Rituximab

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:

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

Reduce drug development failure rates

Build, train, & validate machine-learning models
with evidence-based and structured datasets.

See how

Build, train, & validate predictive machine-learning models with structured datasets.

See how

Associated Conditions

Contraindications & Blackbox Warnings

Avoid life-threatening adverse drug events

Improve clinical decision support with information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.

Learn more

Avoid life-threatening adverse drug events & improve clinical decision support.

Learn more

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	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 C_max 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 C_max 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 AUC_0-180 was 9787 µg/mL⋅day (range from 4838 to 20446 µg/mL⋅day). In adult patients given the same dose, the AUC_0-180 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

Improve decision support & research outcomes

With structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates.

Learn more

Improve decision support & research outcomes with our structured adverse effects data.

Learn more

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 software
Abatacept	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.
Adalimumab	The risk or severity of infection can be increased when Adalimumab is combined with Rituximab.
Adenovirus type 7 vaccine live	The risk or severity of infection can be increased when Adenovirus type 7 vaccine live is combined with Rituximab.
Aducanumab	The risk or severity of adverse effects can be increased when Rituximab is combined with Aducanumab.
Aldesleukin	The risk or severity of adverse effects can be increased when Aldesleukin is combined with Rituximab.
Alefacept	The risk or severity of adverse effects can be increased when Rituximab is combined with Alefacept.

Identify potential medication risks

Easily compare up to 40 drugs with our drug interaction checker.

Get severity rating, description, and management advice.

Learn more

Food Interactions

No interactions found.

Products

Drug product information from 10+ global regions

Our datasets provide approved product information including:
dosage, form, labeller, route of administration, and marketing period.

Access now

Access drug product information from over 10 global regions.

Access now

International/Other Brands

MabThera (Roche) / Riabni

Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Blitzima	Injection, solution, concentrate	500 mg	Intravenous	Celltrion Healthcare Hungary Kft.	2020-11-24	Not applicable
Blitzima	Injection, solution, concentrate	100 mg	Intravenous	Celltrion Healthcare Hungary Kft.	2020-11-24	Not applicable
Mabthera	Injection, solution, concentrate	500 mg	Intravenous	Roche Registration Gmb H	2021-02-11	Not applicable
Mabthera	Injection, solution	1600 mg	Subcutaneous	Roche Registration Gmb H	2021-02-11	Not applicable
Mabthera	Injection, solution, concentrate	100 mg	Intravenous	Roche Registration Gmb H	2021-02-11	Not applicable
Mabthera	Injection, solution	1400 mg	Subcutaneous	Roche Registration Gmb H	2021-02-11	Not applicable
Riabni	Injection, solution	100 mg/10mL	Intravenous	AMGEN INC	2021-01-06	Not applicable
Riabni	Injection, solution	500 mg/50mL	Intravenous	AMGEN INC	2021-01-06	Not applicable
Riabni	Solution	10 mg / mL	Intravenous	Amgen	2021-04-21	Not applicable
Ritemvia	Injection, solution, concentrate	100 mg	Intravenous	Celltrion Healthcare Hungary Kft.	2020-12-16	2021-08-16

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
Rituxan Hycela	Rituximab (120 mg/1mL) + Hyaluronidase (human recombinant) (2000 U/1mL)	Injection, solution	Subcutaneous	Genentech, Inc.	2017-06-22	Not applicable

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]

External Links

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

Phase	Status	Purpose	Conditions	Count
4	Active Not Recruiting	Prevention	Kidney Transplantation	1
4	Active Not Recruiting	Treatment	Anti-Neutrophil Cytoplasmic Antibody-Associated Vasculitis / Granulomatosis With Polyangiitis / Microscopic Polyangiitis (MPA)	1
4	Active Not Recruiting	Treatment	Function of Renal Transplant	1
4	Active Not Recruiting	Treatment	Thyroid Associated Ophthalmopathy	1
4	Completed	Other	Autoimmune Disorder / Kidney Transplantation	1
4	Completed	Prevention	Autoimmune Adrenocortical Failure	1
4	Completed	Prevention	Kidney Transplantation	1
4	Completed	Treatment	Acute Lymphoblastic Leukemia (ALL)	1
4	Completed	Treatment	Anaplastic Large Cell Lymphoma / Burkitt Lymphoma (BL) / Lymphoma, Lymphoblastic / Mediastinal Neoplasms	1
4	Completed	Treatment	Chronic Lymphocytic Leukemia (CLL)	1

Pharmacoeconomics

Manufacturers

Roche

Packagers

Biogen Idec Inc.
F Hoffmann-La Roche Ltd.
Genentech Inc.

Dosage Forms

Form	Route	Strength
Solution	Intravenous; Subcutaneous	10 mg
Solution, concentrate	Intravenous	500 mg
Solution	Intravenous	100 mg
Injection	Intravenous
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
Injection, solution	Intravenous
Injection, solution	Subcutaneous
Solution	Intravenous	10 mg/ml
Injection	Intravenous	10 mg/ml
Solution	Intravenous	10 mg
Injection, solution	Subcutaneous	1400 mg
Solution, concentrate	Intravenous
Solution	Subcutaneous	120 mg
Solution	Intravenous
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	Intravenous	100 mg/10mL
Injection, solution	Intravenous	500 mg/50mL
Solution, concentrate	Intravenous	10 mg
Injection, solution, concentrate	Intravenous
Injection, solution, concentrate	Intravenous; Parenteral	100 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)
CA2149329	No	2008-07-15	2013-11-12
CA1336826	No	1995-08-29	2012-08-29
US5736137	No	1998-04-07	2015-04-07

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

Build, predict & validate machine-learning models

Use our structured and evidence-based datasets to unlock new
insights and accelerate drug research.

Learn more

Use our structured and evidence-based datasets to unlock new insights and accelerate drug research.

Learn more

Details1. B-lymphocyte antigen CD20

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

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]
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]
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]
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]
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]
Rituxan FDA label [File]

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

Rituximab

Identification

References:

Pharmacology

Interactions

Products

Categories

Chemical Identifiers

References

Clinical Trials

Pharmacoeconomics

Properties

Targets

References