Rituximab
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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
Download FASTA FormatReferences:
- Rituximab - CAS 174722-31-7 [Link]
- 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
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Used in combination to treat Active, moderate to severe rheumatoid arthritis Regimen in combination with: Methotrexate (DB00563) •••••••••••• ••••• •••••••••• •••••••• •• ••• •• •••• ••• •••••••••• ••••••••• ••••••••• Used in combination to treat Chronic lymphocytic leukemia (cll) Regimen in combination with: Cyclophosphamide (DB00531), Fludarabine (DB01073), Hyaluronidase (human recombinant) (DB06205) •••••••••••• ••••• ••••••••• Used in combination to treat Chronic lymphocytic leukemia (cll) Regimen in combination with: Cyclophosphamide (DB00531), Fludarabine (DB01073) •••••••••••• ••••• ••••••••• Used in combination to treat Diffuse large b-cell lymphoma (dlbcl) Regimen in combination with: Vincristine (DB00541), Cyclophosphamide (DB00531), Doxorubicin (DB00997), Prednisone (DB00635), Hyaluronidase (human recombinant) (DB06205) •••••••••••• ••••• ••••••••• Used in combination to treat Diffuse large b-cell lymphoma (dlbcl) Regimen in combination with: Cyclophosphamide (DB00531), Vincristine (DB00541), Doxorubicin (DB00997), Prednisone (DB00635) •••••••••••• ••••• ••••••••• - Contraindications & Blackbox Warnings
- Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API
- 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
Target Actions Organism AB-lymphocyte antigen CD20 antibodyregulatorHumans - 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/Enzyme Allele name Genotype(s) Defining Change(s) Type(s) Description Details Low affinity immunoglobulin gamma Fc region receptor III-A FCGR3A (G;G) / (G;T) T > G Effect Directly Studied Patients 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.
Drug Interaction Integrate drug-drug
interactions in your softwareAbatacept Rituximab may increase the immunosuppressive activities of Abatacept. Abciximab The risk or severity of bleeding can be increased when Abciximab is combined with Rituximab. Acebutolol Acebutolol may increase the hypotensive activities of Rituximab. Acenocoumarol The risk or severity of bleeding can be increased when Acenocoumarol is combined with Rituximab. Acetylsalicylic acid The risk or severity of bleeding can be increased when Acetylsalicylic acid is combined with Rituximab. - Food Interactions
- No interactions found.
Products
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- International/Other Brands
- MabThera (Roche) / Riabni
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Blitzima Injection, solution, concentrate 500 mg Intravenous Celltrion Healthcare Hungary Kft. 2020-11-24 Not applicable EU Blitzima Injection, solution, concentrate 100 mg Intravenous Celltrion Healthcare Hungary Kft. 2020-11-24 Not applicable EU Mabthera Injection, solution, concentrate 500 mg Intravenous Roche Registration Gmbh 2021-02-11 Not applicable EU Mabthera Injection, solution 1600 mg Subcutaneous Roche Registration Gmbh 2021-02-11 Not applicable EU Mabthera Injection, solution, concentrate 100 mg Intravenous Roche Registration Gmbh 2021-02-11 Not applicable EU - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Rituxan Hycela Rituximab (120 mg/1mL) + Hyaluronidase (human recombinant) (2000 U/1mL) Injection, solution Subcutaneous Genentech, Inc. 2017-06-22 Not applicable US Rituxan Hycela Rituximab (120 mg/1mL) + Hyaluronidase (human recombinant) (2000 U/1mL) Injection, solution Subcutaneous Genentech, Inc. 2017-06-22 Not applicable US
Categories
- ATC Codes
- L01FA01 — Rituximab
- Drug Categories
- Amino Acids, Peptides, and Proteins
- Antibodies
- Antibodies, Monoclonal
- Antibodies, Monoclonal, Murine-Derived
- Antineoplastic Agents
- Antineoplastic Agents, Immunological
- Antirheumatic Agents
- Biologics for Rheumatoid Arthritis Treatment
- Blood Proteins
- Cancer immunotherapy
- CD20 (Clusters of Differentiation 20) inhibitors
- CD20-directed Antibody Interactions
- CD20-directed Cytolytic Antibody
- Globulins
- Immunoglobulins
- Immunologic Factors
- Immunoproteins
- Immunosuppressive Agents
- Immunotherapy
- Monoclonal antibodies and antibody drug conjugates
- Myelosuppressive Agents
- Narrow Therapeutic Index Drugs
- Proteins
- Serum Globulins
- 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
- 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]
- 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]
- 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]
- 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]
- 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]
- Emer JJ, Claire W: Rituximab: a review of dermatological applications. J Clin Aesthet Dermatol. 2009 May;2(5):29-37. [Article]
- 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]
- 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]
- FDA approves first biosimilar for treatment of adult patients with non-Hodgkin’s lymphoma [Link]
- FDA Approves Two New Indications for Rituxan in Patients With Non-Hodgkin's Lymphoma [Link]
- FDA approves first treatment for children with rare diseases that cause inflammation of small blood vessels [Link]
- FDA Approved Drug Products: Rituxan (rituximab) for intravenous use [Link]
- FDA Approved Drug Products: TRUXIMA (rituximab-abbs) injection, for intravenous use [Link]
- FDA Approved Drug Products: RUXIENCE (rituximab-pvvr) injection, for intravenous use [Link]
- FDA Approved Drug Products: RIABNI (rituximab-arrx) injection, for intravenous use [Link]
- FDA Approved Drug Products: RITUXAN HYCELA (rituximab and hyaluronidase human) injection, for subcutaneous use [Link]
- Genentech: RITUXAN (rituximab) SDS [Link]
- FDA Approved Drug Products: RUXIENCE® (rituximab-pvvr) injection, for intravenous use (October 2023) [Link]
- External Links
- UniProt
- P01857
- Genbank
- J00228
- PubChem Substance
- 46505820
- 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
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package Phase Status Purpose Conditions Count Start Date Why Stopped 100+ additional columns Unlock 175K+ rows when you subscribe.View sample dataNot Available Active Not Recruiting Not Available Large B-Cell / Large B-Cell, Diffuse / Lymphoma 1 somestatus stop reason just information to hide Not Available Active Not Recruiting Treatment Diffuse Large B-Cell Lymphoma (DLBCL) / Non-Hodgkin's Lymphoma (NHL) 1 somestatus stop reason just information to hide Not Available Approved for Marketing Not Available Chronic Lymphocytic Leukemia 1 somestatus stop reason just information to hide Not Available Completed Not Available Auto-immune Encephalitis / Cognitive Impairment (CI) 1 somestatus stop reason just information to hide Not Available Completed Not Available B-Cell Chronic Lymphocytic Leukemia / Non-Hodgkin's Lymphoma (NHL) 1 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Roche
- Packagers
- Biogen Idec Inc.
- F Hoffmann-La Roche Ltd.
- Genentech Inc.
- Dosage Forms
Form Route Strength Solution Intravenous 100.000 mg Solution Intravenous 100.0 mg Solution Intravenous; Subcutaneous 10 mg Solution, concentrate Intravenous 500 mg Solution Intravenous 100 mg Injection Intravenous 1400 MG/11.7ML Injection, solution Subcutaneous 1600 mg Injection, solution, concentrate Intravenous 10 mg/1ml Injection, solution, concentrate Intravenous 100 mg Injection, solution, concentrate Intravenous 500 mg Solution 10 mg/1ml Solution Intravenous 500 mg Injection Intravenous 100 mg/10ml Injection, solution, concentrate Intravenous 100 MG/10ML Injection, solution Intravenous 120 mg/mL Injection Intravenous 500 mg/50ml Injection, solution, concentrate Intravenous 500 MG/50ML Solution Intravenous 10 mg/ml Injection Intravenous 10 mg/ml Solution Intravenous 10 mg Injection, solution Subcutaneous 1400 mg Solution, concentrate Intravenous 10 mg/ml Solution Subcutaneous 120 mg Injection; injection, solution, concentrate Intravenous 10 MG/ML Solution Intravenous 500.000 mg Injection, solution Intravenous 10 mg/1mL Solution Intravenous 10 mg / mL Injection, solution Subcutaneous Solution Subcutaneous 1400 mg / 11.7 mL Solution Subcutaneous 1600 mg / 13.4 mL Injection, solution, concentrate 100 mg/10ml Injection, solution, concentrate 500 mg/50ml Solution Intravenous 100 mg/10ml Solution Intravenous 500 mg/50ml Injection, solution Intravenous 100 mg/10mL Injection, solution Intravenous 500 mg/50mL Injection, solution, concentrate Intravenous; Parenteral 100 MG Solution, concentrate Intravenous 10 mg Injection, solution, concentrate Intravenous; Parenteral 500 MG Solution Intravenous 100 mg / 10 mL Solution Intravenous 500 mg / 50 mL Injection, solution 1400 mg/11.7ml - Prices
Unit description Cost Unit Rituxan 10 mg/ml Concentrate 10ml Vial 708.17USD vial Rituxan 10 mg/ml vial 68.09USD ml DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region CA2149329 No 2008-07-15 2013-11-12 Canada CA1336826 No 1995-08-29 2012-08-29 Canada US5736137 No 1998-04-07 2015-04-07 US
Properties
- State
- Liquid
- Experimental Properties
Property Value Source melting point (°C) 61 °C (FAB fragment) http://crdd.osdd.net/raghava/thpdb/display_thppid_sub.php?details=Th1062 hydrophobicity -0.414 http://crdd.osdd.net/raghava/thpdb/display_thppid_sub.php?details=Th1062 isoelectric point 8.68 http://crdd.osdd.net/raghava/thpdb/display_thppid_sub.php?details=Th1062
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- AntibodyRegulator
- General Function
- B-lymphocyte-specific membrane protein that plays a role in the regulation of cellular calcium influx necessary for the development, differentiation, and activation of B-lymphocytes (PubMed:12920111, PubMed:3925015, PubMed:7684739). Functions as a store-operated calcium (SOC) channel component promoting calcium influx after activation by the B-cell receptor/BCR (PubMed:12920111, PubMed:18474602, PubMed:7684739)
- Specific Function
- epidermal growth factor receptor binding
- Gene Name
- MS4A1
- Uniprot ID
- P11836
- Uniprot Name
- B-lymphocyte antigen CD20
- Molecular Weight
- 33076.99 Da
References
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- 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]
- 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]
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- Rituxan FDA label [File]
Drug created at June 13, 2005 13:24 / Updated at August 02, 2024 07:21