Chiral drugs: The FDA perspective on manufacturing and control

Molecular thermodynamics of solid‐fluid and solid‐solid equilibria

“…FDA guidelines emphasize ''chiral control'' in drug formulations, involving issues, such as the enantiomeric composition of the drugs, the pharmacological activity of the individual enantiomers, and the rate of interconversion of the enantiomers under different conditions. 25 A key aspect from an intellectual property perspective is that an API that was originally patented and marketed as a racemic mixture can be subsequently patented and marketed as a single enantiomer. AstraZeneca's proton pump inhibitor drugs Prilosec and Nexium provide a good example.…”

Enantiospecific analysis: Applications in bioanalysis and metabolism

“…Two chromatographic approaches are available for the resolution of enantiomers: (1) the indirect approach involving the formation of stable or covalent diastereoisomeric derivatives by reaction of the enantiomeric analyte(s) with a homochiral (optically pure) or chiral derivatising agent (CDA); and (2) the direct approach involving the formation of unstable, or transient diasteroisomers, by interaction of the analyte(s) with a chiral solvent or surface. Both of these approaches have a number of advantages and limitations which will be addressed below.…”

“…However, irrespective of the decision to develop either a single isomer or racemic drug, in the current regulatory climate there will be a continuing requirement for enantiospecific analysis and thus modem drug development presents a considerable Please send reprint request to: Dr AI. Hutt challenge for the pharmaceutical analyst and separation scientist (1,2).…”

Preparative separation and identification of derivatized β-methylphenylalanine enantiomers by chiral SFC, HPLC and NMR for development of new peptide ligand mimetics in drug discovery

“…However, amino acids are also chiral molecules. Consequently, with the increasing demands for production of enantiomerically pure compounds in the fields of pharmaceuticals, peptide research, etc., these chiral separations have become an important analytical task [7].…”