Cixutumumab

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Cixutumumab
Monoclonal antibody
Type Whole antibody
Source Human
Target IGF-1 receptor
Clinical data
Routes of
administration
IV
ATC code
  • none
Identifiers
CAS Number
ChemSpider
  • none
UNII
KEGG
Chemical and physical data
Formula C6500H10052N1724O2036S44
Molar mass 146.3 kg/mol
 NYesY (what is this?)  (verify)

Cixutumumab (IMC-A12) is a human monoclonal antibody for the treatment of solid tumors.[1][2]

This drug was developed by ImClone Systems, since acquired by Eli Lilly, using phage display technology from Dyax.

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 of PI3K/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, enables oncogenic transformation, and suppresses apoptosis; IGF-1R signaling has been implicated in tumorigenesis and metastasis.[3]

Research[edit]

Phase II clinical trials have been completed in patients with non-small cell lung cancer,[4][5] [6] metastatic rhabdomyosarcoma,[7] metastatic prostate cancer,[8] metastatic pancreatic cancer,[9] metastatic esophageal cancer,[10] bone cancer,[11][12] sarcoma,[13] solid tumors,[14] ocular melanoma,[15] hepatocellular carcinoma,[16][17], breast cancer[18] 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.[19]

References[edit]

  1. ^ Statement On A Nonproprietary Name Adopted By The Usan Council - Cixutumumab American Medical Association.
  2. ^ McKian, KP; Haluska, P (2009). "Cixutumumab". Expert Opinion on Investigational Drugs. 18 (7): 1025–33. PMC 2939377Freely accessible. PMID 19548856. doi:10.1517/13543780903055049. 
  3. ^ [1] National Cancer InstituteTemplate:Http://www.cancer.gov/drugdictionary/?CdrID=561575
  4. ^ https://clinicaltrials.gov/ct2/show/NCT01263782
  5. ^ https://clinicaltrials.gov/ct2/show/NCT00955305
  6. ^ https://clinicaltrials.gov/ct2/show/NCT00986674
  7. ^ https://clinicaltrials.gov/ct2/show/NCT01055314
  8. ^ https://clinicaltrials.gov/ct2/show/NCT01120236
  9. ^ https://clinicaltrials.gov/ct2/show/NCT00617708
  10. ^ https://clinicaltrials.gov/ct2/show/NCT01142388
  11. ^ https://clinicaltrials.gov/ct2/show/NCT01016015
  12. ^ https://clinicaltrials.gov/ct2/show/NCT00668148
  13. ^ https://clinicaltrials.gov/ct2/show/NCT01614795
  14. ^ https://clinicaltrials.gov/ct2/show/NCT00831844
  15. ^ https://clinicaltrials.gov/ct2/show/NCT01413191
  16. ^ https://clinicaltrials.gov/ct2/show/NCT00906373
  17. ^ https://clinicaltrials.gov/ct2/show/NCT00639509
  18. ^ https://clinicaltrials.gov/ct2/show/NCT00728949
  19. ^ https://www.lilly.com/pipeline/index.html