A survey of solid form landscape: Trends in occurrence and distribution of various solid forms and challenges in solid form selection.

Item request has been placed! ×
Item request cannot be made. ×
loading   Processing Request
  • Additional Information
    • Source:
      Publisher: Elsevier Country of Publication: United States NLM ID: 2985195R Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1520-6017 (Electronic) Linking ISSN: 00223549 NLM ISO Abbreviation: J Pharm Sci Subsets: MEDLINE
    • Publication Information:
      Publication: 2016- : New York, NY : Elsevier
      Original Publication: Easton, Pa., American Pharmaceutical Assn.
    • Subject Terms:
    • Abstract:
      This survey provides a comprehensive analysis of solid form screens for 476 new chemical entities (NCEs) conducted at Pharmaron from 2016 to 2023. The findings from this survey reveal notable trends in polymorphism, salt formation, crystallization behavior and molecular weight (MW) distribution of the NCEs evaluated. Most solid form screens were conducted to select the preferred solid form for Investigational New Drug (IND) enabling projects, others were for candidate selection or late-stage development. Comparison to published historical data was made to show changes in occurrence of counterions/co-formers for salts/co-crystals, polymorphs, and the distribution of MWs over time. Increased complexity in the solid-form landscape and selection of the development form are discussed, including challenges in crystallization and selection of lead forms. The distribution of types of crystal forms and the observation of emerging and disappearing polymorphs are presented. These results highlight the evolving challenges and considerations in solid form screening and form selection and offer insights for future pharmaceutical development and crystallization strategies.
      Competing Interests: Declaration of competing interest Pharmaron is a Contract Resource Organization and performs work at the request of the international biotech and pharmaceutical companies (sponsors) under a fee-for-service work contract. All authors are employed by Pharmaron, Inc. All rights and privileges are assigned to the companies who contract the work. The dataset is a collection of solid form data from the projects’ reports; no chemical structure or specific project information are disclosed. The authors declare that they have no known competing financial interests or personal relationships that could appear to influence the work reported in this paper.
      (Copyright © 2024 American Pharmacists Association. Published by Elsevier Inc. All rights reserved.)
    • Contributed Indexing:
      Keywords: Chemical space; Co-crystal; Hydrate; IND; Multicomponent crystal; NCE; Polymorph screen; Salt screen; Solid form selection; Solvate
    • Accession Number:
      0 (Pharmaceutical Preparations)
      0 (Salts)
      0 (Drugs, Investigational)
    • Publication Date:
      Date Created: 20241104 Date Completed: 20241222 Latest Revision: 20241222
    • Publication Date:
      20241223
    • Accession Number:
      10.1016/j.xphs.2024.10.045
    • Accession Number:
      39491672