• Mantle cell lymphoma (MCL) in patients who have not responded to ≥1 previous therapy.
• Chronic lymphocytic leukemia (CLL) or small lymphocytic lymphoma (SLL).

Contraindicated in:

• Concurrent use of strong CYP3A4 inducers/inhibitors
• Severe hepatic impairment
• OB: Pregnancy;
• Lactation: Lactation.

Use Cautiously in:

• Concurrent use of moderate inhibitors of CYP3A4 (↓ dose of acalabrutinib)
• Concurrent use of antiplatelet agents/anticoagulants (↑ risk of bleeding)
• Surgical procedures (if possible withhold for 3–7 days pre- and post-operatively)
• Pedi: Safety and effectiveness not established in children.

CV: atrial fibrillation/flutter.

Derm: rash.

GI: abdominal pain, constipation, diarrhea, nausea, vomiting.

GU: ↑ serum creatinine.

Hemat: anemia, hemorrhage, neutropenia, thrombocytopenia.

MS: myalgia.

Neuro: headache, PROGRESSIVE MULTIFOCAL LEUKOENCEPHALOPATHY (PML).

Misc: fatigue, infection, second malignancy.

Drug-Drug:

• Strong CYP3A inhibitors, including itraconazole can significantly ↑ levels and risk of toxicity; avoid concurrent use. If short-term use of strong CYP3A inhibitor is necessary, acalabrutinib may be temporarily interrupted.
• Moderate CYP3A4 inhibitors may ↑ levels and risk of toxicity; avoid concurrent use; if concurrent therapy is necessary, ↓ acalabrutinib dose.
• Strong CYP3A inducers, including rifampin significantly ↓ blood levels and effectiveness; avoid concurrent use; if concurrent therapy is necessary, ↑ acalabrutinib dose.
• Proton pump inhibitors, H₂ receptor antagonists, or antacids may ↓ levels; separate antacids from acalabrutinib by ≥2 hr; take acalabrutinib 2 hr before H₂ receptor antagonist; avoid concurrent use with proton pump inhibitors.

• Capsules: 100 mg;
• Tablets: 100 mg;

• PO (Adults): 100 mg twice daily until disease progression or unacceptable toxicity. In patients with CLL or SLL, when given in combination with obinutuzumab, initiate acalabrutinib in Cycle 1 and administer prior to obinutuzumab when given on the same day. Concurrent use of moderate CYP3A inhibitors: 100 mg once daily until disease progression or unacceptable toxicity; Concurrent use of strong CYP3A inducers: 200 mg twice daily until disease progression or unacceptable toxicity.

Calquence

• Binds to and inactivates the enzymatic activity of Bruton tyrosine kinase (BTK), which leads to inhibition of B-cell proliferation and survival.

• Decreased progression of MCL.
• Improved progression-free survival in CLL/SLL.

Therapeutic Classification: antineoplastics

Pharmacologic Classification: kinase inhibitors

Absorption: 25% bioavailability following oral administration.

Distribution: Widely distributed to tissues.

Protein Binding: 97.5%.

Metabolism/Excretion: Metabolized in the liver primarily by the CYP3A enzyme system to an active metabolite (ACP-5862) (50% less potent than acalabrutinib with regard to BTK inhibition). One minor metabolite has antineoplastic activity. Metabolites are mostly eliminated in feces (84%), 12% excreted in urine.

Half-life: Acalabrutinib: 0.9 hr; ACP-5862: 6.9 hr.

(plasma concentrations)

• Instruct patient to take medication as directed. If dose is missed by >3 hrs, omit dose and take next dose at regularly scheduled time; do not double doses.
• Advise patient to use protective clothing and sunscreen and avoid sun exposure to prevent secondary skin malignancies.
• Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications.
• Instruct patient to notify health care professional if signs of bleeding (blood in stools or black, tarry stools, pink or brown urine, unexpected bleeding, severe or uncontrolled bleeding, vomit blood or vomit that looks like coffee grounds, cough up blood or blood clots, dizziness, weakness, confusion, changes in speech, prolonged headache), infection (fever, chills, flu-like symptoms) or heart rhythm problems (fast or irregular heartbeat, feeling lightheaded or dizzy, fainting, shortness of breath, chest discomfort).
• Rep: May cause fetal harm and dystocia. Advise females of reproductive potential to use effective contraception during and for at least 1 wk after last dose and to avoid breastfeeding for at least 2 wks after last dose. Advise patient to notify health care professional promptly if pregnancy is suspected.

a-KAL-a-broo-ti-nib

NDC Code^*

• 0310- AstraZeneca Pharmaceuticals LP
  • 0310-0512- CALQUENCE
    • 0310-0512-28- 28 CAPSULE, GELATIN COATED in 1 BOTTLE (0310-0512-28)

• 0310- AstraZeneca Pharmaceuticals LP
  • 0310-0512- CALQUENCE
    • 0310-0512-60- 60 CAPSULE, GELATIN COATED in 1 BOTTLE (0310-0512-60)