Details of the Drug

General Information of Drug (ID: DMLNCE0)

Drug Name
Cetuximab
Synonyms Erbitux; Cetuximab (genetical recombination); Erbitux (TN); Cetuximab (USAN/INN); Cetuximab (genetical recombination) (JAN); novel EGFR mAb inhibitors
Indication
Disease Entry ICD 11 Status REF
Colorectal cancer 2B91.Z Approved [1]
Laryngeal squamous cell carcinoma N.A. Approved [2]
Lung cancer 2C25.0 Approved [3]
Plasma cell myeloma 2A83.1 Approved [4]
Salivary gland squamous cell carcinoma N.A. Approved [5]
Colon cancer 2B90.Z Investigative [6]
Gastric cancer 2B72 Investigative [7]
Pharyngeal squamous cell carcinoma N.A. Investigative [8]
⏷ Show the Full List of Indication(s)
Therapeutic Class
Anticancer Agents
Drug Type
Antibody
Sequence
>heavy chain
QVQLKQSGPGLVQPSQSLSITCTVSGFSLTNYGVHWVRQSPGKGLEWLGVIWSGGNTDYN
TPFTSRLSINKDNSKSQVFFKMNSLQSNDTAIYYCARALTYYDYEFAYWGQGTLVTVSAA
STKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSG
LYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKVEPKSCDKTHTCPPCPAPELLGGP
SVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNS
TYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDEL
TKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQ
QGNVFSCSVMHEALHNHYTQKSLSLSPGK
>light chain
DILLTQSPVILSVSPGERVSFSCRASQSIGTNIHWYQQRTNGSPRLLIKYASESISGIPS
RFSGSGSGTDFTLSINSVESEDIADYYCQQNNNWPTTFGAGTKLELKRTVAAPSVFIFPP
SDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTLT
LSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC
ADMET Property
Absorption Tmax
The time to maximum plasma concentration (Tmax) is 3 h [9]
Clearance
The sytemic clearance of drug is 0.103 L/h [10]
Half-life
The concentration or amount of drug in body reduced by one-half in 112 hours [9]
Metabolism
The drug is metabolized via the reticuloendothelial system and protein catabolism by a target\mediated disposition pathway [11]
Adverse Drug Reaction (ADR)
ADR Term Variation Related DOT DOT ID REF
Neoplasm related morbidities Not Available EGFR OTAPLO1S [12]
Cross-matching ID
DrugBank ID
DB00002
TTD ID
D0N5OV
Repurposed Drugs (RPD) Click to Jump to the Detailed RPD Information of This Drug

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Epidermal growth factor receptor (EGFR) TTGKNB4 EGFR_HUMAN Not Available [13]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Epidermal growth factor receptor (EGFR) OTAPLO1S EGFR_HUMAN Drug Response [12]
Low affinity immunoglobulin gamma Fc region receptor II-a (FCGR2A) OT0OUDUT FCG2A_HUMAN Drug Response [14]
Low affinity immunoglobulin gamma Fc region receptor III-A (FCGR3A) OTOWXCF3 FCG3A_HUMAN Drug Response [14]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Molecular Expression Atlas of This Drug

The Studied Disease Colorectal cancer
ICD Disease Classification 2B91.Z
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Epidermal growth factor receptor (EGFR) DTT EGFR 1.04E-65 -0.89 -1.53
Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Cetuximab (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Rabeprazole DMMZXIW Moderate Increased risk of hypomagnesemia by the combination of Cetuximab and Rabeprazole. Bacterial infection [1A00-1C4Z] [15]
Dexlansoprazole DM1DBV5 Moderate Increased risk of hypomagnesemia by the combination of Cetuximab and Dexlansoprazole. Gastro-oesophageal reflux disease [DA22] [15]
Omeprazole DM471KJ Moderate Increased risk of hypomagnesemia by the combination of Cetuximab and Omeprazole. Gastro-oesophageal reflux disease [DA22] [15]
Pantoprazole DMSVOCZ Moderate Increased risk of hypomagnesemia by the combination of Cetuximab and Pantoprazole. Gastro-oesophageal reflux disease [DA22] [15]
Thalidomide DM70BU5 Major Additive thrombogenic effects by the combination of Cetuximab and Thalidomide. Multiple myeloma [2A83] [16]
Methoxsalen DME8FZ9 Moderate Increased risk of photosensitivity reactions by the combination of Cetuximab and Methoxsalen. Mycosis fungoides [2B01] [17]
Omacetaxine mepesuccinate DMPU2WX Moderate Additive immunosuppressive effects by the combination of Cetuximab and Omacetaxine mepesuccinate. Myeloproliferative neoplasm [2A20] [18]
Esomeprazole DM7BN0X Moderate Increased risk of hypomagnesemia by the combination of Cetuximab and Esomeprazole. Peptic ulcer [DA61] [15]
Verteporfin DMIY6DB Moderate Increased risk of photosensitivity reactions by the combination of Cetuximab and Verteporfin. Psoriasis [EA90] [19]
⏷ Show the Full List of 9 DDI Information of This Drug

References

1 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6882).
2 Cetuximab enhances oridonin-induced apoptosis through mitochondrial pathway and endoplasmic reticulum stress in laryngeal squamous cell carcinoma cells. Toxicol In Vitro. 2020 Sep;67:104885.
3 Cetuximab for treating non-small cell lung cancer. Expert Opin Biol Ther. 2018 Apr;18(4):483-493.
4 SOT101 induces NK cell cytotoxicity and potentiates antibody-dependent cell cytotoxicity and anti-tumor activity. Front Immunol. 2022 Oct 10;13:989895.
5 Patient-derived head and neck cancer organoids allow treatment stratification and serve as a tool for biomarker validation and identification. Med. 2023 May 12;4(5):290-310.e12.
6 Colon cancer. Crit Rev Oncol Hematol. 2010 May;74(2):106-33.
7 Assessment of a HER2 scoring system for colorectal cancer: results from a validation study. Mod Pathol. 2015 Nov;28(11):1481-91.
8 Head and neck squamous cell carcinoma. Nat Rev Dis Primers. 2020 Nov 26;6(1):92.
9 FDA Approved Drug Products: ERBITUX (cetuximab) injection, for intravenous use
10 Dirks NL, Nolting A, Kovar A, Meibohm B: Population pharmacokinetics of cetuximab in patients with squamous cell carcinoma of the head and neck. J Clin Pharmacol. 2008 Mar;48(3):267-78. doi: 10.1177/0091270007313393. Epub 2008 Jan 24.
11 Veve MP, Wagner JL: Lefamulin: Review of a Promising Novel Pleuromutilin Antibiotic. Pharmacotherapy. 2018 Sep;38(9):935-946. doi: 10.1002/phar.2166. Epub 2018 Aug 20.
12 ADReCS-Target: target profiles for aiding drug safety research and application. Nucleic Acids Res. 2018 Jan 4;46(D1):D911-D917. doi: 10.1093/nar/gkx899.
13 Molecular inhibition of angiogenesis and metastatic potential in human squamous cell carcinomas after epidermal growth factor receptor blockade. Mol Cancer Ther. 2002 May;1(7):507-14.
14 FCGR2A and FCGR3A polymorphisms associated with clinical outcome of epidermal growth factor receptor expressing metastatic colorectal cancer patients treated with single-agent cetuximab. J Clin Oncol. 2007 Aug 20;25(24):3712-8. doi: 10.1200/JCO.2006.08.8021.
15 FDA. U.S. Food and Drug Administration "FDA Drug Safety Communication: Low magnesium levels can be associated with long-term use of proton pump inhibitor drugs (PPIs).".
16 Figg WD, Arlen P, Gulley J, et al. "A randomized phase II trial of docetaxel (taxotere) plus thalidomide in androgen-independent prostate cancer." Semin Oncol 28(4 Suppl 15) (2001): 62-6. [PMID: 11685731]
17 Cerner Multum, Inc. "Australian Product Information.".
18 Product Information. Synribo (omacetaxine). Teva Pharmaceuticals USA, North Wales, PA.
19 Cerner Multum, Inc. "UK Summary of Product Characteristics.".