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  1. Wikipedia
    https://en.wikipedia.org › wiki › Chiral_switch

    Chiral switch - Wikipedia

    • A chiral switch is a chiral drug that has already approved as racemate but has been re-developed as a single enantiomer. The term chiral switching was introduced by Agranat and Caner in 1999 to describe the development of single enantiomers from racemate drugs. For example, levofloxacin is a chiral switch of racemic ofloxacin. The essential principle of a chiral s… 展开

    The concept

    The chiral switch concept is illustrated in the diagram. This chiral switch is from (±)-ibuprofen to (S)-(+) … 展开

    Advantages

    There are several possible potential benefits to chiral switching or chiral specific drugs. These include:
    1. An improved (less complex, more selective) pharmacodynamic profile
    2. A higher … 展开

    Regulatory environment

    The roles of regulatory agencies also continue to evolve with respect to the development of chiral switches. An interesting concept brought up in the FDA policy is that of "bridging studies". When a sponsor/innovat… 展开

    Putting chirality to work: the strategy of chiral switches - Nature
    The strategy of enantiomeric pairs of patents of single enantiomers — E 1 and E 2 — in a chiral switch consists of two patents claiming simultaneously that E 1 and E 2 are pharmacologically ...
    Nature · https://www.nature.com/articles/nrd915
    CC-BY-SA 许可证中的维基百科文本
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    The concept
    Advantages
    Regulatory environment
     
  1. Nature
    https://www.nature.com › articles

    Putting chirality to work: the strategy of chiral switches

    2002年10月1日 · The strategy of enantiomeric pairs of patents of single enantiomers — E 1 and E 2 — in a chiral switch consists of two patents claiming simultaneously that E 1 and E 2 are pharmacologically ...

  2. Wikipedia
    https://en.wikipedia.org › wiki › Racemic_mixture

    Racemic mixture - Wikipedia

  3. Wikipedia
    https://en.wikipedia.org › wiki › Chirality

    Chirality - Wikipedia

    In chemistry, chirality usually refers to molecules. Two mirror images of a chiral molecule are called enantiomers or optical isomers. Pairs of enantiomers are often designated as "right-", "left-handed" or, if they have no bias, "achiral".

  4. 维基百科
    https://zh.wikipedia.org › wiki › 手性

    手性 - 维基百科，自由的百科全书

  5. MDPI
    https://www.mdpi.com

    Chiral Switch: Between Therapeutical Benefit and …

    2022年1月24日 · The term chiral switch refers to the replacement on the market of a previously approved racemate with its single enantiomer version. The potential advantages of chiral switch can be related to a higher therapeutic …

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    What is chiral switch?
    Chiral switch, a re-engineering approach, has enabled in the remarketing of a number of racemic drugs as chiral specific enantiomer products. Chiral switching strategy is the way most blockbuster drugs have entered the market as enantiopure drugs. A more appropriate term may be unichiral.

    Chiral switch - Wikipedia

    en.wikipedia.org
    What makes a chiral switch successful?
    Successful chiral switches emerge from racemic drugs that have efficacy and/or safety that can be enhanced, leading to significantly superior single enantiomers that are patentable and compete effectively with cheaper generic versions of the racemates.

    Putting chirality to work: the strategy of chiral switches

    nature.com
    Is chiral switch a 'line extension' of a racemic drug?
    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.

    Putting chirality to work: the strategy of chiral switches

    nature.com
    Are chiral switches worth it?
    However, the attractions of the chiral switch can be viewed as a double-edged sword: whereas advantages, such as reducing the dose compared with the racemate, are of value, the best that can be expected is a halving of the recommended dose, which itself might not be sufficient to justify the switch.

    Putting chirality to work: the strategy of chiral switches

    nature.com
    Which criterion is used in chiral switches?
    This shows the application of the criterion of 'non- OBVIOUSNESS ' (inventiveness) in chiral switches. These patents were preceded by US Patent 5,693,818 (dated 2 December 1997, issued to Astra AB), which claimed Na +, Mg 2+ and other salts of (+)- and (−)-omeprazole and processes for their preparation 69.

    Putting chirality to work: the strategy of chiral switches

    nature.com
    Why is chiral switch important in esomeprazole?
    When the chiral switch is developed by the proprietor of the racemate, it is advantageous for the single enantiomer to reach the market before the expirations of the patents of the racemate, and before the incursion of the respective generic drugs. This was the case with esomeprazole. In the present context, the pricing policy is important.

    Putting chirality to work: the strategy of chiral switches

    nature.com
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  7. Nature
    https://www.nature.com › articles

    Chiral switches bring new twist to photonics - Nature

  8. RSC Publishing
    https://pubs.rsc.org › en › content › articlelanding › cc

    A chiral switch: balancing between equilibrium and non …

  9. ACS Publications
    https://pubs.acs.org › doi

    The Quest for Secondary Pharmaceuticals: Drug …

    2023年1月17日 · The current Perspective introduces the drug repurposing/chiral-switches combination strategy, overviewing representative cases of chiral drugs that have undergone this combination: ketamine, flurbiprofen, fenfluramine, …

  10. The Lancet
    https://www.thelancet.com › journals › lancet › article › fulltext

    Chiral switches - The Lancet