ADC Development Services Targeting FGFR2

Antibody-drug conjugates (ADCs) have obtained a lot of attention due to its potential in the cancer treatment, which possess significant advantages including the specificity of targeted antibody and potent antitumor activity of small molecular drug. So far, a variety of ADCs have been designed, evaluated and several ADCs have been approved for cancer therapy.

Creative Biolabs is a leading biotechnology company in the field of ADCs related services. With years of experience and professional bio-conjugation technology, we offer a wide range of ADC development services against various tumor-associated antigens such as the FGFR2 to help you fulfill novel drug discovery project effectively.

Introduction of FGFR2

FGFR2 (Fibroblast growth factor receptor 2), also known as CD332, is a transmembrane receptor tyrosine kinase encoded by the FGFR2 gene that located at chromosome 10 in human. It belongs to the conserved fibroblast growth factor receptor family, which contains an extracellular region, a hydrophobic membrane domain, and a cytoplasmic tyrosine kinase moiety. FGFR2 interacts with the fibroblast growth factors to trigger a cascade of downstream signals and regulate the mitogenesis and differentiation. Besides, FGFR2 plays a critical role in the embryonic development, tissue repair, survival and angiogenesis. It is highly expressed on many cancer type cells, including triple-negative breast cancer, pancreatic, esophageal, hepatocellular, colorectal, ovarian, gastric, non-small-cell lung cancer (NSCLC), and glioma, while it is limitedly expressed in normal tissues. Thus, FGFR2 is regarded as an attractive target in the targeted cancer immunotherapy.

Fig.1 Mechanisms of pathogenic cancer cell FGF signalling. (Turner, 2010)

Anti-FGFR2 ADC in Solid Tumors

Aprutumab ixadotin (also known as BAY1187982) is a novel ADC against the FGFR2, which is composed of a fully human anti-FGFR2 monoclonal antibody (BAY 1179470) linked to an innovative auristatin W derivative via a non-cleavable linker. Auristatin W derivative is a new potent microtubule-disrupting agent first used in the ADC. Upon the ADC binds to the target cells, it can be internalized and then release the payload to induce the tumor cell death. Aprutumab ixadotin has been found has significant dose-dependent tumor regression in patient-derived xenograft (PDX) models in preclinical studies. In addition, aprutumab ixadotin displayed long half-life and was stable in the circulatory system. Clinical trials data demonstrated that aprutumab ixadotin has powerful antitumor activity with acceptable safety and tolerability in patients with advanced, refractory solid tumor. Thus, aprutumab ixadotin is the first ADC to target FGFR2 in the treatment of advanced tumors and is a promising therapeutic agent in cancer therapy.

Fig.2 Aprutumab ixadotin (BAY1187982) is investigated in the clinical trials.

What Can We Do for You?

Creative Biolabs offers fast turnaround and cost-effective ADCs services targeting the FGFR2 for the treatment of solid tumors. Based on years of experience on specific antibody development, potent drug synthesis and bio-conjugation, our scientists focus on optimizing protein-drug conjugation according to your requirements. Creative Biolabs’ first-class technology platforms and optimal conjugation strategies will promote your novel ADC drug development project in a significantly reduced timeline. If you are interested in our services, please contact us for more information.

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