Drug intelligence / Profile preview

pertuzumab + trastuzumab + imbotolimod

Development stage
Unknown
Lead developer
Bolt Biotherapeutics
Modality
Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

This drug is a combination of **pertuzumab**, **trastuzumab**, and **imbotolimod**. Pertuzumab and trastuzumab are monoclonal antibodies targeting the human epidermal growth factor receptor 2 (**HER2**), a receptor overexpressed in certain cancers, most notably breast cancer. Both antibodies bind to different regions of the HER2 extracellular domain, leading to inhibition of receptor signaling, prevention of HER2 dimerization (pertuzumab), and induction of immune-mediated cytotoxicity such as antibody-dependent cellular cytotoxicity (ADCC) and complement-dependent cytotoxicity (CDC). Imbotolimod is a **Toll-like receptor 7/8 (TLR7/8) agonist**, covalently linked to trastuzumab as an immune-stimulating antibody conjugate (ISAC), designed to further enhance innate and adaptive immune responses against HER2-expressing tumor cells. The combination aims to augment antitumor efficacy by engaging both direct HER2 inhibition and potent immune stimulation, including increased cytokine and chemokine release and tumor myeloid activation. This combination is under investigation for **HER2-positive cancers**, with the ISAC component (trastuzumab imbotolimod) showing promising activity in preclinical and early clinical studies[5][7][8].

02

Targets

TLR8 (Toll-like receptor 8)TLR7 (Toll-like receptor 7)ERBB2 (Erb-b2 receptor tyrosine kinase 2)

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