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carfilzomib (Kyprolis)
Proteasome Inhibitors
Administration: iv

How it is administered

Carfilzomib is administered as an intravenous (IV) infusion. It comes as a sterile, white to off-white lyophilized powder in single-dose vials, available in strengths of 10 mg, 30 mg, and 60 mg. The medication is given by a healthcare professional, typically in a hospital or clinic setting. The infusion time and dosing schedule depend on the specific regimen and combination with other medications, but it is commonly given once or twice weekly.

Carfilzomib should not be given as an intravenous push or bolus. It is always diluted and infused over a set period (usually 10 or 30 minutes, depending on the regimen).

How it works

Carfilzomib is a proteasome inhibitor. It works by blocking the activity of proteasomes, which are enzyme complexes inside cells that break down proteins. In multiple myeloma and other blood cancers, cancer cells rely heavily on proteasomes to remove damaged or unneeded proteins. By inhibiting proteasomes, carfilzomib causes an accumulation of proteins within the cancer cells, leading to cell stress and ultimately cell death (apoptosis).

This targeted action helps slow down or stop the growth of cancerous plasma cells in the bone marrow. Carfilzomib’s effect is particularly useful in treating multiple myeloma, a cancer of plasma cells, especially in patients whose disease has returned (relapsed) or has not responded to previous treatments (refractory).

Common side effects

  • Anemia (low red blood cell count)
  • Fatigue
  • Thrombocytopenia (low platelet count)
  • Nausea
  • Fever (pyrexia)
  • Dyspnea (shortness of breath)
  • Diarrhea
  • Headache
  • Cough
  • Peripheral edema (swelling)

When used in combination therapies, other common side effects include hypertension (high blood pressure), upper respiratory tract infection, insomnia, and muscle spasms. Serious side effects can include heart problems, kidney problems, infusion reactions, and increased risk of infections.

Who Should take it

Carfilzomib is indicated for adults with relapsed or refractory multiple myeloma, especially those who have received one to three previous lines of therapy. It can be used alone or in combination with other medications such as lenalidomide and dexamethasone, dexamethasone alone, daratumumab and dexamethasone, or isatuximab and dexamethasone.

It is generally prescribed when other treatments have stopped working or the disease has come back. Your healthcare provider will determine if carfilzomib is appropriate based on your treatment history, current health, and response to prior therapies.

Who should not take it

There are no absolute contraindications listed for carfilzomib. However, it should be used with caution in certain patients:

  • Patients with severe cardiac problems, such as recent heart failure, uncontrolled arrhythmias, or recent heart attack, may be at higher risk for complications.
  • Patients with severe liver impairment or severe kidney impairment may require dose adjustments or close monitoring.
  • Carfilzomib can cause fetal harm, so it should not be used in pregnant women. Effective contraception is recommended for women of childbearing potential and their partners.

Always discuss your full medical history with your healthcare provider before starting carfilzomib.

Commonly used with

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

  • Lenalidomide and dexamethasone
  • Dexamethasone alone
  • Daratumumab (or daratumumab and hyaluronidase-fihj) and dexamethasone
  • Isatuximab and dexamethasone

These combinations help improve treatment effectiveness and are chosen based on your prior treatments and overall health.

Commonly tested with

Carfilzomib has been tested in clinical trials with several other medications for blood cancers, especially multiple myeloma. These include:

  • Lenalidomide
  • Dexamethasone
  • Daratumumab (both intravenous and subcutaneous forms)
  • Isatuximab
  • Melphalan and prednisone (though this combination showed increased toxicity and is not recommended for newly diagnosed, transplant-ineligible patients)

Clinical trials have also compared carfilzomib-based regimens to other standard therapies to determine the best approach for relapsed or refractory multiple myeloma.

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