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acalabrutinib (Calquence)
Tyrosine Kinase Inhibitors

How it is administered

Acalabrutinib is taken by mouth as a tablet or capsule. The typical dose is 100 mg approximately every 12 hours (twice daily). It should be swallowed whole with water and can be taken with or without food. Do not chew, crush, dissolve, or cut the tablets or open the capsules. If you miss a dose by more than 3 hours, skip that dose and take the next one at the usual time.

How it works

Acalabrutinib is a targeted therapy known as a Bruton tyrosine kinase (BTK) inhibitor. BTK is an important protein in B cells, a type of white blood cell involved in many blood cancers, including Marginal Zone Lymphoma (MZL) and other B-cell lymphomas. BTK helps B cells grow, survive, and move around the body. Acalabrutinib blocks BTK’s activity by forming a strong bond with it, which stops the signals that tell cancerous B cells to grow and divide. This helps slow down or stop the progression of the cancer.

By inhibiting BTK, acalabrutinib reduces the abnormal growth and survival of malignant B cells, which is beneficial in treating certain blood cancers. It is designed to be more selective than some other BTK inhibitors, which may help reduce side effects related to off-target activity.

Common side effects

  • Diarrhea
  • Upper respiratory tract infection (such as sinus or throat infections)
  • Headache
  • Musculoskeletal pain (muscle or joint aches)
  • Lower respiratory tract infection (such as pneumonia)
  • Fatigue
  • Rash
  • Nausea
  • Bruising
  • Low blood counts (anemia, neutropenia, thrombocytopenia)

Serious side effects can include infections, bleeding, heart rhythm problems, liver problems, and development of other cancers (especially skin cancer). Regular monitoring by your healthcare team is important.

Who Should take it

Acalabrutinib is approved for adults with certain types of blood cancers, including:

  • Mantle cell lymphoma (MCL), both previously untreated (in combination with bendamustine and rituximab) and for those who have received at least one prior therapy.
  • Chronic lymphocytic leukemia (CLL) or small lymphocytic lymphoma (SLL).

While acalabrutinib is not specifically approved for Marginal Zone Lymphoma (MZL), it may be considered in certain cases where other therapies are not suitable, as it targets similar pathways involved in B-cell cancers. Your doctor will determine if acalabrutinib is appropriate for your specific situation.

Who should not take it

There are no absolute contraindications listed for acalabrutinib, but caution should be used in certain patients:

  • Patients with severe liver impairment should avoid acalabrutinib, as it can increase drug levels and 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.
  • Women should not breastfeed during treatment and for at least 2 weeks after the last dose.

Discuss your full medical history and all medications with your doctor before starting acalabrutinib, especially if you have a history of liver problems, bleeding disorders, heart rhythm problems, or frequent infections.

Commonly used with

For previously untreated mantle cell lymphoma, acalabrutinib is commonly used in combination with bendamustine and rituximab. In chronic lymphocytic leukemia or small lymphocytic lymphoma, it may be used alone or with obinutuzumab.

Your doctor may also prescribe supportive medications to help manage side effects or prevent infections, depending on your individual needs.

Commonly tested with

Acalabrutinib has been tested in clinical trials with:

  • Bendamustine and rituximab (for mantle cell lymphoma)
  • Obinutuzumab (for chronic lymphocytic leukemia and small lymphocytic lymphoma)
  • Other standard therapies for B-cell malignancies, such as idelalisib and chlorambucil, for comparison in clinical studies.
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