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Updated: Jun 9, 2025

Quantitative Structure-Activity Relationship, Activity Prediction, and Molecular Dynamics of Non-nucleotide Reverse Transcriptase Inhibitors
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An updated patent review of SOS1 inhibitors (2022-present)

Guizhen Zhou1,2, Chuan Zhou3, Xinyi Ma1,4

  • 1Drug Discovery and Design Center, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, China.

Expert Opinion on Therapeutic Patents
|October 22, 2024
PubMed
Abstract

Insights

New patents show SOS1 inhibitors targeting KRAS-driven tumors. While promising, these SOS1 inhibitors face challenges in clinical efficacy, safety, and pharmacokinetics, requiring further development.

Area of Science:

  • Oncology
  • Drug Discovery
  • Molecular Biology

Background:

  • SOS1 (Son of Sevenless homolog 1) is a guanine nucleotide exchange factor essential for KRAS activation.
  • KRAS activation drives tumor initiation and progression through downstream signaling pathways.
  • Inhibiting SOS1 is a therapeutic strategy for KRAS-driven cancers.

Purpose of the Study:

  • To review recent patents (2022-2024) for SOS1 inhibitors and SOS1-KRAS modulators.
  • To assess the development status and clinical challenges of these inhibitors.

Main Methods:

  • Literature review of patents using Cortellis Drug Discovery Intelligence.
  • Analysis of 15 patent applications from 5 applicants.
  • Evaluation of preclinical and clinical data for SOS1 inhibitors.

Main Results:

  • Numerous patents for SOS1 inhibitors have emerged since 2022.
  • Most SOS1 inhibitors are in preclinical development; few are in clinical trials.
  • Challenges include limited monotherapy efficacy, safety concerns, and suboptimal pharmacokinetic properties.

Conclusions:

  • SOS1 inhibitors modulate key cancer pathways (RAS/MAPK, PI3K/AKT/mTOR).
  • Despite in vitro success, clinical translation requires addressing safety, PK, and PD issues.
  • Further research is needed to optimize SOS1 inhibitors for therapeutic use.
Keywords:
KRASSOS1cancerdrug discoveryinhibitor

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