Enantiomers in pharmaceuticals often have different biological activities
Multiple recent pharmaceutical and pharmacological studies confirm that enantiomers frequently exhibit differences in pharmacokinetics, metabolism, and biological or pharmacological activity.
The retrieved literature consistently supports the claim that pharmaceutical enantiomers often have different biological and pharmacological activities, pointing to stereoselective pharmacokinetics, metabolism, and receptor interactions across various drug classes.
Chen L, Yan T, Huang D, Xu W, Liu Y, Wang X, Li H. Stereoselectivity of In Vivo Processes and Bioactivity of Farrerol Enantiomers.. 2025. https://doi.org/10.3390/molecules30092038
Demonstrates that farrerol enantiomers exhibit stereoselective pharmacokinetics and differences in enzyme inhibition and binding affinity.
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Bialer M, Perucca E. From barbiturates to ganaxolone: The importance of chirality in drug development and in understanding the actions of old and new antiseizure medications.. 2025. https://doi.org/10.1016/j.pharmthera.2025.108808
Reviews antiseizure medications and highlights established stereochemical differences in pharmacokinetics and pharmacodynamics between enantiomers.
Seyfinejad B, Jouyban K, Houshyar J, Jabbaripour Sarmadian A, Jouyban A. Enantioselective analysis of metoprolol in plasma of hypertensive patients undergoing long-term therapy: Insights for personalized medicine.. 2025. https://doi.org/10.34172/bi.32645
Observes stereoselective pharmacokinetics and chiral plasma ratio variations in long-term metoprolol therapy.
Bazeli B, Shkumatov AV, Schenck S, Vanherck JC, Janssens A, Spieser SAH, Marchand D, Roelens R, Chaltin P, Marchand A, Vriens J, Voets T, Brunner JD. Stereoselectivity and functional plasticity of a common ligand-binding pocket in TRPM3.. 2026. https://doi.org/10.1038/s41467-026-71226-0
Shows that TRPM3 channels exhibit distinct stereoselectivity for specific enantiomeric agonists and antagonists.
Várnagy E, Tóth G, Hosztafi S, Malanga M, Fejős I, Béni S. Enantioselective Complexation of Xylopinine: A Cyclodextrin-Assisted CE and NMR Study.. 2025. https://doi.org/10.3390/ijms26199405
Notes that tetrahydroprotoberberine alkaloid enantiomers frequently display enantiomer-specific pharmacological effects.
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