Rituximab Treats Autoimmune Diseases and Cancer

English name：Rituximab
CAS number：174722-31-7
Molecular formula: C6416H9874N1688O1987S44
Molecular weight: 0
EINECS No.:
Related categories: biochemical reagents-protein; drug substance; mAb 18; drug substance and intermediates; chemical reagents
The Mol file: Mol File
constitutional formula:

Nature of rituximabStorage
conditions: Store at-80 C
Form: liquid
Color: colorless to pale yellow
 

Brief introduction

Rituximab antigen research drug trade name (MabThera), is developed by Genentech company, anti-CD20 human / mouse chimeric monoclonal antibody (by mouse against CD20 monoclonal antibody Chemicalbook variable Fab and human IgG 1 antibody constant region Fc fragment), the main mechanism of action is depletion of CD20 positive B cells (cause pemphigus antibody "culprit"). At present, there are already domestic generic drugs of rituximab in China.

Pharmacological effects and their effects

Mechanism rituximab is a specific against B cells chimeric mouse-human monoclonal antibody, and only expressed in B cells and mature B cells surface CD20 recognition and specific binding, highly targeted cytotoxic, anti-proliferative effect and induce apoptosis, through constant consumption of ChemicalbookB cells to produce blocking antibody. Because CD20 does not appear in hematopoietic stem cells, normal plasma cells and other normal tissues, rituximab can effectively avoid extensive immunosuppression and has a high safety profile. It was first approved by the US Food and Drug Administration for the treatment of non-Hodgkin's lymphoma.

Indication

1. Non-Hodgkin's lymphoma (NHL).
2. Chronic lymphocytic leukemia (CLL).
3. Rheumatoid arthritis (RA): adult patients with moderate to severe acquired RA who respond poorly to treatment with one or more TNF antagonists.
4. Wegener Granuloma (WG) and microscopic polyvasculitis (MPA) are combined with glucocorticoids in adult patients.

Untoward effect

1)Lymphoid malignant disease: the common adverse reactions in NHL clinical trials are: infusion reactions, fever, lymphopenia, chills, infection, and weakness. Common adverse reactions in CLL clinical trials are: infusion reactions and neutropenia.

2)Rheumatoid arthritis (RA): common adverse reactions in clinical trials: upper respiratory tract infection, nasopharyngitis, urinary tract infection, and bronchitis. Other important adverse effects include infusion reactions, severe infections, and cardiovascular events.

3) Wegener's granuloma (WG) and microscopic polyvasculitis (MPA): common adverse reactions in clinical studies are infection, nausea, diarrhea, headache, muscle spasm, anemia, peripheral edema. Other important adverse reactions include infusion reactions.

Bioactivity

Rituximab (anti-CD20) is a chimeric anti-CD20 monoclonal antibody that binds to the CD20 antigen on B cells with a binding affinity of 5 nM.MW: 143.86 KD.

Target spot

Target Value

CD20

In vitro study

The potency of Rituximab depends on its complement dependent toxicity (CDC), complement dependent cytotoxicity (CDCC), antibody-dependent cytotoxicity (ADCC) and apoptosis induction. Rituximab Can induce the death of malignant B cells in vitro. The strength of the action efficacy varies with the different targeted cells. In vitro, ChemicalbookRituximab-induced cellular changes were: p38MAPK, NF- κ B, ERK 1 / 2, AKT anti-apoptotic, inhibition of the survival signaling pathway. Rituximab Highly effective for mediating the complement-dependent toxicity (CMC) of different B cell lines and malignant B cells. The CD20-binding capacity of Rituximab is concentration-dependent.

In vivo research

Some in vivo tumor models have demonstrated that the antitumor activity of rituximab depends on complement (at least in part). Rituximab Can deplete B cells and persist for several months, so Chemicalbook can be used as an effective regimen for the treatment of B cell-mediated autoimmune diseases. In the treatment of hematological tumors, Rituximab is widely used and is currently in drug development for the treatment of several autoimmune diseases.

Security information

Toxic Substance Data :174722-31-7 (Hazardous Substances Data)

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