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A therapeutic patent overview of MDM2/X-targeted therapies (2014-2018)

Lukasz Skalniak1, Ewa Surmiak1, Tad A Holak1

  • 1a Department of Organic Chemistry, Faculty of Chemistry , Jagiellonian University , Krakow , Poland.

Expert Opinion on Therapeutic Patents
|March 2, 2019
PubMed
Abstract

Insights

MDM2/X antagonists reactivate the p53 tumor suppressor to inhibit cancer growth. Recent patents (2014-2018) show advancements in these drugs, including combination therapies and novel PROTAC technologies.

Area of Science:

  • Oncology
  • Molecular Biology
  • Drug Discovery

Background:

  • MDM2 and MDMX proteins inhibit the p53 tumor suppressor, promoting cancer evolution.
  • Blocking MDM2/X-p53 interaction reactivates p53, inhibiting cancer growth in p53 wild-type cells.
  • Numerous chemical entities have been developed to antagonize MDM2/X and reactivate p53 over the past two decades.

Purpose of the Study:

  • To review therapeutic patents for MDM2/X antagonists from 2014-2018.
  • To present patents involving drug combinations with MDM2/X antagonists.
  • To highlight trends and advancements in the field of MDM2/X antagonists for cancer treatment.

Main Methods:

  • Review of therapeutic patents published between 2014 and 2018.
  • Analysis of patents focusing on MDM2/X antagonists and their use in cancer therapy.
  • Identification of patents related to combination treatments and novel technologies like PROTAC.

Main Results:

  • Several known chemical scaffolds for MDM2/X antagonists were further developed.
  • Numerous lead compounds entered clinical trials for cancer patients during this period.
  • Limitations of MDM2 antagonists spurred research into combination strategies and dual-targeting approaches (e.g., PROTAC).

Conclusions:

  • The period 2014-2018 saw significant progress in the development of MDM2/X antagonists.
  • Combination therapies and novel targeting strategies like PROTAC are emerging trends to overcome limitations.
  • Continued research into MDM2/X antagonists holds promise for improved cancer treatment outcomes.
Keywords:
MDM2 antagonistMDMX antagonistPROTACcancerclinical studiesp53protein-protein interactionsmall-molecule inhibitors

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