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Background: HER2 (human epidermal growth factor receptor 2), also known as erbB-2 or CD340, is a tyrosine kinase of the EFGR family of proteins. There is no known ligand, but it can form homodimers or heterodimers with other HER proteins. Once active, it activates the MAPK (mitogen-activated protein kinase) and PI3K (phosphatidylinositol-3 kinase) signaling pathways resulting in cell cycle progression and cell proliferation. HER2 over-expression is also known to occur in breast, ovarian, stomach, lung adenocarcinoma, aggressive forms of uterine cancer and gastric cancer. In 1990 the FDA approved the use of the monoclonal antibody trastuzumab in breast and stomach cancer. Other strategies to target HER2 that have been approved include ADCs (antibody-drug conjugate) and margetuximab (an HER2 antibody that can alter the Fc-receptor affinity to CD16 and induce cytotoxicity). The use of small molecule tyrosine kinase inhibitors, alone or in combinatory therapy, has shown great promise in the treatment of HER2+ breast cancer (BC). However, resistance to treatment, for instance by mutations on HER2 or upregulation of other HER receptors, has been described. Neratinib, a pan-HER2 inhibitor, was approved in 2017 for early-stage BC, as adjuvant anti-HER2 therapy after trastuzumab treatment. However, side effects limit its use. The development of treatments able to target early-stage cancer, with minimal side effects and resistance development, will bring major benefits to HER2+ oncology patients.
Description: ORM-5029 is a first-in-class human epidermal growth factor receptor 2 (HER2)-targeted antibody-drug conjugate (ADC) comprised of SMol006, a highly potent GSPT1 degrader, conjugated to Pertuzumab. ORM-5029 can be used for study of cancer1.
Endotoxin Level: < 1 EU/mg
Format: Aqueous buffer solution.
Purity: ≥90%
Storage Stability: Store at -80°C, protect from light.
Target: HER2
Uniprot: P04626
Warnings: Avoid freeze/thaw cycles.
Biosafety Level: Not applicable (BSL-1)
References: 1. Sara A. Hurvitz, et al., 2023 Journal of Clinical Oncology. (41)16: TPS1114.
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