Timigutuzumab Overview

Introduction Mechanisms Clinical Applications Clinical Projects What We Provide

Introduction of Timigutuzumab

Recent breakthroughs in cancer therapeutics have led to the development of Timigutuzumab (TrasGEX™), a cutting-edge glyco-engineered humanized monoclonal antibody. This innovative therapeutic agent specifically targets HER2/ERBB2/CD340, addressing a critical challenge in modern oncology. Under abnormal conditions, where HER2 serves as a key driver of tumor proliferation and metastatic spread, its overexpression characterizes some of the most aggressive forms of cancer, including breast and gastric malignancies.

The development of the anti-HER2 antibody Timigutuzumab represents a significant advancement. Its sophisticated design incorporates two distinct therapeutic mechanisms: precise binding to the HER2 extracellular domain to interrupt cancer-promoting signals, and enhanced immune response activation through antibody-dependent cellular cytotoxicity (ADCC), achieved through careful glycoengineering. Although Timigutuzumab remains in the investigational stages, preliminary clinical trial results have been remarkably promising, highlighting its significant potential for further development in advanced clinical settings.

Biological and Chemical Properties of Timigutuzumab

Protein Chemical Formula

C6428H9912N1712O2010S42

Protein Average Weight

The average weight of the protein is approximately 148 kDa.

The Mechanism of Timigutuzumab Action

Understanding the complexity of HER2/ERBB2 has been crucial in developing targeted therapies like Timigutuzumab. As a transmembrane receptor tyrosine kinase within the EGFR family, HER2 typically maintains modest expression levels in healthy tissues, playing a vital role in normal cellular processes. When activated, this receptor initiates a sophisticated cascade of cellular signals through pathways like PI3K/AKT and MAPK, essentially providing cancer cells with a survival advantage while promoting their rapid multiplication. However, this process becomes particularly problematic in treatment-resistant cancers, where HER2's ability to circumvent natural cell death mechanisms poses a significant therapeutic challenge. HER2 is overexpressed in certain cancers, transforming it into a powerful driver of disease progression. The implications of HER2 overexpression extend beyond mere cellular proliferation—it creates a perfect storm of aggressive tumor behavior by enabling cancer cells to resist programmed death and spread more readily throughout the body. The story of HER2's role in cancer progression reveals why it has become such a critical therapeutic target.

Timigutuzumab has a specially engineered structure that allows it to bind directly to HER2's extracellular domain, effectively preventing the receptor dimerization that typically triggers these harmful signaling cascades. Beyond this direct interference, Timigutuzumab's enhanced ADCC capability, achieved through careful Fc-engineering, mobilizes the body's immune system— particularly natural killer cells—to identify and eliminate cancer cells marked by the antibody. This dual-action mechanism, combining direct target inhibition with immune system activation, represents a sophisticated approach to combating HER2-positive cancers.

Figure 1. Different Molecular mechanisms for anti-HER2 Therapy (Timigutuzumab Act as a Monoclonal Antibodies to Bind to HER2)Figure 1. Various Molecular Approaches for HER2+ BC Therapy (Timigutuzumab Belongs to Monoclonal Antibodies).1

The Clinical Applications of Timigutuzumab

The clinical journey of Timigutuzumab has primarily focused on patients with HER2-positive cancers, where its potential as a targeted immunotherapy is being carefully evaluated. Phase I clinical investigations have revealed encouraging results regarding both safety and efficacy. This noteworthy Phase I trial involved 50 patients with advanced HER2-positive tumors, predominantly breast and gastric cancers. The results were promising: about half of the participants showed clinical benefit, including one complete response and two partial responses. Perhaps equally significant was the observation that the enhanced ADCC mechanism effectively reduced tumor burden in multiple cases, lending credence to the theoretical advantages of glycoengineering in improving immune-mediated cancer therapy. This study has documented generally mild to moderate infusion-related side effects, while pharmacokinetic data demonstrated a favorable half-life of approximately 263 hours at the 720 mg dose level, suggesting the possibility of convenient dosing schedules.

As Timigutuzumab advances toward Phase II trials, researchers are exploring its potential both as a standalone treatment and in combination with other HER2-targeted therapies. The ongoing investigation focuses on optimizing dosing strategies and understanding long-term outcomes across diverse patient populations. Through these continued efforts, Creative Biolabs remains committed to developing Timigutuzumab as a cutting-edge therapeutic antibody, underscoring the critical importance of precise HER2 targeting in modern oncology.

Clinical Projects of Timigutuzumab*

NCT ID Study Title Study Status Conditions Sponsor Start Date
NCT01409343 TrasGEX™: Phase 1 Study in Cancer Patients Completed Solid Tumors Glycotope GmbH 2011-08-04

* The table was excerpted from the following website: https://clinicaltrials.gov/study/NCT01409343?term=TrasGEX&rank=1#study-overview

What We Provide

Timigutuzumab

Anti-Human ERBB2 Recombinant Antibody (Timigutuzumab)

We provide high-quality timigutuzumab for use in Enzyme-Linked Immunosorbent Assay, Immunohistochemistry, Immunofluorescence, Immunoprecipitation, Flow Cytometry, Functional Studies. The product is for lab research use only, not for diagnostic, therapeutic, or any in vivo human use.

Specification
  • Immunogen
  • The details of the immunogen for this antibody are not available.
  • Host Species
  • Human
  • Derivation
  • Humanized
  • Type
  • IgG1, κ
  • Specificity
  • Human ERBB2
  • Species Reactivity
  • Human
  • Applications
  • Used for immunoassay techniques such as: Enzyme-Linked Immunosorbent Assay; Immunohistochemistry; Immunofluorescence; Immunoprecipitation; Flow Cytometry; Functional Studies
  • Conjugate
  • Unconjugated
  • CAS
  • 1665274-14-5
  • Generic Name
  • Timigutuzumab
  • UNII
  • A5HYI6N66H
  • Related Disease
  • Cancers

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Reference
  1. Lv, Quanxia, et al. "Molecular mechanisms and translational therapies for human epidermal receptor 2 positive breast cancer." International journal of molecular sciences 17.12 (2016): 2095. Distributed under Open Access license CC BY 4.0, without modification.

For research use only. Not intended for any clinical use.

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