Drug intelligence / Profile preview

BT1718

Development stage
Phase 2
Lead developer
Bicycle Therapeutics
Modality
Small Molecules, 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

BT1718 is a first-in-class Bicycle Drug Conjugate (BDC), also referred to as a Bicycle Toxin Conjugate, developed by Bicycle Therapeutics. It consists of a constrained bicyclic peptide that binds with high affinity and specificity to membrane type 1-matrix metalloprotease (MT1-MMP; also known as MMP14), which is overexpressed in many solid tumors and associated with poor prognosis. The peptide is covalently linked via a hindered disulfide linker to DM1, a potent anti-tubulin cytotoxic agent. Upon binding MT1-MMP on tumor cells, the conjugate delivers DM1 directly into the tumor microenvironment or cell interior, leading to inhibition of tubulin polymerization and induction of apoptosis in cancer cells. Preclinical studies have shown target-dependent efficacy in xenograft models resistant to standard therapies[1][3][5]. Clinical trials have evaluated its safety and efficacy in advanced solid tumors[2][3].

02

Targets

TUBB (Tubulin (alpha and beta subunits))MMP14 (Matrix metalloproteinase 14)

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