Drug intelligence / Profile preview

BT7455

Development stage
Preclinical
Lead developer
Bicycle Therapeutics
Modality
Cyclic Peptides → Modified Peptides → Peptides, Small Molecules
01

Overview

BT7455 is a fully synthetic, tumor-targeted immune cell agonist (TICA) developed by Bicycle Therapeutics. It is designed as a bicyclic peptide-based molecule with two functional arms: one targets Ephrin type-A receptor 2 (EphA2), which is overexpressed in several human cancers and associated with poor prognosis, and the other targets CD137 (also known as 4-1BB), a member of the TNF receptor superfamily involved in activating T cells and NK cells. By engaging both EphA2 on tumor cells and CD137 on immune effector cells, BT7455 delivers highly potent, localized CD137 agonism to tumors expressing EphA2. This dual targeting leads to robust anti-tumor activity through stimulation of cytotoxic T lymphocytes and modulation of the tumor immune microenvironment. Preclinical studies have demonstrated picomolar potency in co-culture assays, induction of cytokines such as IL-2 and IFNγ, strong anti-tumor efficacy including complete responses in mouse models, favorable pharmacokinetics, and good tolerability without significant cytokine or liver enzyme elevation[1][2][3][4][5].

02

Targets

EPHA2 (Ephrin type-A receptor 2)TNFRSF9 (CD137 extracellular domain)

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