.jpeg)
{{ variable.name }}
Generic name: Rituximab
Trade name: Rituxan
All names: Rituximab, Rituxan, Ristova, Rituxan, Truxima, rituximab-abbs, Ruxienc e, rituximab-pvvr
Indications:
1. Used to treat certain types of cancer (such as non-Hodgkin lymphoma, chronic lymphocytic leukemia). It works by slowing or stopping the growth of cancer cells.
2. Used to treat rheumatoid arthritis and reduce joint pain and swelling.
3. Used to treat certain types of blood vessel diseases and can reduce the swelling of blood vessels.
4. Used to treat certain skin diseases (pemphigus vulgaris). It helps reduce the number of skin lesions.
Dosage:
Rituximab is administered by intravenous infusion. Patients should receive acetaminophen (Tylenol) and an antihistamine before the infusion to reduce the severity of infusion reactions.
Patients with rheumatoid arthritis should also receive methylprednisolone (Medrol, Depo-Medrol) 100 mg or a similar medication 30 minutes before the infusion to reduce the severity of infusion reactions.
Non-Hodgkin's B-cell lymphoma: 375 mg/m2 weekly for 4 to 8 weeks or longer.
Chronic lymphocytic leukemia: 375 mg/m² IV on Day 1 of the first cycle (given 1 day before FC chemotherapy for the first cycle), then 500 mg/m² IV on Day 1 of subsequent cycles (given on the same day as FC chemotherapy) repeated for a cycle of 28 days x 6 cycles
Granulomatosis with polyangiitis or microscopic polyangiitis: 375 mg/m² IV weekly 4 weeks
Rheumatoid arthritis: intravenous infusion of 1000 mg, repeat after 2 weeks (2 infusions at 2-week intervals are one course of treatment) Repeat the course every 24 weeks or according to clinical evaluation (but not earlier than 16 weeks)
Adverse reactions:
> 10%
Non-Hodgkin lymphoma
Angioedema (11%)
Weakness (26%), chills (33%), dizziness (10%), fever (53%), headache (19%)
Pruritus (14%), rash (15%)
Abdominal pain (14%), diarrhea (10%), nausea (23%), vomiting (10%)
Leukopenia (14%), lymphopenia (48%), moderate Neutropenia (14%), thrombocytopenia (12%)
Back pain (10%), myalgia (10%)
Cough (13%), rhinitis (12%)
Infection (31%), night sweats ( 15%)
GPA and MPA vascular inflammation
Nausea (18%)
Diarrhea (17%)
Headache (17%)
Muscle cramps (17%)
Anemia (16%)
Peripheral edema (16%)
Insomnia (14%)
Joint pain (13%)
Cough (13%)
Fatigue (13%)
Increased alanine aminotransferase (13%)
Hypertension (12%)
Static electricity (11%)
Infusion reaction (58%)
Depression (18%)
Herpes simplex (13 %)
Alopecia (13%)
1-10%
Non-Hodgkin lymphoma
Puffiness
Flush
Hypertension
Anxiety
Poverty Blood
Hyperglycemia
Bronchospasm, dyspnea, sinusitis, throat irritation, urticaria
Rheumatoid (rituximab + methotrexate vs methotrexate)
Hypertension
Anxiety, fatigue, chills, migraine, paresthesia, fever
Pruritus, urticaria
Indigestion, nausea, upper abdominal pain
Hypercholesterolemia
Joint pain
Rhinitis, throat inflammation, upper respiratory tract infection
p>
GPA and MPA vasculitis
Dyspnea (10%)
Leukopenia (10%)
Skin rash (10%)
Fatigue (8%)
Epigastric pain (5%)
Conjunctiva inflammation (5%)
Dizziness, headache (5%)
Herpes zoster (5%)
Irritability (5%)
Myalgia (5%)
Fever (5%)
Tachycardia (5%)
Pruritus Itching, skin disorders, papillomas, urticaria (5%)
Frequency not defined
Tumor lysis syndrome
Lymphoid malignancies
Hypoglobulinaemia
Post-marketing reports
Hematology: Complete blood cell Penopenia, bone marrow hypoplasia, grade 3-4 moderate granulocytopenia or late onset, hyperviscosity syndrome of Waldenstrom's macroglobulinemia, prolonged hypoglobulinemia
Cardiac: Fatal heart failure
Immune/autoimmune events: uveitis, optic nerve vasculitis, systemic vasculitis, pleurisy, lupus-like syndrome, serum sickness, polyarticular arthritis, and vasculitides of rash
Infections: An increase in fatal infections from viral infections, including progressive multifocal leukoencephalopathy (PML), HIV-associated lymphoma, and reported grade 3 and 4 infections Increased incidence
Neoplasia: disease progression in Kaposi's sarcoma
Skin: severe mucocutaneous reactions
Gastrointestinal tract: intestinal obstruction and perforation
Lungs: fatal bronchiolitis obliterans and fatal interstitial lung disease
Nervous Systemic: Posterior Reversible Encephalopathy Syndrome (PRES)/Reversible Posterior Leukoencephalopathy Syndrome (RPLS)
Contraindications:
Rituximab is contraindicated in patients with known hypersensitivity to any component of this drug and to murine protein.
Precautions:
Before using rituximab, tell your doctor or pharmacist if you are allergic to it. Or if you have other allergies. This product may contain inactive ingredients that may cause allergic reactions or other problems. Contact your pharmacist for more details.
Before using this medication, tell your doctor or pharmacist your medical history, especially of: lung disease, heart problems (such as irregular heartbeat, previous heart attack), bleeding/blood disorders, current/recent infection.
This medicine may make you dizzy. Alcohol or marijuana (cannabis) can make you dizzy. Do not drive, use machinery, or do anything that requires caution until you can do so safely. Limit alcoholic beverages. If you use marijuana (cannabis), talk to your doctor.
Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).
Rituximab can make you more susceptible to infections or may make a current infection worse. Avoid contact with infected people (e.g., chickenpox, measles, influenza) that may be spread to others. Please consult your doctor if you have been infected or for more details.
No immunization/vaccination without doctor’s consent. Avoid contact with people who have recently received live vaccines (such as flu shots inhaled through the nose).
To reduce the chance of cuts, scrapes, or injuries, use caution with sharp objects, such as razors and nail clippers, and avoid activities such as contact sports.
Older adults may be at greater risk of heart problems (such as irregular heart rhythm) or lung disease while using this drug.
During pregnancy, this medication should be used only when clearly needed. It may harm an unborn baby. Ask about reliable forms of birth control while using this medication and for 1 year after stopping treatment. If you are pregnant, discuss the risks and benefits of this medication with your doctor right away.
It is not known whether this drug passes into breast milk. Due to the possible danger to the baby, breastfeeding is not recommended while using this medication and for at least 6 months after treatment. Consult your doctor before breastfeeding.
Storage:
Unused vials: refrigerated at 2-8°C (36-46°F); protect vials from direct sunlight
Dilute solutions: store at 2-8°C (36-46°F) 24 hours; shown to be stable at room temperature for 24 hours
Mechanism of action:
Rituximab is a human-mouse chimeric monoclonal antibody that can specifically bind to the transmembrane antigen CD20. CD20 antigen is located on the surface of pre-B and mature B lymphocytes, while hematopoietic stem cells, pre-pre-B cells, normal plasma cells or other normal tissues do not express CD20. More than 95% of B-cell non-Hodgkin lymphoma tumor cells express CD20. After antigen-antibody binding, CD20 will not be internalized or shed from the cell membrane into the surrounding environment. CD20 does not circulate in plasma as free antigen and therefore cannot compete with antibodies for binding. After rituximab binds to the CD20 antigen on B cells, it initiates an immune response that mediates B cell lysis. Possible mechanisms of B cell lysis include: complement-dependent cytotoxicity (CDC), antibody-dependent cellular cytotoxicity (ADCC). After the first infusion of rituximab, the peripheral B lymphocyte count decreased significantly and was lower than the normal level. It began to recover after 6 months and returned to normal between 9 and 12 months after the completion of treatment. In vitro experiments have shown that rituximab can increase the sensitivity of drug-resistant human B lymphoma cell lines to the cytotoxic effects of certain chemotherapy drugs.
Efficacy and safety:
1. B-cell malignant tumors
1) Non-Hodgkin's lymphoma (NHL)
In a phase II clinical trial, 40 patients with newly treated FL were treated with rituximab + CHOP for 6 cycles, with an overall effective rate of 95% and a CR rate of 55%. . Foreign studies have shown that R-FCM treatment for relapsed patients can prolong the PFS of the patients. Laurie et al. used rituximab and CHOP combined treatment in 292 patients with advanced diffuse large B-cell NHL in British Columbia. 140 patients in the CHOP group were treated with the combination. There were 152 cases in the combination treatment group. The results showed that the overall survival rate of the combination treatment group was significantly higher than that of the CHOP group. At the same time, the study analyzed the impact of age on treatment. There was no significant difference in the overall survival rate and 2a disease-free survival rate, indicating that the combination of rituximab and CHOP was not affected by the age of the patient. A large number of Clinical research and application have shown that rituximab combined with chemotherapy can significantly improve the remission rate, prolong the remission time, and is safe without age restrictions. In addition, the use of rituximab combined with radionuclides in the treatment of NHL has achieved significant results, providing a new treatment model for the treatment of lymphoma.
2) Therapeutic lymphocytic leukemia (CLL)
Treatment of 50 patients (including 40 cases of CLL), intravenous infusion of 375mg/m2 for the first time, and increased from 500mg to 2250mg/m2 for the second time. The patients showed an obvious dose-effect response relationship, with the lowest The dose response rate is 22%, and the maximum dose response rate is 75%. The MD1Anderson Cancer Center research group can increase the CR rate by combining fludarabine + cyclophosphamide with rituximab. Some scholars believe that combined chemotherapy will increase hematological toxicity. The treatment of CLL should take into account the prognostic factors of the disease and quality of life.
3) Multiple myeloma (MM)
Plasma cells in MM patients express a small number and low density of CD20. Therefore, it is necessary to increase the expression of CD20 on the surface of MM tumor cells to make rituximab effective against MM tumor cells. Domestic experimental results show that when the concentration of thalidomide is greater than 100Ixg/mL or greater than 150Ixg/mL combined with 16Ixg/mL of rituximab, it is effective for initial treatment or relapsed and refractory treatment respectively. The inhibitory effect of tumor cell colony formation in MM patients was greater than that of the same concentration of thalidomide or rituximab alone, indicating that thalidomide can increase the inhibitory effect of rituximab on MM cell growth, which may be related to the former's upregulation of CD20 expression in tumor cells. From this experiment, the clinical use of thalidomide and rituximab in combination with newly treated or relapsed and refractory MM patients may be another direction in the treatment of MM.
2. Autoimmune diseases
1) B lymphocytes and immune abnormalities
B lymphocytes are one of the main members of the acquired immune response. Their development process mainly goes through the following stages): pre-B lymphocytes, immature B lymphocytes, initial B lymphocytes, mature B lymphocytes and memory B lymphocytes, and finally differentiate into antibody-producing plasma cells. CD20+ B lymphocytes participate in immunity including: production of immunoglobulins, which act through immunoglobulins; presentation of self-antigens by B lymphocytes to other immune cells Regulation of immune cells; B lymphocytes affect other antigen-presenting cells such as dendritic cells. B lymphocytes can secrete interleukin (IL-4, IL-10) and other cytokines to act on other immune cells. Abnormal interactions between B cells and T cells have a negative impact on immune diseases. Rituximab is a monoclonal antibody directed against the CD20 molecule on the surface of B lymphocytes. It can bind to the CD20 molecule on the cell surface with high affinity, leading to the elimination of bound B lymphocytes and a significant reduction in the number of B lymphocytes in the body.
2) Application of B cell depletion in autoimmune diseases
Systemic lupus erythematosus: 6 active lupus patients who failed traditional immunosuppressive treatment were treated with Rituximab + CTX, 3 of whom had type IV lupus nephritis. 1 had central nervous system disease, and 2 Anti-dsDNA antibody titers were significantly reduced in 4 patients, hemoglobin and erythrocyte sedimentation rate were significantly improved in 4 patients, and renal lesions were improved in 2 patients without obvious side effects. This combined treatment regimen can better prevent the production of HACAs and can effectively eliminate memory B cells. The prospect of rituximab for the treatment of SLE is optimistic .However, current literature reports are mostly based on individual case reports and lack large-scale prospective, randomized controlled, multi-center clinical trials. Regarding whether to combine with other cytotoxic drugs or hormones, whether the therapeutic effect of SLE patients with certain/certain clinical manifestations is more obvious than that of other patients, how to choose the treatment endpoint, and whether to use it in combination Whether cytotoxic drugs or pre-treatment with full dose Rituxan can prevent the production of HACAs. In most patients who receive Rituxan, B cells will return to the peripheral blood after 6 months. Whether this will lead to the recurrence of the disease, the timing and dosage of re-treatment, these issues require controlled trials or accumulation of experience.
3. Rheumatoid arthritis (RA): reported 5 female patients with active progressive erosion of RA who did not respond to the combination of MTX and cyclosporine A, 2 of whom were ineffective with anti-TNF treatment. After receiving anti-CD20 treatment alone (weekly RTX 375mg/m2 intravenous infusion for 4 weeks), 2 patients were found to have significant improvement. (ACR70 and ACR50 respectively), 2 cases were effective (ACR20), and 1 case was ineffective.
4. Idiopathic thrombocytopenic purpura (ITP): The efficacy of rituximab in 12 patients with refractory ITP (including 4 cases of Evans syndrome) was retrospectively analyzed. All of them received more than one conventional treatment and were ineffective. 6 of them also received corticosteroids or other immunosuppressants during treatment with rituximab. As a result, 5 patients achieved CR, and effective responders were seen in both splenectomy and non-splenectomy patients. Rituxan is a new biological agent that treats rituximab. The toxicity of the treatment is relatively small, and it can play a certain role in the treatment of refractory ITP with severe bleeding symptoms. It can be used as an effective alternative treatment for patients who are ineffective with conventional drugs. At the same time, its efficacy in ITP has also attracted more attention to the role of the humoral immune mechanism in ITP. However, the high price of rituximab limits its widespread clinical application. On the other hand, its specific mechanism of action and reasonable treatment options require further research.
5. Others
Some reports indicate that Rituximab has good therapeutic response in the treatment of thrombotic thrombocytopenic purpura, coagulation disorders caused by increased acquired factor VIII antibodies, hemolytic anemia and refractory Greave’s disease. There are also case reports of its use in the treatment of primary nephrotic syndrome, Wegener’s granulomatosis, etc.