Target General Infomation
Target ID
T73215
Former ID
TTDS00268
Target Name
B-lymphocyte antigen CD20
Gene Name
MS4A1
Synonyms
B-lymphocyte surface antigen B1; Bp35; CD20; Leu-16; MS4A1
Target Type
Successful
Disease Autoimmune diabetes [ICD10: E08-E13]
Bacterial infections [ICD9: 001-009, 010-018, 020-027, 030-041, 080-088, 090-099, 100-104; ICD10: A00-B99]
B-cell lymphoma [ICD9: 202.8; ICD10: C85.1]
Chronic lymphocytic leukaemia [ICD10: C91]
Cancer [ICD9: 140-229; ICD10: C00-C96]
Cluster headache [ICD10: G44.0]
Chronic lymphocytic leukaemia; Non-hodgkin's lymphoma; Systemic lupus erythematosus [ICD9:710; ICD10: C91, C85, M32]
Diffuse large B-cell lymphoma; Multiple sclerosis [ICD9: 202.8, 340; ICD10: C85.1, G35]
Hematologic malignancies [ICD9: 200-209; ICD10: C81-C86]
Lymphoma [ICD9: 202.8, 208.9; ICD10: C81-C86]
Lymphoma; Non-hodgkin's lymphoma [ICD9: 200, 202, 202.8; ICD10: C81-C86, C82-C85]
Late-stage follicular lymphoma [ICD9: 202.0, 202.8; ICD10: C81-C86, C82]
Mantle cell lymphoma [ICD9: 200.4, 202.8, 203.0, 208.9; ICD10: C81-C86, C85.7, C90.0, C91-C95]
Multiple scierosis [ICD9: 340; ICD10: G35]
Multiple sclerosis; Primary progressive [ICD9: 340; ICD10: G35]
Multiple scierosis; Rheumatoid arthritis [ICD9:340, 710-719, 714; ICD10: G35, M05-M06]
Non-hodgkin's lymphoma [ICD10: C85]
Non-hodgkin's lymphoma; Follicular lymphoma [ICD9: 200, 202, 202.0, 202.8; ICD10: C81-C86, C82, C82-C85]
Pemphigus disease [ICD9: 694.4; ICD10: L10]
Relapsing or primary progressive forms of multiple sclerosis [ICD10: G35]
Rheumatold arthritis; Follicular lymphoma [ICD9: 202.0, 714; ICD10: C82, M05-M06]
Rheumatoid arthritis [ICD9: 710-719, 714; ICD10: M05-M06]
Unspecified [ICD code not available]
Function
This protein may be involved in the regulation of B-cell activation and proliferation.
BioChemical Class
CD20 ca(2+) channel
Target Validation
T73215
UniProt ID
Sequence
MTTPRNSVNGTFPAEPMKGPIAMQSGPKPLFRRMSSLVGPTQSFFMRESKTLGAVQIMNG
LFHIALGGLLMIPAGIYAPICVTVWYPLWGGIMYIISGSLLAATEKNSRKCLVKGKMIMN
SLSLFAAISGMILSIMDILNIKISHFLKMESLNFIRAHTPYINIYNCEPANPSEKNSPST
QYCYSIQSLFLGILSVMLIFAFFQELVIAGIVENEWKRTCSRPKSNIVLLSAEEKKEQTI
EIKEEVVGLTETSSQPKNEEDIEIIPIQEEEEEETETNFPEPPQDQESSPIENDSSP
Drugs and Mode of Action
Drug(s) Ibritumomab Drug Info Approved Non-hodgkin's lymphoma [1]
Obinutuzumab Drug Info Approved Chronic lymphocytic leukaemia [2], [3]
Ocrelizumab Drug Info Approved Relapsing or primary progressive forms of multiple sclerosis [4]
Ofatumumab Drug Info Approved Chronic lymphocytic leukaemia [5], [6]
Rituxan Hemotalogy/oncology Drug Info Approved Non-hodgkin's lymphoma [7]
Rituximab Drug Info Approved Non-hodgkin's lymphoma [8], [9]
Tositumomab Drug Info Approved Non-hodgkin's lymphoma [1], [10]
Bevacizumab + Rituximab Drug Info Phase 3 Lymphoma; Non-hodgkin's lymphoma [11]
MK-8808 Drug Info Phase 3 Late-stage follicular lymphoma [12]
Ofatumumab Drug Info Phase 3 Diffuse large B-cell lymphoma; Multiple sclerosis [5], [6]
PF-05280586 Drug Info Phase 3 Cluster headache [13]
Rituxan Immunology Drug Info Phase 3 Pemphigus disease [14]
AME-133v Drug Info Phase 2 Non-hodgkin's lymphoma [15], [16]
ATM AVI Drug Info Phase 2 Bacterial infections [17]
Ibritumomab Drug Info Phase 2 Mantle cell lymphoma [18], [19]
Iodine-131-tositumomab Drug Info Phase 2 Discovery agent [20]
Ofatumumab Drug Info Phase 2 Rheumatold arthritis; Follicular lymphoma [5], [6]
SBI-087 Drug Info Phase 2 Multiple scierosis; Rheumatoid arthritis [21]
TRU-015 Drug Info Phase 2 Lymphoma [22]
Ublituximab Drug Info Phase 2 Chronic lymphocytic leukaemia [23]
Veltuzumab Drug Info Phase 2 Chronic lymphocytic leukaemia; Non-hodgkin's lymphoma; Systemic lupus erythematosus [24], [25]
DI-Leu16-IL2 Drug Info Phase 1/2 B-cell lymphoma [26]
FBT-A05 Drug Info Phase 1/2 Chronic lymphocytic leukaemia [27]
BM-ca Drug Info Phase 1 Non-hodgkin's lymphoma [28]
CD20Bi aATC Drug Info Phase 1 Non-hodgkin's lymphoma [29]
Iboctadekin + rituximab Drug Info Phase 1 Non-hodgkin's lymphoma; Follicular lymphoma [30]
MK-8808 Drug Info Phase 1 Rheumatoid arthritis [12]
Rituximab Drug Info Phase 1 Hematologic malignancies [8], [9]
Modulator 2LM20-4 Drug Info [31]
Anti-CD20 engineered toxin bodies Drug Info [31]
ATM AVI Drug Info [31]
CD20Bi aATC Drug Info [29]
DI-Leu16-IL2 Drug Info [32]
DXL-625 Drug Info [31]
MEDI-552 Drug Info
Veltuzumab Drug Info [33]
Inhibitor Anti-CD-20 mab Drug Info [31]
SBI-087 Drug Info [34]
Agonist MK-8808 Drug Info [35]
Antagonist PF-05280586 Drug Info [36]
TRU-015 Drug Info [37]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Hematopoietic cell lineage
References
REF 1Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20.
REF 22013 FDA drug approvals. Nat Rev Drug Discov. 2014 Feb;13(2):85-9.
REF 3(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6941).
REF 4Drugs@FDA (Edaravone)
REF 5Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
REF 6(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6778).
REF 7Impact of Rituximab (Rituxan) on the Treatment of B-Cell Non-Hodgkin's Lymphoma. P T. 2010 March; 35(3): 148-157.
REF 8Disease-modifying agents for multiple sclerosis: recent advances and future prospects. Drugs. 2008;68(17):2445-68. doi: 10.2165/0003495-200868170-00004.
REF 9(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6780).
REF 10(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6781).
REF 11ClinicalTrials.gov (NCT00486759) A Study of Bevacizumab (Avastin) in Combination With Rituximab (MabThera) and CHOP (Cyclophosphamide, Hydroxydaunorubicin [Doxorubicin], Oncovin [Vincristine], Prednisone) Chemotherapy in Patients With Diffuse Large B-cell Lymphoma. U.S. National Institutes of Health.
REF 12Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800034367)
REF 13ClinicalTrials.gov (NCT02213263) A Study Of PF-05280586 (Rituximab-Pfizer) Or MabThera (Rituximab-EU) For The First-Line Treatment Of Patients With CD20-Positive, Low Tumor Burden, Follicular Lymphoma (REFLECTIONS B328-06). U.S. National Institutes of Health.
REF 14ClinicalTrials.gov (NCT02383589) A Randomized, Double-Blind Study to Evaluate the Efficacy and Safety of Rituximab Versus MMF in Patients With Pemphigus Vulgaris. U.S. National Institutes of Health.
REF 15ClinicalTrials.gov (NCT00354926) Safety and Efficacy Study of an Anti-CD20 Monoclonal Antibody (AME-133v) to Treat Non-Hodgkin's Lymphoma. U.S. National Institutes of Health.
REF 16J Clin Oncol 30, 2012 (suppl, abstr 8081).
REF 17Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800037513)
REF 18Radiation dosimetry results from a Phase II trial of ibritumomab tiuxetan (Zevalin) radioimmunotherapy for patients with non-Hodgkin's lymphoma and mild thrombocytopenia. Cancer Biother Radiopharm. 2003 Apr;18(2):165-78.
REF 19(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6777).
REF 20ClinicalTrials.gov (NCT01224821) Dosimetry/Validation Study of 131Iodine-Anti B1 (Murine) Radioimmunotherapy for Chemotherapy Refractory Low Grade B Cell Lymphomas and Low Grade Lymphomas That Have Transformed to Higher Grade Histologies. U.S. National Institutes of Health.
REF 21ClinicalTrials.gov (NCT01008852) Study Evaluating The Efficacy And Safety Of SBI-087 In Seropositive Subjects With Active Rheumatoid Arthritis. U.S. National Institutes of Health.
REF 22ClinicalTrials.gov (NCT00634933) Study Evaluating 2 Dosing Regimens Of TRU-015 In Rheumatoid Arthritis. U.S. National Institutes of Health.
REF 23Clinical pipeline report, company report or official report of TG THERAPEUTICS.
REF 24ClinicalTrials.gov (NCT01390545) VELVET, a Dose Range Finding Trial of Veltuzumab in Subjects With Moderate to Severe Rheumatoid Arthritis. U.S. National Institutes of Health.
REF 25(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 8268).
REF 26ClinicalTrials.gov (NCT01874288) Phase I/II Study of De-immunized DI-Leu16-IL2 Immunocytokine Administered Subcutaneously in Patients With B-cell NHL. U.S. National Institutes of Health.
REF 27Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800030721)
REF 28Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800033790)
REF 29CD20-Targeted T Cells after Stem Cell Transplantation for High Risk and Refractory Non-Hodgkin's Lymphoma. Biol Blood Marrow Transplant. 2013 June; 19(6): 925-933.
REF 30J Clin Oncol 27:15s, 2009 (suppl, abstr 8566).
REF 31(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2628).
REF 32National Cancer Institute Drug Dictionary (drug id 599668).
REF 33Veltuzumab, an anti-CD20 mAb for the treatment of non-Hodgkin's lymphoma, chronic lymphocytic leukemia and immune thrombocytopenic purpura. Curr Opin Mol Ther. 2009 Apr;11(2):200-7.
REF 34Translational Mini-Review Series on B Cell-Directed Therapies: Recent advances in B cell-directed biological therapies for autoimmune disorders. Clin Exp Immunol. 2009 August; 157(2): 198-208.
REF 35Rituximab (monoclonal anti-CD20 antibody): mechanisms of action and resistance. Oncogene. 2003 Oct 20;22(47):7359-68.
REF 36Comparative nonclinical assessments of the proposed biosimilar PF-05280586 and rituximab (MabThera?). Toxicol Pathol. 2014 Oct;42(7):1069-81.
REF 37TRU-015, a small modular immunopharmaceutical (SMIP?? drug candidate directed against CD20, demonstrates clinical improvement in subjects with rheumatoid arthritis. Arthritis Res Ther. 2007; 9(Suppl 3): P32.

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