Literature DB >> 24066264

Chiral Switch Drugs for Asthma and Allergies: True Benefit or Marketing Hype.

Kathryn Blake1, Hengameh Raissy.   

Abstract

Enantiomers are one of several possible molecular configurations present in a drug that has at least 1 chiral center. A drug containing 2 or more enatiomers is called a racemic mixture. Enatiomers are being developed from racemic mixtures as drugs in their own right often to extend patent protection of highly popular drugs. However, the therapeutic advantages of single enantiomer drugs developed for respiratory use such as levalbuterol, arformoterol, and levocetirizine over their racemate has been disappointing. In addition, single enantiomer drugs may be several fold more expensive than the racemic drug. New single enantiomer drugs, which are stable (no interconversion back to the racemate) and have fewer adverse effects and a more predictable pharmacodynamic or pharmacokinetic profile would confer a therapeutic advantage and thus would be beneficial for clinical use.

Entities:  

Year:  2013        PMID: 24066264      PMCID: PMC3777548          DOI: 10.1089/ped.2013.0285

Source DB:  PubMed          Journal:  Pediatr Allergy Immunol Pulmonol        ISSN: 2151-321X            Impact factor:   1.349


  34 in total

1.  Efficacy of racemic albuterol versus levalbuterol used as a continuous nebulization for the treatment of acute asthma exacerbations: a randomized, double-blind, clinical trial.

Authors:  Matthew Wilkinson; Blake Bulloch; Pam Garcia-Filion; Laine Keahey
Journal:  J Asthma       Date:  2011-01-29       Impact factor: 2.515

Review 2.  Single-enantiomer drugs: elegant science, disappointing effects.

Authors:  Peter Mansfield; David Henry; Anne Tonkin
Journal:  Clin Pharmacokinet       Date:  2004       Impact factor: 6.447

3.  Absorption, distribution, metabolism and excretion of [14C]levocetirizine, the R enantiomer of cetirizine, in healthy volunteers.

Authors:  M S Benedetti; M Plisnier; J Kaise; L Maier; E Baltes; C Arendt; N McCracken
Journal:  Eur J Clin Pharmacol       Date:  2001-10       Impact factor: 2.953

4.  The predicated demise of racemic new molecular entities is an exaggeration.

Authors:  Israel Agranat; Silvya R Wainschtein; Enav Z Zusman
Journal:  Nat Rev Drug Discov       Date:  2012-12       Impact factor: 84.694

5.  A cumulative dose, safety and tolerability study of arformoterol in pediatric subjects with stable asthma.

Authors:  J Hinkle; J Hinson; E Kerwin; E Goodwin; K Sciarappa; L Curry; J P Hanrahan
Journal:  Pediatr Pulmonol       Date:  2011-05-16

6.  The acute and sub-chronic effects of levocetirizine, cetirizine, loratadine, promethazine and placebo on cognitive function, psychomotor performance, and weal and flare.

Authors:  I Hindmarch; S Johnson; R Meadows; T Kirkpatrick; Z Shamsi
Journal:  Curr Med Res Opin       Date:  2001       Impact factor: 2.580

7.  The effect of the enantiomers of formoterol on inherent and induced tone in guinea-pig trachea and human bronchus.

Authors:  D Schmidt; B L Källström; B Waldeck; D Branscheid; H Magnussen; K F Rabe
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  2000-04       Impact factor: 3.000

8.  The effect of formoterol over 24 h in patients with asthma: the role of enantiomers.

Authors:  Jan Lötvall; Mona Palmqvist; Jaro Ankerst; Gunnar Persson; Johan Rosenborg; Thomas Bengtsson; Zsuzsanna Rott; Magdolna Poczi; Agnes Devai; Bertil Waldeck
Journal:  Pulm Pharmacol Ther       Date:  2004-12-22       Impact factor: 3.410

9.  The comparison of cetirizine, levocetirizine and placebo for the treatment of childhood perennial allergic rhinitis.

Authors:  Chih-Fang Lee; Hai-Lun Sun; Ko-Hsiu Lu; Min-Sho Ku; Ko-Huang Lue
Journal:  Pediatr Allergy Immunol       Date:  2008-10-06       Impact factor: 6.377

10.  Comparative efficacy of cetirizine and levocetirizine in chronic idiopathic urticaria.

Authors:  Geeta Garg; Gurvinder P Thami
Journal:  J Dermatolog Treat       Date:  2007       Impact factor: 3.359

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  2 in total

Review 1.  Long-Acting β2-Agonists in Asthma: Enantioselective Safety Studies are Needed.

Authors:  Glenn A Jacobson; Sharanne Raidal; Morten Hostrup; Luigino Calzetta; Richard Wood-Baker; Mark O Farber; Clive P Page; E Haydn Walters
Journal:  Drug Saf       Date:  2018-05       Impact factor: 5.606

Review 2.  Chiral Switch: Between Therapeutical Benefit and Marketing Strategy.

Authors:  Gabriel Hancu; Adriana Modroiu
Journal:  Pharmaceuticals (Basel)       Date:  2022-02-17
  2 in total

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