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CORE TECHNOLOGY

GI-101

A novel bispecific fusion protein for immuno-oncology

Immuno-oncology project

A novel bispecific
CD80-lgG4Fc-IL-2v
GI-101

Features

Features
A novel bispecific CD80-lgG4 Fc-IL-2v for immuno-oncology

Promotes the generation of cancer-specific effector T cell (Teff) in lymph nodes, and induces the activation and proliferation of tumor-infiltrating Teff and NK cells.

Controls the immuno-suppressive function of regulatory T cells (Tregs) in tumor microenvironment (TME)

Restores T cell function and anti-cancer immune responses in TME

Secures its safety in GLP toxicity study

DESCRIPTION

Mechanism
Core Mechanism GI-101
  • 01 Maintaining CD80 expression
    In lymph nodes, CD80 of antigen-presenting cells (APCs) binds to CTLA-4 of regulatory T cells (Treg), which in turn, downregulates the expression of CD80. By binding to CTLA-4 on Treg, GI-101 maintains CD80 expression on APC.
  • 02 T cell Activation
    APC presents cancer antigens to Naive T cells (Naïve T), which is accompanied by the binding of CD80 on APC and CD28 on Naïve T. This activates Naïve T into cancer-specific T cells that can target and kill cancer cells.
  • 03 T cell Proliferation
    The IL-2 variant (Interleukin-2 variant) of GI-101 acts as a signal transmitter which promotes the activation and proliferation of cancer-specific, effector T cell (Teff) by binding to its IL-2 receptors.
  • 04 Restoring T cell function
    Teff travels to the tumor microenvironment (TME) and faces a variety of immune suppressive signals. In TME, CD80 of GI-101 binds to CTLA-4 expressed on the surface of Teff and Treg,
    restoring anti-cancer immune responses.
  • 05 Tumor Cell Death
    The IL-2 variant of GI-101 binds to the IL-2 receptors of Teff and natural killer cells (NK cell). This activates Teff and NK cell, further promoting tumor cell death in TME.

data

data
GI-101 Data
01Proliferation and activation of immune cells

GI-101 induces in vitro proliferation of functional CD8+ T cells with robust cytotoxicity compared
to rhIL-2

02PD effects following repeated administration of GI-101 in monkeys
(PD effects)

GI-101 shows dose-dependent
increase of blood lymphocytes
(PD effects)
with a consistent magnitude following repeated administration

03Combination therapy with ICIs

GI-101 displays synergistic anti-cancer effects in combination with pembrolizumab (Keytruda®)
in humanized mice model

04GI-101 monotherapy

GI-101 promotes a significant increase of tumor-infiltrating lymphocyte (TIL)
in tumor tissues.