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The predicated demise of racemic new molecular entities is an exaggeration

Nature Reviews Drug Discovery volume 11, pages 972–973 (2012)Cite this article

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Since 2003, Nature Reviews Drug Discovery has consistently published reports of annual new drug approvals by the US Food and Drug Administration (FDA) (2011 FDA drug approvals. Nature Rev. Drug Discov. 11, 91–94 (2012))1. These informative summaries provide an opportunity for us to introduce drug chirality in the analysis of the trends in the development of new drugs.

The chirality of drugs has become a major theme in the design, discovery, development, patenting and marketing of new drugs2,3. For many years the pharmacopoeias were dominated by racemates. However, this trend was inverted owing to the emergence of new technologies in the 1980s that allowed the preparation of single enantiomers in substantial quantities; it was also inverted as a result of E. J. Arien's effective rediscovery and outspoken advocacy of the significance of stereochemistry in therapeutic action and his preference for single-enantiomer drugs over racemic drugs4. It has been accepted since the early 1980s that most of the biological activity observed for a racemate often resides within a single enantiomer.

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Figure 1: The chirality of NMEs.

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Author notes

  1. Silvya R. Wainschtein

    Present address: Silvya R. Wainschtein was previously at the Institute of Chemistry, The Hebrew University of Jerusalem, Philadelphia Bldg 201/205, Edmond J. Safra Campus, Jerusalem 91904, Israel. Present address: School of Chemistry, Tel Aviv University, Tel Aviv 69978, Israel.,

Authors and Affiliations

  1. Israel Agranat is at the Institute of Chemistry, The Hebrew University of Jerusalem, Philadelphia Bldg 201/205, Edmond J. Safra Campus, Jerusalem 91904, Israel.,

    Israel Agranat

  2. Enav Z. Zusman is at the Department of Life and Medical Sciences, Tel Aviv University, Tel Aviv 69978, Israel.,

    Enav Z. Zusman

Authors
  1. Israel Agranat
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  2. Silvya R. Wainschtein
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Correspondence to Israel Agranat.

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Agranat, I., Wainschtein, S. & Zusman, E. The predicated demise of racemic new molecular entities is an exaggeration. Nat Rev Drug Discov 11, 972–973 (2012). https://doi.org/10.1038/nrd3657-c1

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