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DIGs can reach much higher concentrations than that achieved by API, which raises great concerns about their clinical toxicities. Therefore, the biological activities of DIG on physiologically relevant target are widely demanded by both clinical investigation and pharmaceutical industry. However, such activity data are not available in any existing pharmaceutical knowledge base, and their potentials in predicting the DIG-target interaction have not been evaluated yet. In this study, the comprehensive assessment and analysis on the biological activities of DIGs were therefore conducted. First, the largest number of DIGs and DFMs were systematically curated and confirmed based on all drugs approved by US Food and Drug Administration. Second, comprehensive activities for both DIGs and DFMs were provided for the first time to pharmaceutical community. Third, the biological targets of each DIG and formulation were fully referenced to available databases that described their pharmaceutical\/biological characteristics. Finally, a variety of popular artificial intelligence techniques were used to assess the predictive potential of DIGs\u2019 activity data, which was the first evaluation on the possibility to predict DIG\u2019s activity. As the activities of DIGs are critical for current pharmaceutical studies, this work is expected to have significant implications for the future practice of drug discovery and precision medicine.<\/jats:p>","DOI":"10.1093\/bib\/bbac160","type":"journal-article","created":{"date-parts":[[2022,4,14]],"date-time":"2022-04-14T11:16:25Z","timestamp":1649934985000},"source":"Crossref","is-referenced-by-count":13,"title":["Biological activities of drug inactive ingredients"],"prefix":"10.1093","volume":"23","author":[{"given":"Chenyang","family":"Zhang","sequence":"first","affiliation":[{"name":"College of Pharmaceutical Sciences, The Second Affiliated Hospital, Zhejiang University School of Medicine, Zhejiang University , Hangzhou 310058, China"}]},{"given":"Minjie","family":"Mou","sequence":"additional","affiliation":[{"name":"College of Pharmaceutical Sciences, The Second Affiliated Hospital, Zhejiang University School of Medicine, Zhejiang University , Hangzhou 310058, China"}]},{"given":"Ying","family":"Zhou","sequence":"additional","affiliation":[{"name":"College of Pharmaceutical Sciences, The Second Affiliated Hospital, Zhejiang University School of Medicine, Zhejiang University , Hangzhou 310058, China"},{"name":"State Key Laboratory for Diagnosis and Treatment of Infectious Disease, Collaborative Innovation Center for Diagnosis and Treatment of Infectious Diseases, Zhejiang Provincial Key Laboratory for Drug Clinical Research and Evaluation, The First Affiliated Hospital, Zhejiang University , 79 QingChun Road, Hangzhou, Zhejiang 310000, China"}]},{"given":"Wei","family":"Zhang","sequence":"additional","affiliation":[{"name":"College of Pharmaceutical Sciences, The Second Affiliated Hospital, Zhejiang University School of Medicine, Zhejiang University , Hangzhou 310058, China"}]},{"given":"Xichen","family":"Lian","sequence":"additional","affiliation":[{"name":"College of Pharmaceutical Sciences, The Second Affiliated Hospital, Zhejiang University School of Medicine, Zhejiang University , Hangzhou 310058, China"}]},{"given":"Shuiyang","family":"Shi","sequence":"additional","affiliation":[{"name":"College of Pharmaceutical Sciences, The Second Affiliated Hospital, Zhejiang University School of Medicine, Zhejiang University , Hangzhou 310058, China"}]},{"given":"Mingkun","family":"Lu","sequence":"additional","affiliation":[{"name":"College of Pharmaceutical Sciences, The Second Affiliated Hospital, Zhejiang University School of Medicine, Zhejiang University , Hangzhou 310058, China"}]},{"given":"Huaicheng","family":"Sun","sequence":"additional","affiliation":[{"name":"College of Pharmaceutical Sciences, The Second Affiliated Hospital, Zhejiang University School of Medicine, Zhejiang University , Hangzhou 310058, China"}]},{"given":"Fengcheng","family":"Li","sequence":"additional","affiliation":[{"name":"College of Pharmaceutical Sciences, The Second Affiliated Hospital, Zhejiang University School of Medicine, Zhejiang University , Hangzhou 310058, China"}]},{"given":"Yunxia","family":"Wang","sequence":"additional","affiliation":[{"name":"College of Pharmaceutical Sciences, The Second Affiliated Hospital, Zhejiang University School of Medicine, Zhejiang University , Hangzhou 310058, China"}]},{"given":"Zhenyu","family":"Zeng","sequence":"additional","affiliation":[{"name":"Innovation Institute for Artificial Intelligence in Medicine of Zhejiang University, Alibaba-Zhejiang University Joint Research Center of Future Digital Healthcare , Hangzhou 330110, China"}]},{"given":"Zhaorong","family":"Li","sequence":"additional","affiliation":[{"name":"Innovation Institute for Artificial Intelligence in Medicine of Zhejiang University, Alibaba-Zhejiang University Joint Research Center of Future Digital Healthcare , Hangzhou 330110, China"}]},{"given":"Bing","family":"Zhang","sequence":"additional","affiliation":[{"name":"Innovation Institute for Artificial Intelligence in Medicine of Zhejiang University, Alibaba-Zhejiang University Joint Research Center of Future Digital Healthcare , Hangzhou 330110, China"}]},{"given":"Yunqing","family":"Qiu","sequence":"additional","affiliation":[{"name":"State Key Laboratory for Diagnosis and Treatment of Infectious Disease, Collaborative Innovation Center for Diagnosis and Treatment of Infectious Diseases, Zhejiang Provincial Key Laboratory for Drug Clinical Research and Evaluation, The First Affiliated Hospital, Zhejiang University , 79 QingChun Road, Hangzhou, Zhejiang 310000, China"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-8069-0053","authenticated-orcid":false,"given":"Feng","family":"Zhu","sequence":"additional","affiliation":[{"name":"College of Pharmaceutical Sciences, The Second Affiliated Hospital, Zhejiang University School of Medicine, Zhejiang University , Hangzhou 310058, China"},{"name":"Innovation Institute for Artificial Intelligence in Medicine of Zhejiang University, Alibaba-Zhejiang University Joint Research Center of Future 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