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Identification
NameRituximab
Accession NumberDB00073  (BTD00014, BIOD00014)
TypeBiotech
GroupsApproved
DescriptionRituxan is a genetically engineered chimeric murine/human monoclonal antibody directed against the CD20 antigen found on the surface of normal and malignant B lymphocytes. The antibody is an IgG1 kappa immunoglobulin containing murine light- and heavy-chain variable region sequences and human constant region sequences. Rituximab is composed of two heavy chains of 451 amino acids and two light chains of 213 amino acids
Protein structureDb00073
Related Articles
Protein chemical formulaC6416H9874N1688O1987S44
Protein average weight143859.7 Da
Sequences
>Rituximab heavy chain chimeric
QVQLQQPGAELVKPGASVKMSCKASGYTFTSYNMHWVKQTPGRGLEWIGAIYPGNGDTSY
NQKFKGKATLTADKSSSTAYMQLSSLTSEDSAVYYCARSTYYGGDWYFNVWGAGTTVTVS
AASTKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQS
SGLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKAEPKSCDKTHTCPPCPAPELLG
GPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQY
NSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRD
ELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSR
WQQGNVFSCSVMHEALHNHYTQKSLSLSPGK
>Rituximab light chain chimeric
QIVLSQSPAILSASPGEKVTMTCRASSSVSYIHWFQQKPGSSPKPWIYATSNLASGVPVR
FSGSGSGTSYSLTISRVEAEDAATYYCQQWTSNPPTFGGGTKLEIKRTVAAPSVFIFPPS
DEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTLTL
SKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC
Download FASTA Format
Synonyms
AntiCD20
Ig gamma-1 chain C region
External Identifiers
  • IDEC-C2B8
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Rituxaninjection, solution10 mg/mLintravenousGenentech, Inc.1997-11-26Not applicableUs
Rituxaninjection, solution10 mg/mLintravenousGenentech, Inc.1997-11-26Not applicableUs
Rituxansolution10 mgintravenousHoffmann La Roche Limited2000-03-20Not applicableCanada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
MabTheraRoche
Brand mixturesNot Available
SaltsNot Available
Categories
UNII4F4X42SYQ6
CAS number174722-31-7
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 CD20-positive non-Hodgkins lymphoma, chronic lymphocytic leukemia, and rheumatoid arthritis.
PharmacodynamicsRituximab binds to the CD20 antigen, which is predominantly expressed on mature B cells and on >90% of B-cell non-Hodgkin's lympohomas. The antibody leads to selective killing of B-cells.
Mechanism of actionThe Fab regions of rituximab binds to the CD20 antigen on B lymphocytes, while the Fc domain recruits antibodies and complements to mediate cell lysis.
Related Articles
AbsorptionNot Available
Volume of distribution
  • 3.1 L
Protein bindingNot Available
Metabolism

Most likely removed by opsonization via the reticuloendothelial system when bound to B lymphocytes, or by human antimurine antibody production

Route of eliminationNot Available
Half life0.8 hours (mammalian reticulocytes, in vitro)
Clearance
  • 0.34 L/day [RA patients]
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated Effects
Interacting Gene/EnzymeSNP RS IDAllele nameDefining changeEffectReference(s)
Low affinity immunoglobulin gamma Fc region receptor III-A
Gene symbol: FCGR3A
UniProt: P08637
rs396991 Not AvailableA > CBetter response to drug therapy (compared to allele A)16609067
SNP Mediated Adverse Drug ReactionsNot Available
Pharmacoeconomics
Manufacturers
  • Roche
Packagers
Dosage forms
FormRouteStrength
Injection, solutionintravenous10 mg/mL
Solutionintravenous10 mg
Prices
Unit descriptionCostUnit
Rituxan 10 mg/ml Concentrate 10ml Vial708.17USD vial
Rituxan 10 mg/ml vial68.09USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA1336826 No1995-08-292012-08-29Canada
CA2149329 No2008-07-152013-11-12Canada
US5736137 No1998-04-072015-04-07Us
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-0.414Not Available
isoelectric point8.68Not Available
References
Synthesis ReferenceNot Available
General References
  1. McLaughlin P, Grillo-Lopez AJ, Link BK, Levy R, Czuczman MS, Williams ME, Heyman MR, Bence-Bruckler I, White CA, Cabanillas F, Jain V, Ho AD, Lister J, Wey K, Shen D, Dallaire BK: Rituximab chimeric anti-CD20 monoclonal antibody therapy for relapsed indolent lymphoma: half of patients respond to a four-dose treatment program. J Clin Oncol. 1998 Aug;16(8):2825-33. [PubMed:9704735 ]
  2. Edwards JC, Szczepanski L, Szechinski J, Filipowicz-Sosnowska A, Emery P, Close DR, Stevens RM, Shaw T: Efficacy of B-cell-targeted therapy with rituximab in patients with rheumatoid arthritis. N Engl J Med. 2004 Jun 17;350(25):2572-81. [PubMed:15201414 ]
  3. Braendstrup P, Bjerrum OW, Nielsen OJ, Jensen BA, Clausen NT, Hansen PB, Andersen I, Schmidt K, Andersen TM, Peterslund NA, Birgens HS, Plesner T, Pedersen BB, Hasselbalch HC: Rituximab chimeric anti-CD20 monoclonal antibody treatment for adult refractory idiopathic thrombocytopenic purpura. Am J Hematol. 2005 Apr;78(4):275-80. [PubMed:15795920 ]
  4. Binder M, Otto F, Mertelsmann R, Veelken H, Trepel M: The epitope recognized by rituximab. Blood. 2006 Sep 15;108(6):1975-8. Epub 2006 May 16. [PubMed:16705086 ]
  5. Burton C, Kaczmarski R, Jan-Mohamed R: Interstitial pneumonitis related to rituximab therapy. N Engl J Med. 2003 Jun 26;348(26):2690-1; discussion 2690-1. [PubMed:12826649 ]
  6. Link [Link]
  7. Link [Link]
External Links
ATC CodesL01XC02
AHFS Codes
  • 10:00.00
PDB Entries
FDA labelDownload (401 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
AbataceptThe risk or severity of adverse effects can be increased when Rituximab is combined with Abatacept.
AcebutololAcebutolol may increase the hypotensive activities of Rituximab.
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Rituximab.
AliskirenAliskiren may increase the hypotensive activities of Rituximab.
AlprenololAlprenolol may increase the hypotensive activities of Rituximab.
AmbrisentanAmbrisentan may increase the hypotensive activities of Rituximab.
AmlodipineAmlodipine may increase the hypotensive activities of Rituximab.
AtenololAtenolol may increase the hypotensive activities of Rituximab.
BelimumabThe risk or severity of adverse effects can be increased when Rituximab is combined with Belimumab.
BenazeprilBenazepril may increase the hypotensive activities of Rituximab.
BendroflumethiazideBendroflumethiazide may increase the hypotensive activities of Rituximab.
BepridilBepridil may increase the hypotensive activities of Rituximab.
BetaxololBetaxolol may increase the hypotensive activities of Rituximab.
BethanidineBethanidine may increase the hypotensive activities of Rituximab.
BevacizumabBevacizumab may increase the cardiotoxic activities of Rituximab.
BimatoprostBimatoprost may increase the hypotensive activities of Rituximab.
BisoprololBisoprolol may increase the hypotensive activities of Rituximab.
BosentanBosentan may increase the hypotensive activities of Rituximab.
BretyliumBretylium may increase the hypotensive activities of Rituximab.
BrimonidineBrimonidine may increase the hypotensive activities of Rituximab.
BupranololBupranolol may increase the hypotensive activities of Rituximab.
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with Rituximab.
CandesartanCandesartan may increase the hypotensive activities of Rituximab.
CandoxatrilCandoxatril may increase the hypotensive activities of Rituximab.
CaptoprilCaptopril may increase the hypotensive activities of Rituximab.
CarteololCarteolol may increase the hypotensive activities of Rituximab.
CarvedilolCarvedilol may increase the hypotensive activities of Rituximab.
CeliprololCeliprolol may increase the hypotensive activities of Rituximab.
Certolizumab pegolRituximab may increase the immunosuppressive activities of Certolizumab pegol.
ChlorothiazideChlorothiazide may increase the hypotensive activities of Rituximab.
ChlorthalidoneChlorthalidone may increase the hypotensive activities of Rituximab.
CilazaprilCilazapril may increase the hypotensive activities of Rituximab.
ClonidineClonidine may increase the hypotensive activities of Rituximab.
ClozapineThe risk or severity of adverse effects can be increased when Rituximab is combined with Clozapine.
CryptenamineCryptenamine may increase the hypotensive activities of Rituximab.
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Rituximab.
CyclothiazideCyclothiazide may increase the hypotensive activities of Rituximab.
DebrisoquinDebrisoquin may increase the hypotensive activities of Rituximab.
DenosumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Rituximab.
DeserpidineDeserpidine may increase the hypotensive activities of Rituximab.
DeslanosideDeslanoside may decrease the cardiotoxic activities of Rituximab.
DiazoxideDiazoxide may increase the hypotensive activities of Rituximab.
DigitoxinDigitoxin may decrease the cardiotoxic activities of Rituximab.
DigoxinDigoxin may decrease the cardiotoxic activities of Rituximab.
DiltiazemDiltiazem may increase the hypotensive activities of Rituximab.
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Rituximab.
DorzolamideDorzolamide may increase the hypotensive activities of Rituximab.
DoxazosinDoxazosin may increase the hypotensive activities of Rituximab.
EfonidipineEfonidipine may increase the hypotensive activities of Rituximab.
EnalaprilEnalapril may increase the hypotensive activities of Rituximab.
EnalaprilatEnalaprilat may increase the hypotensive activities of Rituximab.
EpoprostenolEpoprostenol may increase the hypotensive activities of Rituximab.
EprosartanEprosartan may increase the hypotensive activities of Rituximab.
FelodipineFelodipine may increase the hypotensive activities of Rituximab.
FenoldopamFenoldopam may increase the hypotensive activities of Rituximab.
FingolimodRituximab may increase the immunosuppressive activities of Fingolimod.
FosinoprilFosinopril may increase the hypotensive activities of Rituximab.
GuanabenzGuanabenz may increase the hypotensive activities of Rituximab.
GuanadrelGuanadrel may increase the hypotensive activities of Rituximab.
GuanethidineGuanethidine may increase the hypotensive activities of Rituximab.
GuanfacineGuanfacine may increase the hypotensive activities of Rituximab.
HexamethoniumHexamethonium may increase the hypotensive activities of Rituximab.
HydralazineHydralazine may increase the hypotensive activities of Rituximab.
HydrochlorothiazideHydrochlorothiazide may increase the hypotensive activities of Rituximab.
HydroflumethiazideHydroflumethiazide may increase the hypotensive activities of Rituximab.
IndapamideIndapamide may increase the hypotensive activities of Rituximab.
IndenololIndenolol may increase the hypotensive activities of Rituximab.
IndoraminIndoramin may increase the hypotensive activities of Rituximab.
IrbesartanIrbesartan may increase the hypotensive activities of Rituximab.
IsradipineIsradipine may increase the hypotensive activities of Rituximab.
LabetalolLabetalol may increase the hypotensive activities of Rituximab.
LacidipineLacidipine may increase the hypotensive activities of Rituximab.
LatanoprostLatanoprost may increase the hypotensive activities of Rituximab.
LeflunomideThe risk or severity of adverse effects can be increased when Rituximab is combined with Leflunomide.
LercanidipineLercanidipine may increase the hypotensive activities of Rituximab.
LisinoprilLisinopril may increase the hypotensive activities of Rituximab.
LofexidineLofexidine may increase the hypotensive activities of Rituximab.
LosartanLosartan may increase the hypotensive activities of Rituximab.
MacitentanMacitentan may increase the hypotensive activities of Rituximab.
ManidipineManidipine may increase the hypotensive activities of Rituximab.
MecamylamineMecamylamine may increase the hypotensive activities of Rituximab.
MetamizoleThe risk or severity of adverse effects can be increased when Metamizole is combined with Rituximab.
MethyldopaMethyldopa may increase the hypotensive activities of Rituximab.
MetipranololMetipranolol may increase the hypotensive activities of Rituximab.
MetolazoneMetolazone may increase the hypotensive activities of Rituximab.
MetoprololMetoprolol may increase the hypotensive activities of Rituximab.
MibefradilMibefradil may increase the hypotensive activities of Rituximab.
MinoxidilMinoxidil may increase the hypotensive activities of Rituximab.
MoexiprilMoexipril may increase the hypotensive activities of Rituximab.
MoxonidineMoxonidine may increase the hypotensive activities of Rituximab.
NadololNadolol may increase the hypotensive activities of Rituximab.
NatalizumabThe risk or severity of adverse effects can be increased when Rituximab is combined with Natalizumab.
NebivololNebivolol may increase the hypotensive activities of Rituximab.
NicardipineNicardipine may increase the hypotensive activities of Rituximab.
NicorandilNicorandil may increase the hypotensive activities of Rituximab.
NiguldipineNiguldipine may increase the hypotensive activities of Rituximab.
NilvadipineNilvadipine may increase the hypotensive activities of Rituximab.
NimodipineNimodipine may increase the hypotensive activities of Rituximab.
NisoldipineNisoldipine may increase the hypotensive activities of Rituximab.
NitrendipineNitrendipine may increase the hypotensive activities of Rituximab.
NitroprussideNitroprusside may increase the hypotensive activities of Rituximab.
OlmesartanOlmesartan may increase the hypotensive activities of Rituximab.
OmapatrilatOmapatrilat may increase the hypotensive activities of Rituximab.
OuabainOuabain may decrease the cardiotoxic activities of Rituximab.
OxprenololOxprenolol may increase the hypotensive activities of Rituximab.
PaclitaxelThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Rituximab.
PargylinePargyline may increase the hypotensive activities of Rituximab.
PenbutololPenbutolol may increase the hypotensive activities of Rituximab.
PentoliniumPentolinium may increase the hypotensive activities of Rituximab.
PerindoprilPerindopril may increase the hypotensive activities of Rituximab.
PhenoxybenzaminePhenoxybenzamine may increase the hypotensive activities of Rituximab.
PhentolaminePhentolamine may increase the hypotensive activities of Rituximab.
PimecrolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Rituximab.
PinacidilPinacidil may increase the hypotensive activities of Rituximab.
PindololPindolol may increase the hypotensive activities of Rituximab.
PolythiazidePolythiazide may increase the hypotensive activities of Rituximab.
PrazosinPrazosin may increase the hypotensive activities of Rituximab.
PropranololPropranolol may increase the hypotensive activities of Rituximab.
QuinaprilQuinapril may increase the hypotensive activities of Rituximab.
Rabies vaccineThe risk or severity of adverse effects can be increased when Rituximab is combined with Rabies vaccine.
RamiprilRamipril may increase the hypotensive activities of Rituximab.
RemikirenRemikiren may increase the hypotensive activities of Rituximab.
RescinnamineRescinnamine may increase the hypotensive activities of Rituximab.
ReserpineReserpine may increase the hypotensive activities of Rituximab.
RiociguatRiociguat may increase the hypotensive activities of Rituximab.
RoflumilastRoflumilast may increase the immunosuppressive activities of Rituximab.
SaprisartanSaprisartan may increase the hypotensive activities of Rituximab.
SelexipagSelexipag may increase the hypotensive activities of Rituximab.
Sipuleucel-TThe therapeutic efficacy of Sipuleucel-T can be decreased when used in combination with Rituximab.
SitaxentanSitaxentan may increase the hypotensive activities of Rituximab.
SpiraprilSpirapril may increase the hypotensive activities of Rituximab.
TacrolimusThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Rituximab.
TelmisartanTelmisartan may increase the hypotensive activities of Rituximab.
TemocaprilTemocapril may increase the hypotensive activities of Rituximab.
TerlipressinTerlipressin may increase the hypotensive activities of Rituximab.
TiboloneTibolone may increase the hypotensive activities of Rituximab.
TicrynafenTicrynafen may increase the hypotensive activities of Rituximab.
TimololTimolol may increase the hypotensive activities of Rituximab.
TofacitinibRituximab may increase the immunosuppressive activities of Tofacitinib.
TolazolineTolazoline may increase the hypotensive activities of Rituximab.
TorasemideTorasemide may increase the hypotensive activities of Rituximab.
TrandolaprilTrandolapril may increase the hypotensive activities of Rituximab.
TrastuzumabTrastuzumab may increase the neutropenic activities of Rituximab.
TravoprostTravoprost may increase the hypotensive activities of Rituximab.
TreprostinilTreprostinil may increase the hypotensive activities of Rituximab.
TrichlormethiazideTrichlormethiazide may increase the hypotensive activities of Rituximab.
TrimazosinTrimazosin may increase the hypotensive activities of Rituximab.
TrimethaphanTrimethaphan may increase the hypotensive activities of Rituximab.
UnoprostoneUnoprostone may increase the hypotensive activities of Rituximab.
ValsartanValsartan may increase the hypotensive activities of Rituximab.
XylometazolineXylometazoline may increase the hypotensive activities of Rituximab.
Food InteractionsNot Available

Targets

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. Treon SP, Hansen M, Branagan AR, Verselis S, Emmanouilides C, Kimby E, Frankel SR, Touroutoglou N, Turnbull B, Anderson KC, Maloney DG, Fox EA: Polymorphisms in FcgammaRIIIA (CD16) receptor expression are associated with clinical response to rituximab in Waldenstrom's macroglobulinemia. J Clin Oncol. 2005 Jan 20;23(3):474-81. [PubMed:15659493 ]
  2. 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 ]
  3. Bowles JA, Wang SY, Link BK, Allan B, Beuerlein G, Campbell MA, Marquis D, Ondek B, Wooldridge JE, Smith BJ, Breitmeyer JB, Weiner GJ: Anti-CD20 monoclonal antibody with enhanced affinity for CD16 activates NK cells at lower concentrations and more effectively than rituximab. Blood. 2006 Oct 15;108(8):2648-54. Epub 2006 Jul 6. [PubMed:16825493 ]
  4. Hatjiharissi E, Xu L, Santos DD, Hunter ZR, Ciccarelli BT, Verselis S, Modica M, Cao Y, Manning RJ, Leleu X, Dimmock EA, Kortsaris A, Mitsiades C, Anderson KC, Fox EA, Treon SP: Increased natural killer cell expression of CD16, augmented binding and ADCC activity to rituximab among individuals expressing the Fc{gamma}RIIIa-158 V/V and V/F polymorphism. Blood. 2007 Oct 1;110(7):2561-4. Epub 2007 May 2. [PubMed:17475906 ]
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 ]
  3. Di Gaetano N, Cittera E, Nota R, Vecchi A, Grieco V, Scanziani E, Botto M, Introna M, Golay J: Complement activation determines the therapeutic activity of rituximab in vivo. J Immunol. 2003 Aug 1;171(3):1581-7. [PubMed:12874252 ]
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. Niwa R, Hatanaka S, Shoji-Hosaka E, Sakurada M, Kobayashi Y, Uehara A, Yokoi H, Nakamura K, Shitara K: Enhancement of the antibody-dependent cellular cytotoxicity of low-fucose IgG1 Is independent of FcgammaRIIIa functional polymorphism. Clin Cancer Res. 2004 Sep 15;10(18 Pt 1):6248-55. [PubMed:15448014 ]
  2. Hatjiharissi E, Hansen M, Santos DD, Xu L, Leleu X, Dimmock EW, Ho AW, Hunter ZR, Branagan AR, Patterson CJ, Kortsaris A, Verselis S, Fox E, Treon SP: Genetic linkage of Fc gamma RIIa and Fc gamma RIIIa and implications for their use in predicting clinical responses to CD20-directed monoclonal antibody therapy. Clin Lymphoma Myeloma. 2007 Jan;7(4):286-90. [PubMed:17324336 ]
  3. Kim DH, Jung HD, Kim JG, Lee JJ, Yang DH, Park YH, Do YR, Shin HJ, Kim MK, Hyun MS, Sohn SK: FCGR3A gene polymorphisms may correlate with response to frontline R-CHOP therapy for diffuse large B-cell lymphoma. Blood. 2006 Oct 15;108(8):2720-5. Epub 2006 Apr 11. [PubMed:16609067 ]
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 ]
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. Hatjiharissi E, Hansen M, Santos DD, Xu L, Leleu X, Dimmock EW, Ho AW, Hunter ZR, Branagan AR, Patterson CJ, Kortsaris A, Verselis S, Fox E, Treon SP: Genetic linkage of Fc gamma RIIa and Fc gamma RIIIa and implications for their use in predicting clinical responses to CD20-directed monoclonal antibody therapy. Clin Lymphoma Myeloma. 2007 Jan;7(4):286-90. [PubMed:17324336 ]
  2. Kim DH, Jung HD, Kim JG, Lee JJ, Yang DH, Park YH, Do YR, Shin HJ, Kim MK, Hyun MS, Sohn SK: FCGR3A gene polymorphisms may correlate with response to frontline R-CHOP therapy for diffuse large B-cell lymphoma. Blood. 2006 Oct 15;108(8):2720-5. Epub 2006 Apr 11. [PubMed:16609067 ]
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
yes
Actions
antibody
General Function:
Mhc class ii protein complex binding
Specific Function:
This protein may be involved in the regulation of B-cell activation and proliferation.
Gene Name:
MS4A1
Uniprot ID:
P11836
Molecular Weight:
33076.99 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. van Meerten T, Hagenbeek A: CD20-targeted therapy: the next generation of antibodies. Semin Hematol. 2010 Apr;47(2):199-210. doi: 10.1053/j.seminhematol.2010.01.007. [PubMed:20350667 ]
  3. Jaglowski SM, Byrd JC: Rituximab in chronic lymphocytic leukemia. Semin Hematol. 2010 Apr;47(2):156-69. doi: 10.1053/j.seminhematol.2010.01.005. [PubMed:20350663 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23