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Tigatuzumab

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Tigatuzumab
Monoclonal antibody
TypeWhole antibody
SourceHumanized(frommouse)
TargetTNFRSF10B(TRAIL-R2)
Clinical data
ATC code
  • none
Identifiers
CAS Number
ChemSpider
  • none
UNII
Chemical and physical data
FormulaC6406H9924N1716O2012S46
Molar mass144646.62g·mol−1
☒NcheckY(what is this?)(verify)

Tigatuzumab(CS-1008) is amonoclonal antibody[1]for the treatment of cancer. As of October 2009,aclinical trialfor the treatment ofpancreatic cancer,[2]Phase II trials forcolorectal cancer,[3]non-small celllung cancer,[4]andovarian cancer[5]have been completed.

The drug targetsmember 10b of the tumor necrosis factor receptor superfamily(TNFRSF10B, better known as death receptor 5 or trail receptor 2), a protein with limited expression in normal tissues but overexpressed in many kinds of tumours, including colon, gastric, pancreatic, lung, and cervical.[6][7]

In 2015, aPhase Istudy was completed to investigate howbiodistribution,quantitative tumor uptake, and antitumor response in patients with metastaticcolorectal cancerwas impacted by CS-1008. These objectives were tracked through use of trace-labeling andSPECTimaging over the course of treatment and found heterogeneity of tigatuzumab uptake in tumors, that tigatuzumab uptake is not dose dependent, and that tigatuzumab uptake is predictive of clinical response in the treatment of metastatic colorectal cancer.[7]

References

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  1. ^"International Nonproprietary Names for Pharmaceutical Substances (INN): List 60"(PDF).WHO Drug Information.
  2. ^"Combination Therapy Targets Pancreatic Cancer Stem Cells".NCI Cancer Bulletin.6(8). 21 April 2009. Archived fromthe originalon 28 July 2011.
  3. ^Clinical trial numberNCT00969033for "CS-1008 Used With Irinotecan Versus Irinotecan Alone in Subjects With Metastatic Colorectal Carcinoma Who Failed First-line Treatment With Oxaliplatin" atClinicalTrials.gov
  4. ^Clinical trial numberNCT00991796for "CS-1008 With Carboplatin/Paclitaxel in Chemotherapy naïve Subjects With Metastatic or Unresectable Non-small Cell Lung Cancer (NSCLC)" atClinicalTrials.gov
  5. ^Clinical trial numberNCT00945191for "Combination Chemotherapy With CS-1008 to Treat Ovarian Cancer" atClinicalTrials.gov
  6. ^"Drug Dictionary: CS-1008".National Cancer Institute.
  7. ^abCiprotti M, Tebbutt NC, Lee FT, Lee ST, Gan HK, McKee DC, et al. (August 2015)."Phase I Imaging and Pharmacodynamic Trial of CS-1008 in Patients With Metastatic Colorectal Cancer".Journal of Clinical Oncology.33(24): 2609–16.doi:10.1200/JCO.2014.60.4256.PMC4881374.PMID26124477.