Tigatuzumab
Monoclonal antibody
TypeWhole antibody
SourceHumanized (from mouse)
TargetTNFRSF10B (TRAIL-R2)
Clinical data
ATC code
  • none
Identifiers
CAS Number
ChemSpider
  • none
UNII
Chemical and physical data
FormulaC6406H9924N1716O2012S46
Molar mass144646.62 g·mol−1
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Tigatuzumab (CS-1008) is a monoclonal antibody[1] for the treatment of cancer. As of October 2009, a clinical trial for the treatment of pancreatic cancer,[2] Phase II trials for colorectal cancer,[3] non-small cell lung cancer,[4] and ovarian cancer[5] have been completed.

The drug targets member 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, a Phase I study was completed to investigate how biodistribution, quantitative tumor uptake, and antitumor response in patients with metastatic colorectal cancer was impacted by CS-1008. These objectives were tracked through use of trace-labeling and SPECT imaging 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

  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 from the original on 28 July 2011.
  3. ↑ Clinical trial number NCT00969033 for "CS-1008 Used With Irinotecan Versus Irinotecan Alone in Subjects With Metastatic Colorectal Carcinoma Who Failed First-line Treatment With Oxaliplatin" at ClinicalTrials.gov
  4. ↑ Clinical trial number NCT00991796 for "CS-1008 With Carboplatin/Paclitaxel in Chemotherapy naïve Subjects With Metastatic or Unresectable Non-small Cell Lung Cancer (NSCLC)" at ClinicalTrials.gov
  5. ↑ Clinical trial number NCT00945191 for "Combination Chemotherapy With CS-1008 to Treat Ovarian Cancer" at ClinicalTrials.gov
  6. ↑ "Drug Dictionary: CS-1008". National Cancer Institute.
  7. 1 2 Ciprotti 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. PMC 4881374. PMID 26124477.
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