|Source||Humanized (from mouse)|
|Chemical and physical data|
|Molar mass||144646.62 g·mol−1|
Tigatuzumab (CS-1008) is a monoclonal antibody As of October 2009 [update] , a clinical trial for the treatment of pancreatic cancer, Phase II trials for colorectal cancer, non-small cell lung cancer, and ovarian cancer have been completed.for the treatment of cancer.
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.
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.
Targeted therapy or molecularly targeted therapy is one of the major modalities of medical treatment (pharmacotherapy) for cancer, others being hormonal therapy and cytotoxic chemotherapy. As a form of molecular medicine, targeted therapy blocks the growth of cancer cells by interfering with specific targeted molecules needed for carcinogenesis and tumor growth, rather than by simply interfering with all rapidly dividing cells. Because most agents for targeted therapy are biopharmaceuticals, the term biologic therapy is sometimes synonymous with targeted therapy when used in the context of cancer therapy. However, the modalities can be combined; antibody-drug conjugates combine biologic and cytotoxic mechanisms into one targeted therapy.
Panitumumab (INN), formerly ABX-EGF, is a fully human monoclonal antibody specific to the epidermal growth factor receptor.
Ipilimumab, sold under the brand name Yervoy, is a monoclonal antibody medication that works to activate the immune system by targeting CTLA-4, a protein receptor that downregulates the immune system.
Matuzumab is a humanized monoclonal antibody for the treatment of cancer. It binds to the epidermal growth factor receptor (EGFR) with high affinity. The mouse monoclonal antibody (mAb425) from which matuzumab was developed at the Wistar Institute in Philadelphia, Pennsylvania
Cediranib is a potent inhibitor of vascular endothelial growth factor (VEGF) receptor tyrosine kinases.
Cixutumumab (IMC-A12) is a human monoclonal antibody for the treatment of solid tumors.
Ramucirumab is a fully human monoclonal antibody (IgG1) developed for the treatment of solid tumors. This drug was developed by ImClone Systems Inc. It was isolated from a native phage display library from Dyax.
Olaparib, sold under the brand name Lynparza, is a medication for the maintenance treatment of BRCA-mutated advanced ovarian cancer in adults. It is a PARP inhibitor, inhibiting poly ADP ribose polymerase (PARP), an enzyme involved in DNA repair. It acts against cancers in people with hereditary BRCA1 or BRCA2 mutations, which include some ovarian, breast, and prostate cancers.
Oncolytics Biotech Inc. is a Canadian company headquartered in Calgary, Alberta, that is developing an intravenously delivered immuno-oncolytic virus called pelareorep for the treatment of solid tumors and hematological malignancies. Pelareorep is a non-pathogenic, proprietary isolate of the unmodified reovirus that: induces selective tumor lysis and promotes an inflamed tumor phenotype through innate and adaptive immune responses.
Brivanib alaninate (INN/USAN) also known as BMS-582664 is an investigational, anti-tumorigenic drug for oral administration. The drug is being developed by Bristol-Myers Squibb for the treatment of hepatocellular carcinoma or HCC, the most common type of liver cancer.
Demcizumab is a humanized monoclonal antibody which is used to treat patients with pancreatic cancer or non-small cell lung cancer. Demcizumab has completed phase 1 trials and is currently undergoing phase 2 trials. Demcizumab was developed by OncoMed Pharmaceuticals in collaboration with Celgene.
Pegdinetanib is an investigational anti-cancer drug that acts as a selective antagonist of vascular endothelial growth factor receptor 2 (VEGFR-2), hindering vascularization of tumors. It is a genetically engineered peptide derivative based on the monobody technology, and is being developed by Adnexus.
Pembrolizumab is a humanized antibody used in cancer immunotherapy. This includes to treat melanoma, lung cancer, head and neck cancer, Hodgkin lymphoma, and stomach cancer. It is given by slow injection into a vein.
Aldoxorubicin (INNO-206) is a tumor-targeted doxorubicin conjugate in development by CytRx. Specifically, it is the (6-maleimidocaproyl) hydrazone of doxorubicin. Essentially, this chemical name describes doxorubicin attached to an acid sensitive linker.
Durvalumab is an FDA-approved immunotherapy for cancer, developed by Medimmune/AstraZeneca. It is a human immunoglobulin G1 kappa (IgG1κ) monoclonal antibody that blocks the interaction of programmed cell death ligand 1 (PD-L1) with the PD-1 (CD279).
Atezolizumab, sold under the brand name Tecentriq, is used to treat urothelial carcinoma, non-small cell lung cancer (NSCLC), triple-negative breast cancer (TNBC), small cell lung cancer (SCLC), and hepatocellular carcinoma (HCC). It is a fully humanized, engineered monoclonal antibody of IgG1 isotype against the protein programmed cell death-ligand 1 (PD-L1).
Sacituzumab govitecan, sold under the brand name Trodelvy, is a Trop-2-directed antibody and topoisomerase inhibitor drug conjugate for the treatment of adults with triple-negative breast cancer (TNBC) that has spread to other parts of the body and have received at least two prior therapies.
Avelumab, sold under the brand name Bavencio, is a fully human monoclonal antibody medication for the treatment of Merkel cell carcinoma, urothelial carcinoma, and renal cell carcinoma.
MM-151 is an oligoclonal mixture of fully human monoclonal antibodies, which binds multiple parts of the EGFR molecule It has started clinical trials in patients with RAS wild-type colorectal cancers (CRCs) that were resistant to other anti-EGFR therapies. It is intended to overcome the problem of cancers becoming resistant to monoclonal antibody therapies.
RO4929097 (RG-4733) is a gamma secretase inhibitor being studied as an anti-cancer drug. Targeting gamma secretase inhibits NOTCH signaling, which is upregulated in many forms of cancer. The drug was initially developed by Roche for the treatment of Alzheimer's disease, but current research focuses on cancer. Production was halted in 2010, but began again in 2014.
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