| Pharmaceutical Information |
| Drug Name |
Cetuximab |
| Drug ID |
BADD_D00422 |
| Description |
Cetuximab is a recombinant chimeric human/mouse IgG1 monoclonal antibody that competitively binds to epidermal growth factor receptor (EGFR) and competitively inhibits the binding of epidermal growth factor (EGF).[A227973] EGFR is a member of the ErbB family of receptor tyrosine kinases found in both normal and tumour cells; it is responsible for regulating epithelial tissue development and homeostasis.[A228083] EGFR has been implicated in various types of cancer, as it is often overexpressed in malignant cells [A227973] and EGFR overexpression has been linked to more advanced disease and poor prognosis.[A227963] EGFR is often mutated in certain types of cancer and serves as a driver of tumorigenesis.[A228083] _In vitro_, cetuximab was shown to mediate anti-tumour effects in numerous cancer cell lines and human tumour xenografts.[A227963]
Approved by the FDA in February 2004 under the brand name ERBITUX, cetuximab is used for the treatment of head and neck cancer and metastatic, KRAS wild-type colorectal cancer, and metastatic colorectal cancer with a BRAF V600E mutation.[A227963,L39045] It has also been investigated in advanced colorectal cancer, EGFR-expressing non-small cell lung cancer (NSCLC), and unresectable squamous cell skin cancer.[L31418] Cetuximab is administered via intravenous infusion and is used as monotherapy or in combination with other chemotherapies, including platinum agents, radiation therapy, [leucovorin], [fluorouracil], and [irinotecan].[L30448] |
| Indications and Usage |
Cetuximab indicated for the treatment of locally or regionally advanced squamous cell carcinoma of the head and neck in combination with radiation therapy. It is indicated for treating a recurrent locoregional disease or metastatic squamous cell carcinoma of the head and neck in combination with platinum-based therapy with fluorouracil. It is indicated for recurrent or metastatic squamous cell carcinoma of the head and neck progressing after platinum-based therapy.[L30448]
Cetuximab is also indicated for K-Ras wild-type, EGFR-expressing, metastatic colorectal cancer as determined by an FDA-approved test in combination with FOLFIRI, a chemotherapy combination that includes [leucovorin], [fluorouracil], and [irinotecan]; in combination with irinotecan in patients who are refractory to irinotecan-based chemotherapy; or as monotherapy in patients who have failed oxaliplatin- and irinotecan-based chemotherapy or who are intolerant to irinotecan.[L30448]
Additionally, cetuximab is also indicated for metastatic colorectal cancer that is BRAF V600E mutation-positive (as determined by an FDA-approved test) in combination with [encorafenib] but only after prior therapy.[L39045]
Cetuximab is not indicated for the treatment of Ras-mutant colorectal cancer or when the results of the Ras mutation tests are unknown.[L30448] |
| Marketing Status |
approved |
| ATC Code |
L01FE01 |
| DrugBank ID |
DB00002
|
| KEGG ID |
D03455
|
| MeSH ID |
D000068818
|
| PubChem ID |
Not Available
|
| TTD Drug ID |
D0N5OV
|
| NDC Product Code |
66733-948; 66733-958; 73424-0561 |
| UNII |
PQX0D8J21J
|
| Synonyms |
Cetuximab | Erbitux | IMC C225 | IMC-C225 | MAb C225 | C225 |
|
| Chemical Information |
| Molecular Formula |
Not Available |
| CAS Registry Number |
205923-56-4 |
| SMILES |
Not Available |
| Chemical Structure |
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| ADRs Induced by Drug |
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