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Insulin-like growth factors (IGFs) are pivotal in cellular processes contributing to normal physiology as well as certain pathologies (e.g., cancer). [3] The IGF family of proteins, also known as the IGF axis, consists of three ligands (insulin, IGF1, IGF2), three cell surface receptors (insulin receptor [IR], IGF1 receptor [IGF1R], IGF2 receptor [IGF2R]), and seven IGF binding proteins ...
The IGF-1 receptor seems to be the "physiologic" receptor—it binds IGF-1 at significantly higher affinity than it binds insulin. [9] Like the insulin receptor, the IGF-1 receptor is a receptor tyrosine kinase—meaning it signals by causing the addition of a phosphate molecule on particular tyrosines.
Linsitinib is an experimental drug candidate for the treatment of various types of cancer. It is an inhibitor of the insulin receptor and of the insulin-like growth factor 1 receptor (IGF-1R). [1] This prevents tumor cell proliferation and induces tumor cell apoptosis. [2]
It is a fully human IgG1 monoclonal antibody directed against the human insulin-like growth factor-1 receptor with potential antineoplastic activity. Cixutumumab selectively binds to membrane-bound IGF-1R, thereby preventing the binding of the ligand IGF-1 and subsequent activation of PI3K/AKT signaling pathway. Downregulation of the PI3K/AKT ...
Low IGF-1 levels are associated with cardiovascular disease, while high IGF-1 levels are associated with cancer. Mid-range IGF-1 levels are associated with the lowest mortality. A synthetic analog of IGF-1, mecasermin, is used for the treatment of growth failure in children with severe IGF-1 deficiency. [15]
Figitumumab (previously CP-751871) is a monoclonal antibody [1] targeting the insulin-like growth factor-1 receptor that was investigated for the treatment of various types of cancer, for example adrenocortical carcinoma [2] and non-small cell lung cancer (NSCLC).
Ganitumab is a human monoclonal antibody against type 1 insulin-like growth factor receptor , designed for the treatment of cancers. [1] [2] Ganitumab was developed by Amgen. A phase III clinical trial (for metastatic pancreatic cancer) was abandoned in August 2012. [3] [4]
Istiratumab (MM-141) is an experimental monoclonal antibody for the treatment of cancer. It is a bispecific antibody targeting IGF-1R and ErbB3. [1] It is in development by Merrimack Pharmaceuticals (In the US) and was awarded orphan drug status for pancreatic cancer. [2]
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