Drug intelligence / Profile preview

BCY6033

Development stage
Preclinical
Lead developer
Bicycle Therapeutics
Modality
Cyclic Peptides → Modified Peptides → Peptides, Peptide-Drug Conjugates → Peptide Conjugates → Peptides
Administration
Intravenous
01

Overview

BCY6033 is an **EphA2-targeted Bicycle Toxin Conjugate** developed by Bicycle Therapeutics for cancer. It is a **peptide-drug conjugate** built from a tumor-targeting bicyclic peptide that binds **erythropoietin-producing hepatocellular receptor A2** and is linked through a cleavable spacer-linker to the microtubule toxin **monomethyl auristatin E**. The intended mechanism is selective delivery of the cytotoxic payload to **EphA2-expressing tumors**, leading to internalization and tumor cell killing. Publicly described work appears to be **preclinical/research-stage**, with activity reported in xenograft models including EphA2-overexpressing solid tumors such as non-small cell lung cancer, prostate cancer, breast cancer, gastric cancer, ovarian cancer, and esophageal cancer.

02

Targets

EPHA2 (Ephrin type-A receptor 2)

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