Calquence

Chronic lymphocytic leukemia (CLL) or small lymphocytic lymphoma (SLL) — in adult patients; Mantle cell lymphoma (MCL) — in adults who have received at least one prior therapy

CLL/SLL: 100 mg orally approximately every 12 hours until disease progression or unacceptable toxicity
MCL: 100 mg approximately every 12 hours until disease progression or unacceptable toxicity
Capsules: Swallow whole with water; may take with or without food
Tablets: Swallow whole; do not cut, crush, or chew
If dose is missed by >3 hours: Skip and resume at next scheduled time

Capsules: 100 mg; Tablets: 100 mg

None listed.

• Serious Infections: Fatal and serious infections reported (21%). Includes opportunistic infections. Consider prophylaxis in at-risk patients.
• Hemorrhage: Fatal and serious hemorrhagic events. Major hemorrhage in 3.6% of patients.
• Cytopenias: Grade 3-4 neutropenia (19%), anemia (8%), thrombocytopenia (7%). Monitor CBC monthly.
• Second Primary Malignancies: Including skin cancers (12%) and other cancers.
• Atrial Fibrillation/Flutter: In 4.5% of patients. Monitor patients with cardiac risk factors.

Headache (38%), diarrhea (31%), musculoskeletal pain (25%), infection (upper respiratory tract 22%), bruising (21%), neutropenia (19%), fatigue (14%), nausea (13%), cough (11%), abdominal pain (9%)

Consult the complete prescribing information for a comprehensive list of adverse reactions and their frequencies.

Consult the complete prescribing information for drug interactions, including effects on CYP enzymes, transporters, and concomitant medications that may require dose adjustments or monitoring.

Consult the full prescribing information for pregnancy-related considerations.

Refer to prescribing information for lactation guidance.

Pediatric safety and efficacy information is detailed in the full label.

Dose modifications for organ impairment are specified in the complete prescribing information.

Acalabrutinib is a selective, irreversible, small-molecule inhibitor of Bruton's tyrosine kinase (BTK). It forms a covalent bond with cysteine 481 in the BTK active site. Acalabrutinib and its active metabolite (ACP-5862) inhibit BTK-mediated activation of downstream signaling proteins CD86 and CD69, inhibiting malignant B-cell proliferation and survival. Acalabrutinib was designed for greater BTK selectivity compared to first-generation BTK inhibitors.

Tmax: 0.75-1 hour. Half-life: ~1 hour (parent); active metabolite (ACP-5862) t½ ~3.5 hours. Protein binding: 97.5%. Metabolized by CYP3A (active metabolite ~50% of parent exposure). Excreted in feces (84%) and urine (12%).

Clinical efficacy and safety data supporting the approval are available in the full prescribing information and from the clinical trials listed below.

• ELEVATE-TN — Acalabrutinib ± obinutuzumab vs. chlorambucil + obinutuzumab in 1L CLL. Phase III, n=535.
  🔬 NCT02475681 ↗ 📄 Primary Publication ↗
• ASCEND — Acalabrutinib vs. idelalisib/rituximab or BR in relapsed/refractory CLL. Phase III, n=310.
  🔬 NCT02970318 ↗ 📄 Primary Publication ↗

Calquence has FDA-approved indications across the following cancer types covered on PipelineEvidence: