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acalabrutinib (Calquence)
Tyrosine Kinase Inhibitors

How it is administered

Acalabrutinib is taken by mouth as a tablet or capsule. The usual dose is 100 mg taken approximately every 12 hours (twice daily), with or without food. Tablets and capsules should be swallowed whole with water and should not be chewed, crushed, dissolved, opened, or cut. If you miss a dose by more than 3 hours, skip the missed dose and take the next dose at the regular time.

How it works

Acalabrutinib is a type of medicine called a Bruton tyrosine kinase (BTK) inhibitor. BTK is a protein that plays a key role in the survival and growth of certain types of blood cancer cells, especially B-cell malignancies. By blocking BTK, acalabrutinib disrupts signals that cancer cells need to grow and divide. This helps to slow down or stop the progression of blood cancers such as mantle cell lymphoma (MCL) and chronic lymphocytic leukemia (CLL).

Acalabrutinib and its active metabolite (ACP-5862) form a bond with the BTK protein, leading to its inactivation. This action prevents B-cell cancer cells from proliferating, moving, and adhering to other cells, which can help control the disease. In clinical studies, acalabrutinib has shown to maintain high levels of BTK inhibition throughout the dosing interval, contributing to its effectiveness in treating blood cancers.

Common side effects

  • Diarrhea
  • Upper respiratory tract infection
  • Headache
  • Musculoskeletal pain
  • Lower respiratory tract infection
  • Fatigue
  • Anemia
  • Neutropenia (low white blood cell count)
  • Thrombocytopenia (low platelet count)

Serious side effects can include infections, bleeding, low blood counts, second primary cancers (including skin cancer), heart rhythm problems (such as atrial fibrillation), and liver problems. Regular blood tests and monitoring are recommended during treatment.

Who Should take it

Acalabrutinib is used to treat adults with certain blood cancers:

  • Mantle cell lymphoma (MCL): It is used in combination with bendamustine and rituximab for adults with previously untreated MCL who cannot have a stem cell transplant. It is also used alone for adults with MCL who have received at least one prior therapy.
  • Chronic lymphocytic leukemia (CLL) or small lymphocytic lymphoma (SLL): It is approved for adults with these conditions, either alone or in combination with other medications.

Your doctor will determine if acalabrutinib is right for you based on your specific type of blood cancer, previous treatments, and overall health.

Who should not take it

Acalabrutinib does not have any absolute contraindications listed, but there are important precautions:

  • Patients with severe liver impairment should avoid acalabrutinib, as the medication can accumulate and increase the risk of side effects.
  • Women who are pregnant or may become pregnant should not take acalabrutinib, as it may cause harm to the unborn baby. Effective contraception is recommended during treatment and for at least 1 week after the last dose.
  • Women should not breastfeed during treatment and for at least 2 weeks after the last dose.

Always inform your healthcare provider about all your medical conditions and medications before starting acalabrutinib.

Commonly used with

Acalabrutinib is often used in combination with other medications for blood cancers:

  • Bendamustine and rituximab (for previously untreated mantle cell lymphoma)
  • Obinutuzumab (for previously untreated chronic lymphocytic leukemia or small lymphocytic lymphoma)

Your doctor may also prescribe supportive medications to help manage side effects or prevent infections.

Commonly tested with

In clinical studies, acalabrutinib has been tested with:

  • Bendamustine and rituximab (for mantle cell lymphoma)
  • Obinutuzumab (for chronic lymphocytic leukemia)
  • Compared to other treatments such as idelalisib plus rituximab or bendamustine plus rituximab in clinical trials for CLL.

These combinations and comparisons help determine the best treatment strategies for different types of blood cancers.

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