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MedKoo product information:

Aderbasib

Description of Aderbasib (INCB007839): Aderbasib is a sheddase inhibitor, is also an orally bioavailable inhibitor of the ADAM (A Disintegrin And Metalloprotease) family of multifunctional membrane-bound proteins with potential antineoplastic activity. Aderbasib represses the metalloproteinase "sheddase" activities of ADAM10 and ADAM17, which may result in the inhibition of tumor cell proliferation. The metalloproteinase domains of ADAMs cleave cell surface proteins at extracellular sites proximal to the cell membrane, releasing or "shedding" soluble protein etcodomains from the cell surface; the disintegrin domains of these multifunctional proteins interact with various components of the extracellular matrix (ECM). ADAM10 processes particular epithelial growth factor receptor (EGFR) ligands and appears to regulate Notch signaling through the cleavage of Notch and its related ligand delta-like ligand-1 (Dll-1). ADAM17 (also known as Tumor necrosis factor-Converting Enzyme or TACE) is involved in processing tumor necrosis factor (TNF) from its membrane bound precursor to its soluble circulating form and in processing ligands for the epidermal growth factor receptor (EGFR) family. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

Current developer:   Incyte.

 INCB7839 is a novel, potent, orally bioavailable sheddase inhibitor (an inhibitor of two different pro-oncogenic mechanisms: generation of active EGFR ligands and generation of a constitutively active HER2 kinase).  INCB7839 in preclinical models: single agent efficacy; synergistic with other EGFR therapies; and synergistic with chemotherapy. Clinical Status: Phase I completed in healthy volunteers: INCB7839 was well-tolerated. In a dose-dependent manner, INCB7839 decreased HER2 ECD levels, a clinically relevant biomarker.A Phase II trial in HER2 positive breast cancer has begun and will be used to determine the effectiveness of INCB7839 in combination with Herceptin. Results from this trial are expected in the second half of 2009. (see:http://www.incyte.com/drugs_product_pipeline.html).

Witters L, Scherle P, Friedman S, Fridman J, Caulder E, Newton R, Lipton A. Synergistic inhibition with a dual epidermal growth factor receptor/HER-2/neu tyrosine kinase inhibitor and a disintegrin and metalloprotease inhibitor. Cancer Res. 2008 Sep 1;68(17):7083-9. PubMed PMID: 18757423.