acalabrutinib (Rx)

Brand and Other Names:Calquence
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Dosing & Uses


Dosage Forms & Strengths


  • 100mg

Mantle Cell Lymphoma

Indicated for mantle cell lymphoma (MCL) in patients who have received ≥1 prior therapy

100 mg PO q12hr

Continue until disease progression or unacceptable toxicity

Chronic Lymphocytic Leukemia or Small Lymphocytic Lymphoma

Indicated for treatment of chronic lymphocytic leukemia (CLL) or small lymphocytic lymphoma (SLL)


  • 100 mg PO q12hr
  • Continue until disease progression or unacceptable toxicity

Combination with obinutuzumab

  • Indicated for patients with previously untreated CLL or SLL
  • Administer for 6 treatment cycles (28-day cycles)
  • Refer to obinutuzumab for infusion rates
  • Cycle 1
    • Days 1-28: Acalabrutinib 100 mg PO q12hr
    • Day 1: Obinutuzumab 100 mg IV infusion
    • Day 2: Obinutuzumab 900 mg IV infusion
    • Days 8 and 15: Obinutuzumab 1000 mg IV infusion
  • Cycles 2-6
    • Day 1-28: Acalabrutinib 100 mg PO q12hr
    • Day 1: Obinutuzumab 1000 mg IV infusion

Dosage Modifications

Refer to the obinutuzumab prescribing information for management of obinutuzumab toxicities

Renal impairment

  • Mild-to-moderate (eGFR ≥30 mL/min/1.73m²): No clinically relevant pharmacokinetics (PK) difference observed
  • Severe (eGFR <30 mL/min/1.73m²) or patients on dialysis: Acalabrutinib PK has not been evaluated

Hepatic impairment

  • Mild-to-moderate (Child-Pugh A or B): No dosage adjustment necessary
  • Severe (Child-Pugh C): Avoid use

Management of Grade ≥3 adverse reactions

  • Grade ≥3 nonhematologic toxicities,
  • Grade 3 thrombocytopenia with bleeding,
  • Grade 4 thrombocytopenia, OR
  • Grade 4 neutropenia lasting >7 days
  • First to second occurrence
    • Interrupt drug
    • Once toxicity resolves to Grade ≤1, resume dose at 100 mg PO BID
  • Third occurrence
    • Interrupt drug
    • Once toxicity resolves to Grade ≤1, reduce dose to 100 mg PO qDay
  • Fourth occurrence
    • Discontinue drug

Coadministration with CYP3A4 inhibitors or inducers

  • Strong CYP3A4 inhibitors: Avoid concomitant use; if CYP3A4 inhibitors will be used short-term (eg, anti-infectives for ≤7 days), interrupt treatment
  • Moderate CYP3A4 inhibitor: 100 mg PO qDay
  • Strong CYP3A4 inducers: Avoid concomitant use; if these inducers cannot be avoided, increase dose to 200 mg PO BID

Coadministration with gastric acid reducing agents

  • Proton pump inhibitors: Avoid concomitant use
  • H2-receptor antagonists: Take dose 2 hr before taking a H2-receptor antagonist
  • Antacids: Separate dosing by at least 2 hr

Safety and efficacy not established



Interaction Checker

and acalabrutinib

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      Serious - Use Alternative

        Significant - Monitor Closely


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            Adverse Effects

            >10% (Monotherapy)

            All grades

            • Hemoglobin decreased (46%)
            • Platelets decreased (44%)
            • Headache (39%)
            • Neutrophils decreased (36%)
            • Diarrhea (31%)
            • Fatigue (28%)
            • Myalgia (21%)
            • Bruising (21%)
            • Nausea (19%)
            • Rash (18%)
            • Abdominal pain (15%)
            • Constipation (15%)

            Grade ≥3

            • Vomiting (13%)
            • Neutrophil decreased (15%)
            • Platelets decreased (12%)
            • Hemoglobin decreased (10%)

            >10% (Combination with Obinutuzumab)

            All grades

            • Infection (69%)
            • Neutropenia (53%)
            • Anemia (52%)
            • Thrombocytopenia (51%)
            • Headache (40%)
            • Upper respiratory tract infection (39%)
            • AST increase (38%)
            • Musculoskeletal pain (37%)
            • Fatigue (34%)
            • Bruising (31%)
            • Alt increased (30%)
            • Diarrhea (29%)
            • Uric acid increase (29%)
            • Rash (26%)
            • Lower respiratory tract infection (24%)
            • Arthralgia (22%)
            • Dizziness (20%)
            • Nausea (20%)
            • Hemorrhage (20%)
            • Urinary tract infection (15%)
            • Bilirubin increase (13%)
            • Lymphocytosis (12%)


            • Neutropenia (37%)
            • Uric acid increased (29%)
            • Infection (22%)
            • Anemia (12%)
            • Thrombocytopenia (12%)
            • Lymphocytosis (11%)

            1-10% (Monotherapy)

            All grades

            • Hemorrhage (8%)
            • Epistaxis (6%)
            • Grade ≥3 H4
            • ALT increase (7%)
            • AST increase (5%)
            • Diarrhea (3.2%)
            • Headache (1.6%)
            • Abdominal pain (1.6%)
            • Vomiting (1.6%)

            1-10% (Combination with Obinutuzumab)

            Grade ≥3

            • Lower respiratory tract infection (8%)
            • Diarrhea (4.5%)
            • Upper respiratory tract infection (2.8%)
            • Fatigue (2.2%)
            • Rash (2.2%)
            • Musculoskeletal pain (2.2%)
            • Hemorrhage (1.7%)
            • Arthralgia (1.1%)
            • Headache (1.1%)

            <1% (Monotherapy)


            • Nausea (0.8%)
            • Fatigue (0.8%)
            • Myalgia (0.8%)
            • Rash (0.8%)
            • Hemorrhage (0.8%)
            • Bilirubin increase (0.6%)

            Postmarketing Reports

            Serious and opportunistic infections






            Serious hemorrhagic events, including fatal events, reported; the mechanism for the bleeding events is not well understood; acalabrutinib may further increase hemorrhage risk in patients receiving antiplatelet or anticoagulant therapies, and patients should be monitored for signs of bleeding; consider the benefit-risk of withholding acalabrutinib for 3-7 days presurgery and postsurgery depending on the type of surgery and the risk of bleeding

            Serious infections (bacterial, viral, or fungal), including fatal events and opportunistic infections, reported; monitor for infection and consider prophylaxis in patients who are at increased risk for opportunistic infections

            Cytopenias reported, including neutropenia, anemia, lymphopenia, and thrombocytopenia; monitor complete blood cell counts monthly during treatment; interrupt treatment, reduce dose, or discontinue treatment as warranted

            Second primary malignancies, including nonskin carcinomas, have occurred in patients with hematologic malignancies treated with acalabrutinib; the most frequent was skin cancer; advise patients regarding need for protection from sun exposure

            Atrial fibrillation and flutter occurred (rare) during clinical trials; monitor for symptoms of arrhythmia (eg, palpitations, dizziness, syncope, dyspnea) and manage as appropriate

            Drug interaction overview

            • Coadministration with CYP3A inhibitors or inducers
              • Acalabrutinib is predominantly metabolized by CYP3A enzymes
              • CYP3A inhibitors are expected to increase acalabrutinib systemic exposure
              • CYP3A inducers are expected to decrease acalabrutinib systemic exposure
              • See Dosage Modifications
            • Coadministration with gastric acid-reducing agents
              • Coadministration with PPIs, H2-antagonists, or antacids may decrease acalabrutinib plasma concentrations
              • See Dosage Modifications

            Pregnancy & Lactation


            Pregnancy testing recommended for females of reproductive potential prior to initiating therapy

            Based on findings in animals, may cause fetal harm when administered to pregnant women

            There are no available data in pregnant women to inform the drug-associated risk

            In animal reproduction studies, administration of acalabrutinib to pregnant rabbits during organogenesis resulted in reduced fetal growth; rabbit maternal exposures (AUC) were ~4 times that of humans given a dose of 100 mg twice daily

            Advise pregnant women of the potential risk to a fetus


            • Therapy may cause embryo-fetal harm and dystocia when administered to pregnant women; advise female patients of reproductive potential to use effective contraception during treatment and for at least 1 week following the last dose; if drug is used during pregnancy, or if patient becomes pregnant while taking drug, patient should be informed of potential hazard to a fetus


            No data are available regarding the presence of acalabrutinib or its active metabolite in human milk, its effects on the breastfed child, or on milk production

            Acalabrutinib and its active metabolite were present in the milk of lactating rats

            Owing to the potential for adverse reactions in a breastfed child, advise lactating women not to breastfeed while taking acalabrutinib and for at least 2 weeks after the final dose

            Pregnancy Categories

            A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA: Information not available.



            Mechanism of Action

            Bruton tyrosine kinase (BTK) inhibitor; 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


            Peak plasma concentration 563 ng/mL (acalabrutinib); 451 ng/mL (ACP-5862)

            Peak plasma time: 0.9 hr (acalabrutinib); 1.6 hr (ACP-5862)

            AUC: 1843 ng·hr/mL (acalabrutinib); 3947 ng·hr/mL (ACP-5862)

            Effect of food

            • In healthy subjects, administration of a single 75-mg dose with a high-fat, high-calorie meal (~918 calories, 59 grams carbohydrate, 59 grams fat, and 39 grams protein) resulted in peak plasma concentration decreased by 73% and peak plasma time was delayed by 1-2 hr


            Protein bound: 97.5% (acalabrutinib); 98.6% (ACP-5862)

            Vd (steady-state): ~101 L (acalabrutinib); 67 L (ACP-5862)


            Predominantly metabolized by CYP3A enzymes, and to a minor extent, by glutathione conjugation and amide hydrolysis, based on in vitro studies

            Active metabolite: ACP-5862 with mean exposure (AUC) ~2- to 3-fold higher than the exposure of acalabrutinib; ACP-5862 is ~50% less potent than acalabrutinib with regard to BTK inhibition


            Half-life:1 hr (acalabrutinib); 3.5 hr (ACP-5862)

            Oral clearance 71 L/hr (acalabrutinib); 13 L/hr (ACP-5862)

            Excretion: 84% feces; 12% urine



            Oral Administration

            Take with or without food

            Swallow capsule whole with water

            Do not open, break, or chew the capsules

            Administer acalabrutinib before obinutuzumab when given on the same day

            Missed dose

            • If a dose is missed by >3 hr, skip dose; take next dose at its regularly scheduled time
            • Do not take extra capsules to make up for a missed dose


            Store at room temperature, 20-25°C (68-77°F); excursions permitted to 15-30°C (59-86°F)





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            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
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