Drug intelligence / Profile preview

zelenectide pevedotin

Development stage
Phase 2
Lead developer
Bicycle Therapeutics
Modality
Cyclic Peptides → Modified Peptides → Peptides, Peptide-Drug Conjugates → Peptide Conjugates → Peptides, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

Zelenectide pevedotin is a Bicycle Toxin Conjugate (BTC), also known as BT8009, developed by Bicycle Therapeutics. It consists of a synthetic bicyclic peptide (zelenectide) that selectively targets the cell adhesion molecule nectin-4 (PVRL4), which is commonly overexpressed in various solid tumors. The peptide is conjugated via a cleavable linker to the cytotoxic payload monomethyl auristatin E (MMAE). Upon binding to nectin-4 on tumor cells, the conjugate is internalized and releases MMAE intracellularly, leading to inhibition of tubulin polymerization and subsequent cell cycle arrest and apoptosis. Zelenectide pevedotin has demonstrated promising antitumor activity with a favorable safety profile in early clinical trials for advanced malignancies such as urothelial carcinoma and breast cancer. Its low molecular weight and short plasma half-life may allow for rapid tumor penetration while minimizing exposure to normal tissues[2][3][4][5][6].

Brand names
zelenectide pevedotin
Other names
BT8009BT-8009BT 8009Bicycle Toxin Conjugate BTCzele
02

Targets

PVRL4 (Nectin cell adhesion molecule 4)TUBB (Tubulin (alpha and beta subunits))

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