Discovery and Characterization of a Late-Appearing Polymorph of Famciclovir

High Resolution Image Download MS PowerPoint Slide Famciclovir (FCV), an antiviral drug widely used to treat herpes zoster (HZ), has previously been reported to exhibit four polymorphs and one hydrate, with crystal structures solved only for Form I and the hydrated form. In this work, a detailed investigation of Form I and a new polymorphic form (Form V) of famciclovir was carried out. Crystallization experiments were performed using different solvents, and the reproducible conditions for obtaining polymorph V are presented. Its structure was determined by single-crystal X-ray diffraction (SXRD) for the first time. The infrared spectra of both polymorphs were compared and interpreted with the assistance of a simulated spectrum. The thermal behavior of both polymorphs was investigated by differential scanning calorimetry (DSC), and the solubilities of each form in ethanol were obtained both by the gravimetric method and the polythermal method. The results reveal an enantiotropic relationship between Forms I and V, with Form V being more stable at room temperature. This study highlights the complexity of polymorphism and its implications for pharmaceutical development.

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Publication Details

Journal
Crystal Growth & Design
Published
2026-07-16
DOI
https://doi.org/10.1021/acs.cgd.6c00333
Primary Topic
Herpesvirus Infections and Treatments
Type
article
Field-Weighted Citation Impact
0.00

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article

Discovery and Characterization of a Late-Appearing Polymorph of Famciclovir

João A. Baptista, Ricardo A. E. Castro, Luciano Cassio Ramos Rais, M. Fátima M. Piedade et al.
Crystal Growth & Design
Herpesvirus Infections and Treatments
article

Discovery and Characterization of a Late-Appearing Polymorph of Famciclovir

João A. Baptista, Ricardo A. E. Castro, Luciano Cassio Ramos Rais, M. Fátima M. Piedade, Éder T. G. Cavaleiro
article en

Abstract

High Resolution Image Download MS PowerPoint Slide Famciclovir (FCV), an antiviral drug widely used to treat herpes zoster (HZ), has previously been reported to exhibit four polymorphs and one hydrate, with crystal structures solved only for Form I and the hydrated form. In this work, a detailed investigation of Form I and a new polymorphic form (Form V) of famciclovir was carried out. Crystallization experiments were performed using different solvents, and the reproducible conditions for obtaining polymorph V are presented. Its structure was determined by single-crystal X-ray diffraction (SXRD) for the first time. The infrared spectra of both polymorphs were compared and interpreted with the assistance of a simulated spectrum. The thermal behavior of both polymorphs was investigated by differential scanning calorimetry (DSC), and the solubilities of each form in ethanol were obtained both by the gravimetric method and the polythermal method. The results reveal an enantiotropic relationship between Forms I and V, with Form V being more stable at room temperature. This study highlights the complexity of polymorphism and its implications for pharmaceutical development.

Crystal Growth & Design
University of Lisbon (PT), Universidade de São Paulo (BR), Institut des Sciences Moléculaires (FR), Rede de Química e Tecnologia (PT), Instituto de Psicologia Comportamental de São Carlos (BR), Instituto de Química de São Carlos (BR), University of Coimbra (PT)
Coordenação de Aperfeiçoamento de Pessoal de Nível Superior, Fundação para a Ciência e a Tecnologia
Openalex Percentile: Top 8%
Herpesvirus Infections and Treatments
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