U.S. FDA Approved Drugs from 2015-June 2020: A Perspective.

Priyadeep Bhutani, Gaurav Joshi, Nivethitha Raja, Namrata Bachhav, Prabhakar K Rajanna, Hemant Bhutani, Atish T Paul, Raj Kumar

Journal: Journal of medicinal chemistry 2021;64(5):2339-2381

PMID: 33617716

Abstract

In the present work, we report compilation and analysis of 245 drugs, including small and macromolecules approved by the U.S. FDA from 2015 until June 2020. Nearly 29% of the drugs were approved for the treatment of various types of cancers. Other major therapeutic areas of focus were infectious diseases (14%); neurological conditions (12%); and genetic, metabolic, and cardiovascular disorders (7-8% each). Itemization of the approved drugs according to the year of approval, sponsor, target, chemical class, major drug-metabolizing enzyme(s), route of administration/elimination, and drug-drug interaction liability (perpetrator or/and victim) is presented and discussed. An effort has been made to analyze the pharmacophores to identify the structural (e.g., aromatic, heterocycle, and aliphatic), elemental (e.g., boron, sulfur, fluorine, phosphorus, and deuterium), and functional group (e.g., nitro drugs) diversity among the approved drugs. Further, descriptor-based chemical space analysis of FDA approved drugs and several strategies utilized for optimizing metabolism leading to their discoveries have been emphasized. Finally, an analysis of drug-likeness for the approved drugs is presented.

Address: Pharmaceutical Candidate Optimization, Biocon Bristol-Myers Squibb R&D Centre, Syngene International Limited, Bangalore 560099, India.; Department of Pharmacy, Birla Institute of Technology and Science (BITS) Pilani, Pilani Campus, Rajasthan 333031, India.; Laboratory for Drug Design and Synthesis, Department of Pharmaceutical Sciences and Natural Products, Central University of Punjab, Bathinda 151001, India.; 1015 E Cozza Drive # 12, Spokane Washington 99208, United States.; Pharmaceutical Development, Biocon Bristol-Myers Squibb R&D Centre, Bristol-Myers Squibb India Private Limited, Bangalore 560099, India.

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