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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
RituxanSolution10 mgIntravenousHoffmann La Roche Limited2000-03-20Not applicableCanada
RituxanInjection, solution10 mg/mLIntravenousGenentech, Inc.1997-11-26Not applicableUs
RituxanInjection, solution10 mg/mLIntravenousGenentech, Inc.1997-11-26Not applicableUs
Rituxan ScSolution120 mgSubcutaneousHoffmann La Roche LimitedNot applicableNot 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
Pharmacology
IndicationFor treatment of CD20-positive non-Hodgkins lymphoma, chronic lymphocytic leukemia, and rheumatoid arthritis.
Structured Indications Not Available
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.
TargetKindPharmacological actionActionsOrganismUniProt ID
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
B-lymphocyte antigen CD20Proteinyes
antibody
HumanP11836 details
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
Interactions
Drug Interactions
DrugInteractionDrug group
AbataceptThe risk or severity of adverse effects can be increased when Rituximab is combined with Abatacept.Approved
AcebutololAcebutolol may increase the hypotensive activities of Rituximab.Approved
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Rituximab.Approved
AdalimumabThe risk or severity of adverse effects can be increased when Adalimumab is combined with Rituximab.Approved
AliskirenAliskiren may increase the hypotensive activities of Rituximab.Approved, Investigational
AlprenololAlprenolol may increase the hypotensive activities of Rituximab.Approved, Withdrawn
ALT-110The risk or severity of adverse effects can be increased when Rituximab is combined with ALT-110.Investigational
AmbrisentanAmbrisentan may increase the hypotensive activities of Rituximab.Approved, Investigational
AmlodipineAmlodipine may increase the hypotensive activities of Rituximab.Approved
AnakinraThe risk or severity of adverse effects can be increased when Anakinra is combined with Rituximab.Approved
AnvirzelAnvirzel may decrease the cardiotoxic activities of Rituximab.Investigational
AtenololAtenolol may increase the hypotensive activities of Rituximab.Approved
BcgThe therapeutic efficacy of Bcg can be decreased when used in combination with Rituximab.Investigational
BelimumabThe risk or severity of adverse effects can be increased when Rituximab is combined with Belimumab.Approved
BenazeprilBenazepril may increase the hypotensive activities of Rituximab.Approved, Investigational
BendroflumethiazideBendroflumethiazide may increase the hypotensive activities of Rituximab.Approved
BepridilBepridil may increase the hypotensive activities of Rituximab.Approved, Withdrawn
BetaxololBetaxolol may increase the hypotensive activities of Rituximab.Approved
BethanidineBethanidine may increase the hypotensive activities of Rituximab.Approved
BevacizumabBevacizumab may increase the cardiotoxic activities of Rituximab.Approved, Investigational
BimatoprostBimatoprost may increase the hypotensive activities of Rituximab.Approved, Investigational
BisoprololBisoprolol may increase the hypotensive activities of Rituximab.Approved
BosentanBosentan may increase the hypotensive activities of Rituximab.Approved, Investigational
BretyliumBretylium may increase the hypotensive activities of Rituximab.Approved
BrimonidineBrimonidine may increase the hypotensive activities of Rituximab.Approved
BupranololBupranolol may increase the hypotensive activities of Rituximab.Approved
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with Rituximab.Approved
CandesartanCandesartan may increase the hypotensive activities of Rituximab.Approved
CandoxatrilCandoxatril may increase the hypotensive activities of Rituximab.Experimental
CaptoprilCaptopril may increase the hypotensive activities of Rituximab.Approved
CarteololCarteolol may increase the hypotensive activities of Rituximab.Approved
CarvedilolCarvedilol may increase the hypotensive activities of Rituximab.Approved, Investigational
CDX-110The risk or severity of adverse effects can be increased when Rituximab is combined with CDX-110.Investigational
CeliprololCeliprolol may increase the hypotensive activities of Rituximab.Approved, Investigational
Certolizumab pegolRituximab may increase the immunosuppressive activities of Certolizumab pegol.Approved
ChlorothiazideChlorothiazide may increase the hypotensive activities of Rituximab.Approved, Vet Approved
ChlorthalidoneChlorthalidone may increase the hypotensive activities of Rituximab.Approved
CilazaprilCilazapril may increase the hypotensive activities of Rituximab.Approved
ClonidineClonidine may increase the hypotensive activities of Rituximab.Approved
ClozapineThe risk or severity of adverse effects can be increased when Rituximab is combined with Clozapine.Approved
CryptenamineCryptenamine may increase the hypotensive activities of Rituximab.Approved
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Rituximab.Approved, Investigational
CyclothiazideCyclothiazide may increase the hypotensive activities of Rituximab.Approved
DebrisoquinDebrisoquin may increase the hypotensive activities of Rituximab.Approved
DenosumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Rituximab.Approved
DeserpidineDeserpidine may increase the hypotensive activities of Rituximab.Approved
DeslanosideDeslanoside may decrease the cardiotoxic activities of Rituximab.Approved
DiazoxideDiazoxide may increase the hypotensive activities of Rituximab.Approved
DigitoxinDigitoxin may decrease the cardiotoxic activities of Rituximab.Approved
DigoxinDigoxin may decrease the cardiotoxic activities of Rituximab.Approved
DihydralazineDihydralazine may increase the hypotensive activities of Rituximab.Investigational
DiltiazemDiltiazem may increase the hypotensive activities of Rituximab.Approved
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Rituximab.Approved, Investigational
DorzolamideDorzolamide may increase the hypotensive activities of Rituximab.Approved
DoxazosinDoxazosin may increase the hypotensive activities of Rituximab.Approved
EfonidipineEfonidipine may increase the hypotensive activities of Rituximab.Approved
EnalaprilEnalapril may increase the hypotensive activities of Rituximab.Approved, Vet Approved
EnalaprilatEnalaprilat may increase the hypotensive activities of Rituximab.Approved
EpoprostenolEpoprostenol may increase the hypotensive activities of Rituximab.Approved
EprosartanEprosartan may increase the hypotensive activities of Rituximab.Approved
EtanerceptThe risk or severity of adverse effects can be increased when Etanercept is combined with Rituximab.Approved, Investigational
FelodipineFelodipine may increase the hypotensive activities of Rituximab.Approved, Investigational
FenoldopamFenoldopam may increase the hypotensive activities of Rituximab.Approved
FingolimodRituximab may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
FosinoprilFosinopril may increase the hypotensive activities of Rituximab.Approved
G17DTThe risk or severity of adverse effects can be increased when Rituximab is combined with G17DT.Investigational
GI-5005The risk or severity of adverse effects can be increased when Rituximab is combined with GI-5005.Investigational
GolimumabThe risk or severity of adverse effects can be increased when Golimumab is combined with Rituximab.Approved
GuanabenzGuanabenz may increase the hypotensive activities of Rituximab.Approved
GuanadrelGuanadrel may increase the hypotensive activities of Rituximab.Approved
GuanethidineGuanethidine may increase the hypotensive activities of Rituximab.Approved
GuanfacineGuanfacine may increase the hypotensive activities of Rituximab.Approved, Investigational
HexamethoniumHexamethonium may increase the hypotensive activities of Rituximab.Experimental
HydralazineHydralazine may increase the hypotensive activities of Rituximab.Approved
HydrochlorothiazideHydrochlorothiazide may increase the hypotensive activities of Rituximab.Approved, Vet Approved
HydroflumethiazideHydroflumethiazide may increase the hypotensive activities of Rituximab.Approved
ImidaprilImidapril may increase the hypotensive activities of Rituximab.Investigational
IndapamideIndapamide may increase the hypotensive activities of Rituximab.Approved
IndenololIndenolol may increase the hypotensive activities of Rituximab.Withdrawn
IndoraminIndoramin may increase the hypotensive activities of Rituximab.Withdrawn
InfliximabThe risk or severity of adverse effects can be increased when Infliximab is combined with Rituximab.Approved
INGN 201The risk or severity of adverse effects can be increased when Rituximab is combined with INGN 201.Investigational
INGN 225The risk or severity of adverse effects can be increased when Rituximab is combined with INGN 225.Investigational
IrbesartanIrbesartan may increase the hypotensive activities of Rituximab.Approved, Investigational
IsradipineIsradipine may increase the hypotensive activities of Rituximab.Approved
KetanserinKetanserin may increase the hypotensive activities of Rituximab.Investigational
LabetalolLabetalol may increase the hypotensive activities of Rituximab.Approved
LacidipineLacidipine may increase the hypotensive activities of Rituximab.Approved
LatanoprostLatanoprost may increase the hypotensive activities of Rituximab.Approved, Investigational
LeflunomideThe risk or severity of adverse effects can be increased when Rituximab is combined with Leflunomide.Approved, Investigational
LercanidipineLercanidipine may increase the hypotensive activities of Rituximab.Approved, Investigational
LisinoprilLisinopril may increase the hypotensive activities of Rituximab.Approved, Investigational
LofexidineLofexidine may increase the hypotensive activities of Rituximab.Approved, Investigational
LosartanLosartan may increase the hypotensive activities of Rituximab.Approved
MacitentanMacitentan may increase the hypotensive activities of Rituximab.Approved
ManidipineManidipine may increase the hypotensive activities of Rituximab.Approved
MecamylamineMecamylamine may increase the hypotensive activities of Rituximab.Approved
MetamizoleThe risk or severity of adverse effects can be increased when Metamizole is combined with Rituximab.Withdrawn
MethyldopaMethyldopa may increase the hypotensive activities of Rituximab.Approved
MetipranololMetipranolol may increase the hypotensive activities of Rituximab.Approved
MetolazoneMetolazone may increase the hypotensive activities of Rituximab.Approved
MetoprololMetoprolol may increase the hypotensive activities of Rituximab.Approved, Investigational
MetyrosineMetyrosine may increase the hypotensive activities of Rituximab.Approved
MibefradilMibefradil may increase the hypotensive activities of Rituximab.Withdrawn
MinoxidilMinoxidil may increase the hypotensive activities of Rituximab.Approved
MoexiprilMoexipril may increase the hypotensive activities of Rituximab.Approved
MoxonidineMoxonidine may increase the hypotensive activities of Rituximab.Approved
NadololNadolol may increase the hypotensive activities of Rituximab.Approved
NaftopidilNaftopidil may increase the hypotensive activities of Rituximab.Investigational
NatalizumabThe risk or severity of adverse effects can be increased when Rituximab is combined with Natalizumab.Approved, Investigational
NebivololNebivolol may increase the hypotensive activities of Rituximab.Approved, Investigational
NicardipineNicardipine may increase the hypotensive activities of Rituximab.Approved
NicorandilNicorandil may increase the hypotensive activities of Rituximab.Approved
NiguldipineNiguldipine may increase the hypotensive activities of Rituximab.Experimental
NilvadipineNilvadipine may increase the hypotensive activities of Rituximab.Approved
NimodipineNimodipine may increase the hypotensive activities of Rituximab.Approved
NisoldipineNisoldipine may increase the hypotensive activities of Rituximab.Approved
NitrendipineNitrendipine may increase the hypotensive activities of Rituximab.Approved
NitroprussideNitroprusside may increase the hypotensive activities of Rituximab.Approved
OlmesartanOlmesartan may increase the hypotensive activities of Rituximab.Approved, Investigational
OmapatrilatOmapatrilat may increase the hypotensive activities of Rituximab.Investigational
OuabainOuabain may decrease the cardiotoxic activities of Rituximab.Approved
OxprenololOxprenolol may increase the hypotensive activities of Rituximab.Approved
PaclitaxelThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Rituximab.Approved, Vet Approved
PargylinePargyline may increase the hypotensive activities of Rituximab.Approved
PenbutololPenbutolol may increase the hypotensive activities of Rituximab.Approved, Investigational
PentoliniumPentolinium may increase the hypotensive activities of Rituximab.Approved
PerindoprilPerindopril may increase the hypotensive activities of Rituximab.Approved
PhenoxybenzaminePhenoxybenzamine may increase the hypotensive activities of Rituximab.Approved
PhentolaminePhentolamine may increase the hypotensive activities of Rituximab.Approved
PimecrolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Rituximab.Approved, Investigational
PinacidilPinacidil may increase the hypotensive activities of Rituximab.Withdrawn
PindololPindolol may increase the hypotensive activities of Rituximab.Approved
PolythiazidePolythiazide may increase the hypotensive activities of Rituximab.Approved
PrazosinPrazosin may increase the hypotensive activities of Rituximab.Approved
PropranololPropranolol may increase the hypotensive activities of Rituximab.Approved, Investigational
QuinaprilQuinapril may increase the hypotensive activities of Rituximab.Approved, Investigational
Rabies vaccineThe risk or severity of adverse effects can be increased when Rituximab is combined with Rabies vaccine.Approved
Rabies vaccineThe therapeutic efficacy of Rabies vaccine can be decreased when used in combination with Rituximab.Approved
RamiprilRamipril may increase the hypotensive activities of Rituximab.Approved
RemikirenRemikiren may increase the hypotensive activities of Rituximab.Approved
RescinnamineRescinnamine may increase the hypotensive activities of Rituximab.Approved
ReserpineReserpine may increase the hypotensive activities of Rituximab.Approved
RilmenidineRilmenidine may increase the hypotensive activities of Rituximab.Investigational
RiociguatRiociguat may increase the hypotensive activities of Rituximab.Approved
RoflumilastRoflumilast may increase the immunosuppressive activities of Rituximab.Approved
SaprisartanSaprisartan may increase the hypotensive activities of Rituximab.Experimental
SelexipagSelexipag may increase the hypotensive activities of Rituximab.Approved
Sipuleucel-TThe therapeutic efficacy of Sipuleucel-T can be decreased when used in combination with Rituximab.Approved
SitaxentanSitaxentan may increase the hypotensive activities of Rituximab.Approved, Investigational, Withdrawn
SpiraprilSpirapril may increase the hypotensive activities of Rituximab.Approved
SRP 299The risk or severity of adverse effects can be increased when Rituximab is combined with SRP 299.Investigational
TacrolimusThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Rituximab.Approved, Investigational
TelmisartanTelmisartan may increase the hypotensive activities of Rituximab.Approved, Investigational
TemocaprilTemocapril may increase the hypotensive activities of Rituximab.Experimental, Investigational
TerlipressinTerlipressin may increase the hypotensive activities of Rituximab.Approved, Investigational
TG4010The risk or severity of adverse effects can be increased when Rituximab is combined with TG4010.Investigational
TiboloneTibolone may increase the hypotensive activities of Rituximab.Approved
TicrynafenTicrynafen may increase the hypotensive activities of Rituximab.Withdrawn
TimololTimolol may increase the hypotensive activities of Rituximab.Approved
TocilizumabThe risk or severity of adverse effects can be increased when Rituximab is combined with Tocilizumab.Approved
TofacitinibThe risk or severity of adverse effects can be increased when Rituximab is combined with Tofacitinib.Approved, Investigational
TolazolineTolazoline may increase the hypotensive activities of Rituximab.Approved, Vet Approved
TorasemideTorasemide may increase the hypotensive activities of Rituximab.Approved
TrandolaprilTrandolapril may increase the hypotensive activities of Rituximab.Approved
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Rituximab.Approved, Investigational
TravoprostTravoprost may increase the hypotensive activities of Rituximab.Approved
TreprostinilTreprostinil may increase the hypotensive activities of Rituximab.Approved, Investigational
TrichlormethiazideTrichlormethiazide may increase the hypotensive activities of Rituximab.Approved, Vet Approved
TrimazosinTrimazosin may increase the hypotensive activities of Rituximab.Experimental
TrimethaphanTrimethaphan may increase the hypotensive activities of Rituximab.Approved
UnoprostoneUnoprostone may increase the hypotensive activities of Rituximab.Approved
ValsartanValsartan may increase the hypotensive activities of Rituximab.Approved, Investigational
VinpocetineVinpocetine may increase the hypotensive activities of Rituximab.Investigational
XylometazolineXylometazoline may increase the hypotensive activities of Rituximab.Approved
Food InteractionsNot 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
Pharmacoeconomics
Manufacturers
  • Roche
Packagers
Dosage forms
FormRouteStrength
Injection, solutionIntravenous10 mg/mL
SolutionIntravenous10 mg
SolutionSubcutaneous120 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
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
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