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], [2]
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 [3]
Clearance
The sytemic clearance of drug is 0.103 L/h [4]
Half-life
The concentration or amount of drug in body reduced by one-half in 112 hours [3]
Metabolism
The drug is metabolized via the reticuloendothelial system and protein catabolism by a target\mediated disposition pathway [5]
Cross-matching ID
DrugBank ID
DB00002
TTD ID
D0N5OV

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 [6], [7], [8]
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 5.84E-05 0.32 0.55
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] [18]
Dexlansoprazole DM1DBV5 Moderate Increased risk of hypomagnesemia by the combination of Cetuximab and Dexlansoprazole. Gastro-oesophageal reflux disease [DA22] [18]
Omeprazole DM471KJ Moderate Increased risk of hypomagnesemia by the combination of Cetuximab and Omeprazole. Gastro-oesophageal reflux disease [DA22] [18]
Pantoprazole DMSVOCZ Moderate Increased risk of hypomagnesemia by the combination of Cetuximab and Pantoprazole. Gastro-oesophageal reflux disease [DA22] [18]
Thalidomide DM70BU5 Major Additive thrombogenic effects by the combination of Cetuximab and Thalidomide. Multiple myeloma [2A83] [19]
Methoxsalen DME8FZ9 Moderate Increased risk of photosensitivity reactions by the combination of Cetuximab and Methoxsalen. Mycosis fungoides [2B01] [20]
Omacetaxine mepesuccinate DMPU2WX Moderate Additive immunosuppressive effects by the combination of Cetuximab and Omacetaxine mepesuccinate. Myeloproliferative neoplasm [2A20] [21]
Esomeprazole DM7BN0X Moderate Increased risk of hypomagnesemia by the combination of Cetuximab and Esomeprazole. Peptic ulcer [DA61] [18]
Verteporfin DMIY6DB Moderate Increased risk of photosensitivity reactions by the combination of Cetuximab and Verteporfin. Psoriasis [EA90] [22]
⏷ 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 2004 approvals: the demise of the blockbuster. Nat Rev Drug Discov. 2005 Feb;4(2):93-4.
3 FDA Approved Drug Products: ERBITUX (cetuximab) injection, for intravenous use
4 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.
5 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.
6 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.
7 Epidermal growth factor receptor-targeted therapy for pancreatic cancer. Semin Oncol. 2002 Oct;29(5 Suppl 14):31-7.
8 Epidermal growth factor receptors as a target for cancer treatment: the emerging role of IMC-C225 in the treatment of lung and head and neck cancers. Semin Oncol. 2002 Feb;29(1 Suppl 4):27-36.
9 Nasopharyngeal carcinoma: Current treatment options and future directions. J Nasopharyng Carcinoma, 2014, 1(16): e16.
10 Triple negative breast cancer--current status and prospective targeted treatment based on HER1 (EGFR), TOP2A and C-MYC gene assessment. Biomed Pap Med Fac Univ Palacky Olomouc Czech Repub. 2009 Mar;153(1):13-7.
11 Gefitinib ('Iressa', ZD1839) and new epidermal growth factor receptor inhibitors. Br J Cancer. 2004 Feb 9;90(3):566-72.
12 Quantitative prediction of fold resistance for inhibitors of EGFR. Biochemistry. 2009 Sep 8;48(35):8435-48.
13 A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22.
14 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. (Target id: 1797).
15 Boehringer Ingelheim. Product Development Pipeline. June 2 2009.
16 Synthesis and Src kinase inhibitory activity of a series of 4-[(2,4-dichloro-5-methoxyphenyl)amino]-7-furyl-3-quinolinecarbonitriles. J Med Chem. 2006 Dec 28;49(26):7868-76.
17 Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
18 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).".
19 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]
20 Cerner Multum, Inc. "Australian Product Information.".
21 Product Information. Synribo (omacetaxine). Teva Pharmaceuticals USA, North Wales, PA.
22 Cerner Multum, Inc. "UK Summary of Product Characteristics.".