HSP90 (Heat Shock Protein 90) is a molecular chaperone that regulates protein folding, stability, and degradation within cells, playing a critical role in maintaining the stability of multiple oncoproteins essential for cancer cell growth and survival.
HSP90 inhibitors have been developed to block the function of these oncoproteins, thereby inhibiting cancer cell growth and survival. This highlights its therapeutic potential in various solid tumors.
Potential anticancer efficacy in ovarian cancer, lung cancer, glioblastoma, and other solid tumors.
Additionally, HSP90-targeted therapy is gaining attention for regulating compensatory pathways in cancer cells resistant to existing target therapies.
Introduction of JIN-001
Oral HSP90 inhibitor.
Targets dysregulated HSP90 expression in various cancers.
Demonstrates potent anticancer efficacy as monotherapy in ovarian cancer, lung cancer, and glioblastoma.
Combination therapy enhances sensitivity to existing anticancer drugs and delays resistance development.
Potential to expand indications to various solid tumors.
Mechanism of Action of JIN-001
Binds to the ATP-binding site of HSP90, inhibiting its function.
This destabilizes client proteins, leading to their degradation.
Client proteins include oncogenic signaling molecules such as EGFR, HER2, ALK, BCR-ABL, AKT, and c-MET.
Key Research Findings of JIN-001
Ovarian Cancer: Combination therapy of JIN-001 with cisplatin demonstrates superior tumor suppression compared to cisplatin alone, reducing the expression of key signaling and cisplatin resistance-related proteins, thereby prolonging the inhibition of cancer cell proliferation.
Lung Cancer
JIN-001 demonstrates tumor suppression without safety issues at tested doses when administered as monotherapy in lung cancer animal models and EGFR-TKI resistant lung cancer cell lines.
Combination of JIN-001 and EGFR-TKI in EGFR-TKI resistant lung cancer cell lines demonstrates tumor suppression without observable toxicity compared to monotherapy.
Glioblastoma
JIN-001 demonstrates blood-brain barrier (BBB) permeability, a major challenge in treating glioblastoma, in in vivo pharmacokinetic analysis.
JIN-001 demonstrates significant therapeutic efficacy in glioblastoma animal models, inhibiting tumor growth and survival via HSP90 regulation. This indicates its high potential as a treatment for central nervous system cancers.