Acalabrutinib

What it is and how it works

Mechanism of Action Acalabrutinib is a small-molecule inhibitor of BTK. Acalabrutinib and its active metabolite, ACP-5862, form a covalent bond with a cysteine residue in the BTK active site, leading to inhibition of BTK enzymatic activity. BTK is a signaling molecule of the B cell antigen receptor (BCR) and cytokine receptor pathways. In B cells, BTK signaling results in activation of pathways necessary for B-cell proliferation, trafficking, chemotaxis, and adhesion. In nonclinical studies, acalabrutinib inhibited BTK-mediated activation of downstream signaling proteins CD86 and CD69 and inhibited malignant B-cell proliferation and tumor growth in mouse xenograft models.

Mechanism class: Tyrosine Kinase Inhibitors

Indications

is a kinase inhibitor indicated: • In combination with bendamustine and rituximab for the treatment of adult patients with previously untreated mantle cell lymphoma (MCL) who are ineligible for autologous hematopoietic stem cell transplantation (HSCT). • For the treatment of adult patients with MCL who have received at least one prior therapy. • For the treatment of adult patients with chronic lymphocytic leukemia (CLL) or small lymphocytic lymphoma (SLL). Previously Untreated Mantle Cell Lymphoma CALQUENCE in combination with bendamustine and rituximab is indicated for the treatment of adult patients with previously untreated mantle cell lymphoma (MCL) who are ineligible for autologous hematopoietic stem cell transplantation (HSCT). Previously Treated Mantle Cell Lymphoma CALQUENCE is indicated for the treatment of adult patients with MCL who have received at least one prior therapy. Chronic Lymphocytic Leukemia or Small Lymphocytic Lymphoma CALQUENCE is indicated for the treatment of adult patients with chronic lymphocytic leukemia (CLL) or small lymphocytic lymphoma (SLL).

Dosage and administration (summary)

Recommended dose is 100 mg orally approximately every 12 hours; swallow whole with water and with or without food. • Advise patients not to break, open, or chew capsules. • Manage toxicities using treatment interruption, dose reduction, or discontinuation. • Avoid CALQUENCE in patients with severe hepatic impairment Recommended Dosage CALQUENCE Administration Instructions Advise patients to swallow capsule whole with water. Advise patients not to open, break or chew the capsules. CALQUENCE may be taken with or without food. If a dose of CALQUENCE is missed by more than 3 hours, it should be skipped and the next dose should be taken at its regularly scheduled time.

Contraindications

None. None.

Warnings and precautions

• Serious and Opportunistic Infections : Monitor for signs and symptoms of infection and treat promptly. • Hemorrhage : Monitor for bleeding and manage appropriately. • Cytopenias : Monitor complete blood counts regularly. • Second Primary Malignancies : Other malignancies have occurred, including skin cancers and other solid tumors. Advise patients to use sun protection. • Cardiac Arrhythmias : Monitor for symptoms of arrhythmias and manage. • Hepatotoxicity, Including Drug-Induced Liver Injury: Monitor hepatic function throughout treatment.

Pregnancy

Pregnancy Risk Summary Based on findings in animals, CALQUENCE may cause fetal harm and dystocia when administered to a pregnant woman. There are no available data in pregnant women to inform the drug-associated risk.

Storage and supply

How Supplied Pack Size Contents NDC Number 60-count bottle Bottle containing 60 capsules 100 mg, hard gelatin capsules with yellow body and blue cap, marked in black ink with ‘ACA 100 mg’ 0310-0512-60 Storage Store at 20°C-25°C (68°F-77°F); excursions permitted to 15°C-30°C (59°F-86°F) .

Source: Acalabrutinib (Calquence) — US FDA prescribing information, 2026-02-19, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.