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]
^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
^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
^Clinical trial number NCT00945191 for "Combination Chemotherapy With CS-1008 to Treat Ovarian Cancer" at ClinicalTrials.gov