Hanmi R&D becomes stronger through cooperation with partners.
- efocipegtrutide (LAPSTriple agonist)
- sonefpeglutide (LAPSGLP-2 analog)
- efpegerglucagon (LAPSGlucagon analog)
- HM97662 (EZH1/2 inhibitor)
- BH3120 (PD-L1/4-1BB BsAb)
- HM15275 (LA-GLP/GIP/GCG)
- HM16390 (LAPSIL-2 analog)
- HM17321 (LA-UCN2)
- HM99462 (SOS1 inhibitor)
- LAPS Glucagon Combo
HM97662 (EZH1/2 inhibitor)
Oncology
Phase 1
Overview
Next generation EZH1/2 dual inhibitor overcoming
the resistance mechanism
Description
the resistance mechanism
Either enhancer of zeste homolog 2 (EZH2) or its homolog EZH1, the enzymatic core subunit of polycomb repressive complex 2 (PRC2), acts an essential role in the maintenance of transcriptional repression by the methylation of histone H3 lysine 27 (H3K27). The dysfunctions of EZH2 or the alterations of regulatory proteins have been reported to be associated with the development and progression of a variety of malignant tumors. Dual inhibition of EZH1 and EZH2 could be more effective than EZH2 inhibition alone in blocking PRC2 functions as an anti-cancer therapy.Therefore, we have developed HM97662 which is an oral, highly potent next generation EZH2 inhibitor with enhanced EZH1 inhibitory activity.
Antitumor activities of HM97662
- Effective target modulation profiles (inhibition of H3K27me3, induction of B-cell differentiation, etc.)
- Potent growth inhibition of a variety of cancer cells associated with EZH2 or regulatory proteins such as ARID1A
- Proven effective inhibition of Tazemetostat-resistant cell growth with elevated EZH1
- Excellent inhibition of tumor growth in xenograft models of cancer cells with altered EZH2 or regulatory proteins
- Potential of restoring weakened anticancer immunity of immune checkpoint inhibitors in cancers with LKB1 loss
Clinical Development
- A phase 1 study is ongoing in Australia and Korea NCT05598151
Publications