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Recent advances in the discovery of PKMYT1-targeting drugs: a patent review (2021-2025)

Yazhou Wang1, Chao Wang1, Feng Ren1,2

  • 1Department of Medicinal Chemistry, Insilico Medicine Shanghai Ltd, Shanghai, China.

Expert Opinion on Therapeutic Patents
|May 21, 2026
PubMed
Abstract

Insights

Protein kinase Myt1 (PKMYT1) inhibitors are rapidly advancing as a novel cancer therapy. Recent clinical trials and patent filings show significant growth, highlighting their potential for treating specific cancer types.

Area of Science:

  • Oncology
  • Molecular Biology
  • Drug Discovery

Background:

  • Protein kinase Myt1 (PKMYT1) regulates mitotic entry by phosphorylating CDK1.
  • PKMYT1 is a promising synthetic lethal target in oncology.
  • The field of PKMYT1 inhibitors has seen rapid growth since 2021.

Purpose of the Study:

  • To review clinical trial reports and patent literature on PKMYT1 inhibitors from 2021 to December 2025.
  • To provide an update on the development of PKMYT1 inhibitors and degraders.
  • To inform strategies for overcoming current limitations in PKMYT1-targeted therapy.

Main Methods:

  • Literature review of clinical trial reports.
  • Patent landscape analysis.
  • Data retrieval from WIPO, EPO, and Cortellis database.

Main Results:

  • Explosive growth in patents for PKMYT1 inhibitors and degraders.
  • Advancement of five PKMYT1 inhibitor candidates into clinical development.
  • Established clinical proof-of-concept for PKMYT1-targeted synthetic lethality.

Conclusions:

  • PKMYT1 inhibitors and degraders show significant potential as a synthetic-lethal strategy for cancers with CCNE1 amplification or FBXW7 alterations.
  • Clinical outcomes from trials like RP-6306 support this therapeutic approach.
  • Further research informed by this review is expected to refine strategies and address limitations.
Keywords:
AI-generationPKMYT1 inhibitorPROTACanticancer drugkinase selectivitysynthetic lethality

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