Dalotuzumab

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Dalotuzumab
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Chemical and physical data
FormulaC6528H10086N1730O2018S40
Molar mass146374.99 g·mol−1
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Dalotuzumab is an anti-IGF1 receptor (IGF1R) humanized monoclonal antibody designed for the potential treatment of various cancers.[1] Common adverse effects include hyperglycemia, nausea, vomiting, and fatigue.[2] Dalotuzumab was developed by Merck and Co., Inc.[3]

Indications

Dalotuzumab is indicated to treat breast cancer, colorectal cancer, multiple myeloma, neuroendocrine tumors, non-small cell lung cancer (NSCLC), pancreatic cancer, and solid tumors.[1]

Adverse effects

Adverse effects of Dalotuzumab:[1][2][4]

Mechanism of action

adaptor proteins, Src-homology collagen (Shc) and insulin receptor substrate (IRS), are phosphorylated and, in turn, trigger the activation of the Ras/Raf/MEK/Erk and phosphoinositide 3-kinase (PI3K)/Akt signaling pathways, respectively.[3] These signaling pathways are involved in the regulation of cell survival and cell cycle progression.[3]

Furthermore,

extracellular domains of IGF1R, effectively blocking ligand activation of the receptor and preventing downstream signaling.[3] Moreover, the binding of Dalotuzumab to IGF1R, as seen with other anti-IGF1R antibodies, downregulates the expression of the receptors by prompting the internalization and degradation of IGF1R.[3]

Figure 1: Mechanism of Action of Dalotuzumab

History

There are more than 30 different anti-IGF1R candidate drugs involved in over 70 industry and academic-initiated clinical trials.[6]

Dalotuzumab (MK-0646) was developed by Merck and Co., Inc. under license from French pharmaceutical company, Pierre Fabre.[3] Dalotuzumab presently remains in clinical trials and has not been granted FDA approval.[7]

References

  1. ^
    PMID 20521225
    .
  2. ^
    PMID 24033707
    .
  3. ^ a b c d e f g h i "Dalotuzumab Overview". Creative Biolabs. Retrieved 2023-01-01.
  4. PMID 21813338
    .
  5. ^
    PMID 32166015
    .
  6. PMID 22415797
    .
  7. ^ "Dalotuzumab". SEER*Rx Interactive Antineoplastic Drugs Database. National Cancer Institute, National Institutes of Health, U.S. Department of Health and Human Services. Retrieved 2023-01-01.
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