[Durgical](https://durgical.com/en/) › [DurgiPedia](https://durgical.com/en/durgipedia/) › [Pharmacology](https://durgical.com/en/pharmacology/) › [Kinase inhibitors (targeted oncology)](https://durgical.com/en/pharmacology/classes/kinase-inhibitors/) › Acalabrutinib # Acalabrutinib ## Kinase inhibitors (targeted oncology)? Kinase inhibitors (targeted oncology) ## High alert? An error with this medicine can cause serious harm: double checks and protocols are used. ## Pregnancy: avoid? Avoid in pregnancy. May harm the fetus: a negative pregnancy test is needed before starting, contraception is used during treatment and for a short time after, and breastfeeding… Second-generation covalent BTK inhibitor, more selective than ibrutinib, taken twice a day for CLL, small lymphocytic lymphoma and mantle cell lymphoma. Updated Nov 1, 2026 ## Quick facts **Group** [Kinase inhibitors (targeted oncology)](https://durgical.com/en/pharmacology/classes/kinase-inhibitors/) **Target** Bruton's tyrosine kinase (BTK) **Used for** Chronic lymphocytic leukaemia · Mantle cell lymphoma **Key effects** Headache · Diarrhoea · Joint and muscle pain **Monitor** Blood count · Signs of infection and bleeding **ATC** L01EL02 No doses: the clinician sets them by the current guideline. On this page - The basics Mechanism of action - Indications - Adverse effects - Pharmacokinetics - Memory aid - Clinical What the labels mean - Safety Contraindications - Key interactions - What is monitored - Administration and safety - Pregnancy and breastfeeding - Nursing care - Study Test yourself - Connections Connections ## Mechanism of action ✂**Bruton's tyrosine kinase (BTK)**Acalabrutinib ⓘ The crystal shows acalabrutinib in the ATP site of the mouse BTK kinase domain, which is nearly identical to the human one. **Target in 3D:** Bruton's tyrosine kinase (BTK). PDB structure 8FD9 (RCSB PDB, public domain). [View the structure at RCSB PDB](https://www.rcsb.org/structure/8FD9) · Drag to rotate · pinch to zoom B-cell cancers depend on signals from the B-cell receptor, which pass through Bruton's tyrosine kinase. Acalabrutinib binds covalently and irreversibly to a cysteine in the BTK active site, switching the kinase off for good; malignant B cells lose their growth and survival signals. It hits other kinases such as EGFR and ITK less than ibrutinib, which is meant to cause fewer off-target effects. - Acalabrutinib binds a cysteine in BTK covalently - B-cell receptor signals are cut off - Malignant B cells stop growing and die ## Indications - Chronic lymphocytic leukaemia and small lymphocytic lymphoma. [Chronic lymphocytic leukaemia →](https://durgical.com/en/conditions/chronic-lymphocytic-leukaemia/) - Mantle cell lymphoma. [Non-Hodgkin lymphoma →](https://durgical.com/en/conditions/non-hodgkin-lymphoma/) ## Adverse effects ### Common - Headache - Diarrhoea, nausea, vomiting, constipation, abdominal pain - Bruising and small red or purple spots - Joint and muscle pain, tiredness, rash ### Serious (rare, important) - Serious infections, including pneumonia - Major bleeding - Cytopenias - Atrial fibrillation and other arrhythmias - Second cancers, especially non-melanoma skin cancer ## Contraindications - No absolute contraindications in the label apart from hypersensitivity; see the warnings ## Key interactions **Some prescription medicines and grapefruit** Some must not be combined with acalabrutinib or change its levels; every new medicine is checked first. ## What is monitored - Blood count - Signs of infection and bleeding - Heart rhythm (palpitations, irregular pulse) - Skin checks; hepatitis B history ## Administration and safety - Oral tablet every 12 hours, with or without food, at about the same times each day. - Swallowed whole with water: not chewed, crushed, dissolved or cut. - Hazardous drug: tablets are handled with care. ## Pregnancy and breastfeeding Avoid in pregnancy. May harm the fetus: a negative pregnancy test is needed before starting, contraception is used during treatment and for a short time after, and breastfeeding is paused. ## Nursing care - Ask about recent surgery, infections, hepatitis B, heart rhythm problems and bleeding disorders before starting. - Teach to report fever, cough, palpitations, fainting, black stools or blood in the urine. - Teach sun protection: protective clothing, sunglasses and sunscreen, because of skin cancer risk. - Review any new medicine and grapefruit with the pharmacist. ## Pharmacokinetics **Absorption** Oral, twice a day, with or without food. **Metabolism** Liver; some medicines and grapefruit change its levels. **Half-life** Short, about 1 hour (its active metabolite about 3.5 hours), yet BTK stays blocked because the binding is covalent. ## Memory aid ACALAbrutinib = ibrutinib with better ACCuracy: the same covalent lock on BTK, fewer off-target kinases. Still watch bleeding, infection and atrial fibrillation. ## Test yourself Think of the answer, then tap the question to see it. ## How does acalabrutinib bind BTK? Covalently and irreversibly, to a cysteine in the active site. ## How does acalabrutinib differ from ibrutinib? It is more selective for BTK, with less effect on kinases such as EGFR and ITK. ## Which skin advice is given to patients on acalabrutinib, and why? Sun protection, because second cancers, especially skin cancers, are more common. [Add to my cards (3)](https://durgical.app/estudiar/?add=/en/pharmacology/acalabrutinib/) [More Pharmacology questions →](https://durgical.com/en/practice/?f=pharmacology) ## What the labels mean **High alert** An error with this medicine can cause serious harm: double checks and protocols are used. **Pregnancy: avoid** Avoid in pregnancy. May harm the fetus: a negative pregnancy test is needed before starting, contraception is used during treatment and for a short time after, and breastfeeding… ## Connections ## Related drugs 2 - [Ibrutinib](https://durgical.com/en/pharmacology/ibrutinib/) - [Rituximab](https://durgical.com/en/pharmacology/rituximab/) ## Related conditions 2 - [Chronic lymphocytic leukaemia](https://durgical.com/en/conditions/chronic-lymphocytic-leukaemia/) - [Non-Hodgkin lymphoma](https://durgical.com/en/conditions/non-hodgkin-lymphoma/) [← Back to the class: Kinase inhibitors (targeted oncology)](https://durgical.com/en/pharmacology/classes/kinase-inhibitors/) Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given. Sources: [Acalabrutinib: MedlinePlus Drug Information](https://medlineplus.gov/druginfo/meds/a618004.html) (MedlinePlus (U.S. National Library of Medicine), 2025); [ATCDDD - ATC/DDD Index](https://atcddd.fhi.no/atc_ddd_index/?code=L01EL02) (WHO Collaborating Centre for Drug Statistics Methodology, 2026); [Structure of BTK kinase domain with the second-generation inhibitor acalabrutinib](https://www.rcsb.org/structure/8FD9) (RCSB Protein Data Bank, 2023). ## **Spotted a mistake?** We are always improving for the community. Tell us what is wrong and our team will review it. Report a mistake Representative model, for educational purposes only. --- Source: https://durgical.com/en/pharmacology/acalabrutinib/ License: CC BY 4.0 (https://creativecommons.org/licenses/by/4.0/). Cite as: DurgiPedia (durgical.com), https://durgical.com/en/pharmacology/acalabrutinib/