Cetuximab

Identification

Summary

Cetuximab is an endothelial growth factor receptor binding fragment used to treat colorectal cancer as well as squamous cell carcinoma of the head and neck.

Brand Names

Erbitux

Generic Name

Cetuximab

DrugBank Accession Number

DB00002

Background

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).⁴ 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.⁹ EGFR has been implicated in various types of cancer, as it is often overexpressed in malignant cells ⁴ and EGFR overexpression has been linked to more advanced disease and poor prognosis.³ EGFR is often mutated in certain types of cancer and serves as a driver of tumorigenesis.⁹ In vitro, cetuximab was shown to mediate anti-tumour effects in numerous cancer cell lines and human tumour xenografts.³

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.^3,13 It has also been investigated in advanced colorectal cancer, EGFR-expressing non-small cell lung cancer (NSCLC), and unresectable squamous cell skin cancer.¹² 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.¹¹

Type

Biotech

Groups

Approved

Biologic Classification

Protein Based Therapies
Monoclonal antibody (mAb)

Protein Structure

Protein Chemical Formula: C₆₄₈₄H₁₀₀₄₂N₁₇₃₂O₂₀₂₃S₃₆
Protein Average Weight: 145781.6 Da

Sequences

>Cetuximab heavy chain
QVQLKQSGPGLVQPSQSLSITCTVSGFSLTNYGVHWVRQSPGKGLEWLGVIWSGGNTDYN
TPFTSRLSINKDNSKSQVFFKMNSLQSNDTAIYYCARALTYYDYEFAYWGQGTLVTVSAA
STKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSG
LYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKVEPKSCDKTHTCPPCPAPELLGGP
SVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNS
TYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDEL
TKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQ
QGNVFSCSVMHEALHNHYTQKSLSLSPGK

>Cetuximab light chain
DILLTQSPVILSVSPGERVSFSCRASQSIGTNIHWYQQRTNGSPRLLIKYASESISGIPS
RFSGSGSGTDFTLSINSVESEDIADYYCQQNNNWPTTFGAGTKLELKRTVAAPSVFIFPP
SDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTLT
LSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC

References:

Therapeutic Targets Database: TTD Biologic drug sequences in fasta format [Link]

Download FASTA Format

Synonyms

Cetuximab
Cétuximab
Cetuximabum

External IDs

ABP-494
BMS 564717
C-225
C225
CMAB-009
CMAB009
IMC-225
IMC-C225
MOAB C225

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Pharmacology

Indication

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.¹¹

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.¹¹

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.¹³

Cetuximab is not indicated for the treatment of Ras-mutant colorectal cancer or when the results of the Ras mutation tests are unknown.¹¹

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Associated Conditions

Indication Type	Indication	Combined Product Details	Approval Level	Patient Characteristics	Dose Form
Treatment of	Locally advanced squamous cell carcinomas of the head and neck (scchn)		••••••••••••	••••••••• •••••••	•••••••••
Used in combination to treat	Metastatic colorectal cancer	Regimen in combination with: Irinotecan (DB00762)	••••••••••••	••••••••• •••••••••• •• •• •••••••••••• ••••• •••••••••• •• •••••••••••••••• ••••••••••••	•••••••••
Used in combination to treat	Metastatic colorectal cancer	Regimen in combination with: Leucovorin (DB00650), Irinotecan (DB00762), Fluorouracil (DB00544)	••••••••••••	••••••••• •••••••••• •• •• •••••••••••• ••••	•••••••••
Treatment of	Metastatic colorectal cancer		••••••••••••	••••••••••• •• ••••••••••• ••••••••• •••••••••• •• •• •••••••••••• ••••	•••••••••
Treatment of	Metastatic colorectal cancer		••••••••••••	•••••••••• •••••••• •• •••••••••••• ••• •••••••••••••••• ••••••••••••• ••••••••• •••••••••• •• •• •••••••••••• ••••	•••••••••

Contraindications & Blackbox Warnings

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Pharmacodynamics

Cetuximab is an anticancer agent that works by inhibiting the growth and survival of epidermal growth factor receptor (EGFR)-expressing tumour cells with high specificity and higher affinity than epidermal growth factor (EGF) and transforming growth factor-alpha (TGF-α), which are natural ligands of EGFR.¹² Cetuximab works by inhibiting the growth and survival of EGFR-positive tumours.³ In vitro, it promotes antibody-dependent cellular cytotoxicity (ADCC) against certain human tumour types. On the contrary, cetuximab does not exert its anti-tumour effects on human tumour xenografts lacking EGFR expression.^3,11

Cetuximab potentiates the cytotoxic effects of chemotherapeutics and radiation therapy when used in combination.¹¹ In human tumour xenograft models in mice, cetuximab and irinotecan synergistically inhibited the growth of orthotopic anaplastic thyroid carcinoma xenografts in vitro and in vivo. Cetuximab potentiated the in vitro anti-proliferative and pro-apoptotic effect of irinotecan and achieved 93% in vivo inhibition of tumour growth when combined with irinotecan, compared to 77% and 79% inhibition when cetuximab and irinotecan were used alone, respectively.⁵

Mechanism of action

The epidermal growth factor receptor (EGFR) is a transmembrane glycoprotein and a type I receptor tyrosine kinase expressed on both normal and malignant cells. It has been investigated as a therapeutic target for anticancer treatment, as it is often upregulated in cancer types, including head and neck, colon, and rectal cancers.¹¹ When activated by its ligand, EGFR undergoes a conformational change and dimerization to form homodimers or heterodimers with another member of the ErbB family of receptors. Dimerization of EGFR activates the intracellular tyrosine kinase region of EGFR and promotes autophosphorylation, initiating a series of downstream signalling cascades, including cell differentiation, proliferation, migration, angiogenesis, and apoptosis. This EGFR signalling pathway is often dysregulated in cancer cells, leading to aberrant cell growth and enhanced cell survival.¹²

Cetuximab is a monoclonal antibody that binds specifically to the EGFR on both normal and tumour cells to competitively inhibit the binding of epidermal growth factor (EGF) and other ligands that are produced by normal and tumour tissue epithelial cells.^2,11 Upon binding to domain III of EGFR - which is the binding site for its growth factor ligands - cetuximab prevents the receptor from adopting an extended conformation and thereby inhibits EGFR activation, as well as phosphorylation and activation of receptor-associated kinases (MAPK, PI3K/Akt, Jak/Stat).^2,8 Inhibition of the EGFR signalling pathway ultimately leads to inhibition of cell cycle progression, cell survival pathways, and tumour cell motility and invasion.³ Cetuximab also induces cell apoptosis and decreases matrix metalloproteinase and vascular endothelial growth factor (VEGF) production.^8,11 In vitro, cetuximab was shown to inhibit tumour angiogenesis.⁵ Binding of cetuximab to EGFR also results in internalization of the antibody-receptor complex, leading to an overall downregulation of EGFR expression.⁴

K-ras is a small G-protein downstream of EGFR that plays an important role in promoting the EGFR signalling cascade: in some malignant cells, K-ras can acquire activating mutations in exon 2 ¹² and thus be continuously active regardless of EGFR regulation.¹¹ Since mutant Ras proteins can isolate the pathway from the effect of EGFR, K-Ras mutations can render EGFR inhibitors like cetuximab ineffective in exerting anti-tumour effects.^11,12 Cetuximab is thus only limited in its use for K-Ras wild-type, EGFR-expressing cancers.¹¹

Target	Actions	Organism
AEpidermal growth factor receptor	binder	Humans
ULow affinity immunoglobulin gamma Fc region receptor III-B	binder	Humans
UComplement C1q subcomponent subunit A	binder	Humans
UComplement C1q subcomponent subunit B	binder	Humans
UComplement C1q subcomponent subunit C	binder	Humans
ULow affinity immunoglobulin gamma Fc region receptor III-A	binder	Humans
UHigh affinity immunoglobulin gamma Fc receptor I	binder	Humans
ULow affinity immunoglobulin gamma Fc region receptor II-a	binder	Humans

Absorption

After administration of a 400 mg/m² initial dose followed by a 250 mg/m² weekly dose, the steady-state levels of cetuximab was reached by the third weekly infusion with mean peak and trough concentrations across studies ranging from 168 µg/mL to 235 µg/mL and 41 µg/mL to 85 µg/mL, respectively.¹¹ T_max is about 3 hours.³

Volume of distribution

The volume of the distribution is about 2-3 L/m² and is independent of dose.¹¹

Protein binding

There is no information available.

Metabolism

Like other monoclonal antibodies, cetuximab is expected to undergo lysosomal degradation by the reticuloendothelial system and protein catabolism by a target‐mediated disposition pathway.⁶

Route of elimination

There is limited information available.

Half-life

After administration of a 400 mg/m² initial dose followed by a 250 mg/m² weekly dose, the mean half-life for cetuximab was approximately 112 hours, with a range of 63 to 230 hours.¹¹

Clearance

In patients with recurrent and/or metastatic squamous cell carcinoma of the head and neck, the estimated clearance rate was 0.103 L/h.⁷ At doses ranging from 200 to 400 mg/m², complete saturation of systemic clearance was observed. In a population pharmacokinetic study, female patients had a 25% lower intrinsic cetuximab clearance than male patients, although there was no evidence of the need for dose modification based on sex.³

Adverse Effects

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Toxicity

The intravenous LD₅₀ is > 300 mg/kg in mice and > 200 mg/kg in rats.¹⁰ There is limited information on the overdose from cetuximab.

In clinical trials, cetuximab was associated with serious and fatal infusion reactions, cardiopulmonary arrest or sudden death, and serious dermatologic toxicities. Pulmonary toxicities, such as interstitial lung disease, interstitial pneumonitis with non-cardiogenic pulmonary edema, and exacerbation of pre-existing fibrotic lung disease have been reported.¹¹

Pathways

Pathway	Category
Cetuximab Action Pathway	Drug action

Pharmacogenomic Effects/ADRs

Interacting Gene/Enzyme	Allele name	Genotype(s)	Defining Change(s)	Type(s)	Description	Details
Low affinity immunoglobulin gamma Fc region receptor II-a	---	(T;T) / (C;T)	H allelle	Effect Directly Studied	Patients with this genotype may have increased progression-free survival time when using cetuximab to treat colorectal cancer.	Details
Low affinity immunoglobulin gamma Fc region receptor III-A	---	(T;T) / (G;T)	G > T	Effect Directly Studied	Patients with this genotype have increased progression-free survival time when using cetuximab to treat colorectal cancer.	Details

Interactions

Drug Interactions

This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.

Drug	Interaction
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Abciximab	The risk or severity of adverse effects can be increased when Cetuximab is combined with Abciximab.
Adalimumab	The risk or severity of adverse effects can be increased when Cetuximab is combined with Adalimumab.
Aducanumab	The risk or severity of adverse effects can be increased when Cetuximab is combined with Aducanumab.
Alemtuzumab	The risk or severity of adverse effects can be increased when Cetuximab is combined with Alemtuzumab.
Alirocumab	The risk or severity of adverse effects can be increased when Cetuximab is combined with Alirocumab.

Food Interactions

No interactions found.

Products

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Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Erbitux	Solution	2 mg / mL	Intravenous	Imclone, Llc	2008-10-28	Not applicable
Erbitux	Injection, solution	5 mg/ml	Intravenous	Merck Europe B.V.	2016-09-08	Not applicable
Erbitux	Solution	2 mg/1mL	Intravenous	ImClone LLC	2007-10-02	Not applicable
Erbitux	Injection, solution	5 mg/ml	Intravenous	Merck Europe B.V.	2016-09-08	Not applicable
Erbitux	Solution	2 mg/1mL	Intravenous	ImClone LLC	2004-02-12	Not applicable

Chemical Identifiers

UNII: PQX0D8J21J
CAS number: 205923-56-4

References

General References

Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
Snyder LC, Astsaturov I, Weiner LM: Overview of monoclonal antibodies and small molecules targeting the epidermal growth factor receptor pathway in colorectal cancer. Clin Colorectal Cancer. 2005 Nov;5 Suppl 2:S71-80. [Article]
Wong SF: Cetuximab: an epidermal growth factor receptor monoclonal antibody for the treatment of colorectal cancer. Clin Ther. 2005 Jun;27(6):684-94. doi: 10.1016/j.clinthera.2005.06.003. [Article]
Harding J, Burtness B: Cetuximab: an epidermal growth factor receptor chemeric human-murine monoclonal antibody. Drugs Today (Barc). 2005 Feb;41(2):107-27. doi: 10.1358/dot.2005.41.2.882662. [Article]
Kim S, Prichard CN, Younes MN, Yazici YD, Jasser SA, Bekele BN, Myers JN: Cetuximab and irinotecan interact synergistically to inhibit the growth of orthotopic anaplastic thyroid carcinoma xenografts in nude mice. Clin Cancer Res. 2006 Jan 15;12(2):600-7. doi: 10.1158/1078-0432.CCR-05-1325. [Article]
Ryman JT, Meibohm B: Pharmacokinetics of Monoclonal Antibodies. CPT Pharmacometrics Syst Pharmacol. 2017 Sep;6(9):576-588. doi: 10.1002/psp4.12224. Epub 2017 Jul 29. [Article]
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. [Article]
Vincenzi B, Zoccoli A, Pantano F, Venditti O, Galluzzo S: Cetuximab: from bench to bedside. Curr Cancer Drug Targets. 2010 Feb;10(1):80-95. doi: 10.2174/156800910790980241. [Article]
Sigismund S, Avanzato D, Lanzetti L: Emerging functions of the EGFR in cancer. Mol Oncol. 2018 Jan;12(1):3-20. doi: 10.1002/1878-0261.12155. Epub 2017 Nov 27. [Article]
Bristol-Myers Squibb Company: Cetuximab Safety Data Sheet [Link]
FDA Approved Drug Products: ERBITUX (cetuximab) injection, for intravenous use [Link]
StatPearls: Cetuximab [Link]
FDA Approved Drug Products: ERBITUX (cetuximab) injection, for intravenous use [Link]

External Links

Genbank: J00228
KEGG Drug: D03455
PubChem Substance: 46507042
RxNav: 318341
ChEMBL: CHEMBL1201577
Therapeutic Targets Database: DNC000788
PharmGKB: PA10040
RxList: RxList Drug Page
Drugs.com: Drugs.com Drug Page
Wikipedia: Cetuximab

FDA label

Download (73.8 KB)

MSDS

Download (84.4 KB)

Clinical Trials

Clinical Trials

Phase	Status	Purpose	Conditions	Count
4	Completed	Treatment	Head And Neck Cancer	1
4	Recruiting	Treatment	Solid Tumors	1
4	Terminated	Treatment	Colorectal Cancer / Metastatic Cancer	1
4	Terminated	Treatment	Head and Neck Neoplasms	1
4	Unknown Status	Treatment	Colorectal Neoplasms / Metastatic Cancer / Neoplasms, Hepatic	1

Pharmacoeconomics

Manufacturers

Not Available

Packagers

Cardinal Health
Catalent Pharma Solutions
ImClone Systems Inc.
Oso Biopharmaceuticals Manufacturing LLC

Dosage Forms

Form	Route	Strength
Injection	Intravenous
Injection, solution	Intravenous	5 mg/ml
Injection, solution	Intravenous; Parenteral	5 MG/ML
Solution	Intravenous	2 mg/1mL
Solution	Intravenous	2 mg / mL
Solution	Intravenous	5.000 mg
Solution	Intravenous	5 mg
Injection, solution	Intravenous	100 mg/20ml
Injection, solution	Intravenous	500 mg/100ml
Solution	Intravenous	5 mg/ml
Solution	Intravenous
Solution	Intravenous	5 mg/1ml

Prices

Not Available

Patents

Patent Number	Pediatric Extension	Approved	Expires (estimated)	Region
CA1340417	No	1999-03-02	2016-03-02

Properties

State

Liquid

Experimental Properties

Property	Value	Source
melting point (°C)	61 °C (FAB fragment), 71 °C (whole mAb)	Vermeer, A.W.P. & Norde, W., Biophys. J. 78:394-404 (2000)
hydrophobicity	-0.413	Not Available
isoelectric point	8.48	Not Available

Targets

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insights and accelerate drug research.

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Details1. Epidermal growth factor receptor

Kind: Protein
Organism: Humans
Pharmacological action: Yes
Actions: Binder

General Function: Ubiquitin protein ligase binding
Specific Function: Receptor tyrosine kinase binding ligands of the EGF family and activating several signaling cascades to convert extracellular cues into appropriate cellular responses. Known ligands include EGF, TG...
Gene Name: EGFR
Uniprot ID: P00533
Uniprot Name: Epidermal growth factor receptor
Molecular Weight: 134276.185 Da

References

Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
Harding J, Burtness B: Cetuximab: an epidermal growth factor receptor chemeric human-murine monoclonal antibody. Drugs Today (Barc). 2005 Feb;41(2):107-27. doi: 10.1358/dot.2005.41.2.882662. [Article]

Details2. Low affinity immunoglobulin gamma Fc region receptor III-B

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Binder

General Function: Not Available
Specific Function: Receptor for the Fc region of immunoglobulins gamma. Low affinity receptor. Binds complexed or aggregated IgG and also monomeric IgG. Contrary to III-A, is not capable to mediate antibody-dependent...
Gene Name: FCGR3B
Uniprot ID: O75015
Uniprot Name: Low affinity immunoglobulin gamma Fc region receptor III-B
Molecular Weight: 26215.64 Da

References

Snyder LC, Astsaturov I, Weiner LM: Overview of monoclonal antibodies and small molecules targeting the epidermal growth factor receptor pathway in colorectal cancer. Clin Colorectal Cancer. 2005 Nov;5 Suppl 2:S71-80. [Article]

Details3. Complement C1q subcomponent subunit A

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Binder

General Function: Not Available
Specific Function: C1q associates with the proenzymes C1r and C1s to yield C1, the first component of the serum complement system. The collagen-like regions of C1q interact with the Ca(2+)-dependent C1r(2)C1s(2) proe...
Gene Name: C1QA
Uniprot ID: P02745
Uniprot Name: Complement C1q subcomponent subunit A
Molecular Weight: 26016.47 Da

References

Deveuve Q, Lajoie L, Barrault B, Thibault G: The Proteolytic Cleavage of Therapeutic Monoclonal Antibody Hinge Region: More Than a Matter of Subclass. Front Immunol. 2020 Feb 11;11:168. doi: 10.3389/fimmu.2020.00168. eCollection 2020. [Article]

Details4. Complement C1q subcomponent subunit B

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Binder

General Function: Not Available
Specific Function: C1q associates with the proenzymes C1r and C1s to yield C1, the first component of the serum complement system. The collagen-like regions of C1q interact with the Ca(2+)-dependent C1r(2)C1s(2) proe...
Gene Name: C1QB
Uniprot ID: P02746
Uniprot Name: Complement C1q subcomponent subunit B
Molecular Weight: 26721.62 Da

References

Deveuve Q, Lajoie L, Barrault B, Thibault G: The Proteolytic Cleavage of Therapeutic Monoclonal Antibody Hinge Region: More Than a Matter of Subclass. Front Immunol. 2020 Feb 11;11:168. doi: 10.3389/fimmu.2020.00168. eCollection 2020. [Article]

Details5. Complement C1q subcomponent subunit C

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Binder

General Function: Not Available
Specific Function: C1q associates with the proenzymes C1r and C1s to yield C1, the first component of the serum complement system. The collagen-like regions of C1q interact with the Ca(2+)-dependent C1r(2)C1s(2) proe...
Gene Name: C1QC
Uniprot ID: P02747
Uniprot Name: Complement C1q subcomponent subunit C
Molecular Weight: 25773.56 Da

References

Deveuve Q, Lajoie L, Barrault B, Thibault G: The Proteolytic Cleavage of Therapeutic Monoclonal Antibody Hinge Region: More Than a Matter of Subclass. Front Immunol. 2020 Feb 11;11:168. doi: 10.3389/fimmu.2020.00168. eCollection 2020. [Article]

Details6. Low affinity immunoglobulin gamma Fc region receptor III-A

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Binder

General Function: Not Available
Specific Function: Receptor for the Fc region of IgG. Binds complexed or aggregated IgG and also monomeric IgG. Mediates antibody-dependent cellular cytotoxicity (ADCC) and other antibody-dependent responses, such as...
Gene Name: FCGR3A
Uniprot ID: P08637
Uniprot Name: Low affinity immunoglobulin gamma Fc region receptor III-A
Molecular Weight: 29088.895 Da

References

Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
Zhang W, Gordon M, Schultheis AM, Yang DY, Nagashima F, Azuma M, Chang HM, Borucka E, Lurje G, Sherrod AE, Iqbal S, Groshen S, Lenz HJ: 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. [Article]

Details7. High affinity immunoglobulin gamma Fc receptor I

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Binder

General Function: Receptor signaling protein activity
Specific Function: High affinity receptor for the Fc region of immunoglobulins gamma. Functions in both innate and adaptive immune responses.
Gene Name: FCGR1A
Uniprot ID: P12314
Uniprot Name: High affinity immunoglobulin gamma Fc receptor I
Molecular Weight: 42631.525 Da

References

Negri DR, Tosi E, Valota O, Ferrini S, Cambiaggi A, Sforzini S, Silvani A, Ruffini PA, Colnaghi MI, Canevari S: In vitro and in vivo stability and anti-tumour efficacy of an anti-EGFR/anti-CD3 F(ab')2 bispecific monoclonal antibody. Br J Cancer. 1995 Oct;72(4):928-33. [Article]

Details8. Low affinity immunoglobulin gamma Fc region receptor II-a

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Binder

General Function: Not Available
Specific Function: Binds to the Fc region of immunoglobulins gamma. Low affinity receptor. By binding to IgG it initiates cellular responses against pathogens and soluble antigens. Promotes phagocytosis of opsonized ...
Gene Name: FCGR2A
Uniprot ID: P12318
Uniprot Name: Low affinity immunoglobulin gamma Fc region receptor II-a
Molecular Weight: 35000.42 Da

References

Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
Zhang W, Gordon M, Schultheis AM, Yang DY, Nagashima F, Azuma M, Chang HM, Borucka E, Lurje G, Sherrod AE, Iqbal S, Groshen S, Lenz HJ: 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. [Article]

Drug created at June 13, 2005 13:24 / Updated at January 02, 2024 23:41

Cetuximab

Identification

References:

Pharmacology

Interactions

Products

Categories

Chemical Identifiers

References

Clinical Trials

Pharmacoeconomics

Properties

Targets

References

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