How it is administered

Carfilzomib is given as an intravenous (IV) infusion. It is available as a sterile, white to off-white lyophilized powder in single-dose vials of 10 mg, 30 mg, or 60 mg. The medication is prepared and diluted by a healthcare professional and administered directly into a vein over a period of 10 to 30 minutes, depending on the specific dosing regimen.

Carfilzomib is not taken by mouth and should only be given by a trained healthcare provider in a medical setting. The dosing schedule can vary, but it is typically given once or twice weekly in cycles, depending on the combination of other medications used and the specific treatment plan for multiple myeloma.

How it works

Carfilzomib is a type of medication known as a proteasome inhibitor. Proteasomes are enzyme complexes inside cells that break down and recycle proteins that are no longer needed. In multiple myeloma, cancerous plasma cells rely on proteasomes to manage the excess proteins they produce. By blocking the proteasome, carfilzomib causes a buildup of unwanted proteins inside the cancer cells, leading to stress and ultimately cell death (apoptosis).

Carfilzomib binds irreversibly to the active sites of the 20S proteasome, which is part of the larger 26S proteasome complex. This action disrupts the normal protein degradation process, specifically targeting the chymotrypsin-like activity of the proteasome. The inhibition is sustained for at least 48 hours after administration, making it effective in stopping the growth and survival of multiple myeloma cells. This targeted approach helps slow down or stop the progression of the disease.

Who Should take it

Carfilzomib is approved for adults with relapsed or refractory multiple myeloma, meaning it is used when the disease has returned after previous treatment or has not responded to other therapies. It can be used alone or in combination with other medications such as dexamethasone, lenalidomide, daratumumab, isatuximab, or daratumumab and hyaluronidase-fihj.

The specific combinations and regimens depend on how many prior treatments a patient has received and how well they tolerated those treatments. Carfilzomib is generally considered for patients who have received one to three prior lines of therapy. Your healthcare provider will determine if carfilzomib is right for you based on your treatment history, current health status, and specific characteristics of your multiple myeloma.

Who should not take it

There are no absolute contraindications listed for carfilzomib, but it should be used with caution in certain patients. People with severe heart problems (such as recent heart failure, heart attack, or uncontrolled arrhythmias), severe liver impairment, or those who have experienced severe allergic reactions to carfilzomib or any of its components may not be suitable candidates.

Carfilzomib can cause serious side effects, including heart problems, kidney failure, lung issues, high blood pressure, blood clots, and severe infusion reactions. Patients with significant pre-existing conditions in these areas should be carefully evaluated before starting treatment. Pregnant women should not use carfilzomib, as it can cause harm to an unborn baby. Women of childbearing potential and men with partners of childbearing potential should use effective contraception during and after treatment.

Commonly used with

Carfilzomib is often used in combination with other medications to treat multiple myeloma. Common combination partners include:

• Dexamethasone (a steroid)
• Lenalidomide (an immunomodulatory drug)
• Daratumumab (an anti-CD38 antibody)
• Isatuximab (another anti-CD38 antibody)
• Daratumumab and hyaluronidase-fihj (a subcutaneous formulation)

The choice of combination depends on your previous treatments and your doctor’s recommendations.

Commonly tested with

Carfilzomib has been tested in clinical trials with a variety of other medications for multiple myeloma, including:

• Lenalidomide and dexamethasone (KRd regimen)
• Dexamethasone alone (Kd regimen)
• Daratumumab and dexamethasone (DKd regimen)
• Daratumumab and hyaluronidase-fihj and dexamethasone
• Isatuximab and dexamethasone (Isa-Kd regimen)

These combinations have been studied to determine the best ways to improve outcomes for patients with relapsed or refractory multiple myeloma.