Drug intelligence / Profile preview

trastuzumab brengitecan + pertuzumab

Development stage
Phase 3
Lead developer
Biokin Pharmaceutical
Modality
Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

T-Bren + pertuzumab is an investigational combination therapy consisting of trastuzumab brengitecan (T-Bren; BL-M07D1), a HER2-directed antibody-drug conjugate (ADC), and pertuzumab, a HER2-targeting monoclonal antibody. Trastuzumab brengitecan comprises a humanized anti-HER2 monoclonal antibody conjugated via a cathepsin B-cleavable linker to Ed-04, a potent topoisomerase I inhibitor payload (a camptothecin derivative), with a drug-to-antibody ratio (DAR) of 8. Pertuzumab is a recombinant humanized monoclonal antibody that binds to extracellular domain II of HER2, preventing HER2 from heterodimerizing with other HER receptors (such as HER3). The combination is being evaluated in clinical trials, including a Phase 3 trial (NCT07518173) for first-line HER2-positive recurrent or metastatic breast cancer and a Phase 2/3 trial (NCT06891833) as neoadjuvant therapy for HER2-positive breast cancer.

Other names
T-Bren + pertuzumab
02

Targets

CTSB (Cathepsin B)TOP1 (DNA Topoisomerase I)FcγR (Low affinity immunoglobulin gamma Fc region receptor II-c)ERBB2 (Erb-b2 receptor tyrosine kinase 2)ERBB3 (Erb-b2 receptor tyrosine kinase 3)

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