Putting chirality to work: the strategy of chiral switches
Abstract
Most of the new drugs reaching the market today are single enantiomers, rather than the racemic mixtures that dominated up to ten years ago. Many of the new single-enantiomer drugs were developed as such, but there are also important examples of new single-enantiomer drugs derived from 'chiral switches' of established racemates. Indeed, a well-timed chiral switch can offer enhanced therapy and further profitability as a 'line extension' of a major racemic drug with patents that are expiring.
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The stereoselective engagement of protein targets is a feature of numerous chemical probes and drugs.
“The stereoselective engagement of protein targets is a feature of numerous chemical probes and drugs15–19”
From Expedited mapping of the ligandable proteome using fully functionalized enantiomeric probe pairs (2019) · cites this paper as [15]
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- Authors
- Agranat, I., Caner, H., & Caldwell, J.
- Affiliations
- Hebrew University of Jerusalem (IL)
- Imperial College London (GB)
- Corresponding author
- Agranat, Israel
- Venue
- Nature Reviews Drug Discovery
- Published
- 2002-10
- Volume
- 1
- Issue
- 10
- Pages
- 753-768
- ISSN
- 1474-1776 (ISSN-L)
- 1474-1784
- OpenAlex
- W1991998089
- Cited by
- 637
- References
- 100
- Citations by year
- 2026: 32 · 2025: 31 · 2024: 43 · 2023: 29 · 2022: 31 · 2021: 36 · 2020: 33 · 2019: 32 · 2018: 32 · 2017: 31 · 2016: 15 · 2015: 31 · 2014: 25 · 2013: 22 · 2012: 32
- FWCI
- 1.67
- Type
- journal article
- Language
- en
- Open access
- closed
- Licence
- www.springer.com/tdm (tdm)
- Locations
- Nature Reviews Drug Discovery (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Physical Sciences › Chemistry › Spectroscopy › Analytical Chemistry and Chromatography
- Physical Sciences › Chemistry › Organic Chemistry › Chemistry and Stereochemistry Studies
- Physical Sciences › Chemistry › Organic Chemistry › Asymmetric Synthesis and Catalysis
- Keywords
- chiral switch, racemic drugs, enantiomers, drug development strategy, line extension, patent expiry, pharmaceutical patents
- MeSH terms
- Animals, Chemistry, Pharmaceutical, Humans, Stereoisomerism, Technology, Pharmaceutical
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