[EN] CAR AND NRF2 DUAL ACTIVATOR AGENTS FOR CYCLOPHOSPHAMIDE-BASED AND DOXORUBICIN-BASED TREATMENTS OF CANCER<br/>[FR] AGENTS ACTIVATEURS DOUBLES DE CAR ET NRF2 POUR DES TRAITEMENTS DU CANCER À BASE DE CYCLOPHOSPHAMIDE ET À BASE DE DOXORUBICINE
申请人:UNIV MARYLAND
公开号:WO2021178684A1
公开(公告)日:2021-09-10
The disclosure relates to selective small molecule dual activators of human constitutive androstane receptor (hCAR) and nuclear factor erythroid 2-related factor 2 (Nrf2), pharmaceutical compositions thereof, and use thereof for the treatment of hematologic malignancies and other cancers. The small molecule dual hCAR and Nrf2 activators in combination with CPA based chemotherapy regimen provides a synergistic effect to help promote cytoxicity of the cyclophosphamide (CPA) based and doxorubicin (DOX) based anticancer treatments including CHOP regimen (CPA, doxorubicin, vincristine, and prednisone) while reducing cardiotixocity associated with DOX.
该公开涉及选择性的人类组成雄烷受体(hCAR)和核因子红细胞2相关因子2(Nrf2)的小分子双活化剂,其药物组合物以及用于治疗血液恶性肿瘤和其他癌症的用途。与CPA基础化疗方案结合使用的小分子双hCAR和Nrf2活化剂提供协同作用,有助于促进环磷酰胺(CPA)和多柔比星(DOX)为基础的抗癌治疗的细胞毒性,包括CHOP方案(CPA、多柔比星、长春碱和泼尼松),同时减少与DOX相关的心毒性。