Drug intelligence / Profile preview

nuzefatide pevedotin + nivolumab

Development stage
Phase 2
Lead developer
Bicycle Therapeutics
Modality
Peptide-Drug Conjugates → Peptide Conjugates → Peptides, Cyclic Peptides → Modified Peptides → Peptides, Monoclonal Antibodies → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

**Nuzefatide pevedotin + nivolumab** is an investigational combination therapy consisting of nuzefatide pevedotin (formerly BT5528), an EphA2-targeting Bicycle Drug Conjugate (BDC), and nivolumab, a programmed death-1 (PD-1) blocking monoclonal antibody. Nuzefatide pevedotin comprises a bicyclic peptide targeting erythropoietin-producing hepatocellular receptor A2 (EphA2) conjugated to the cytotoxic payload monomethyl auristatin E (MMAE) via a cleavable linker. Nivolumab is an IgG4 monoclonal antibody that binds to PD-1, preventing its interaction with PD-L1 and PD-L2 to restore T-cell mediated anti-tumor immune responses. This combination is being evaluated in Phase 1/2 clinical trials for the treatment of advanced solid tumors, including metastatic urothelial carcinoma (mUC), ovarian cancer, non-small cell lung cancer (NSCLC), triple-negative breast cancer (TNBC), head and neck squamous cell carcinoma (HNSCC), and gastric/upper gastrointestinal cancer.

Other names
BT5528 + nivolumabBT5528 + Opdivonuzefatide pevedotin + Opdivo
02

Targets

EPHA2 (Ephrin type-A receptor 2)PDCD1 (Programmed cell death protein 1 receptor)CD274 (Programmed cell death protein 1 ligand 1)PDCD1LG2 (Programmed cell death 1 ligand 2)TUBB (Tubulin (alpha and beta subunits))

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