Brief Title: Arginase Inhibitor INCB001158 as a Single Agent and in Combination With Immune Checkpoint Therapy in Patients With Advanced/Metastatic Solid Tumors

INTRODUCTION

• Org Study ID: INCB 01158-101
• Secondary ID: Mk3475 Keynote 741
• NTC ID: NCT02903914
• Sponsor: Incyte Corporation

BRIEF SUMMARY

This study is an open-label Phase 1/Phase 2 evaluation of INCB001158 as a single agent and in
combination with immune checkpoint therapy in patients with advanced/metastatic solid tumors.

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DETAILED DESCRIPTION

This study is an open-label Phase 1 evaluation of INCB001158 as a single agent and in
combination with immune checkpoint therapy in patients with advanced/metastatic solid tumors.

Single Agent INCB001158:

Patients with advanced/metastatic solid tumors will be enrolled into escalating monotherapy
dose cohorts to determine the Recommended Phase 2 Dose (RP2D) of INCB001158. Additional
patients with NSCLC, Colorectal Cancer (CRC), and other tumors including SCCHN, RCC, Gastric,
Bladder and Melanoma will be enrolled at the single agent RP2D.

Combination Treatment:

Patients with advanced/metastatic NSCLC, Melanoma, Urothelial, Microsatellite Instability
(MSI)/ Microsatellite Stable (MSS) CRC, Gastric, SCCHN and Mesothelioma will be enrolled into
separate cohorts of combination therapy (INCB001158 and Pembrolizumab) to determine the RP2D.

In the dose expansion phase, additional patients with NSCLC, Melanoma, Urothelial, MSI/MSS
CRC, Gastric, SCCHN and Mesothelioma will be treated with the combination of INCB001158 and
Pembrolizumab at the RP2D.

All patients will be assessed for safety, pharmacokinetics, biomarkers and tumor response.

• Overall Status
  Recruiting
• Start Date
  September 14, 2016
• Phase
  Phase 1/Phase 2
• Study Type
  Interventional