Ibrutinib Drug

 

What is ibrutinib?

 

Ibrutinib is an oral medication primarily used to treat certain types of blood cancers, including chronic lymphocytic leukemia (CLL), mantle cell lymphoma (MCL), Waldenström’s macroglobulinemia (WM), marginal zone lymphoma (MZL), and chronic graft-versus-host disease (cGVHD). It is classified as a Bruton’s tyrosine kinase (BTK) inhibitor. 

1. Chronic Lymphocytic Leukemia (CLL): Ibrutinib is used both as a first-line treatment and in cases where the disease has relapsed or is refractory.
2. Mantle Cell Lymphoma (MCL): Approved for patients who have received at least one prior therapy.
3. Waldenström’s Macroglobulinemia (WM): Used to treat this rare type of non-Hodgkin lymphoma.
4. Marginal Zone Lymphoma (MZL): For patients who require systemic therapy and have received at least one prior anti-CD20-based therapy.
5. Chronic Graft-Versus-Host Disease (cGVHD): Used after failure of one or more lines of systemic therapy.

Ibrutinib, sold under the brand name Imbruvica.

 

FDA Approval of Ibrutinib

The Generic has seen a series of FDA approvals since its introduction. Initially approved in November 2013 for mantle cell lymphoma, its use was expanded in February 2014 to include chronic lymphocytic leukemia (CLL). 

In 2015, it gained approval for treating Waldenström’s macroglobulinemia (WM). March 2016 saw a new indication for CLL, followed by another expansion in May 2016 to cover both CLL and small lymphocytic lymphoma (SLL). 

In January 2017, it was approved for adults with relapsed/refractory marginal zone lymphoma (MZL) requiring systemic therapy after at least one prior anti-CD20-based therapy. 

August 2017 marked its approval for treating graft-versus-host disease, the first FDA-approved drug for this condition. 

A tablet formulation was approved in February 2018, and later that year, in August, its combination with rituximab was approved for adults with WM. Most recently, in January 2019, a combination with obinutuzumab was approved for previously untreated CLL/SLL.

 

Mechanism of Action

Ibrutinib is a medication used to treat certain types of cancer, particularly blood cancers like chronic lymphocytic leukemia (CLL) and mantle cell lymphoma (MCL). Here’s a simple explanation of how it works:

Understanding Cancer Growth: Cancer cells grow and multiply using various signaling pathways inside the cells. These pathways act like communication networks, telling the cells when to grow and divide.

Role of BTK Protein: One key protein involved in these signaling pathways is called Bruton’s tyrosine kinase (BTK). BTK helps send signals that promote the growth and survival of cancer cells, especially in blood cancers.

How does Ibrutinib Works: Ibrutinib is a type of drug known as a BTK inhibitor. It specifically targets and binds to the BTK protein. By doing this, ibrutinib blocks the BTK protein’s activity.

Blocking Growth Signals: When ibrutinib binds to BTK, it effectively turns off the signals that tell the cancer cells to grow and survive. This interrupts the cancer cells’ ability to multiply and spread.

Promoting Cancer Cell Death: Without the growth and survival signals from BTK, the cancer cells become weaker and are more likely to die off. This helps to control the cancer and reduce the number of cancer cells in the body.

In summary, ibrutinib works by targeting and inhibiting the BTK protein in cancer cells. By blocking BTK, it stops the signals that promote cancer cell growth and survival, leading to the death of the cancer cells and helping to control the cancer.

 

Ibrutinib Side Effects

The Capsule is used to treat several conditions, and while many side effects are common across different indications, there can be variations based on the specific disease being treated and the patient population.

Ibrutinib cll side effects – Chronic Lymphocytic Leukemia (CLL) and Small Lymphocytic Lymphoma (SLL)

Common Side Effects:

• Diarrhea
• Fatigue
• Nausea
• Bruising
• Musculoskeletal pain
• Rash

Serious Side Effects:

• Increased risk of infections
• Bleeding (including severe hemorrhage)
• Atrial fibrillation
• Hypertension
• Tumor lysis syndrome (rare)

Mantle Cell Lymphoma (MCL)

Common Side Effects:

• Diarrhea
• Fatigue
• Nausea
• Bruising
• Upper respiratory tract infection
• Rash

Serious Side Effects:

• Bleeding
• Infections
• Atrial fibrillation
• Peripheral edema

Waldenström’s Macroglobulinemia (WM)

Common Side Effects of ibrutinib:

• Diarrhea
• Fatigue
• Nausea
• Bruising
• Muscle spasms

Serious Side Effects:

• Bleeding
• Atrial fibrillation
• Infections
• Pneumonia

Marginal Zone Lymphoma (MZL)

Common Side Effects:

• Diarrhea
• Fatigue
• Nausea
• Bruising
• Cough
• Rash

Serious Side Effects:

• Bleeding
• Infections
• Atrial fibrillation
• Hypertension

Chronic Graft-Versus-Host Disease (cGVHD)

Common Side Effects:

• Fatigue
• Bruising
• Diarrhea
• Nausea
• Muscle spasms

Serious Side Effects:

• Bleeding
• Infections
• Pneumonia
• Atrial fibrillation

Combination Therapy (with Rituximab or Obinutuzumab)

Common Side Effects:

• Diarrhea
• Fatigue
• Nausea
• Bruising
• Pyrexia (fever)
• Rash

Serious Side Effects:

• Infusion-related reactions (specific to combination with monoclonal antibodies)
• Infections
• Bleeding
• Atrial fibrillation
• Neutropenia (low white blood cell count)

General Monitoring and Management

Regardless of the indication, patients taking ibrutinib require regular monitoring for blood counts, liver and kidney function, and signs of infection, bleeding, and cardiovascular issues. Adjustments to dosage or supportive treatments may be necessary based on the patient’s response and side effect profile.

 

Ibrutinib Package Insert

 

Dosage and Administration 

Ibrutinib is administered orally, typically once daily. Ibrutinib capsules and tablets should be swallowed whole with a glass of water. Do not open, break, or chew them.

 

Ibrutinib Dose:

Chronic Lymphocytic Leukemia (CLL) and Small Lymphocytic Lymphoma (SLL)

• Monotherapy: 420 mg once daily. (three ibrutinib 140 mg)
• In Combination with Rituximab or Obinutuzumab: 420 mg once daily.

Mantle Cell Lymphoma (MCL)

• Monotherapy: 560 mg once daily. (four 140 mg)

Waldenström’s Macroglobulinemia (WM)

• Monotherapy: 420 mg once daily. (three 140 mg)
• In Combination with Rituximab: 420 mg once daily.

Marginal Zone Lymphoma (MZL)

• Monotherapy: 560 mg once daily for patients who require systemic therapy and have received at least one prior anti-CD20-based therapy.

Chronic Graft-Versus-Host Disease (cGVHD)

• Monotherapy: 420 mg once daily after failure of one or more lines of systemic therapy.

For dose modification contact your doctor because dose modification depends on ibrutinib adverse effects you are going through.

 

Missed a dose?

If you miss a dose of ibrutinib Take it as soon as you remember on the same day. Do not take an extra dose to make up for the missed one. Simply take the next dose at your regular scheduled time the following day. Try to take ibrutinib at the same time each day to maintain consistent blood levels of the medication. Never take two doses at once to compensate for a missed dose, as this can increase the risk of side effects.

 

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