gz17-6.02

GZ17-6.02 is a synthetically manufactured small molecule compound composed of three active ingredients: curcumin, harmine, and isovanillin[2][3][5][7]. It is under clinical investigation primarily as an anti-cancer agent for solid tumors, lymphoma, and multiple myeloma[2][3][5]. Mechanistically, GZ17-6.02 induces apoptosis in tumor cells through caspase-3 activation and PARP cleavage; it also initiates a DNA damage response via ataxia-telangiectasia mutated (ATM) activation that leads to autophagy and cell death[1][8]. The drug inhibits key pathways involved in tumor progression by attenuating macrophage infiltration and inhibiting phosphorylation of mediators such as Src kinase[1], mammalian target of rapamycin complex 1/2, eukaryotic translation initiation factor 2 subunit alpha (eIF2α), nuclear factor kappa-light-chain-enhancer of activated B cells (NFκB), the Hippo pathway (YAP/TAZ), among others[2][3][7]. GZ17-6.02 has demonstrated synergistic effects with proteasome inhibitors (e.g., bortezomib) and other chemotherapeutics across various cancer types including prostate cancer, renal carcinoma, breast cancer, colorectal cancer, pancreatic cancer, hepatic cancers, biliary cancers, non-small cell lung cancer (NSCLC), melanoma (cutaneous and uveal), sarcoma and actinic keratoses[2][3][4][5][6]. The drug received its IND from the FDA in 2018; phase I trials have established a recommended phase 2 dose of 375 mg orally twice daily with an overall favorable safety profile marked by reversible grade 1–3 liver enzyme elevations[2].

Other names

super enhancer inhibitor gz17-6.02