| Monoclonal antibody | |
|---|---|
| Type | Whole antibody |
| Source | Human |
| Target | IGF-1 receptor |
| Clinical data | |
| Routes of administration | IV |
| ATC code |
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| Identifiers | |
| CAS Number | |
| ChemSpider |
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| UNII | |
| KEGG |
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| Chemical and physical data | |
| Formula | C6500H10052N1724O2036S44 |
| Molar mass | 146336.59 g·mol−1 |
| | |
Cixutumumab (IMC-A12) is a humanmonoclonal antibody for the treatment of solid tumors.[1][2]
This drug was developed byImClone Systems, since acquired byEli Lilly, usingphage display technology fromDyax.[citation needed]
It is a fully human IgG1 monoclonal antibody directed against the human insulin-like growth factor-1 receptor (IGF-1R) with potential antineoplastic activity. Cixutumumab selectively binds to membrane-bound IGF-1R, thereby preventing the binding of the ligand IGF-1 and subsequent activation ofPI3K/AKT signaling pathway. Downregulation of the PI3K/AKT survival pathway may result in the induction of cancer cell apoptosis and may decrease cancer cellular proliferation. IGF-1R, a receptor tyrosine kinase of the insulin receptor superfamily overexpressed by many cancer cell types, stimulates cell proliferation, enablesoncogenic transformation, and suppresses apoptosis; IGF-1R signaling has been implicated in tumorigenesis and metastasis.[3]
Phase II clinical trials have been completed in patients withnon-small cell lung cancer,[4][5][6] metastaticrhabdomyosarcoma,[7] metastaticprostate cancer,[8] metastaticpancreatic cancer,[9] metastaticesophageal cancer,[10]bone cancer,[11]sarcoma,[12] solid tumors,[13]ocular melanoma,[14]hepatocellular carcinoma,[15][16]breast cancer[17] and other forms of cancer. Despite these extensive trials, more than 45 phase I and II clinical trials in total, phase III trials have never been undertaken and Eli Lilly has removed cixutumumab from their development pipeline.[18]
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