Rituximab: Current and Future scope
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Rituximab: Current and Future scope

Published on May 12, 2022   -  4 min read


Rituximab is a monoclonal antibody drug used against various cancers and autoimmune conditions like pemphigus and non-Hodgkin lymphoma. Read the article to know more.

What Is Rituximab Indicated For?

Rituximab is basically a chimeric monoclonal antibody that belongs to a subclass of the immunoglobulin G1 (IgG1). This monoclonal antibody drug can treat and significantly improve the prognosis as per current research in conditions ranging from pemphigus, non-Hodgkin’s lymphoma, and even autoimmune diseases like rheumatoid arthritis to life-threatening cancers.

What Are the Structure and Pharmacokinetics of Rituximab?

The monoclonal antibody structure is, in turn, comprised of two regions:

1. Murine Variable Region (Fab region):

This region has specific and varied sections defining a target antigen. The antibody attracts and secures an exclusive antigen causing or allowing the binding of Rituximab (IgG1) to the pre-B and mature B lymphocyte cells.

2. Constant human region (Fc region):

Rituximab is generally considered safe and tolerable in most patients with only mild, infusion-related complications. Though infectious complications can also exist, with supervision, physician support, and guidance, clinical trials with this drug in many patients globally have shown long-term efficacy and tolerability. However, the dosing in dermatological conditions may vary depending on the physician’s perspective of the treatment strategy.

Rituximab secondarily also acts upon immune cells like autoreactive T-effector cells, regulatory T cells, monocyte-derived macrophages, etc. The bioavailability of this drug is 100 % with intravenous infusion and an approximate elimination half-life that varies from 30 to 400 hours depending on the dosing regimen and duration of the advocated treatment plan.

What Is the Mechanism of Action of Rituximab?

Most autoimmune diseases associated with skin eruptions and blisters (the significant being pemphigus disease) are nearly always related to the production of autoantibodies against specific components found in the epidermis or the dermo-epidermal junction of the skin. About 20 CD4+ T-cells are pivotal for the autoantibody response against the desmosomal molecular adhesiveness in pemphigus vulgaris cases wherein desmoglein 3 (Dsg3) and Dsg1 are affected.

According to clinical research, the count or frequency of autoreactive CD4+ T cells, along with the determination of the peripheral serum autoantibody titers quantification, showed the following results in patients with good long-term prognosis in their general systemic health, i.e., Rituximab drug can induce peripheral B-cell depletion for the first 6 to 12 months. This can potentially lead to a decline of serum autoantibodies with clinical improvement outcomes in most pemphigus vulgaris patients.

Furthermore, the quantities of Dsg3-specific CD4+ T cells also have been identified to decrease among the serum antibodies. Hence its primary mechanism of action or effect lies in the depletion of autoreactive B cells and the specific downregulation of Dsg3-specific CD4+ T cells.

What Are the Clinical Trials and Efficacy of Rituximab?

Rituximab’s role has been fundamental in clinical trials and research, especially in T-cell-mediated autoimmune diseases. The most common condition in T cell-mediated disease is rheumatoid arthritis which has excellent scope in dosing regimen. It has also been used recently for conditions not directly linked to autoantibody production in patients suffering from atopic dermatitis.

It has been attributed that Rituximab can be used in the treatment of scleroderma, idiopathic thrombocytopenic purpura, angioedema, vitiligo, cutaneous lupus erythematosus, Castleman’s disease, and Schnitzler syndrome, etc.

Rituximab can potentially cause a decline in the B-cell production of one of the defined or unidentified autoantibodies, similar to its role in treating pemphigus diseases. Also, in conditions like SLE (systemic lupus erythematosus), Rituximab acts through the disruption or disturbance within the B and T-cell interactions. This leads to autoreactivity within the T-cell populations causing SLE.

What Is the Dosing Regimen of Rituximab?

In NHL, the prescribed dosing of Rituximab is usually an intravenous infusion of 375mg/m2 once weekly for four to eight consecutive weeks. It forms a dosing regimen either as a single agent or in combination with other chemotherapy agents. In RA, the dosing is two intravenous infusions of 1000 mg, usually given with an approximate gap of two weeks or 15 days from the previous dose.

Many physicians also advocate the administration of Methotrexate and Rituximab. Similarly, in autoimmune dermatologic disease or disorders, the commonly prescribed dosing range is around 375mg/m2 administered as an intravenous infusion weekly for four consecutive weeks. Regimens using Rituximab alongside other active medications such as immunosuppressants or immuno-modulator drugs have shown to be clinically effective for determining the long-term success rates of this drug usage in these patients.

Also, in some instances, even high-dose intravenous immunoglobulin (IVIG) can be beneficial in the treatment of varied autoimmune diseases. Most research studies on this drug now focus open the efficacy and the potential for reduction of autoantibodies in pemphigus Vulgaris severe patients ( treated with the combination of Rituximab (375mg/m2) and IVIG (2g/kg).

What Are the Adverse Effects of Rituximab?

The occurrence or incidence of any adverse events with Rituximab is usually low or generally uncommon in patients with no history of systemic or underlying undetected diseases. Apart from a few manifestations resulting from IV infusion, they can be well tolerated.

Some patients report symptoms of possible fever, chills, headache, weakness, nausea, itching, or skin rash. The physician or dermatologist can then advise temporary stoppage or reduction in the intravenous infusion till the patient’s symptoms are relieved or reversed. In addition, the physician can give prior medication to halt such adverse events ( in cases with immunosuppressive or severe systemic disease ) with analgesics, antihistamines, or glucocorticoids. In case of reactions, these patients should report immediately to their health care provider or physician for an emergency.

The listed conditions that Rituximab can potentially trigger an adverse reaction are:

  • Hepatitis B infections.

  • Hypersensitivity reactions of anaphylaxis.

  • History of patients with pulmonary events.

  • Cardiac arrhythmias.

  • Patients with renal failure.

  • Hematological disorders like hemolytic anemias, cytopenias, and progressive multifocal leuko-encephalopathy infection.

  • Gastrointestinal perforations.

  • Cancers.

Though the possibility is low except for limited infusion effects that eventually wear out, these severe adverse effects can be triggered due to immunosuppression, poor systemic health, or underlying, undetected malignancies. Only then the probability of a patient experiencing an adverse event occurs.


Although the FDA has approved Rituximab for treating non-Hodgkins lymphoma and rheumatoid arthritis, this drug has demonstrated significant clinical and therapeutic efficacy. Hence, it is an excellent futuristic drug in various other autoimmune and immune-mediated dermatological conditions for which even traditional therapy has failed or caused significant intolerance or side effects.

Frequently Asked Questions


What Does Rituximab Target?

Rituximab targets the CD20 protein present on the surface of B cells. B cells are a type of white blood cell involved in the immune response. It stimulates the death of B cells by attaching to CD20, which lowers the immunological response. This may be advantageous in conditions where B lymphocytes are involved in the development of the illness, such as non-Hodgkin's lymphoma, chronic lymphocytic leukemia, and rheumatoid arthritis.


What Function Does Rituximab Serve?

The FDA (Food and Drug Administration) has approved Rituximab for the treatment of several autoimmune conditions, including granulomatosis with polyangiitis, chronic lymphocytic leukemia, rheumatoid arthritis, and non-Hodgkin's lymphoma. In certain cases, the medication has demonstrated effectiveness in lowering disease activity, enhancing symptoms, and achieving remission. Rituximab has also been used off-label to treat lupus and multiple sclerosis, in addition to other autoimmune diseases.


Is Rituxan Effective?

Rituxan is the brand name for Rituximab. Non-Hodgkin lymphoma, chronic lymphocytic leukemia, and other autoimmune disorders have responded well to Rituximab therapy. Rituximab has been shown in clinical trials to be efficient in lowering disease activity, improving symptoms, and producing remission in patients. Rituximab's effectiveness might, however, differ from person to person and from condition to condition, just like with any drug.


Is Rituximab Considered a High-Risk Medication?

There are several potential side effects of Rituximab, such as infusion reactions, infections, and an elevated risk of various malignancies. While most individuals tolerate the medicine well, there is a generally accepted minimal chance of significant adverse effects. While contemplating Rituximab as a therapeutic option, it is crucial to balance the dangers and potential benefits, as with any medicine.


Are There Alternatives to Rituximab?

Monoclonal antibodies and small molecule inhibitors are just two of the alternatives for Rituximab that can be used to treat autoimmune disorders. The illness being treated, medical history, current medications, and general health status will determine the therapy option. To choose the best course of therapy, it's crucial to consult with a healthcare professional frequently.


What Is the Recommended Duration for Rituximab Treatment?

Rituximab is a drug that is used to treat transplant rejection, autoimmune illnesses, and several types of cancer. The course of Rituximab treatment is determined by the patient's reaction to the medication as well as the underlying illness treated. For instance, Rituximab is frequently used alongside chemotherapy in the treatment of non-Hodgkin's lymphoma and the course of therapy may persist for several months. Rituximab's duration of usage in autoimmune illnesses varies depending on the patient's reaction to treatment, and it may be repeated as often as required to keep the disease under control.


How Long Is It Safe to Take Rituximab?

The individual's response to treatment and the underlying medical condition being treated dictates the length of Rituximab treatment. Rituximab may be used for a brief time in some circumstances and for a longer duration in others. Rituximab may be used for several years to treat autoimmune illnesses, but the treatment plan is frequently individualized based on the patient's disease activity and response to therapy.


When Was Rituximab First Used?

The US Food and Drug Administration (FDA) initially authorized Rituximab in 1997 for the management of non-Hodgkin lymphoma. Since then, it has also been licensed for the treatment of autoimmune conditions like lupus, multiple sclerosis, and rheumatoid arthritis.


What Are Rituximab’s Long-Term Effects?

Rituximab's long-term effects are determined by the underlying medical condition being treated and the patient's reaction to the medication. It is generally well tolerated. However, it can have side effects like all medicines do. Rituximab frequently causes fever, chills, lethargy, and headaches as side effects. Since it inhibits the immune system, prolonged use of the drug may also raise the risk of infection. Moreover, there have been indications that Rituximab raises the chance of acquiring specific cancers, including lymphoma and skin cancer.


Who Should Stay Away From Rituximab?

Rituximab should not be used by people who are allergic to them. The drug shouldn't be taken in people with active infections since it can further depress the immune system and raise infection risk. Rituximab should also be avoided by women who are pregnant or nursing since it may affect the fetus or newborn. Finally, those who have a history of specific cancers may need to avoid Rituximab or require closer monitoring while undergoing treatment.


Does Rituximab Result in Baldness?

Yes, one of the known negative effects of Rituximab therapy is hair loss. In clinical trials, hair loss was observed in 10 % to 15 % of Rituximab-treated patients. Hair loss often starts within the first few months of treatment and is only transitory. But on occasion, hair loss might be irreversible. If one is suffering hair loss while taking Rituximab treatment, it is vital to discuss this with the doctor.


Does Rituximab Harm the Liver?

Indeed, there have been instances where Rituximab has caused liver damage. Rituximab therapy has, on occasion, been connected to liver damage, including hepatitis and liver failure. Before beginning Rituximab therapy, it's crucial to let the doctor know if the patient has a history of liver illness or is taking any drugs that can impair liver function. To check for any potential liver damage during treatment, routine liver function tests may be required.


How Dangerous Is Rituximab?

Rituximab has a minimal toxicity profile and is typically well tolerated. But, it can have adverse effects, some of which may be serious, just like any medicine. Rituximab's most frequent adverse effects are infections, tiredness, fever, and chills. Infusion responses, heart issues, lung issues, and severe infections are just a few of the uncommon but potentially significant adverse effects. Throughout Rituximab therapy, the doctor should keep a close eye out for any possible side effects.


What Is the Most Typical Justification for Stopping Rituximab?

Disease progression is the most prevalent justification for stopping Rituximab therapy. Non-Hodgkin lymphoma and chronic lymphocytic leukemia are two malignancies of the blood and immune system that are primarily treated with Rituximab. The doctor could suggest changing to a different treatment if cancer spreads while receiving Rituximab medication.


Is Rituximab Used in the Treatment of COVID-19?

The FDA has not yet given Rituximab approval to treat COVID-19. It has, however, occasionally been employed off-label to treat severe COVID-19 infections. It is still being investigated whether Rituximab is a useful treatment for COVID-19. Therefore, this isn't yet known. It's crucial to talk to a doctor for any concerns regarding Rituximab and COVID-19.

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Last reviewed at:
12 May 2022  -  4 min read




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