, metastasis and chemoresistance. HSP90 is a protein that assists other proteins to be more stabile and promotes tumor growth.
RNK05047 binds to both BRD4 and HSP90 resulting in the breakdown of these proteins which inhibits the growth of cancer cells.
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