Synergistic Machine Learning Accelerated Discovery of Nanoporous Inorganic Crystals as Non-Absorbable Oral Drugs.

Journal: Advanced materials (Deerfield Beach, Fla.)
PMID:

Abstract

Machine learning (ML) has taken drug discovery to new heights, where effective ML training requires vast quantities of high-quality experimental data as input. Non-absorbable oral drugs (NODs) have unique safety advantage for chronic diseases due to their zero systemic exposure, but their empirical discovery is still time-consuming and costly. Here, a synergistic ML method, integrating small data-driven multi-layer unsupervised learning, in silico quantum-mechanical computations, and minimal wet-lab experiments is devised to identify the finest NODs from massive inorganic materials to achieve multi-objective function (high selectivity, large capacity, and stability). Based on this method, a NH-form nanoporous zeolite with merlinoite (MER) framework (NH-MER) is discovered for the treatment of hyperkalemia. In three different animal models, NH-MER shows a superior safety and efficacy profile in reducing blood K without Na release, which is an unmet clinical need in chronic kidney disease and Gordon's syndrome. This work provides a synergistic ML method to accelerate the discovery of NODs and other shape-selective materials.

Authors

  • Liang Xiang
    School of Biomedical Engineering, Shanghai Jiao Tong University, Shanghai, 200240, P. R. China.
  • Jiangzhi Chen
    School of Physics Science and Engineering, Tongji University, Shanghai, 200092, P. R. China.
  • Xin Zhao
    Florida International University.
  • Jinbin Hu
    School of Physics Science and Engineering, Tongji University, Shanghai, 200092, P. R. China.
  • Jia Yu
    Institutes for Systems Genetics, Frontiers Science Center for Disease-related Molecular Network, West China Hospital, Sichuan University, Chengdu 610212, Sichuan, China; School of Clinical Medicine, Soochow University, Suzhou 215123, Jiangsu, China.
  • Xiaodong Zeng
    School of Biomedical Engineering, Shanghai Jiao Tong University, Shanghai, 200240, P. R. China.
  • Tianzhi Liu
    School of Biomedical Engineering, Shanghai Jiao Tong University, Shanghai, 200240, P. R. China.
  • Jie Ren
    Digital Clinical Measures, Translational Medicine, Merck & Co., Inc., Rahway, NJ, United States.
  • Shiyi Zhang
    Department of Psychiatry, the First Affiliated Hospital, Zhejiang University School of Medicine, Hangzhou 310003, China; The Key Laboratory of Mental Disorder Management in Zhejiang Province, Hangzhou 310003, China.