acalabrutinib maleate: prescribing and clinical use
Focused clinical detail for use alongside current product information, local policy and patient-specific assessment.
acalabrutinib maleate: clinical details
Prescribing considerations
- Treatment should be initiated and supervised by a clinician experienced with anticancer treatments.
- Review bleeding history, antithrombotic therapy, infections, hepatitis B status, cardiac history, renal and hepatic function, tumour burden and interacting treatments.
- Consider planned interruption around surgery or invasive dental procedures according to individual bleeding risk.
- Severe hepatic impairment is not recommended; severe renal impairment requires an individual benefit-risk assessment and close toxicity monitoring.
- Patients with severe cardiovascular disease were excluded from clinical studies.
Contraindications and cautions
- Hypersensitivity to acalabrutinib or any excipient.
- Warfarin and other vitamin K antagonists should not be administered concurrently.
- Avoid strong CYP3A inhibitors and strong CYP3A inducers where possible.
Monitoring
- Full blood count as clinically indicated.
- Signs of bleeding and infection, including opportunistic infection.
- Hepatitis B screening before treatment and specialist management if serology is positive.
- Palpitations, syncope, chest pain or dyspnoea; obtain an ECG when indicated.
- Renal function and hydration, particularly with renal impairment.
- Skin examination and sun-protection counselling.
- Tumour lysis risk in people with bulky disease.
- New pulmonary symptoms in the relevant combination setting.
- New neurological, cognitive or behavioural symptoms suggesting PML.
Clinical pharmacology
Acalabrutinib selectively and covalently inhibits BTK; its active metabolite ACP-5862 also inhibits BTK. Acalabrutinib is predominantly metabolised by CYP3A and has minimal renal elimination.
Formulation and product differences
- The selected product is a film-coated tablet containing the maleate salt of acalabrutinib.
- The maleate tablet has improved solubility at higher gastric pH and can be co-administered with acid-reducing treatments.
- Tablets must be swallowed whole and must not be crushed, dissolved, chewed or divided.
acalabrutinib maleate preparations and strengths
Tablet
Route: Oral
Strengths: 100 mg
acalabrutinib maleate interactions
A specialist or pharmacist should check all medicines and herbal products because acalabrutinib is affected by CYP3A and may alter exposure to some other treatments.
Strong CYP3A/P-gp inhibitors, including clarithromycin, itraconazole, posaconazole, voriconazole and ritonavir
They can markedly increase acalabrutinib exposure and toxicity; concurrent use should generally be avoided and managed by the cancer team.
Strong CYP3A inducers, including rifampicin, carbamazepine and phenytoin
They can substantially reduce acalabrutinib exposure and may reduce effectiveness, so concurrent use should be avoided.
St John's wort
It can unpredictably reduce acalabrutinib exposure and should be avoided.
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.