Trends in the development of chiral drugs

Caner, Hava; Groner, Efrat; Levy, L; Agranat, Israel

doi:10.1016/s1359-6446(03)02904-0

Cited by 365 publications

(258 citation statements)

References 11 publications

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“…Ultimamente, temos assistido à avaliação de licenças para colocar no mercado fármacos enantiomericamente puros, administrados anteriormente como racematos (um processo chamado de chiral switching), assim como ao investimento em técnicas inovadoras de obtenção e controle de enantiômeros no desenvolvimento de novos fármacos. [38][39][40] Desde 2000, a preferência da indústria farmacêutica é para aprovar moléculas quirais na sua forma enantiomérica pura (Figura 3). 41 Em 2012, dos cinco medicamentos mais vendidos nos EUA, destacam-se quatro medicamentos de marca cujos fármacos são enantiômeros puros:…”

Section: Fármacos Quiraisunclassified

Chiral Pharmaceuticals in Diverse Environmental Matrices: Occurrence, Removal and Toxicity

Ribeiro¹,

Afonso²,

Castro³

et al. 2016

Química Nova

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Section: Fármacos Quiraisunclassified

Chiral Pharmaceuticals in Diverse Environmental Matrices: Occurrence, Removal and Toxicity

Ribeiro¹,

Afonso²,

Castro³

et al. 2016

Química Nova

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“…[1][2][3] In some cases, only one of the enantiomers of a chiral drug contributes to its pharmacodynamic behavior, while the other shows no or a much weaker effect as well as side-effects or even toxicity. [4] Besides the use of single enantiomers in the pharmaceutical industry, enantiomerically pure compounds are becoming significant in the production of other chemical products increasingly, such as agrochemicals, fragrances, and foods. [5] Currently, separation of racemic mixtures is typically performed by column chromatography [6], preferential crystallization [7] or kinetic resolution [8].…”

Section: Introductionmentioning

confidence: 99%

<b>pH- and Thermo-Induced Specific Permeability of Chiral Amino Acids through the Peptide Grafted Poly(<i>N</i>-isopropylamide)Network Membrane</b>

Nagata

Higuchi

2013

Sen-i Gakkaishi

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In this article we prepared an amphiphilic peptide, (L-Leu-L-Lys)8, grafted poly(N -isopropylacrylamide) network membrane. The graft content of the peptide and the content of the cross-linker were 4% and 16%, respectively. We investigated the permeability of L-and D-phenylalanine through this membrane. The pH-and thermo-induced permeability changes of the network membrane were observed. Under the neutral condition (pH 6.5 and 20°C), the peptide grafted PNIPAm network membrane showed a significant difference between the permeability of Lphenylalanine and D-phenylalanine. The maximum permselectivity (α=2.6) was achieved under this condition. At temperatures above the LCST of PNIPAm, PNIPAm polymers become hydrophobic ; hence, the membrane shrunk. And under these conditions the permeable path for L-and D-phenylalanine was formed in the membrane which results in the non-permselectivity through this membrane.

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“…It is not uncommon for one enantiomer to be active while other isomer is toxic in biological systems. The pharmaceutical industry has raised its emphasis on the generation of enantiomerically pure compounds before under taking phamarmacokinetic, metabolic, physiological, and toxicological evaluation in the search for drugs with grater therapeutic benefits and low toxicity [1,2]. Nowadays, chiral separations are playing more and more important role for the analysis of single enantiomers in the field of pharmaceutical industry [3].…”

Section: Introductionmentioning

confidence: 99%

Development and Validation of Chiral HPLC Method for Identification and Quantification of (R)-Enantiomer in Ezetimibe

Rao¹,

Venkatanarayana²,

Madhusudhan³

et al. 2012

AJAC

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A normal phase enantioselective high performance liquid chromatographic method was developed for enantiomeric resolution of Ezetimibe it reduces the overall delivery of cholesterol to the liver. The enantiomers of Ezetimibe were resolved on a Chiral Pak AS-H (250 × 4.6 mm, 5 µm) column using a mobile phase system containing n-hexane, ethanol, 2-propanol and trifloroacetic acid (84:12:4:0.1 v/v). The resolution between enantiomers was found to be more than 2.0. The limit of detection and limit of quantification of (R)-enantiomer were found to be 0.2 µg/mL and 0.5 µg/mL, respectively, for 10 µL injection volume. The sample solution and mobile phase were found to be stable for at least 48 h. The final optimized method was successfully applied to separate (R)-enantiomer from Ezetimibe and was proven to be reproducible and accurate for the quantitative determination of (R)-enantiomer in bulk drugs.

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Trends in the development of chiral drugs

Cited by 365 publications

References 11 publications

Chiral Pharmaceuticals in Diverse Environmental Matrices: Occurrence, Removal and Toxicity

Chiral Pharmaceuticals in Diverse Environmental Matrices: Occurrence, Removal and Toxicity

<b>pH- and Thermo-Induced Specific Permeability of Chiral Amino Acids through the Peptide Grafted Poly(<i>N</i>-isopropylamide)Network Membrane</b>

Development and Validation of Chiral HPLC Method for Identification and Quantification of (R)-Enantiomer in Ezetimibe

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