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Identification
NameCetuximab
Accession NumberDB00002  (BTD00071, BIOD00071)
TypeBiotech
GroupsApproved
DescriptionCetuximab is an epidermal growth factor receptor binding FAB. Cetuximab is composed of the Fv (variable; antigen-binding) regions of the 225 murine EGFr monoclonal antibody specific for the N-terminal portion of human EGFr with human IgG1 heavy and kappa light chain constant (framework) regions. Cetuximab is marketed under the brand Erbitux® by Eli Lilly and Company. In the United States, a regimen of cetuximab costs approximately $30,790 for an eight-week course.
Protein structureDb00002
Related Articles
Protein chemical formulaC6484H10042N1732O2023S36
Protein average weight145781.6 Da
Sequences
>Cetuximab heavy chain
QVQLKQSGPGLVQPSQSLSITCTVSGFSLTNYGVHWVRQSPGKGLEWLGVIWSGGNTDYN
TPFTSRLSINKDNSKSQVFFKMNSLQSNDTAIYYCARALTYYDYEFAYWGQGTLVTVSAA
STKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSG
LYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKVEPKSCDKTHTCPPCPAPELLGGP
SVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNS
TYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDEL
TKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQ
QGNVFSCSVMHEALHNHYTQKSLSLSPGK
>Cetuximab light chain
DILLTQSPVILSVSPGERVSFSCRASQSIGTNIHWYQQRTNGSPRLLIKYASESISGIPS
RFSGSGSGTDFTLSINSVESEDIADYYCQQNNNWPTTFGAGTKLELKRTVAAPSVFIFPP
SDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTLT
LSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC
Download FASTA Format
Synonyms
Cetuximab
Cétuximab
Cetuximabum
Immunoglobulin G 1 (human-mouse monoclonal C 225 gamma 1 - chain anti-human epidermal growt factor receptor), disulfide wit human-mouse monoclonal C 225 kappa - chain, dimer
External Identifiers
  • BMS 564717
  • C225
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
ErbituxSolution2 mgIntravenousIm Clone Llc2008-10-28Not applicableCanada
ErbituxSolution2 mg/mLIntravenousIm Clone Llc2007-10-02Not applicableUs
ErbituxInjection, solution5 mg/mlIntravenousMerck K Ga A2004-06-29Not applicableEu
ErbituxInjection, solution5 mg/mlIntravenousMerck K Ga A2004-06-29Not applicableEu
ErbituxSolution2 mg/mLIntravenousIm Clone Llc2004-02-12Not applicableUs
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIPQX0D8J21J
CAS number205923-56-4
Pharmacology
IndicationCetuximab, 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 colorectal carcinoma in patients who are intolerant to irinotecan-based chemotherapy.
Structured Indications Not Available
PharmacodynamicsUsed in the treatment of colorectal cancer, cetuximab binds specifically to the epidermal growth factor receptor (EGFr, HER1, c-ErbB-1) 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 other ligands, such as transforming growth factor–alpha. Binding of cetuximab to the EGFr blocks phosphorylation and activation of receptor-associated kinases, resulting in inhibition of cell growth, induction of apoptosis, decreased matrix metalloproteinase secretion and reduced vascular endothelial growth factor production.
Mechanism of actionCetuximab 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.
TargetKindPharmacological actionActionsOrganismUniProt ID
Epidermal growth factor receptorProteinyes
antagonist
HumanP00533 details
Low affinity immunoglobulin gamma Fc region receptor III-BProteinunknownNot AvailableHumanO75015 details
Complement C1r subcomponentProteinunknownNot AvailableHumanP00736 details
Complement C1q subcomponent subunit AProteinunknownNot AvailableHumanP02745 details
Complement C1q subcomponent subunit BProteinunknownNot AvailableHumanP02746 details
Complement C1q subcomponent subunit CProteinunknownNot AvailableHumanP02747 details
Low affinity immunoglobulin gamma Fc region receptor III-AProteinunknownNot AvailableHumanP08637 details
Complement C1s subcomponentProteinunknownNot AvailableHumanP09871 details
High affinity immunoglobulin gamma Fc receptor IProteinunknownNot AvailableHumanP12314 details
Low affinity immunoglobulin gamma Fc region receptor II-aProteinunknownNot AvailableHumanP12318 details
Low affinity immunoglobulin gamma Fc region receptor II-bProteinunknownNot AvailableHumanP31994 details
Low affinity immunoglobulin gamma Fc region receptor II-cProteinunknownNot AvailableHumanP31995 details
Related Articles
AbsorptionNot Available
Volume of distribution

appeared to be independent of dose and approximated the vascular space of 2-3 L/m2.

Protein bindingNot Available
MetabolismNot Available
Route of eliminationNot Available
Half lifeThe mean half-life for Cetuximab is 114 hours (range 75-188 hours).
Clearance

Female patients had 25% lower intrinsic clearance than male patients.

ToxicityPulmonary Toxicity Interstitial lung disease (ILD) was reported in 3 of 633 (<0.5%) patients with advanced colorectal cancer receiving cetuximab. Interstitial pneumonitis with non-cardiogenic pulmonary edema resulting in death was reported in one case. Two patients had pre-existing fibrotic lung disease and experienced an acute exacerbation of their disease while receiving cetuximab in combination with irinotecan. In the clinical investigational program, an additional case of interstitial pneumonitis was reported in a patient with head and neck cancer treated with cetuximab and cisplatin. The onset of symptoms occurred between the fourth and eleventh doses of treatment in all reported cases.
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Cetuximab Action PathwayDrug actionSMP00474
SNP Mediated Effects
Interacting Gene/EnzymeSNP RS IDAllele nameDefining changeEffectReference(s)
Low affinity immunoglobulin gamma Fc region receptor II-a
Gene symbol: FCGR2A
UniProt: P12318
rs1801274 Not AvailableH allelleIncreased progression free survival17704420
Low affinity immunoglobulin gamma Fc region receptor III-A
Gene symbol: FCGR3A
UniProt: P08637
rs396991 Not AvailableA > CBetter response to drug therapy (longer progression free survival) with the F allele17704420
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Cetuximab.Approved
ALT-110The therapeutic efficacy of ALT-110 can be decreased when used in combination with Cetuximab.Investigational
AnvirzelAnvirzel may decrease the cardiotoxic activities of Cetuximab.Investigational
BelimumabThe risk or severity of adverse effects can be increased when Cetuximab is combined with Belimumab.Approved
BevacizumabBevacizumab may increase the cardiotoxic activities of Cetuximab.Approved, Investigational
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with Cetuximab.Approved
CDX-110The therapeutic efficacy of CDX-110 can be decreased when used in combination with Cetuximab.Investigational
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Cetuximab.Approved, Investigational
DeslanosideDeslanoside may decrease the cardiotoxic activities of Cetuximab.Approved
DigitoxinDigitoxin may decrease the cardiotoxic activities of Cetuximab.Approved
DigoxinDigoxin may decrease the cardiotoxic activities of Cetuximab.Approved
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Cetuximab.Approved, Investigational
G17DTThe therapeutic efficacy of G17DT can be decreased when used in combination with Cetuximab.Investigational
GI-5005The therapeutic efficacy of GI-5005 can be decreased when used in combination with Cetuximab.Investigational
INGN 201The therapeutic efficacy of INGN 201 can be decreased when used in combination with Cetuximab.Investigational
INGN 225The therapeutic efficacy of INGN 225 can be decreased when used in combination with Cetuximab.Investigational
OuabainOuabain may decrease the cardiotoxic activities of Cetuximab.Approved
PaclitaxelThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Cetuximab.Approved, Vet Approved
Rabies vaccineThe therapeutic efficacy of Rabies vaccine can be decreased when used in combination with Cetuximab.Approved
SRP 299The therapeutic efficacy of SRP 299 can be decreased when used in combination with Cetuximab.Investigational
TG4010The therapeutic efficacy of TG4010 can be decreased when used in combination with Cetuximab.Investigational
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Cetuximab.Approved, Investigational
Food InteractionsNot Available
References
Synthesis ReferenceNot Available
General References
  1. Hosokawa N, Yamamoto S, Uehara Y, Hori M, Tsuchiya KS: Effect of thiazinotrienomycin B, an ansamycin antibiotic, on the function of epidermal growth factor receptor in human stomach tumor cells. J Antibiot (Tokyo). 1999 May;52(5):485-90. [PubMed:10480573 ]
  2. Wakita H, Takigawa M: Activation of epidermal growth factor receptor promotes late terminal differentiation of cell-matrix interaction-disrupted keratinocytes. J Biol Chem. 1999 Dec 24;274(52):37285-91. [PubMed:10601294 ]
  3. Suwa T, Ueda M, Jinno H, Ozawa S, Kitagawa Y, Ando N, Kitajima M: Epidermal growth factor receptor-dependent cytotoxic effect of anti-EGFR antibody-ribonuclease conjugate on human cancer cells. Anticancer Res. 1999 Sep-Oct;19(5B):4161-5. [PubMed:10628369 ]
  4. Burke P, Schooler K, Wiley HS: Regulation of epidermal growth factor receptor signaling by endocytosis and intracellular trafficking. Mol Biol Cell. 2001 Jun;12(6):1897-910. [PubMed:11408594 ]
  5. Viloria-Petit A, Crombet T, Jothy S, Hicklin D, Bohlen P, Schlaeppi JM, Rak J, Kerbel RS: Acquired resistance to the antitumor effect of epidermal growth factor receptor-blocking antibodies in vivo: a role for altered tumor angiogenesis. Cancer Res. 2001 Jul 1;61(13):5090-101. [PubMed:11431346 ]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  7. Schrag D: The price tag on progress--chemotherapy for colorectal cancer. N Engl J Med. 2004 Jul 22;351(4):317-9. [PubMed:15269308 ]
  8. 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. [PubMed:16336752 ]
External Links
ATC CodesL01XC06
AHFS CodesNot Available
PDB Entries
FDA labelDownload (73.8 KB)
MSDSDownload (84.4 KB)
Clinical Trials
Clinical Trials
PhaseStatusPurposeConditionsCount
1Active Not RecruitingTreatmentANAPLASTIC ASTROCYTOMA (AOA) / Glioblastoma Multiforme (GBM)1
1Active Not RecruitingTreatmentAdvanced Solid Tumors1
1Active Not RecruitingTreatmentCancer, Advanced1
1Active Not RecruitingTreatmentColorectal Cancers1
1Active Not RecruitingTreatmentLocally Advanced Cancer in the Anal Region1
1Active Not RecruitingTreatmentNeoplasms2
1Active Not RecruitingTreatmentSquamous Cell Carcinoma of the Head and Neck (SCCHN)1
1CompletedDiagnosticCancers / Refractory Solid Tumors1
1CompletedTreatmentAdenocarcinoma of the Colon / Adenocarcinoma of the Rectum / Advanced Adult Primary Liver Cancer / Carcinoma of the Appendix / Gastrointestinal Stromal Tumors / Metastatic Gastrointestinal Carcinoid Tumor / Metastatic Squamous Neck Cancer With Occult Primary / Recurrent Adenoid Cystic Carcinoma of the Oral Cavity / Recurrent Adult Primary Liver Cancer / Recurrent Anal Cancer / Recurrent Basal Cell Carcinoma of the Lip / Recurrent Colon Cancer / Recurrent Esophageal Cancer / Recurrent Esthesioneuroblastoma of the Paranasal Sinus and Nasal Cavity / Recurrent Extrahepatic Bile Duct Cancer / Recurrent Gallbladder Cancer / Recurrent Gastric Cancer / Recurrent Gastrointestinal Carcinoid Tumor / Recurrent Inverted Papilloma of the Paranasal Sinus and Nasal Cavity / Recurrent Lymphoepithelioma of the Nasopharynx / Recurrent Lymphoepithelioma of the Oropharynx / Recurrent Metastatic Squamous Neck Cancer With Occult Primary / Recurrent Midline Lethal Granuloma of the Paranasal Sinus and Nasal Cavity / Recurrent Mucoepidermoid Carcinoma of the Oral Cavity / Recurrent Non-small Cell Lung Cancer / Recurrent Pancreatic Cancer / Recurrent Rectal Cancer / Recurrent Salivary Gland Cancer / Recurrent Small Intestine Cancer / Recurrent Squamous Cell Carcinoma of the Hypopharynx / Recurrent Squamous Cell Carcinoma of the Larynx / Recurrent Squamous Cell Carcinoma of the Lip and Oral Cavity / Recurrent Squamous Cell Carcinoma of the Nasopharynx / Recurrent Squamous Cell Carcinoma of the Oropharynx / Recurrent Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity / Recurrent Verrucous Carcinoma of the Larynx / Recurrent Verrucous Carcinoma of the Oral Cavity / Small Intestine Adenocarcinoma / Small Intestine Leiomyosarcoma / Small Intestine Lymphoma / Stage IV Adenoid Cystic Carcinoma of the Oral Cavity / Stage IV Anal Cancer / Stage IV Basal Cell Carcinoma of the Lip / Stage IV Colon Cancer / Stage IV Esophageal Cancer / Stage IV Esthesioneuroblastoma of the Paranasal Sinus and Nasal Cavity / Stage IV Gastric Cancer / Stage IV Inverted Papilloma of the Paranasal Sinus and Nasal Cavity / Stage IV Lymphoepithelioma of the Nasopharynx / Stage IV Lymphoepithelioma of the Oropharynx / Stage IV Midline Lethal Granuloma of the Paranasal Sinus and Nasal Cavity / Stage IV Mucoepidermoid Carcinoma of the Oral Cavity / Stage IV Non-Small Cell Lung Cancer / Stage IV Pancreatic Cancer / Stage IV Rectal Cancer / Stage IV Salivary Gland Cancer / Stage IV Squamous Cell Carcinoma of the Hypopharynx / Stage IV Squamous Cell Carcinoma of the Larynx / Stage IV Squamous Cell Carcinoma of the Lip and Oral Cavity / Stage IV Squamous Cell Carcinoma of the Nasopharynx / Stage IV Squamous Cell Carcinoma of the Oropharynx / Stage IV Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity / Stage IV Verrucous Carcinoma of the Larynx / Stage IV Verrucous Carcinoma of the Oral Cavity / Tongue Cancer / Unresectable Extrahepatic Bile Duct Cancer / Unresectable Gallbladder Cancer1
1CompletedTreatmentAdenocarcinoma of the Colon / Adenocarcinoma of the Rectum / Recurrent Colon Cancer / Recurrent Rectal Cancer / Stage IV Colon Cancer / Stage IV Rectal Cancer1
1CompletedTreatmentAdvanced Cancers2
1CompletedTreatmentCancer of the Colon / Colon Cancer / Colon Neoplasms / Colonic Cancers / Colonic Neoplasms1
1CompletedTreatmentCancer, Advanced1
1CompletedTreatmentCancer, Advanced / Liver Cancer1
1CompletedTreatmentCancers1
1CompletedTreatmentCarcinoma, Colorectal / Colorectal Cancers / Colorectal Tumors / Neoplasms, Colorectal1
1CompletedTreatmentColorectal Adenocarcinoma / Colorectal Cancers1
1CompletedTreatmentColorectal Cancers5
1CompletedTreatmentColorectal Cancers / Head and Neck Cancers / Lung Cancers1
1CompletedTreatmentColorectal Cancers / Non-Small-Cell Lung Carcinoma (NSCLC) / Other Tumors With EGFR Dependence / Squamous Cell Head and Neck Cancer / Triple Negative Breast Cancer (TNBC)1
1CompletedTreatmentHead and Neck Cancers3
1CompletedTreatmentHead and Neck Cancers / Laryngeal Cancer / Oral Cancers / Pharyngeal Cancer / Squamous Carcinoma1
1CompletedTreatmentMalignant Solid Tumours1
1CompletedTreatmentMetastatic Colorectal Cancers1
1CompletedTreatmentNeoplasms1
1CompletedTreatmentNeoplasms Metastasis / Non-Small-Cell Lung Carcinoma (NSCLC)1
1CompletedTreatmentNeoplasms, Head and Neck1
1CompletedTreatmentNon-Small-Cell Lung Carcinoma (NSCLC)3
1CompletedTreatmentRecurrent Colon Cancer / Recurrent Rectal Cancer / Stage III Colon Cancer / Stage III Rectal Cancer / Stage IV Colon Cancer / Stage IV Rectal Cancer1
1CompletedTreatmentRecurrent Head and Neck Cancer1
1CompletedTreatmentTumors, Solid1
1Not Yet RecruitingTreatmentCarcinoma, Squamous Cell of Head and Neck1
1Not Yet RecruitingTreatmentColorectal Cancers1
1RecruitingNot AvailableCarcinoma, Squamous Cell of Head and Neck / Squamous Cell Carcinoma of the Head and Neck (SCCHN) / Squamous Cell Carcinoma, Head And Neck1
1RecruitingTreatmentAdvanced Cancers3
1RecruitingTreatmentAdvanced Nonhematologic Malignancies1
1RecruitingTreatmentAdvanced Solid Tumors / Cancers1
1RecruitingTreatmentCancers1
1RecruitingTreatmentCarcinoma, Squamous Cell of Head and Neck / Squamous Cell Carcinoma (SCC)1
1RecruitingTreatmentColorectal Cancers / Head and Neck Cancers1
1RecruitingTreatmentHead and Neck Squamous Cell Cancer1
1RecruitingTreatmentMetastatic Breast Cancer (MBC)1
1RecruitingTreatmentNeoplasms1
1RecruitingTreatmentNeoplasms Metastasis / Neoplasms, Colorectal1
1RecruitingTreatmentNeoplasms, Head and Neck1
1RecruitingTreatmentPatients With Advanced or Metastatic Solid Tumors1
1RecruitingTreatmentSquamous Cell Carcinoma of the Head and Neck (SCCHN)3
1TerminatedTreatmentColon Cancer1
1TerminatedTreatmentColorectal Cancers1
1TerminatedTreatmentNeoplasms1
1WithdrawnTreatmentAdvanced Cancers1
1WithdrawnTreatmentTumors1
1, 2Active Not RecruitingTreatmentBasaloid Squamous Cell Carcinoma / Carcinoma, Adenosquamous Cell / Carcinoma, Undifferentiated / Squamous Cell Carcinoma of the Head and Neck (SCCHN)1
1, 2Active Not RecruitingTreatmentCarcinoma, Colorectal1
1, 2Active Not RecruitingTreatmentColorectal Cancers2
1, 2Active Not RecruitingTreatmentHead and Neck Cancers1
1, 2Active Not RecruitingTreatmentLung Cancers / Unspecified Adult Solid Tumor, Protocol Specific1
1, 2Active Not RecruitingTreatmentPlatinum-Resistant Squamous Cell Carcinoma of the Head and Neck1
1, 2CompletedTreatmentCancers of the Head and Neck / Neoplasms, Head and Neck1
1, 2CompletedTreatmentColon/Rectal Cancer / Colon/Rectal Cancer Rectal Cancer / Rectal Cancers1
1, 2CompletedTreatmentColorectal Cancers1
1, 2CompletedTreatmentHead and Neck Cancers2
1, 2CompletedTreatmentIncurable Metastatic Colorectal Carcinoma / Incurable Progressive, Recurrent or Metastatic Squamous Cell Carcinoma of the Head and Neck1
1, 2CompletedTreatmentMetastatic Colorectal Cancer (MCRC)1
1, 2CompletedTreatmentMetastatic Colorectal Cancers2
1, 2CompletedTreatmentNon-Small-Cell Lung Carcinoma (NSCLC)1
1, 2CompletedTreatmentPancreatic Cancer Metastatic1
1, 2CompletedTreatmentSquamous Cell Cancer2
1, 2Not Yet RecruitingTreatmentHead and Neck Cancers / Locally Advanced / Unresectable1
1, 2Not Yet RecruitingTreatmentNeoplasms, Oropharyngeal / Oropharyngeal Cancers / Squamous Carcinoma / Squamous Cell Carcinoma (SCC)1
1, 2RecruitingTreatmentAnaplastic Astrocytoma (AA) / Brainstem Glioma / Diffuse Intrinsic Pontine Glioma (DIPG) / Fibrillary Astrocytoma of Brain / Glioblastoma Multiforme / Glioma of Brainstem / Mixed Oligodendroglioma-Astrocytoma / Pilomyxoid Astrocytoma1
1, 2RecruitingTreatmentCancer, Advanced / Cancer, Breast / Colorectal Cancers / Esophageal Cancers / Gastric Cancers1
1, 2RecruitingTreatmentCarcinoma, Adenoid Cystic1
1, 2RecruitingTreatmentCarcinoma, Urothelial / Colorectal Adenocarcinoma (CRC) / Gastric Adenocarcinoma / Renal Cell Carcinoma (RCC)1
1, 2RecruitingTreatmentGlioblastoma Multiforme1
1, 2RecruitingTreatmentHead and Neck Squamous Cell Carcinoma (HNSCC) / Nasopharyngeal Cancers1
1, 2RecruitingTreatmentMetastatic Colorectal Cancers / Squamous Cell Carcinoma of Head and Neck1
1, 2RecruitingTreatmentNeoplasms, Colorectal / Tumors, Solid1
1, 2RecruitingTreatmentTumors, Solid1
1, 2SuspendedTreatmentSquamous Cell Carcinoma of the Head and Neck (SCCHN)1
1, 2TerminatedTreatmentColorectal Cancers / Head and Neck Cancers / Neoplasms Metastasis1
1, 2TerminatedTreatmentHead and Neck Cancers2
1, 2TerminatedTreatmentMetastatic Colorectal Cancers1
1, 2TerminatedTreatmentPancreatic Cancers1
1, 2TerminatedTreatmentSquamous Cell Carcinoma of the Head and Neck (SCCHN)1
2Active Not RecruitingNot AvailableTumors, Solid1
2Active Not RecruitingTreatmentAndrogen-independent Prostate Cancer1
2Active Not RecruitingTreatmentC-met Overexpression / Metastatic Colorectal Cancers1
2Active Not RecruitingTreatmentCancer, Breast1
2Active Not RecruitingTreatmentCarcinoma, Colorectal1
2Active Not RecruitingTreatmentCervical Cancers1
2Active Not RecruitingTreatmentCholangiocarcinomas1
2Active Not RecruitingTreatmentColorectal Cancers3
2Active Not RecruitingTreatmentHead and Neck Cancers4
2Active Not RecruitingTreatmentHead and Neck Squamous Cell Carcinoma (HNSCC)2
2Active Not RecruitingTreatmentHepatic Lesions / Liver Metastases / Metastatic Colorectal Cancers1
2Active Not RecruitingTreatmentLung Cancers1
2Active Not RecruitingTreatmentMetastatic Breast Cancer (MBC)1
2Active Not RecruitingTreatmentMetastatic Colorectal Cancers5
2Active Not RecruitingTreatmentMultiple Myeloma, Neoplasms1
2Active Not RecruitingTreatmentNasopharyngeal Carcinoma1
2Active Not RecruitingTreatmentNeoadjuvant Treatment / Rectal Neoplasms1
2Active Not RecruitingTreatmentNeoplasms, Esophageal1
2Active Not RecruitingTreatmentNeoplasms, Head and Neck1
2Active Not RecruitingTreatmentRectal Cancers2
2Active Not RecruitingTreatmentSquamous Cell Carcinoma of the Head and Neck (SCCHN)2
2Active Not RecruitingTreatmentStage III Non-Small Cell Lung Cancer1
2CompletedNot AvailableMalignant Gliomas1
2CompletedNot AvailableTumors, Solid1
2CompletedDiagnosticCancers1
2CompletedTreatmentAdenocarcinoma Of Esophagus / Squamous Cell Carcinoma of Esophagus1
2CompletedTreatmentAdenocarcinoma of Colon / Adenocarcinoma of Rectum / Metastatic Disease1
2CompletedTreatmentAdenocarcinomas1
2CompletedTreatmentAdvanced Biliary Cancer1
2CompletedTreatmentAdvanced Colorectal Cancer1
2CompletedTreatmentAdvanced Non-Small Cell Lung Cancer1
2CompletedTreatmentBladder Cancers1
2CompletedTreatmentCancer of Head and Neck1
2CompletedTreatmentCancer of the Larynx / Cancer of the Oral Cavity / Cancer of the Pharynx / Head and Neck Cancers / Nose Neoplasms / Paranasal Sinus Neoplasms1
2CompletedTreatmentCancer of the Lung / Carcinomas / Neoplasms, Lung / Non-Small-Cell Lung Carcinoma (NSCLC)1
2CompletedTreatmentCancer, Advanced1
2CompletedTreatmentCancer, Breast1
2CompletedTreatmentCancers1
2CompletedTreatmentCarcinoma of the Head and Neck1
2CompletedTreatmentCarcinoma, Colorectal1
2CompletedTreatmentCarcinoma, Colorectal / Colorectal Cancers / Colorectal Tumors1
2CompletedTreatmentColon Cancer1
2CompletedTreatmentColon Cancer / Rectum Cancer1
2CompletedTreatmentColorectal Cancer (CRC)1
2CompletedTreatmentColorectal Cancers5
2CompletedTreatmentColorectal Cancers / Liver Metastases1
2CompletedTreatmentColorectal Cancers / Neoplasms Metastasis1
2CompletedTreatmentColorectal Cancers / Unresectable Liver Metastasis1
2CompletedTreatmentEndometrial Cancers1
2CompletedTreatmentEsophageal Cancers1
2CompletedTreatmentEsophageal Cancers / Gastric Cancers / Neoplasms Metastasis1
2CompletedTreatmentGastric Cancer Adenocarcinoma Metastatic1
2CompletedTreatmentGastric Cancers4
2CompletedTreatmentGastric Cancers / Stomach Cancer1
2CompletedTreatmentHead and Neck Cancers5
2CompletedTreatmentHead and Neck Cancers / Head and Neck Squamous Cell Carcinoma (HNSCC)1
2CompletedTreatmentHead and Neck Cancers / Squamous Cell Carcinoma (SCC)1
2CompletedTreatmentHepatocellular Carcinomas1
2CompletedTreatmentHypopharynx Cancer / Larynx Cancer1
2CompletedTreatmentLarynx Carcinoma / Squamous Cell Carcinoma of the Hypopharynx1
2CompletedTreatmentLocally Advanced / Metastatic / Unresectable1
2CompletedTreatmentLung Cancers3
2CompletedTreatmentLung Cancers / Non-Small-Cell Lung Carcinoma (NSCLC)1
2CompletedTreatmentMetastatic Breast Cancer (MBC) / Triple Negative Locally Advanced Non-resectable Breast Cancer1
2CompletedTreatmentMetastatic Colorectal Cancers8
2CompletedTreatmentMucinous Gastrointestinal Adenocarcinoma1
2CompletedTreatmentNasopharyngeal Carcinoma2
2CompletedTreatmentNeoplasms, Breast1
2CompletedTreatmentNeoplasms, Colorectal1
2CompletedTreatmentNeoplasms, Head and Neck3
2CompletedTreatmentNeoplasms, Head and Neck / Squamous Cell Carcinoma (SCC)1
2CompletedTreatmentNon Small Cell Lung Cancer (NSCLC)1
2CompletedTreatmentNon-Small-Cell Lung Cancer (NSCLC)1
2CompletedTreatmentNon-Small-Cell Lung Carcinoma (NSCLC)8
2CompletedTreatmentPancreatic Cancer Metastatic1
2CompletedTreatmentPancreatic Cancers4
2CompletedTreatmentPreviously Untreated Metastatic Colorectal Cancer1
2CompletedTreatmentRectal Cancers3
2CompletedTreatmentRectal Neoplasms1
2CompletedTreatmentSarcomas1
2CompletedTreatmentSkin Diseases / Squamous Cell Carcinoma (SCC)1
2CompletedTreatmentSquamous Cell Carcinoma (SCC)2
2CompletedTreatmentSquamous Cell Carcinoma of the Head and Neck (SCCHN)1
2CompletedTreatmentSquamous Cell Carcinoma of the Head and Neck Cancer1
2CompletedTreatmentTime to Progression1
2CompletedTreatmentUrologic Neoplasms1
2Not Yet RecruitingTreatmentCarcinomas / Unknown Primary Neoplasms1
2Not Yet RecruitingTreatmentNon Small Cell Lung Cancer (NSCLC)1
2Not Yet RecruitingTreatmentRectum Cancer1
2Not Yet RecruitingTreatmentSquamous Cell Cancers of the Head and Neck1
2Not Yet RecruitingTreatmentSquamous Cell Carcinoma of the Head and Neck (SCCHN)1
2RecruitingBasic ScienceMetastatic Colorectal Cancers1
2RecruitingPreventionHead and Neck Cancers1
2RecruitingScreeningColorectal Cancers1
2RecruitingTreatmentAdenocarcinoma of Gallbladder / Cholangiocarcinomas1
2RecruitingTreatmentAdvanced Solid Tumors / Multiple Myeloma (MM) / Non-Hodgkin's Lymphoma (NHL)1
2RecruitingTreatmentCancer of the Cervix1
2RecruitingTreatmentCancers1
2RecruitingTreatmentCarcinoma, Squamous Cell of Head and Neck1
2RecruitingTreatmentColorectal Cancers3
2RecruitingTreatmentColorectal Cancers / Liver Metastases1
2RecruitingTreatmentComplex Regional Pain Syndromes (CRPS) / Neuralgia1
2RecruitingTreatmentEsophageal Cancers2
2RecruitingTreatmentHead Neck Cancer Squamous Cell1
2RecruitingTreatmentHead and Neck Cancers4
2RecruitingTreatmentHead and Neck Cancers / Recurrent1
2RecruitingTreatmentHead and Neck Cancers / Squamous Cell Carcinoma of the Head and Neck (SCCHN)1
2RecruitingTreatmentHead and Neck Squamous Cell Carcinoma (HNSCC)1
2RecruitingTreatmentHead and Neck / Recurrent Disease / Squamous Cell Carcinoma (SCC)1
2RecruitingTreatmentHypopharyngeal Cancer / Laryngeal Cancer / Oropharyngeal Cancers1
2RecruitingTreatmentIncurable Colorectal Cancer / RAS-wild-type1
2RecruitingTreatmentLiver Only Metastasis From KRAS Exon 2 Wild Type (Under Protocol 1.0-1.2 Edition) and RAS Wild Type (Under Protocol 2.0 Edition) Colorectal Cancer1
2RecruitingTreatmentLocally Advanced Thoracic Middle-lower Segment Esophageal Squamous Cell Carcinoma1
2RecruitingTreatmentMetastatic Cancers1
2RecruitingTreatmentMetastatic Colon Cancer1
2RecruitingTreatmentMetastatic Colorectal Cancers8
2RecruitingTreatmentMetastatic or Recurrent HNSCC1
2RecruitingTreatmentNasopharyngeal Carcinoma1
2RecruitingTreatmentNeoplasms by Site / Neoplasms, Head and Neck / Squamous Cell Cancers of the Head and Neck1
2RecruitingTreatmentNeoplasms, Head and Neck1
2RecruitingTreatmentNeoplasms, Oropharyngeal1
2RecruitingTreatmentNon-Small-Cell Lung Carcinoma (NSCLC)2
2RecruitingTreatmentSquamous Cell Carcinoma (SCC)1
2RecruitingTreatmentSquamous Cell Carcinoma of the Head and Neck (SCCHN)4
2RecruitingTreatmentSquamous Cell Carcinoma of the Head / Squamous Cell Carcinoma of the Neck1
2TerminatedTreatmentCancer of Larynx1
2TerminatedTreatmentCervix Cancer1
2TerminatedTreatmentColorectal Cancers8
2TerminatedTreatmentColorectal Cancers / Metastases1
2TerminatedTreatmentEsophageal Cancers1
2TerminatedTreatmentGlioblastomas1
2TerminatedTreatmentHead and Neck Cancers / Squamous Carcinoma1
2TerminatedTreatmentHead and Neck Squamous Cell Cancer1
2TerminatedTreatmentLaryngeal Neoplasms / Mouth Neoplasms / Neoplasms, Head and Neck / Pharyngeal Neoplasms1
2TerminatedTreatmentMetastatic Colorectal Cancers2
2TerminatedTreatmentMultiple Myeloma (MM)1
2TerminatedTreatmentNasopharyngeal Carcinoma1
2TerminatedTreatmentNeoplasms, Colorectal1
2TerminatedTreatmentNon-Small-Cell Lung Carcinoma (NSCLC)2
2TerminatedTreatmentProstatic Neoplasms1
2TerminatedTreatmentRectal Cancers2
2TerminatedTreatmentResectable Esophageal Cancer1
2TerminatedTreatmentSquamous Cell Cancers of the Head and Neck1
2WithdrawnNot AvailableNeoplasms, Lung / Non-Small-Cell Lung Carcinoma (NSCLC)1
2WithdrawnTreatmentColon Cancer / Colorectal Cancers1
2WithdrawnTreatmentEsophageal Carcinoma1
2WithdrawnTreatmentHead and Neck Cancers2
2WithdrawnTreatmentHuman Papilloma Virus (HPV) / Squamous Cell Carcinoma of the Head and Neck (SCCHN)1
2WithdrawnTreatmentLung Cancers1
2WithdrawnTreatmentMetastatic Colorectal Cancers1
2WithdrawnTreatmentSquamous Cell Carcinoma of the Penis1
2, 3Not Yet RecruitingTreatmentColorectal Cancers1
3Active Not RecruitingTreatmentColorectal Cancers1
3Active Not RecruitingTreatmentColorectal Cancers / Neoplasms Metastasis1
3Active Not RecruitingTreatmentHNSCC1
3Active Not RecruitingTreatmentMetastatic Colorectal Cancers3
3Active Not RecruitingTreatmentSquamous Cell Carcinoma of the Head and Neck (SCCHN)1
3CompletedTreatmentColorectal Cancers2
3CompletedTreatmentEpidermal Growth Factor Receptor (EGFR) Expressing Metastatic Colorectal Cancer1
3CompletedTreatmentGastric Cancers1
3CompletedTreatmentHead and Neck Squamous Cell Carcinoma (HNSCC)1
3CompletedTreatmentMetastatic Colorectal Cancers3
3CompletedTreatmentNon Small Cell Lung Cancer (NSCLC)1
3CompletedTreatmentNon-Small-Cell Lung Carcinoma (NSCLC)2
3RecruitingTreatmentAntineoplastic Agents1
3RecruitingTreatmentBRAF V600E-mutant Metastatic Colorectal Cancer1
3RecruitingTreatmentCarcinoma, Squamous Cell of Head and Neck1
3RecruitingTreatmentHPV Positive Oropharyngeal Squamous Cell Carcinoma1
3RecruitingTreatmentHead Neck Cancer Squamous Cell Recurrent1
3RecruitingTreatmentHead and Neck Cancers1
3RecruitingTreatmentLocally Advanced Head and Neck Cancer1
3RecruitingTreatmentMetastatic Colorectal Cancers / Skin Toxicities1
3RecruitingTreatmentNasopharyngeal Carcinoma1
3RecruitingTreatmentOropharyngeal Squamous Cell Carcinoma1
3RecruitingTreatmentSquamous Cell Carcinoma of the Head and Neck (SCCHN)2
3WithdrawnTreatmentColorectal Cancers1
4Active Not RecruitingTreatmentMetastatic Colorectal Cancers1
4RecruitingTreatmentHead and Neck Cancers1
4RecruitingTreatmentNeoplasms Metastasis / Neoplasms, Colorectal / Neoplasms, Liver1
4RecruitingTreatmentNeoplasms, Head and Neck1
4TerminatedTreatmentColorectal Cancers / Neoplasms Metastasis1
Not AvailableActive Not RecruitingNot AvailableEpidermoid Head and Neck Cancer1
Not AvailableActive Not RecruitingNot AvailableMetastatic Colorectal Cancers2
Not AvailableCompletedNot AvailableHead and Neck Cancers1
Not AvailableCompletedNot AvailableNeoplasms, Colorectal1
Not AvailableRecruitingTreatmentColorectal Cancers / Liver Metastasis1
Not AvailableRecruitingTreatmentHpv / Squamous Cell Carcinoma of the Oropharynx1
Not AvailableRecruitingTreatmentPancreatic Cancers1
Not AvailableTerminatedNot AvailableLA SCCHN / Unresectable Locally Advanced Squamous Cell Carcinoma of Head and Neck1
Not AvailableTerminatedNot AvailableNeoplasms, Colorectal2
Not AvailableTerminatedNot AvailableSquamous Cell Carcinoma (SCC)1
Not AvailableTerminatedTreatmentEsophageal Adenocarcinomas1
Not AvailableTerminatedTreatmentHead and Neck Squamous Cell Cancer1
Not AvailableWithdrawnNot AvailableNeoplasms, Squamous Cell1
Not AvailableWithdrawnTreatmentColorectal Cancers / Liver Metastases1
Not AvailableWithdrawnTreatmentHead and Neck Cancers1
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Injection, solutionIntravenous5 mg/ml
SolutionIntravenous2 mg
SolutionIntravenous2 mg/mL
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA1340417 No1999-03-022016-03-02Canada
Properties
StateLiquid
Experimental Properties
PropertyValueSource
melting point61 °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
Taxonomy
DescriptionNot Available
KingdomOrganic Compounds
Super ClassOrganic Acids
ClassCarboxylic Acids and Derivatives
Sub ClassAmino Acids, Peptides, and Analogues
Direct ParentPeptides
Alternative ParentsNot Available
SubstituentsNot Available
Molecular FrameworkNot Available
External DescriptorsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
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, TGFA/TGF-alpha, amphiregulin, epigen/EPGN, BTC/betacellulin, epiregulin/EREG and HBEGF/heparin-binding EGF. Ligand binding triggers receptor homo- and/or heterodimerization and autophosphorylation on ke...
Gene Name:
EGFR
Uniprot ID:
P00533
Molecular Weight:
134276.185 Da
References
  1. Hosokawa N, Yamamoto S, Uehara Y, Hori M, Tsuchiya KS: Effect of thiazinotrienomycin B, an ansamycin antibiotic, on the function of epidermal growth factor receptor in human stomach tumor cells. J Antibiot (Tokyo). 1999 May;52(5):485-90. [PubMed:10480573 ]
  2. Wakita H, Takigawa M: Activation of epidermal growth factor receptor promotes late terminal differentiation of cell-matrix interaction-disrupted keratinocytes. J Biol Chem. 1999 Dec 24;274(52):37285-91. [PubMed:10601294 ]
  3. Suwa T, Ueda M, Jinno H, Ozawa S, Kitagawa Y, Ando N, Kitajima M: Epidermal growth factor receptor-dependent cytotoxic effect of anti-EGFR antibody-ribonuclease conjugate on human cancer cells. Anticancer Res. 1999 Sep-Oct;19(5B):4161-5. [PubMed:10628369 ]
  4. Burke P, Schooler K, Wiley HS: Regulation of epidermal growth factor receptor signaling by endocytosis and intracellular trafficking. Mol Biol Cell. 2001 Jun;12(6):1897-910. [PubMed:11408594 ]
  5. Viloria-Petit A, Crombet T, Jothy S, Hicklin D, Bohlen P, Schlaeppi JM, Rak J, Kerbel RS: Acquired resistance to the antitumor effect of epidermal growth factor receptor-blocking antibodies in vivo: a role for altered tumor angiogenesis. Cancer Res. 2001 Jul 1;61(13):5090-101. [PubMed:11431346 ]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
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 cytotoxicity and phagocytosis. May serve as a trap for immune complexes in the peripheral circulation which does not activate neutrophils.
Gene Name:
FCGR3B
Uniprot ID:
O75015
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. [PubMed:16336752 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Serine-type peptidase activity
Specific Function:
C1r B chain is a serine protease that combines with C1q and C1s to form C1, the first component of the classical pathway of the complement system.
Gene Name:
C1R
Uniprot ID:
P00736
Molecular Weight:
80118.04 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. [PubMed:17139284 ]
  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. [PubMed:17016423 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
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) proenzyme complex, and efficient activation of C1 takes place on interaction of the globular heads of C1q with the Fc regions of IgG or IgM antibody present in immune complexes.
Gene Name:
C1QA
Uniprot ID:
P02745
Molecular Weight:
26016.47 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. [PubMed:17139284 ]
  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. [PubMed:17016423 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
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) proenzyme complex, and efficient activation of C1 takes place on interaction of the globular heads of C1q with the Fc regions of IgG or IgM antibody present in immune complexes.
Gene Name:
C1QB
Uniprot ID:
P02746
Molecular Weight:
26721.62 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. [PubMed:17139284 ]
  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. [PubMed:17016423 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
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) proenzyme complex, and efficient activation of C1 takes place on interaction of the globular heads of C1q with the Fc regions of IgG or IgM antibody present in immune complexes.
Gene Name:
C1QC
Uniprot ID:
P02747
Molecular Weight:
25773.56 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. [PubMed:17139284 ]
  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. [PubMed:17016423 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
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 phagocytosis.
Gene Name:
FCGR3A
Uniprot ID:
P08637
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. [PubMed:17139284 ]
  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. [PubMed:17016423 ]
  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. [PubMed:17704420 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Serine-type endopeptidase activity
Specific Function:
C1s B chain is a serine protease that combines with C1q and C1r to form C1, the first component of the classical pathway of the complement system. C1r activates C1s so that it can, in turn, activate C2 and C4.
Gene Name:
C1S
Uniprot ID:
P09871
Molecular Weight:
76683.905 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. [PubMed:17139284 ]
  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. [PubMed:17016423 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
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
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. [PubMed:7547242 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
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 antigens.
Gene Name:
FCGR2A
Uniprot ID:
P12318
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. [PubMed:17139284 ]
  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. [PubMed:17016423 ]
  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. [PubMed:17704420 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Not Available
Specific Function:
Receptor for the Fc region of complexed or aggregated immunoglobulins gamma. Low affinity receptor. Involved in a variety of effector and regulatory functions such as phagocytosis of immune complexes and modulation of antibody production by B-cells. Binding to this receptor results in down-modulation of previous state of cell activation triggered via antigen receptors on B-cells (BCR), T-cells ...
Gene Name:
FCGR2B
Uniprot ID:
P31994
Molecular Weight:
34043.355 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. [PubMed:17139284 ]
  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. [PubMed:17016423 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Transmembrane signaling receptor activity
Specific Function:
Receptor for the Fc region of complexed immunoglobulins gamma. Low affinity receptor. Involved in a variety of effector and regulatory functions such as phagocytosis of immune complexes and modulation of antibody production by B-cells.
Gene Name:
FCGR2C
Uniprot ID:
P31995
Molecular Weight:
35577.96 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. [PubMed:17139284 ]
  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. [PubMed:17016423 ]
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Drug created on June 13, 2005 07:24 / Updated on January 04, 2017 13:41