This review article is aimed at providing an overview of the current market of chiral drugs by exploring which is the nowadays tendency, for the pharmaceutical industry, either to exploit the chiral switching practice from already marketed racemates or to develop de novo enantiomerically pure compounds. A concise illustration of the main techniques developed to assess the absolute configuration (AC) and enantiomeric purity of chiral drugs has been given, where greater emphasis was placed on the contribution of enantioselective chromatography (HPLC, SFC and UHPC). Afterwards, we focused our study on the cohort of 45 new drugs that have been approved by the US Food and Drug Administration (FDA) in 2015. We extracted the chemical structure of the new drugs from the FDA approval chemistry reviews available on the database of the agency’s Center for Drug Evaluation and Research (CDER), and we selected a subgroup (i.e., 44% of the cohort) of small-molecule active pharmaceutical ingredients (APIs) containing one or more chirality centers.

The market of chiral drugs: chiral switches versus de novo enantiomerically pure compounds / Calcaterra, Andrea; D'Acquarica, Ilaria. - In: JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS. - ISSN 0731-7085. - ELETTRONICO. - 147:Special Issue(2018), pp. 323-340. [10.1016/j.jpba.2017.07.008]

The market of chiral drugs: chiral switches versus de novo enantiomerically pure compounds

Calcaterra, Andrea;D'acquarica, Ilaria
2018

Abstract

This review article is aimed at providing an overview of the current market of chiral drugs by exploring which is the nowadays tendency, for the pharmaceutical industry, either to exploit the chiral switching practice from already marketed racemates or to develop de novo enantiomerically pure compounds. A concise illustration of the main techniques developed to assess the absolute configuration (AC) and enantiomeric purity of chiral drugs has been given, where greater emphasis was placed on the contribution of enantioselective chromatography (HPLC, SFC and UHPC). Afterwards, we focused our study on the cohort of 45 new drugs that have been approved by the US Food and Drug Administration (FDA) in 2015. We extracted the chemical structure of the new drugs from the FDA approval chemistry reviews available on the database of the agency’s Center for Drug Evaluation and Research (CDER), and we selected a subgroup (i.e., 44% of the cohort) of small-molecule active pharmaceutical ingredients (APIs) containing one or more chirality centers.
chiral drugs; chiral switch; enantiomeric excess determination; enantioselective chromatography; racemates; single-enantiomer drugs; analytical chemistry; drug discovery; pharmaceutical science; spectroscopy; clinical biochemistry
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The market of chiral drugs: chiral switches versus de novo enantiomerically pure compounds / Calcaterra, Andrea; D'Acquarica, Ilaria. - In: JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS. - ISSN 0731-7085. - ELETTRONICO. - 147:Special Issue(2018), pp. 323-340. [10.1016/j.jpba.2017.07.008]
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11573/1021394
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