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Updated: Feb 2, 2026

Solid-phase Submonomer Synthesis of Peptoid Polymers and their Self-Assembly into Highly-Ordered Nanosheets
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Phase I Study of AMG 337, a Highly Selective Small-molecule MET Inhibitor, in Patients with Advanced Solid Tumors

David S Hong1, Patricia LoRusso2, Omid Hamid3

  • 1Department of Investigational Cancer Therapeutics, The University of Texas MD Anderson Cancer Center, Houston, Texas. dshong@mdanderson.org.

Clinical Cancer Research : an Official Journal of the American Association for Cancer Research
|November 15, 2018
PubMed
Abstract

Insights

AMG 337, an oral MET inhibitor, demonstrated manageable toxicity in a phase I trial. The recommended dose for further studies is 300 mg once daily, showing promise in MET-amplified tumors.

Area of Science:

  • Oncology
  • Pharmacology
  • Clinical Trials

Background:

  • MET signaling pathway dysregulation is implicated in various advanced solid tumors.
  • Targeted therapies inhibiting MET are under investigation for cancer treatment.

Purpose of the Study:

  • To evaluate the safety, tolerability, pharmacokinetics, and preliminary efficacy of AMG 337, a novel oral MET inhibitor.
  • To determine the maximum tolerated dose (MTD) and recommended Phase II dose of AMG 337.

Main Methods:

  • A first-in-human, open-label, Phase I dose-escalation study of AMG 337 in patients with advanced solid tumors.
  • Modified 3+3+3 design for dose escalation, followed by dose expansion in MET-amplified patients.
  • Assessment of adverse events (AEs), MTD, pharmacokinetics, and clinical response.

Main Results:

  • 111 patients received AMG 337. The MTD was established at 300 mg once daily.
  • Most frequent treatment-related AEs included headache (63%) and nausea (31%).
  • Objective response rate was 9.9% overall and 29.6% in MET-amplified patients.

Conclusions:

  • AMG 337 is orally administered and generally well-tolerated with manageable toxicities.
  • The recommended Phase II dose is 300 mg once daily.
  • Promising response rates in heavily pretreated MET-amplified tumors warrant further investigation.

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