Identification

Summary

Rituximab is a monoclonal anti-CD20 antibody used to treat non-Hodgkin's lymphoma, chronic lymphocytic leukemia, Wegener's granulomatosis, pemphigus vulgaris, and rheumatoid arthritis.

Brand Names
MabThera, Riabni, Rituxan, Rituxan Hycela, Ruxience, Truxima
Generic Name
Rituximab
DrugBank Accession Number
DB00073
Background

Rituximab 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 6, Label. It was originally approved by the U.S. FDA in 1997 as a single agent to treat patients with B-cell Non-Hodgkin's Lymphoma (NHL) 10, however, has now been approved for a variety of conditions Label. On November 28, 2018, the US FDA approved Truxima, the first biosimilar to Rituxan (Rituximab) 9.

Type
Biotech
Groups
Approved
Biologic Classification
Protein Based Therapies
Monoclonal antibody (mAb)
Protein Structure
Protein Chemical Formula
C6416H9874N1688O1987S44
Protein Average Weight
143859.7 Da
Sequences
>Rituximab heavy chain chimeric
QVQLQQPGAELVKPGASVKMSCKASGYTFTSYNMHWVKQTPGRGLEWIGAIYPGNGDTSY
NQKFKGKATLTADKSSSTAYMQLSSLTSEDSAVYYCARSTYYGGDWYFNVWGAGTTVTVS
AASTKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQS
SGLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKAEPKSCDKTHTCPPCPAPELLG
GPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQY
NSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRD
ELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSR
WQQGNVFSCSVMHEALHNHYTQKSLSLSPGK
>Rituximab light chain chimeric
QIVLSQSPAILSASPGEKVTMTCRASSSVSYIHWFQQKPGSSPKPWIYATSNLASGVPVR
FSGSGSGTSYSLTISRVEAEDAATYYCQQWTSNPPTFGGGTKLEIKRTVAAPSVFIFPPS
DEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTLTL
SKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC
References:
  1. Rituximab - CAS 174722-31-7 [Link]
Download FASTA Format
Synonyms
  • Rituximab
  • rituximab-abbs
  • rituximab-arrx
  • rituximab-pvvr
External IDs
  • GP2013
  • IDEC-102
  • IDEC-C2B8
  • PF 05280586
  • PF-05280586
  • RG-105

Pharmacology

Indication

Rituximab is indicated for the treatment of adult patients with relapsed or refractory, low-grade or follicular, CD20-positive, B-cell non-Hodgkin’s Lymphoma (NHL) as a single agent. Also, it is indicated for the treatment of adult patients with previously untreated follicular, CD20-positive, B-cell NHL in combination with first line chemotherapy and, in patients achieving a complete or partial response to a rituximab product in combination with chemotherapy, as single-agent maintenance therapy.12,13,14,15,16 Additionally, rituximab is indicated for the treatment of adult patients with non-progressing (including stable disease), low-grade, CD20-positive, B-cell NHL as a single agent after first-line cyclophosphamide, vincristine, and prednisone (CVP) chemotherapy; and previously untreated diffuse large B-cell, CD20-positive NHL in combination with cyclophosphamide, doxorubicin, vincristine, prednisone (CHOP) or other anthracycline-based chemotherapy regimens.12,13,14,15,16

Rituximab, in combination with fludarabine and cyclophosphamide (FC), is indicated for the treatment of adult patients with previously untreated and previously treated CD20-positive chronic lymphocytic leukemia (CLL).12,13,14,15,16 In combination with methotrexate, rituximab is indicated for the treatment of adult patients with moderately-to severely-active rheumatoid arthritis who have had an inadequate response to one or more TNF antagonist therapies.12,13,14,15 Additionally, rituximab, in combination with glucocorticoids, is indicated for the treatment of adult and pediatric patients 2 years of age and older with Granulomatosis with Polyangiitis (GPA) (Wegener’s Granulomatosis) and Microscopic Polyangiitis (MPA).12,13,14,15

RITUXAN (rituximab injection for intravenous use) is indicated for the treatment of pediatric patients aged 6 months and older with previously untreated, advanced stage, CD20-positive diffuse large B-cell lymphoma (DLBCL), Burkitt lymphoma (BL), Burkitt-like lymphoma (BLL) or mature B-cell acute leukemia (B-AL) in combination with chemotherapy; as well as the treatment of adult patients with moderate to severe pemphigus vulgaris.12 These indications for RITUXAN are not included in the labels of rituximab biosimilar products (rituximab-arrx, rituximab-abbs, rituximab-pvvr).13,14,15 The combination product RITUXAN HYCELA (rituximab and hyaluronidase human injection, for subcutaneous use) is not indicated for the treatment of non-malignant conditions.16

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Associated Conditions
Contraindications & Blackbox Warnings
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Pharmacodynamics

Rituximab is a chimeric murine/human monoclonal antibody that binds to the CD20 antigen. CD20 is predominantly expressed on the surface of pre-B and mature B-lymphocytes, allowing rituximab to target and promote lysis in this specific type of cells.6,7,12. In Non-Hodgkin's Lymphoma patients, rituximab treatment depleted circulating and tissue-based B-cells. In a study that included 166 patients, CD19-positive B-cells were depleted within three weeks, and in 83% of patients, cell depletion lasted up to 6-9 months. B-cell levels started to recover at approximately 6 months and returned to normal 12 months after treatment was completed. Approximately 14% of Non-Hodgkin's Lymphoma patients had IgM or IgG serum levels below the normal range 12.

Most rheumatoid arthritis (RA) patients treated with rituximab showed a near-complete depletion of peripheral B lymphocytes within 2 weeks after the first dose. Peripheral B-cell depletion was sustained for at least 6 months, and in approximately 4% of RA patients, peripheral B-cell depletion was sustained for more than 3 years after a single course of rituximab treatment.12 Total IgG, IgA, and, more specifically, IgM levels were lower 24 weeks after the first cycle of rituximab treatment (2.8%, 0.8% and 10% below the lower limit of normal, respectively). However, the clinical consequences of this decrease in immunoglobulin levels in RA patients are not clear at this time. Treatment with rituximab in patients with RA was also associated with a decreased level of inflammation markers.12

In patients with granulomatosis with polyangiitis (GPA) and microscopic polyangiitis (MPA) treated with rituximab, CD19 B-cells in peripheral blood were depleted to less than 10 cells/μl after the first two infusions. By month 6, approximately 84% of patients had the same level of peripheral blood CD19 B-cells, and by month 12, 81% of patients demonstrated signs of B-cell return with counts >10 cells/μL. By Month 18, the majority of patients (87%) had counts >10 cells/μL 12.

Mechanism of action

Rituximab is a monoclonal antibody that targets CD20, an antigen expressed on the surface of pre-B and mature B-lymphocytes 1,2,3,12. About 85% of non-Hodgkin’s lymphoma (NHL) cases are B-cell lymphomas, characterized by the high expression of CD19, CD20 and CD22 cell surface antigens.7 CD20 is involved in cell cycle regulation, apoptosis and calcium signaling. By targeting CD20, rituximab promotes cell lysis while sparing hematopoietic and plasma cells without this surface antigen.6,7 It has been suggested that cell lysis mechanisms triggered by rituximab include complement-dependent cytotoxicity (CDC) and antibody-dependent cell-mediated cytotoxicity (ADCC) 12. Rituximab is part of the immunoglobulin G1 (IgG1) subclass of antibodies, and is formed by a murine variable region (Fab region) and a human constant region (Fc region). The Fab region gives rituximab its specificity for CD20, while the Fc region interacts with cell surface receptors to activate the immune system, leading to the depletion of circulating B lymphocytes 6.

In regards to the mechanism of action in rheumatoid arthritis (RA), B-cells are thought to play a role in the pathogenesis of RA and the associated condition of chronic synovitis.12 B-cells may act at various sites in the autoimmune/inflammatory process through the production of rheumatoid factor (RF) and other autoantibodies, antigen presentation, T-cell activation, and the production of proinflammatory cytokines 12. The administration of rituximab in this condition has resulted in significant clinical and symptomatic improvements 2,12. Rituximab is also indicated for the treatment of granulomatosis with polyangiitis (GPA) and microscopic polyangiitis (MPA), two conditions characterized by the presence of circulating antineutrophil cytoplasmic antibodies and increased B-cell activity. It has been suggested that rituximab depletes CD20+ B-cells at a higher rate in GPA and MPA patients with high levels of Fc receptor-like 5 (FCRL5).8

TargetActionsOrganism
AB-lymphocyte antigen CD20
antibody
regulator
Humans
Absorption

Rituximab follows a linear pharmacokinetic model.5 In patients with non-Hodgkin’s lymphoma (NHL) administered 4 doses of 375 mg/m2 of rituximab (IV) weekly, detectable levels were observed 3-6 months after treatment completion. The pharmacokinetic profile of rituximab administered in combination with 6 cycles of CHOP (cyclophosphamide, doxorubicin, vincristine, and prednisone) chemotherapy was similar to the one observed when administered alone.12 In patients with rheumatoid arthritis (RA) administered 2 doses of 500 mg of rituximab, the Cmax of the first and second infusions were 157 (SD ± 46) and 183 (SD ± 55) mcg/mL. In patients administered 2 doses of 1,000 mg of rituximab, the Cmax of the first and second infusions were 318 (SD ± 86) and 381 (SD ± 98) mcg/mL.12

In pediatric patients (6-17 years old) with granulomatosis with polyangiitis (GPA) or microscopic polyangiitis (MPA) given four doses of 375 mg/m2 of rituximab intravenously once a week, the AUC0-180 was 9787 µg/mL⋅day (range from 4838 to 20446 µg/mL⋅day). In adult patients given the same dose, the AUC0-180 of rituximab was 10302 µg/mL⋅day (range from 3653 to 21874 µg/mL⋅day).12 The bioavailability of rituximab administered intravenously is expected to be close to 100%. Compared to rituximab administered intravenously, the bioavailability of RITUXAN HYCELA, a combination product of rituximab and hyaluronidase (human recombinant), is 64.6% in patients with follicular lymphoma and 63.4% in patients with chronic lymphocytic leukemia (CLL).16

Volume of distribution

Based on a pharmacokinetic analysis that included 2005 patients with rheumatoid arthritis (RA), the volume of distribution of rituximab is 3.1 L.12 In pediatric patients (6-17 years old) with granulomatosis with polyangiitis (GPA) or microscopic polyangiitis (MPA) given four doses of 375 mg/m2 of rituximab intravenously once a week, the volume of distribution was 2.28 L (range from 1.43 to 3.17 L). In adult patients given the same dose, the volume of distribution was 3.12 L (range from 2.42 to 3.91 L).12 In patients with pemphigus vulgaris given an intravenous infusion of 1000 mg of rituximab on days 1, 15, 168, and 182, the volume of distribution was 3.49 L (range from 2.48 to 5.22 L).12

Protein binding

Not available.

Metabolism

As a monoclonal antibody, rituximab is expected to be metabolized by proteases throughout the body.

Route of elimination

Monoclonal antibodies (mAb) such as rituximab trigger the formation of antidrug antibodies (ADAs) that form ADA-mAb immune complexes. The endogenous elimination of these immune complexes is mediated by the reticuloendothelial system, most likely via fragment crystallizable-gamma (Fcγ)-mediated endocytosis5.

Half-life

In patients with non-Hodgkin's lymphoma (NHL) treated with rituximab once a week or once every three weeks (n=298), the median terminal elimination half-life was 22 days (range of 6.1-52 days).12 In patients with chronic lymphocytic leukemia (CLL) treated with rituximab (n=21), the estimated median terminal half-life was 32 days (range of 14-62 days).12

Based on a pharmacokinetic analysis that included 2005 patients with rheumatoid arthritis (RA), the mean terminal elimination half-life of rituximab is 18.0 days.12 In pediatric patients (6-17 years old) with granulomatosis with polyangiitis (GPA) or microscopic polyangiitis (MPA) given four doses of 375 mg/m2 of rituximab intravenously once a week, the terminal half-life was 22 days (range from 11 to 42 days). In adult patients given the same dose, the terminal half-life was 25 days (range from 11 to 52 days).12

In patients with pemphigus vulgaris given an intravenous infusion of 1000 mg of rituximab, the terminal half-life was 21.1 days (range from 9.3 to 36.2 days) in the first infusion cycle (days 1 and 15), and 26.2 days (range from 16.4 to 42.8 days) in the second infusion cycle (days 168 and 182).12

Clearance

In patients with non-Hodgkin’s lymphoma (NHL), those with higher CD19-positive cell counts or larger measurable tumor lesions at pretreatment had higher rituximab clearance 12. Based on a pharmacokinetic analysis that included 2005 patients with rheumatoid arthritis (RA), the clearance of rituximab is 0.335 L/day.12

In pediatric patients (6-17 years old) with granulomatosis with polyangiitis (GPA) or microscopic polyangiitis (MPA) given four doses of 375 mg/m2 of rituximab intravenously once a week, clearance was 0.222 L/day (range from 0.0996 to 0.381 L/day). In adult patients given the same dose, clearance was 0.279 L/day (range from 0.113 to 0.653 L/day).12

In patients with pemphigus vulgaris given an intravenous infusion of 1000 mg of rituximab, clearance was 0.30 L/day (range from 0.16 to 1.51 L/day) in the first infusion cycle (days 1 and 15), and 0.24 L/day (range from 0.13 to 0.45 L/day) in the second infusion cycle (days 168 and 182).12

Adverse Effects
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Toxicity

Toxicity information regarding rituximab is not readily available. Patients experiencing an overdose are at an increased risk of severe adverse effects such as fatal infusion-related reactions and severe mucocutaneous reactions. Symptomatic and supportive measures are recommended. No long-term animal studies have been performed to establish the carcinogenic or mutagenic potential of rituximab or to determine potential effects on fertility in males or females 12. The maximum tolerated dose of rituximab in mice administered intraperitoneally is higher than 100 mg/kg.17

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Interacting Gene/EnzymeAllele nameGenotype(s)Defining Change(s)Type(s)DescriptionDetails
Low affinity immunoglobulin gamma Fc region receptor III-AFCGR3A(G;G) / (G;T)T > GEffect Directly StudiedPatients with this genotype have increased frequency of anti-tumor response when using rituximab to treat diffuse large B-cell lymphoma, follicular lymphoma, or [follicular non-Hodgkin lymphoma].Details

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AbataceptRituximab may increase the immunosuppressive activities of Abatacept.
AbciximabThe risk or severity of bleeding can be increased when Abciximab is combined with Rituximab.
AcebutololAcebutolol may increase the hypotensive activities of Rituximab.
AcenocoumarolThe risk or severity of bleeding can be increased when Acenocoumarol is combined with Rituximab.
Acetylsalicylic acidThe risk or severity of bleeding can be increased when Acetylsalicylic acid is combined with Rituximab.
AdalimumabThe risk or severity of infection can be increased when Adalimumab is combined with Rituximab.
Adenovirus type 7 vaccine liveThe risk or severity of infection can be increased when Adenovirus type 7 vaccine live is combined with Rituximab.
AducanumabThe risk or severity of adverse effects can be increased when Rituximab is combined with Aducanumab.
AldesleukinThe risk or severity of adverse effects can be increased when Aldesleukin is combined with Rituximab.
AlefaceptThe risk or severity of adverse effects can be increased when Rituximab is combined with Alefacept.
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Food Interactions
No interactions found.

Products

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International/Other Brands
MabThera (Roche) / Riabni
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
BlitzimaInjection, solution, concentrate500 mgIntravenousCelltrion Healthcare Hungary Kft.2020-11-24Not applicableEU flag
BlitzimaInjection, solution, concentrate100 mgIntravenousCelltrion Healthcare Hungary Kft.2020-11-24Not applicableEU flag
MabtheraInjection, solution, concentrate500 mgIntravenousRoche Registration Gmb H2021-02-11Not applicableEU flag
MabtheraInjection, solution1600 mgSubcutaneousRoche Registration Gmb H2021-02-11Not applicableEU flag
MabtheraInjection, solution, concentrate100 mgIntravenousRoche Registration Gmb H2021-02-11Not applicableEU flag
MabtheraInjection, solution1400 mgSubcutaneousRoche Registration Gmb H2021-02-11Not applicableEU flag
RiabniInjection, solution100 mg/10mLIntravenousAMGEN INC2021-01-06Not applicableUS flag
RiabniInjection, solution500 mg/50mLIntravenousAMGEN INC2021-01-06Not applicableUS flag
RiabniSolution10 mg / mLIntravenousAmgen2021-04-21Not applicableCanada flag
RitemviaInjection, solution, concentrate100 mgIntravenousCelltrion Healthcare Hungary Kft.2020-12-162021-08-16EU flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
Rituxan HycelaRituximab (120 mg/1mL) + Hyaluronidase (human recombinant) (2000 U/1mL)Injection, solutionSubcutaneousGenentech, Inc.2017-06-22Not applicableUS flag
Rituxan HycelaRituximab (120 mg/1mL) + Hyaluronidase (human recombinant) (2000 U/1mL)Injection, solutionSubcutaneousGenentech, Inc.2017-06-22Not applicableUS flag

Categories

ATC Codes
L01XC02 — Rituximab
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
Not Available
Kingdom
Organic Compounds
Super Class
Organic Acids
Class
Carboxylic Acids and Derivatives
Sub Class
Amino Acids, Peptides, and Analogues
Direct Parent
Peptides
Alternative Parents
Not Available
Substituents
Not Available
Molecular Framework
Not Available
External Descriptors
Not Available
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
4F4X42SYQ6
CAS number
174722-31-7

References

Synthesis Reference

Anderson, DR., et al. (1998). Therapeutic application of chimeric and radiolabeled antibodies to human B lymphocyte restricted differentiation antigen for treatment of B cell lymphoma (U.S. Patent No. US 5,736,137 A). U.S. Patent and Trademark Office. https://patentimages.storage.googleapis.com/04/bf/17/b9f758df63e314/US5736137.pdf

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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
  5. Ryman JT, Meibohm B: Pharmacokinetics of Monoclonal Antibodies. CPT Pharmacometrics Syst Pharmacol. 2017 Sep;6(9):576-588. doi: 10.1002/psp4.12224. Epub 2017 Jul 29. [Article]
  6. Emer JJ, Claire W: Rituximab: a review of dermatological applications. J Clin Aesthet Dermatol. 2009 May;2(5):29-37. [Article]
  7. Dotan E, Aggarwal C, Smith MR: Impact of Rituximab (Rituxan) on the Treatment of B-Cell Non-Hodgkin's Lymphoma. P T. 2010 Mar;35(3):148-57. [Article]
  8. Owczarczyk K, Cascino MD, Holweg C, Tew GW, Ortmann W, Behrens T, Schindler T, Langford CA, St Clair EW, Merkel PA, Spiera R, Seo P, Kallenberg CG, Specks U, Lim N, Stone J, Brunetta P, Prunotto M: Fc receptor-like 5 and anti-CD20 treatment response in granulomatosis with polyangiitis and microscopic polyangiitis. JCI Insight. 2020 Sep 17;5(18). pii: 136180. doi: 10.1172/jci.insight.136180. [Article]
  9. FDA approves first biosimilar for treatment of adult patients with non-Hodgkin’s lymphoma [Link]
  10. FDA Approves Two New Indications for Rituxan in Patients With Non-Hodgkin's Lymphoma [Link]
  11. FDA approves first treatment for children with rare diseases that cause inflammation of small blood vessels [Link]
  12. FDA Approved Drug Products: Rituxan (rituximab) for intravenous use [Link]
  13. FDA Approved Drug Products: TRUXIMA (rituximab-abbs) injection, for intravenous use [Link]
  14. FDA Approved Drug Products: RUXIENCE (rituximab-pvvr) injection, for intravenous use [Link]
  15. FDA Approved Drug Products: RIABNI (rituximab-arrx) injection, for intravenous use [Link]
  16. FDA Approved Drug Products: RITUXAN HYCELA (rituximab and hyaluronidase human) injection, for subcutaneous use [Link]
  17. Genentech: RITUXAN (rituximab) SDS [Link]
UniProt
P01857
Genbank
J00228
PubChem Substance
46505820
RxNav
121191
ChEMBL
CHEMBL1201576
Therapeutic Targets Database
DAP000382
PharmGKB
PA451261
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Rituximab
FDA label
Download (257 KB)
MSDS
Download (117 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4Active Not RecruitingPreventionKidney Transplantation1
4Active Not RecruitingTreatmentAnti-Neutrophil Cytoplasmic Antibody-Associated Vasculitis / Granulomatosis With Polyangiitis / Microscopic Polyangiitis (MPA)1
4Active Not RecruitingTreatmentFunction of Renal Transplant1
4Active Not RecruitingTreatmentThyroid Associated Ophthalmopathy1
4CompletedOtherAutoimmune Disorder / Kidney Transplantation1
4CompletedPreventionAutoimmune Adrenocortical Failure1
4CompletedPreventionKidney Transplantation1
4CompletedTreatmentAcute Lymphoblastic Leukemia (ALL)1
4CompletedTreatmentAnaplastic Large Cell Lymphoma / Burkitt Lymphoma (BL) / Lymphoma, Lymphoblastic / Mediastinal Neoplasms1
4CompletedTreatmentChronic Lymphocytic Leukemia (CLL)1

Pharmacoeconomics

Manufacturers
  • Roche
Packagers
  • Biogen Idec Inc.
  • F Hoffmann-La Roche Ltd.
  • Genentech Inc.
Dosage Forms
FormRouteStrength
SolutionIntravenous; Subcutaneous10 mg
Solution, concentrateIntravenous500 mg
SolutionIntravenous100 mg
InjectionIntravenous
Injection, solutionSubcutaneous1600 mg
Injection, solution, concentrateIntravenous10 mg/1ml
Injection, solution, concentrateIntravenous100 mg
Injection, solution, concentrateIntravenous500 mg
Solution10 mg/1ml
SolutionIntravenous500 mg
InjectionIntravenous100 mg
Injection, solutionIntravenous
Injection, solutionSubcutaneous
SolutionIntravenous10 mg/ml
InjectionIntravenous10 mg/ml
SolutionIntravenous10 mg
Injection, solutionSubcutaneous1400 mg
Solution, concentrateIntravenous
SolutionSubcutaneous120 mg
SolutionIntravenous
Injection, solutionIntravenous10 mg/1mL
SolutionIntravenous10 mg / mL
Injection, solutionSubcutaneous
SolutionSubcutaneous1400 mg / 11.7 mL
SolutionSubcutaneous1600 mg / 13.4 mL
Injection, solutionIntravenous100 mg/10mL
Injection, solutionIntravenous500 mg/50mL
Solution, concentrateIntravenous10 mg
Injection, solution, concentrateIntravenous
Injection, solution, concentrateIntravenous; Parenteral100 MG
Injection, solution, concentrateIntravenous; Parenteral500 MG
SolutionIntravenous100 mg / 10 mL
SolutionIntravenous500 mg / 50 mL
Injection, solution1400 mg/11.7ml
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)Region
CA2149329No2008-07-152013-11-12Canada flag
CA1336826No1995-08-292012-08-29Canada flag
US5736137No1998-04-072015-04-07US flag

Properties

State
Liquid
Experimental Properties
PropertyValueSource
melting point (°C)61 °C (FAB fragment)http://crdd.osdd.net/raghava/thpdb/display_thppid_sub.php?details=Th1062
hydrophobicity-0.414http://crdd.osdd.net/raghava/thpdb/display_thppid_sub.php?details=Th1062
isoelectric point8.68http://crdd.osdd.net/raghava/thpdb/display_thppid_sub.php?details=Th1062

Targets

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Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Antibody
Regulator
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
Uniprot Name
B-lymphocyte antigen CD20
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. [Article]
  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. [Article]
  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. [Article]
  4. 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. [Article]
  5. Phuah J, Wong EA, Gideon HP, Maiello P, Coleman MT, Hendricks MR, Ruden R, Cirrincione LR, Chan J, Lin PL, Flynn JL: Effects of B Cell Depletion on Early Mycobacterium tuberculosis Infection in Cynomolgus Macaques. Infect Immun. 2016 Apr 22;84(5):1301-1311. doi: 10.1128/IAI.00083-16. Print 2016 May. [Article]
  6. Hayashi K, Nagasaki E, Kan S, Ito M, Kamata Y, Homma S, Aiba K: Gemcitabine enhances rituximab-mediated complement-dependent cytotoxicity to B cell lymphoma by CD20 upregulation. Cancer Sci. 2016 May;107(5):682-9. doi: 10.1111/cas.12918. Epub 2016 Apr 7. [Article]
  7. Kyriakidis I, Vasileiou E, Rossig C, Roilides E, Groll AH, Tragiannidis A: Invasive Fungal Diseases in Children with Hematological Malignancies Treated with Therapies That Target Cell Surface Antigens: Monoclonal Antibodies, Immune Checkpoint Inhibitors and CAR T-Cell Therapies. J Fungi (Basel). 2021 Mar 5;7(3). pii: jof7030186. doi: 10.3390/jof7030186. [Article]
  8. Rituxan FDA label [File]

Drug created at June 13, 2005 13:24 / Updated at July 02, 2022 12:49