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

Type
Biotech
Groups
Approved
Biologic Classification
Protein Based Therapies
Monoclonal antibody (mAb)
Protein Structure
Db00002
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:
  1. 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

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.12

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.12

Cetuximab is not indicated for the treatment of Ras-mutant colorectal cancer or when the results of the Ras mutation tests are unknown.12

Pharmacology
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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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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.13 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.3,12

Cetuximab potentiates the cytotoxic effects of chemotherapeutics and radiation therapy when used in combination.12 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.12 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.13

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.2,12 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.8,12 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 13 and thus be continuously active regardless of EGFR regulation.12 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.12,13 Cetuximab is thus only limited in its use for K-Ras wild-type, EGFR-expressing cancers.12

TargetActionsOrganism
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.12 Tmax is about 3 hours.3

Volume of distribution

The volume of the distribution is about 2-3 L/m2 and is independent of dose.12

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.12

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.11 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.12

Pathways
PathwayCategory
Cetuximab Action PathwayDrug action
Pharmacogenomic Effects/ADRs
Interacting Gene/EnzymeAllele nameGenotype(s)Defining Change(s)Type(s)DescriptionDetails
Low affinity immunoglobulin gamma Fc region receptor II-a---(T;T) / (C;T)H allelleEffect Directly StudiedPatients 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 > TEffect Directly StudiedPatients 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.
DrugInteraction
AbciximabThe risk or severity of adverse effects can be increased when Cetuximab is combined with Abciximab.
AdalimumabThe risk or severity of adverse effects can be increased when Cetuximab is combined with Adalimumab.
AlemtuzumabThe risk or severity of adverse effects can be increased when Cetuximab is combined with Alemtuzumab.
AlirocumabThe risk or severity of adverse effects can be increased when Cetuximab is combined with Alirocumab.
AnsuvimabThe risk or severity of adverse effects can be increased when Cetuximab is combined with Ansuvimab.
Anthrax immune globulin humanThe risk or severity of adverse effects can be increased when Cetuximab is combined with Anthrax immune globulin human.
Antilymphocyte immunoglobulin (horse)The risk or severity of adverse effects can be increased when Cetuximab is combined with Antilymphocyte immunoglobulin (horse).
Antithymocyte immunoglobulin (rabbit)The risk or severity of adverse effects can be increased when Cetuximab is combined with Antithymocyte immunoglobulin (rabbit).
Asfotase alfaThe risk or severity of adverse effects can be increased when Cetuximab is combined with Asfotase alfa.
AtezolizumabThe risk or severity of adverse effects can be increased when Cetuximab is combined with Atezolizumab.
Interactions
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Food Interactions
No interactions found.

Products

Products
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Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
ErbituxSolution2 mg/1mLIntravenousImClone LLC2007-10-02Not applicableUS flag
ErbituxInjection, solutionIntravenousMerck Europe B.V.2016-09-08Not applicableEU flag
ErbituxInjection, solutionIntravenousMerck Europe B.V.2016-09-08Not applicableEU flag
ErbituxSolution2 mg/1mLIntravenousImClone LLC2004-02-12Not applicableUS flag
ErbituxSolution2 mgIntravenousImClone LLC2008-10-28Not applicableCanada flag

Categories

ATC Codes
L01XC06 — Cetuximab
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
Not Available
Kingdom
Organic Compounds
Super Class
Organic Acids
Class
Carboxylic Acids and Derivatives
Sub Class
Amino Acids, Peptides, and Analogues
Direct Parent
Peptides
Alternative Parents
Not Available
Substituents
Not Available
Molecular Framework
Not Available
External Descriptors
Not Available
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
PQX0D8J21J
CAS number
205923-56-4

References

General References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
  2. 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]
  3. 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]
  4. 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]
  5. 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]
  6. 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]
  7. 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]
  8. 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]
  9. 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]
  10. ImClone Systems: Cetuximab Material Safety Data Sheet [Link]
  11. Bristol-Myers Squibb Company: Cetuximab Safety Data Sheet [Link]
  12. FDA Approved Drug Products: ERBITUX (cetuximab) injection, for intravenous use [Link]
  13. StatPearls: Cetuximab [Link]
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
AHFS Codes
  • 10:00.00 — Antineoplastic Agents
FDA label
Download (73.8 KB)
MSDS
Download (84.4 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4TerminatedTreatmentColorectal Cancers / Neoplasms Metastasis1
4TerminatedTreatmentNeoplasms, Head and Neck1
4Unknown StatusTreatmentHead and Neck Carcinoma1
4Unknown StatusTreatmentMetastatic Colorectal Cancer (MCRC)1
4Unknown StatusTreatmentNeoplasms Metastasis / Neoplasms, Colorectal / Neoplasms, Hepatic1
3Active Not RecruitingTreatmentAdenocarcinoma of Lung Stage IV / Recurrent Large Cell Lung Carcinoma / Recurrent Lung Adenocarcinoma / Recurrent Squamous Cell Lung Carcinoma / Stage IV Large Cell Lung Carcinoma / Stage IV Squamous Cell Lung Carcinoma1
3Active Not RecruitingTreatmentBRAF V600E-mutant Metastatic Colorectal Cancer1
3Active Not RecruitingTreatmentCarcinoma, Colorectal1
3Active Not RecruitingTreatmentCarcinoma, Squamous Cell of Head and Neck1
3Active Not RecruitingTreatmentEsophageal Cancers1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Cardinal Health
  • Catalent Pharma Solutions
  • ImClone Systems Inc.
  • Oso Biopharmaceuticals Manufacturing LLC
Dosage Forms
FormRouteStrength
InjectionIntravenous
Injection, solutionIntravenous; Parenteral
SolutionIntravenous2 mg/1mL
SolutionIntravenous2 mg
Solution, concentrateIntravenous100 mg
Injection, solutionIntravenous
SolutionIntravenous
SolutionIntravenous5 mg/1ml
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
CA1340417No1999-03-022016-03-02Canada flag

Properties

State
Liquid
Experimental Properties
PropertyValueSource
melting point (°C)61 °C (FAB fragment), 71 °C (whole mAb)Vermeer, A.W.P. & Norde, W., Biophys. J. 78:394-404 (2000)
hydrophobicity-0.413Not Available
isoelectric point8.48Not Available

Targets

Drugtargets
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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
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
  2. 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]
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
  1. 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]
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
  1. 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]
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
  1. 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]
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
  1. 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]
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
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. 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]
  3. 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]
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
  1. 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]
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
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. 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]
  3. 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 on June 13, 2005 13:24 / Updated on May 10, 2021 04:39