Cetuximab

EGFR Inhibitor

DB00002

Approved Indication

Cetuximab, used in combination with irinotecan, is indicated for the treatment of EGFR-expressing, metastatic colorectal carcinoma in patients who are refractory to irinotecan-based chemotherapy. Cetuximab administered as a single agent is indicated for the treatment of EGFR-expressing, metastatic c

12 Targets

22 Resistance Mutations

110 References

3D Structure No structure available

No co-crystal structure available

Protein Targets

EGFR P00533 ✓ C1QA P02745 C1QB P02746 C1QC P02747 C1R P00736 C1S P09871 FCGR1A P12314 FCGR2A P12318 FCGR2B P31994 FCGR2C P31995 FCGR3A P08637 FCGR3B O75015

Mechanism of Action

Cetuximab binds to the epidermal growth factor receptor (EGFr) on both normal and tumor cells. EGFr is over-expressed in many colorectal cancers. Cetuximab competitively inhibits the binding of epidermal growth factor (EGF) and TGF alpha, thereby reducing their effects on cell growth and metastatic spread.

Resistance Mutations — 120 resistance samples observed in COSMIC

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BRAF

p.V600E 5 p.V640E 1

KRAS

p.G12A 5 p.G12C 5 p.G12D 5 p.G12R 5 p.G12S 5 p.G12V 5 p.G13D 5 p.Q61H 5 p.Q61L 5 p.Q61R 5

MAP2K1

p.K57T 5

NRAS

p.G12D 5 p.G12S 5 p.G13R 5 p.G60D 4 p.G60R 2 p.Q61H 5 p.Q61K 5 p.Q61L 5 p.Q61R 5

Resistance mutations sourced from COSMIC Drug Resistance database. Cyan = on-target · Amber = off-target · numbered badge = PubMed references for that mutation

Details

DrugBank ID DB00002 ↗

Approval Date 2004-02-12

Molecular Weight — g/mol

Drug Class EGFR Inhibitor

ATC Codes L01XC06

Synonyms Cetuximab, Cétuximab, Cetuximabum

ChEMBL CHEMBL1201577 ↗

Drug References (DrugBank)

PMID:10480573 PMID:10601294 PMID:10628369 PMID:11408594 PMID:11431346 PMID:11752352 PMID:15269308 PMID:16336752