An updated patent review of AKT inhibitors (2020 - present)

Expert Opin Ther Pat. 2023 Jul-Dec;33(9):549-564. doi: 10.1080/13543776.2023.2273895. Epub 2023 Nov 28.

Abstract

Introduction: Protein kinase B (Akt), an essential protein in the PI3K/Akt/mTOR signaling pathway, plays a crucial role in tumor progression. Over the past two years, different types of Akt modulators have continued to emerge in the patent literature.

Areas covered: This review focuses on the patent literature covering small molecule inhibitors, peptides, PROTACs, and antisense nucleic acids targetingAkt from 2020 to present. Also, we discuss the outcomes of several clinical trials, combination strategies for different mechanisms, and the application of Akt regulators in other non-oncology indications.Our search for relevant information was conducted using various databases, including the European Patent Office, SciFinder, andPubMed, from 01.2020 to 04.2023.

Expert opinion: In recent years, some combination therapeutic strategies involvingAkt inhibitors have shown promising clinical outcomes. Future research can be directed toward developing new applications of Akt inhibitors, which may have implications for other diseases beyond cancer. New attempts suggest that targeting allosteric sites may be a potential solution to the problem of isoform selectivity.Furthermore, directly knocking out Akt protein by using the degraderssuggests a promising direction for future development.

Keywords: Akt; PROTAC; cancer; clinical trial; combination; inhibitor.

Publication types

  • Review

MeSH terms

  • Angiogenesis Inhibitors
  • Antineoplastic Agents* / pharmacology
  • Antineoplastic Agents* / therapeutic use
  • Humans
  • Neoplasms* / drug therapy
  • Patents as Topic
  • Phosphatidylinositol 3-Kinases / metabolism
  • Protein Kinase Inhibitors / pharmacology
  • Protein Kinase Inhibitors / therapeutic use
  • Proto-Oncogene Proteins c-akt / metabolism

Substances

  • Proto-Oncogene Proteins c-akt
  • Antineoplastic Agents
  • Phosphatidylinositol 3-Kinases
  • Protein Kinase Inhibitors
  • Angiogenesis Inhibitors