파이프라인
한미약품은 축적된 연구 개발 기술력을 바탕으로 항암, 대사성, 심혈관 · 신장계, 희귀질환 치료제 분야에서
다양한 혁신신약을 개발하고 있습니다.

주요 파이프라인 소개

한미약품과 인류의 건강을 위한 창조와 혁신 그리고 도전 정신을 함께 할 파트너사를 찾습니다.

HM97662 (EZH1/2 inhibitor)

OVERVIEW

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 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

A novel and potent EZH1/2 dual inhibitor, HM97662 demonstrates antitumor activity in T-cell lymphoma
Poster, American Association for Cancer Research (AACR) 114th Annual meeting, 2023
Overcoming immune checkpoint blockade resistance via EZH1/2 dual inhibition by HM97662 in KRAS/LKB1 mutated NSCLC
Poster, American Association for Cancer Research (AACR) 113th Annual meeting, 2022
A novel and potent EZH1/2 dual inhibitor, HM97662, demonstrates antitumor activity in malignant tumors
Poster, American Association for Cancer Research (AACR) 112th Annual meeting, 2021