Drug intelligence / Profile preview

gefitinib + PD-1 inhibitor

Development stage
Unknown
Lead developer
AstraZeneca
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous
01

Overview

GT101 + PD-1 inhibitor is a combination therapy consisting of the small-molecule epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) **gefitinib** (referred to by the study code **GT101** in specific clinical protocols) and a **PD-1 inhibitor** (a class of monoclonal antibodies targeting the programmed cell death protein 1 receptor). This combination is primarily being investigated by **The First Affiliated Hospital of USTC** for the treatment of advanced non-small cell lung cancer (NSCLC), particularly in patients with EGFR mutations. Gefitinib works by binding to the adenosine triphosphate (ATP)-binding site of the EGFR tyrosine kinase domain, thereby inhibiting downstream signaling pathways that promote tumor cell proliferation and survival. The PD-1 inhibitor component (which may include specific agents such as sintilimab or tislelizumab depending on the trial) blocks the interaction between PD-1 on T cells and its ligands (PD-L1/PD-L2) on tumor cells, restoring the immune system's ability to recognize and eliminate cancer cells. The combination aims to overcome resistance to TKI monotherapy and enhance therapeutic efficacy through synergistic oncogenic pathway inhibition and immune activation.

Other names
gefitinib plus PD-1 inhibitor
02

Targets

PDCD1 (Programmed cell death protein 1 receptor)ERBB2 (Erb-b2 receptor tyrosine kinase 2)

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