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Identification
NameTrastuzumab
Accession NumberDB00072  (BTD00098, BIOD00098)
TypeBiotech
GroupsApproved, Investigational
Description

A recombinant IgG1 kappa, humanized monoclonal antibody that selectively binds with high affinity in a cell-based assay (Kd = 5 nM) to the extracellular domain of the human epidermal growth factor receptor protein. Produced in CHO cell culture.

Protein structureDb00072
Related Articles
Protein chemical formulaC6470H10012N1726O2013S42
Protein average weight145531.5 Da
Sequences
>Anti-HER2 Light chain (1 and 2)
DIQMTQSPSSLSASVGDRVTITCRASQDVNTAVAWYQQKPGKAPKLLIYSASFLYSGVPS
RFSGSRSGTDFTLTISSLQPEDFATYYCQQHYTTPPTFGQGTKVEIKRTVAAPSVFIFPP
SDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTLT
LSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC
>Anti-HER2 Heavy chain (1 and 2)
EVQLVESGGGLVQPGGSLRLSCAASGFNIKDTYIHWVRQAPGKGLEWVARIYPTNGYTRY
ADSVKGRFTISADTSKNTAYLQMNSLRAEDTAVYYCSRWGGDGFYAMDYWGQGTLVTVSS
ASTKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSS
GLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKVEPPKSCDKTHTCPPCPAPELLG
GPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQY
NSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRD
ELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSR
WQQGNVFSCSVMHEALHNHYTQKSLSLSPGK
Download FASTA Format
Synonyms
Anti HER2
Ig gamma-1 chain C region
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Herceptinpowder for solution440 mgintravenousHoffmann La Roche Limited1999-08-23Not applicableCanada
HerceptinkitGenentech, Inc.1998-09-25Not applicableUs
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
HerclonRoche
Brand mixtures
NameLabellerIngredients
Perjeta-herceptinHoffmann La Roche Limited
SaltsNot Available
Categories
UNIIP188ANX8CK
CAS number180288-69-1
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
Pharmacology
IndicationFor treatment of early stage HER2-positive breast cancer, or metastatic breast cancer that substantially overexpress HER2.
PharmacodynamicsUsed in the treatment of HER2-positive breast cancer. HER2 protein overexpression is observed in 25%-30% of primary breast cancers.Trastuzumab has been shown, in both in vitro assays and in animals, to inhibit the proliferation of human tumorcells that overexpress HER2. It is a mediator of antibody dependent cellular cytotoxicity, in that the binding of the antibody to HER2 overexpressing cells leads to preferential cell death.
Mechanism of actionTrastuzumab binds to the HER2 (or c-erbB2) proto-oncogene, an EGF receptor-like protein found on 20-30% of breast cancer cells. The binding leads to antibody mediated (complement mediated) killing of the HER2 positive cells.
Related Articles
AbsorptionPeak and trough plasma concentrations at steady state (between weeks 16 and 32) approximately 123 and 79 mcg/mL, respectively.
Volume of distribution
  • 44 mL/kg
Protein bindingNot Available
Metabolism

Most likely removed by opsonization via the reticuloendothelial system.

Route of eliminationNot Available
Half lifeaverage 28.5 days. Pharmacokinetics are nonlinear; increased doses are associated with increased mean half-life and decreased clearance.
Clearance

Elimination may involve clearance of IgG through the reticuloendothelial system.

ToxicityAdministration of trastuzumab can result in ventricular dysfunction and congestive heart failure. Risk of cardiotocity is especially elevated in patients recieving concurrent anthracycline or cyclophosphamide therapy.
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Trastuzumab Action PathwayDrug actionSMP00476
SNP Mediated Effects
Interacting Gene/EnzymeSNP RS IDAllele nameDefining changeEffectReference(s)
Fibroblast growth factor receptor 4
Gene symbol: FGFR4
UniProt: P22455
rs351855 Not AvailableC AlleleReduced response to herceptin16822847
SNP Mediated Adverse Drug Reactions
Interacting Gene/EnzymeSNP RS IDAllele nameDefining changeAdverse ReactionReference(s)
Receptor tyrosine-protein kinase erbB-2
Gene symbol: ERBB2
UniProt: P04626
rs1801200 Not AvailableG Allele, heterozygoteCardiotoxicity17693647
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Kit
Powder for solutionintravenous440 mg
Solution; kit; powder for solutionintravenous
Prices
Unit descriptionCostUnit
Herceptin 440 mg Solution Vial3581.2USD vial
Herceptin 440 mg vial3443.46USD vial
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2103059 No2005-03-222012-06-15Canada
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-0.415Not Available
isoelectric point8.45Not Available
References
Synthesis ReferenceNot Available
General References
  1. Bange J, Zwick E, Ullrich A: Molecular targets for breast cancer therapy and prevention. Nat Med. 2001 May;7(5):548-52. [PubMed:11329054 ]
  2. Menard S, Pupa SM, Campiglio M, Tagliabue E: Biologic and therapeutic role of HER2 in cancer. Oncogene. 2003 Sep 29;22(42):6570-8. [PubMed:14528282 ]
  3. Kute T, Lack CM, Willingham M, Bishwokama B, Williams H, Barrett K, Mitchell T, Vaughn JP: Development of Herceptin resistance in breast cancer cells. Cytometry A. 2004 Feb;57(2):86-93. [PubMed:14750129 ]
  4. Albanell J, Codony J, Rovira A, Mellado B, Gascon P: Mechanism of action of anti-HER2 monoclonal antibodies: scientific update on trastuzumab and 2C4. Adv Exp Med Biol. 2003;532:253-68. [PubMed:12908564 ]
  5. Tan AR, Swain SM: Ongoing adjuvant trials with trastuzumab in breast cancer. Semin Oncol. 2003 Oct;30(5 Suppl 16):54-64. [PubMed:14613027 ]
  6. Nebija D, Kopelent-Frank H, Urban E, Noe CR, Lachmann B: Comparison of two-dimensional gel electrophoresis patterns and MALDI-TOF MS analysis of therapeutic recombinant monoclonal antibodies trastuzumab and rituximab. J Pharm Biomed Anal. 2011 Dec 5;56(4):684-91. doi: 10.1016/j.jpba.2011.07.006. Epub 2011 Jul 18. [PubMed:21813259 ]
External Links
ATC CodesL01XC03
AHFS CodesNot Available
PDB Entries
FDA labelDownload (41 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
AbataceptTrastuzumab may increase the neutropenic activities of Abatacept.
AdalimumabTrastuzumab may increase the neutropenic activities of Adalimumab.
AlemtuzumabTrastuzumab may increase the neutropenic activities of Alemtuzumab.
AltretamineTrastuzumab may increase the neutropenic activities of Altretamine.
AmsacrineTrastuzumab may increase the neutropenic activities of Amsacrine.
AnakinraTrastuzumab may increase the neutropenic activities of Anakinra.
Anti-thymocyte Globulin (Rabbit)Trastuzumab may increase the neutropenic activities of Anti-thymocyte Globulin (Rabbit).
AzacitidineTrastuzumab may increase the neutropenic activities of Azacitidine.
AzathioprineTrastuzumab may increase the neutropenic activities of Azathioprine.
BasilTrastuzumab may increase the neutropenic activities of Basil.
BasiliximabTrastuzumab may increase the neutropenic activities of Basiliximab.
BelataceptTrastuzumab may increase the neutropenic activities of Belatacept.
BelimumabThe risk or severity of adverse effects can be increased when Trastuzumab is combined with Belimumab.
BetamethasoneTrastuzumab may increase the neutropenic activities of Betamethasone.
BleomycinTrastuzumab may increase the neutropenic activities of Bleomycin.
BlinatumomabTrastuzumab may increase the neutropenic activities of Blinatumomab.
Brentuximab vedotinTrastuzumab may increase the neutropenic activities of Brentuximab vedotin.
BudesonideTrastuzumab may increase the neutropenic activities of Budesonide.
BusulfanTrastuzumab may increase the neutropenic activities of Busulfan.
CabazitaxelTrastuzumab may increase the neutropenic activities of Cabazitaxel.
CanakinumabTrastuzumab may increase the neutropenic activities of Canakinumab.
CapecitabineTrastuzumab may increase the neutropenic activities of Capecitabine.
CarboplatinTrastuzumab may increase the neutropenic activities of Carboplatin.
CarmustineTrastuzumab may increase the neutropenic activities of Carmustine.
Certolizumab pegolTrastuzumab may increase the neutropenic activities of Certolizumab pegol.
ChlorambucilTrastuzumab may increase the neutropenic activities of Chlorambucil.
CisplatinTrastuzumab may increase the neutropenic activities of Cisplatin.
CladribineTrastuzumab may increase the neutropenic activities of Cladribine.
ClofarabineTrastuzumab may increase the neutropenic activities of Clofarabine.
CorticotropinTrastuzumab may increase the neutropenic activities of Corticotropin.
Cortisone acetateTrastuzumab may increase the neutropenic activities of Cortisone acetate.
CyclophosphamideTrastuzumab may increase the neutropenic activities of Cyclophosphamide.
CyclosporineTrastuzumab may increase the neutropenic activities of Cyclosporine.
CytarabineTrastuzumab may increase the neutropenic activities of Cytarabine.
DacarbazineTrastuzumab may increase the neutropenic activities of Dacarbazine.
DactinomycinTrastuzumab may increase the neutropenic activities of Dactinomycin.
DasatinibTrastuzumab may increase the neutropenic activities of Dasatinib.
DaunorubicinTrastuzumab may increase the cardiotoxic activities of Daunorubicin.
DexamethasoneTrastuzumab may increase the neutropenic activities of Dexamethasone.
DinutuximabTrastuzumab may increase the neutropenic activities of Dinutuximab.
DocetaxelTrastuzumab may increase the neutropenic activities of Docetaxel.
DoxorubicinTrastuzumab may increase the cardiotoxic activities of Doxorubicin.
EculizumabTrastuzumab may increase the neutropenic activities of Eculizumab.
EpirubicinTrastuzumab may increase the cardiotoxic activities of Epirubicin.
EstramustineTrastuzumab may increase the neutropenic activities of Estramustine.
EtanerceptTrastuzumab may increase the neutropenic activities of Etanercept.
EtoposideTrastuzumab may increase the neutropenic activities of Etoposide.
EverolimusTrastuzumab may increase the neutropenic activities of Everolimus.
FingolimodTrastuzumab may increase the neutropenic activities of Fingolimod.
FloxuridineTrastuzumab may increase the neutropenic activities of Floxuridine.
FludarabineTrastuzumab may increase the neutropenic activities of Fludarabine.
FludrocortisoneTrastuzumab may increase the neutropenic activities of Fludrocortisone.
FluorouracilTrastuzumab may increase the neutropenic activities of Fluorouracil.
GemcitabineTrastuzumab may increase the neutropenic activities of Gemcitabine.
Gemtuzumab ozogamicinTrastuzumab may increase the neutropenic activities of Gemtuzumab ozogamicin.
Glatiramer AcetateTrastuzumab may increase the neutropenic activities of Glatiramer Acetate.
golimumabTrastuzumab may increase the neutropenic activities of golimumab.
HydrocortisoneTrastuzumab may increase the neutropenic activities of Hydrocortisone.
HydroxyureaTrastuzumab may increase the neutropenic activities of Hydroxyurea.
Ibritumomab tiuxetanTrastuzumab may increase the neutropenic activities of Ibritumomab.
IbrutinibTrastuzumab may increase the neutropenic activities of Ibrutinib.
IdarubicinTrastuzumab may increase the cardiotoxic activities of Idarubicin.
IdelalisibTrastuzumab may increase the neutropenic activities of Idelalisib.
IfosfamideTrastuzumab may increase the neutropenic activities of Ifosfamide.
ImatinibTrastuzumab may increase the neutropenic activities of Imatinib.
ImiquimodTrastuzumab may increase the neutropenic activities of Imiquimod.
InfliximabTrastuzumab may increase the neutropenic activities of Infliximab.
IrinotecanTrastuzumab may increase the neutropenic activities of Irinotecan.
L-PhenylalanineTrastuzumab may increase the neutropenic activities of L-Phenylalanine.
LeflunomideTrastuzumab may increase the neutropenic activities of Leflunomide.
LenalidomideTrastuzumab may increase the neutropenic activities of Lenalidomide.
LomustineTrastuzumab may increase the neutropenic activities of Lomustine.
MechlorethamineTrastuzumab may increase the neutropenic activities of Mechlorethamine.
MelphalanTrastuzumab may increase the neutropenic activities of Melphalan.
MercaptopurineTrastuzumab may increase the neutropenic activities of Mercaptopurine.
MethotrexateTrastuzumab may increase the neutropenic activities of Methotrexate.
MethylprednisoloneTrastuzumab may increase the neutropenic activities of Methylprednisolone.
MitomycinTrastuzumab may increase the neutropenic activities of Mitomycin.
MitoxantroneTrastuzumab may increase the neutropenic activities of Mitoxantrone.
Mycophenolate mofetilTrastuzumab may increase the neutropenic activities of Mycophenolate mofetil.
Mycophenolic acidTrastuzumab may increase the neutropenic activities of Mycophenolic acid.
NatalizumabTrastuzumab may increase the neutropenic activities of Natalizumab.
NelarabineTrastuzumab may increase the neutropenic activities of Nelarabine.
NilotinibTrastuzumab may increase the neutropenic activities of Nilotinib.
ObinutuzumabTrastuzumab may increase the neutropenic activities of Obinutuzumab.
OsimertinibTrastuzumab may increase the neutropenic activities of Osimertinib.
OxaliplatinTrastuzumab may increase the neutropenic activities of Oxaliplatin.
PaclitaxelThe serum concentration of Paclitaxel can be decreased when it is combined with Trastuzumab.
PalbociclibTrastuzumab may increase the neutropenic activities of Palbociclib.
PanobinostatTrastuzumab may increase the neutropenic activities of Panobinostat.
PazopanibTrastuzumab may increase the neutropenic activities of Pazopanib.
PegaspargaseTrastuzumab may increase the neutropenic activities of Pegaspargase.
PemetrexedTrastuzumab may increase the neutropenic activities of Pemetrexed.
PentostatinTrastuzumab may increase the neutropenic activities of Pentostatin.
PomalidomideTrastuzumab may increase the neutropenic activities of Pomalidomide.
PralatrexateTrastuzumab may increase the neutropenic activities of Pralatrexate.
PrednisoloneTrastuzumab may increase the neutropenic activities of Prednisolone.
PrednisoneTrastuzumab may increase the neutropenic activities of Prednisone.
ProcarbazineTrastuzumab may increase the neutropenic activities of Procarbazine.
Repository corticotropinTrastuzumab may increase the neutropenic activities of Repository corticotropin.
RilonaceptTrastuzumab may increase the neutropenic activities of Rilonacept.
RituximabTrastuzumab may increase the neutropenic activities of Rituximab.
RuxolitinibTrastuzumab may increase the neutropenic activities of Ruxolitinib.
SecukinumabTrastuzumab may increase the neutropenic activities of Secukinumab.
SiltuximabTrastuzumab may increase the neutropenic activities of Siltuximab.
SirolimusTrastuzumab may increase the neutropenic activities of Sirolimus.
SorafenibTrastuzumab may increase the neutropenic activities of Sorafenib.
StreptozocinTrastuzumab may increase the neutropenic activities of Streptozocin.
SunitinibTrastuzumab may increase the neutropenic activities of Sunitinib.
TacrolimusTrastuzumab may increase the neutropenic activities of Tacrolimus.
TemozolomideTrastuzumab may increase the neutropenic activities of Temozolomide.
TemsirolimusTrastuzumab may increase the neutropenic activities of Temsirolimus.
TeniposideTrastuzumab may increase the neutropenic activities of Teniposide.
TeriflunomideTrastuzumab may increase the neutropenic activities of Teriflunomide.
ThalidomideTrastuzumab may increase the neutropenic activities of Thalidomide.
ThiotepaTrastuzumab may increase the neutropenic activities of Thiotepa.
TioguanineTrastuzumab may increase the neutropenic activities of Tioguanine.
TocilizumabTrastuzumab may increase the neutropenic activities of Tocilizumab.
TofacitinibTrastuzumab may increase the neutropenic activities of Tofacitinib.
TopotecanTrastuzumab may increase the neutropenic activities of Topotecan.
TositumomabTrastuzumab may increase the neutropenic activities of Tositumomab.
TrabectedinTrastuzumab may increase the neutropenic activities of Trabectedin.
Trastuzumab emtansineTrastuzumab may increase the neutropenic activities of ado-trastuzumab emtansine.
TretinoinTrastuzumab may increase the neutropenic activities of Tretinoin.
TriamcinoloneTrastuzumab may increase the neutropenic activities of Triamcinolone.
UstekinumabTrastuzumab may increase the neutropenic activities of Ustekinumab.
VedolizumabTrastuzumab may increase the neutropenic activities of Vedolizumab.
VinblastineTrastuzumab may increase the neutropenic activities of Vinblastine.
VincristineTrastuzumab may increase the neutropenic activities of Vincristine.
VindesineTrastuzumab may increase the neutropenic activities of Vindesine.
VinorelbineTrastuzumab may increase the neutropenic activities of Vinorelbine.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antibody
General Function:
Transmembrane signaling receptor activity
Specific Function:
Protein tyrosine kinase that is part of several cell surface receptor complexes, but that apparently needs a coreceptor for ligand binding. Essential component of a neuregulin-receptor complex, although neuregulins do not interact with it alone. GP30 is a potential ligand for this receptor. Regulates outgrowth and stabilization of peripheral microtubules (MTs). Upon ERBB2 activation, the MEMO1-...
Gene Name:
ERBB2
Uniprot ID:
P04626
Molecular Weight:
137909.27 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  2. Leveque D, Gigou L, Bergerat JP: Clinical pharmacology of trastuzumab. Curr Clin Pharmacol. 2008 Jan;3(1):51-5. [PubMed:18690878 ]
  3. Lin A, Rugo HS: The role of trastuzumab in early stage breast cancer: current data and treatment recommendations. Curr Treat Options Oncol. 2007 Feb;8(1):47-60. [PubMed:17660958 ]
  4. Treish I, Schwartz R, Lindley C: Pharmacology and therapeutic use of trastuzumab in breast cancer. Am J Health Syst Pharm. 2000 Nov 15;57(22):2063-76; quiz 2077-9. [PubMed:11098307 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
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. 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:
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:
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. 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. Curnow RT: Clinical experience with CD64-directed immunotherapy. An overview. Cancer Immunol Immunother. 1997 Nov-Dec;45(3-4):210-5. [PubMed:9435876 ]
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 ]
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. Bowles JA, Weiner GJ: CD16 polymorphisms and NK activation induced by monoclonal antibody-coated target cells. J Immunol Methods. 2005 Sep;304(1-2):88-99. [PubMed:16109421 ]
  2. Shahied LS, Tang Y, Alpaugh RK, Somer R, Greenspon D, Weiner LM: Bispecific minibodies targeting HER2/neu and CD16 exhibit improved tumor lysis when placed in a divalent tumor antigen binding format. J Biol Chem. 2004 Dec 24;279(52):53907-14. Epub 2004 Oct 7. [PubMed:15471859 ]
  3. Kubo M, Morisaki T, Kuroki H, Tasaki A, Yamanaka N, Matsumoto K, Nakamura K, Onishi H, Baba E, Katano M: Combination of adoptive immunotherapy with Herceptin for patients with HER2-expressing breast cancer. Anticancer Res. 2003 Nov-Dec;23(6a):4443-9. [PubMed:14666732 ]
  4. Yamaguchi Y, Hironaka K, Okawaki M, Okita R, Matsuura K, Ohshita A, Toge T: HER2-specific cytotoxic activity of lymphokine-activated killer cells in the presence of trastuzumab. Anticancer Res. 2005 Mar-Apr;25(2A):827-32. [PubMed:15868915 ]
  5. Xie Z, Guo N, Yu M, Hu M, Shen B: A new format of bispecific antibody: highly efficient heterodimerization, expression and tumor cell lysis. J Immunol Methods. 2005 Jan;296(1-2):95-101. Epub 2004 Nov 19. [PubMed:15680154 ]
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. Suzuki E, Niwa R, Saji S, Muta M, Hirose M, Iida S, Shiotsu Y, Satoh M, Shitara K, Kondo M, Toi M: A nonfucosylated anti-HER2 antibody augments antibody-dependent cellular cytotoxicity in breast cancer patients. Clin Cancer Res. 2007 Mar 15;13(6):1875-82. [PubMed:17363544 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Oxygen binding
Specific Function:
Catalyzes the formation of aromatic C18 estrogens from C19 androgens.
Gene Name:
CYP19A1
Uniprot ID:
P11511
Molecular Weight:
57882.48 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
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Drug created on June 13, 2005 07:24 / Updated on March 14, 2016 09:58