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First-in-Human Phase I Study of Merestinib, an Oral Multikinase Inhibitor, in Patients with Advanced Cancer

Aiwu Ruth He1, Roger B Cohen2, Crystal S Denlinger3

  • 1Department of Medicine, Georgetown University Medical Center, Washington, DC, USA arh29@georgetown.edu.

The Oncologist
|March 6, 2019
PubMed
Abstract

Insights

Merestinib, an oral kinase inhibitor, showed a tolerable safety profile and anticancer activity in advanced cancer patients. Further clinical investigation is warranted for this potential new cancer therapy.

Area of Science:

  • Oncology
  • Pharmacology

Background:

  • Phase I clinical trial evaluating merestinib, an oral antiproliferative and antiangiogenic kinase inhibitor.
  • Investigated safety, tolerability, and determined a recommended Phase II dose and schedule for advanced cancer patients.

Purpose of the Study:

  • To assess the safety and tolerability of merestinib in patients with advanced cancer.
  • To establish a recommended Phase II dose and schedule for merestinib treatment.

Main Methods:

  • Multicenter, nonrandomized, open-label, Phase I study (NCT01285037) with dose escalation, confirmation, and expansion cohorts.
  • Combination safety testing with cetuximab, cisplatin, gemcitabine, and ramucirumab.
  • Evaluation of safety, tolerability, antitumor activity, and pharmacokinetics.

Main Results:

  • Recommended dose of merestinib: 120 mg once daily, based on acceptable safety and exposure.
  • Observed one complete response and three partial responses in cholangiocarcinoma patients.
  • 32% (60/186) of patients achieved stable disease as best response.

Conclusions:

  • Merestinib exhibits a tolerable safety profile and potential anticancer activity in advanced cancers.
  • Further clinical investigation is warranted for merestinib as a monotherapy or in combination therapies.
Keywords:
CholangiocarcinomaColorectal cancerHead and neck squamous cell cancerLY2801653Merestinib

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