ArticleJournal of medicinal chemistry2022
Discovery of BT8009: A Nectin-4 Targeting Bicycle Toxin Conjugate for the Treatment of Cancer.
Article in Journal of medicinal chemistry, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 51 papers.
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Who cites it
51 citing papers in PubMed, 86 citations in OpenAlex.
- First-in-Human, Phase I/II Dose Escalation and Expansion Study of Zelenectide Pevedotin in Patients With Advanced Solid Tumors: Results From Monotherapy Dose Escalation.Journal of clinical oncology : official journal of the American Society of Clinical Oncology · 2025Trial
- Genetically Encoded Lysine-Selective Photocyclization Enables Phage Display Selection of Cyclic Peptide Binders.Angewandte Chemie (International ed. in English) · 2026Article
- Discovery of a Novel Tripeptide Linker that Broadens the Therapeutic Window of Auristatin-Based Antibody-Drug Conjugates by Reducing Bone Marrow Toxicity.Bioconjugate chemistry · 2026Article
- Cyclic Peptides in Modern Drug Discovery: Trends and Therapeutic Directions.Journal of medicinal chemistry · 2026Review
- Peptides as programmable molecular scaffolds: from chemical synthesis and engineering to translational medicine.RSC chemical biology · 2026Review
- Preclinical Theranostic Study ofACS omega · 2026Article
- Peptides as multifunctional linchpins in targeted drug conjugates.RSC medicinal chemistry · 2026Review
- Preliminary biological evaluation of a [EJNMMI radiopharmacy and chemistry · 2026Article
- Receptor-Mediated Drug Delivery: Redefining Targeted Drug Conjugates in Oncology.Pharmaceutics · 2026Review
- Unlocking the potential of EphA2 with precision-guided cancer therapy: bicycle drug conjugates.Journal of translational medicine · 2026Review
- Bismuth Bicycles.Journal of peptide science : an official publication of the European Peptide Society · 2026Review
- From Cloudy to Clear: A Strategy to Resolve the Complex Structural Elucidation of Bicycle Drug Conjugate Zelenectide Pevedotin by NMR.Bioconjugate chemistry · 2026Article
- Isothiocyanate-mediated cyclization of phage-displayed peptides enables discovery of macrocyclic binders.Science advances · 2026Article
- Nectin-4 PET for predicting enfortumab vedotin dose-response in urothelial carcinoma.Science advances · 2026Article
- Biodistribution, dosimetry, and preliminary imaging of the novel Nectin-4-targeting PET tracer [⁶⁸Ga]Ga-FZ-NR-1 in humans.EJNMMI research · 2026Article
- Staging metastatic urothelial cancer with Nectin-4 imaging using Gallium-68-N188 PET/CT.BJU international · 2026Article
- Metastatic Triple Negative Breast Cancer: Navigating a Rapidly Evolving Therapeutic Landscape.Oncology research · 2026Review
- Research hotspots and frontier analysis of the novel immune checkpoint Nectin-4.Human vaccines & immunotherapeutics · 2025Review
- Design of Bicyclic Peptide Tandems Mimicking the Homodimeric GDF15 Protein to Inhibit GDF15-GFRaL-RET Complex Cell Signaling.Journal of medicinal chemistry · 2025Article
- "Precision on Two Wheels"─Structural Refinement ofJournal of medicinal chemistry · 2025Article
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Authors and funding
13 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Bicycle toxin conjugates (BTCs) are a promising new class of molecules for targeted delivery of toxin payloads into tumors. Herein we describe the discovery of BT8009, a Nectin-4 targeting BTC currently under clinical evaluation. Nectin-4 is overexpressed in multiple tumor types and is a clinically validated target for selective delivery of cytotoxic payloads. A Nectin-4 targeting bicyclic peptide was identified by phage display, which showed highly selective binding for Nectin-4 but suffered from low plasma stability and poor physicochemical properties. Multiparameter chemical optimization involving introduction of non-natural amino acids resulted in a lead Bicycle that demonstrated high affinity for Nectin-4, good stability in biological matrices, and a much-improved physicochemical profile. The optimized Bicycle was conjugated to the cytotoxin Monomethyl auristatin E via a cleavable linker to give the targeted drug conjugate BT8009, which demonstrates potent anticancer activity in in vivo rodent models.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.