“Atropisomeric” Drugs: Basic Concept and Example of Application to Drug Development - Pharmacology & Pharmacy

PP > Vol.11 No.1, January 2020

Pharmacology & Pharmacy

Volume 11, Issue 1 (January 2020)

ISSN Print: 2157-9423 ISSN Online: 2157-9431

Google-based Impact Factor: 0.70 Citations h5-index & Ranking

“Atropisomeric” Drugs: Basic Concept and Example of Application to Drug Development ()

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DOI: 10.4236/pp.2020.111001 1,234 Downloads 2,873 Views Citations

Author(s)

Robert B. Raffa^1,2,3*, Joseph V. Pergolizzi Jr.^1,4, Robert Taylor Jr.⁴

Affiliation(s)

¹Neumentum Inc., Palo Alto, CA, USA.
²College of Pharmacy, University of Arizona, Tucson, AZ, USA.
³School of Pharmacy, Temple University, Philadelphia, PA, USA.
⁴NEMA Research Inc., Naples, FL, USA.

ABSTRACT

Many therapeutic drugs are racemates; i.e. they are chiral molecules consisting of “left”- and “right-handed” enantiomers (stereoisomers that are mirror images of each other, and are non-superimposable). In some cases, both enantiomers of the drug contribute to some extent (or equally) to the therapeutic effect; in other cases they contribute not at all. The same is true for the adverse effects of racemate drugs: the adverse effects of a racemate drug can be greater-than, less-than, or equal to one or the other enantiomer. An unusual situation arises when a drug consists of “atropisomers”, stereoisomers arising because of hindered rotation about a single chemical bond. We summarize the concept of atropisomerism, and give examples.

KEYWORDS

Atropisomer, Chirality, Pharmacotherapy, Drug Development, NaV1.7 Inhibitor

Share and Cite:

Raffa, R. , Pergolizzi Jr., J. and Taylor Jr., R. (2020) “Atropisomeric” Drugs: Basic Concept and Example of Application to Drug Development. Pharmacology & Pharmacy, 11, 1-8. doi: 10.4236/pp.2020.111001.

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