EpicentRx Inc., 11099 North Torrey Pines Road, Suite 160, La Jolla, California 92037, United States.
SciClone Pharmaceuticals Co., Ltd., 22 Floor, Shanghai Central Plaza, No. 381 Middle Huaihai Road, Huangpu, Shanghai 200020, China.
J Med Chem. 2021 Jun 10;64(11):7261-7271. doi: 10.1021/acs.jmedchem.1c00599. Epub 2021 May 27.
After extensive screening of aerospace compounds in an effort to source a novel anticancer agent, RRx-001, a first-in-class dinitroazetidine small molecule, was selected for advancement into preclinical and clinical development. RRx-001 is a minimally toxic small molecule with a distinct chemical structure and mechanism of action. The paradox of RRx-001 is that it mediates both antitumor cytotoxicity and normal tissue protection. The question of exactly how RRx-001 does this, and by means of what mechanism(s), depending on the route of delivery, intravenous or intratumoral, are explored. RRx-001 is currently in phase 2 and 3 clinical trials for the treatment of multiple solid tumor malignancies and as a supportive care drug.
经过广泛筛选航天化合物，以寻找一种新型的抗癌药物，RRx-001，一种首创的二硝基氮杂环丁烷小分子，被选中进行临床前和临床开发。RRx-001 是一种具有独特化学结构和作用机制的低毒性小分子。RRx-001 的矛盾之处在于，它既能介导抗肿瘤细胞毒性，又能保护正常组织。RRx-001 究竟是如何做到这一点的，以及通过何种机制（取决于给药途径，静脉内或肿瘤内），正在进行探索。RRx-001 目前正处于治疗多种实体瘤恶性肿瘤和支持性护理药物的 2 期和 3 期临床试验阶段。
