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acalabrutinib (Calquence)
Tyrosine Kinase Inhibitors

How it is administered

Acalabrutinib is taken orally, usually as a tablet or capsule. The recommended dose for adults with chronic lymphocytic leukemia (CLL) is 100 mg by mouth approximately every 12 hours, with or without food. The tablet or capsule should be swallowed whole with water and should not be chewed, crushed, dissolved, or cut. If you miss a dose by more than 3 hours, skip that dose and take the next dose at the usual time. Do not take extra tablets or capsules to make up for a missed dose.

How it works

Acalabrutinib is a small-molecule inhibitor of Bruton tyrosine kinase (BTK), a protein that plays a key role in the survival and growth of B cells, including cancerous B cells found in CLL. By blocking BTK, acalabrutinib interrupts signals that help cancer cells grow and survive. This leads to reduced proliferation and increased death of malignant B cells. In clinical studies, acalabrutinib and its active metabolite (ACP-5862) form a covalent bond with BTK, leading to sustained inhibition of its activity. This mechanism helps control the progression of CLL and other B-cell malignancies by targeting the pathways necessary for cancer cell proliferation, movement, and adhesion.

Common side effects

  • Diarrhea
  • Upper respiratory tract infection (such as sinusitis or nasopharyngitis)
  • Headache
  • Musculoskeletal pain (including muscle aches and joint pain)
  • Lower respiratory tract infection (such as pneumonia or bronchitis)
  • Fatigue
  • Anemia (low red blood cell count)
  • Neutropenia (low white blood cell count)
  • Thrombocytopenia (low platelet count)
  • Bruising

Most side effects are mild to moderate, but some can be serious, such as infections, bleeding, or changes in blood counts. Your healthcare provider will monitor you regularly for these effects.

Who Should take it

Acalabrutinib is indicated for adults with chronic lymphocytic leukemia (CLL) or small lymphocytic lymphoma (SLL). It can be used alone or in combination with other medications, such as obinutuzumab. It is also approved for certain types of mantle cell lymphoma (MCL). Your doctor may recommend acalabrutinib if you have been diagnosed with CLL or SLL, regardless of whether you have received previous treatments. The decision to use acalabrutinib will depend on your specific medical history, other health conditions, and previous therapies.

Who should not take it

There are no absolute contraindications listed for acalabrutinib. However, it should be used with caution in people with severe liver impairment, as its use is not recommended in this group. Patients should inform their healthcare provider about all medications they are taking, especially strong CYP3A inhibitors or inducers, as these can affect how acalabrutinib works. Women who are pregnant or breastfeeding should not take acalabrutinib, as it may cause harm to the unborn baby or nursing infant. Always discuss your full medical history with your doctor before starting this medication.

Commonly used with

Acalabrutinib is often used in combination with other medications for CLL, such as obinutuzumab (an antibody therapy). In mantle cell lymphoma, it may be combined with bendamustine and rituximab. Your doctor will determine the best combination based on your specific type of blood cancer and treatment history.

Commonly tested with

Acalabrutinib has been studied in combination with obinutuzumab for previously untreated CLL and with bendamustine and rituximab for mantle cell lymphoma. It has also been compared to other treatments such as idelalisib plus rituximab or bendamustine plus rituximab in clinical trials for relapsed or refractory CLL. These combinations and comparisons help determine the most effective and safest ways to use acalabrutinib in treating blood cancers.

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