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The analysis of the market success of FDA approvals by probing top 100 bestselling drugs

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Abstract

Target-oriented drug discovery is the main research paradigm of contemporary drug discovery. In target-oriented approaches, we attempt to maximize in vitro drug potency by finding the optimal fit to the target. This can result in a higher molecular complexity, in particular, the higher molecular weight (MW) of the drugs. However, a comparison of the successful developments of pharmaceuticals with the general trends that can be observed in medicinal chemistry resulted in the conclusion that the so-called molecular obesity is an important reason for the attrition rate of drugs. When analyzing the list of top 100 drug bestsellers versus all of the FDA approvals, we discovered that on average lower-complexity (MW, ADMET score) drugs are winners of the top 100 list in terms of numbers but that, especially, up to some optimal MW value, a higher molecular complexity can pay off with higher incomes. This indicates that slim drugs are doing better but that fat drugs are bigger fishes to catch.

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Acknowledgments

Anonymous reviewers were kindly acknowledged for a valuable remarks allowing for a substantial improvement of the original text. JP kindly thank the financial support of NCBR Grants ORGANOMET No: PBS2/A5/40/2014 and TANGO1/266384/NCBR/2015.

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Authors and Affiliations

  1. Institute of Chemistry, University of Silesia, Szkolna 9, 40-006, Katowice, Poland

    Jaroslaw Polanski, Jacek Bogocz & Aleksandra Tkocz

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  1. Jaroslaw Polanski
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  2. Jacek Bogocz
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  3. Aleksandra Tkocz
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Correspondence to Jaroslaw Polanski.

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Polanski, J., Bogocz, J. & Tkocz, A. The analysis of the market success of FDA approvals by probing top 100 bestselling drugs. J Comput Aided Mol Des 30, 381–389 (2016). https://doi.org/10.1007/s10822-016-9912-5

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  • DOI: https://doi.org/10.1007/s10822-016-9912-5

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