Acalabrutinib

What is Acalabrutinib?

• Acalabrutinib (Calquence) is a kinase inhibitor used to treat various types of non-Hodgkin lymphoma, including mantle cell lymphoma (MCL) and chronic lymphocytic leukemia/small lymphocytic leukemia (CLL/SLL).

Acalabrutinib

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Flower cell in mantle cell lymphoma

What are the uses of this medicine?

Acalabrutinib (Calquence) is a prescription medicine used to treat adults with:

• Mantle cell lymphoma (MCL) who have received at least one prior treatment for their cancer.
• Chronic lymphocytic leukemia (CLL) or small lymphocytic lymphoma (SLL).

How does this medicine work?

• Acalabrutinib (a kal" a broo' ti nib) is an orally available, small molecule inhibitor of Bruton’s tyrosine kinase (BTK), which is an essential component in the B cell receptor signaling pathway.
• Inhibition of this pathway prevents B cell activation, differentiation and proliferation.
• Deficiency of BTK is the cause of X linked (Bruton’s) agammaglobulinemia, and B cell receptor signaling through BTK has been shown to be critical for proliferation and survival of malignant B lymphocytes in mantle cell lymphoma and CLL.
• Unlike ibrutinib, another BTK inhibitor, acalabrutinib has a high degree of specificity for BTK and has little or no activity against EGFR and other tyrosine kinases.

Who Should Not Use this medicine ?

• This medicine have no usage limitations.

What drug interactions can this medicine cause?

• Taking CALQUENCE with certain other medications may affect how CALQUENCE works and can cause side effects. Especially tell your healthcare provider if you take a blood thinner medicine.
• Avoid co-administration with strong CYP3A inhibitors. Dose adjustments may be recommended.
• Avoid co-administration with strong CYP3A inducers. Dose adjustments may be recommended.
• Avoid co-administration with proton pump inhibitors (PPIs). Stagger dosing with H2-receptor antagonists and antacids.

Is this medicine FDA approved?

• Acalabrutinib was approved for medical use in the United States in 2017, and in the European Union in November 2020.

How should this medicine be used?

Recommended dosage:

• For patients with MCL, CLL, or SLL, the recommended dose of CALQUENCE is 100 mg taken orally approximately every 12 hours until disease progression or unacceptable toxicity.

Recommended Dosage for Hepatic Impairment

• Avoid administration of CALQUENCE in patients with severe hepatic impairment.
• Dose modifications are not required for patients with mild or moderate hepatic impairment.

Concomitant Use with Gastric Acid Reducing Agents:

• Proton Pump Inhibitors: Avoid concomitant use.
• H2-Receptor Antagonists: Take CALQUENCE 2 hours before taking a H2-receptor antagonist.

Administration:

• Take CALQUENCE 2 times a day (about 12 hours apart).
• Take CALQUENCE with or without food.
• Swallow CALQUENCE capsules whole with a glass of water. Do not open, break, or chew capsules.
• If you need to take an antacid medicine, take it either 2 hours before or 2 hours after you take CALQUENCE.
• If you need to take certain other medicines called acid reducers (H-2 receptor blockers), take CALQUENCE 2 hours before the acid reducer medicine.
• If you miss a dose of CALQUENCE, take it as soon as you remember. If it is more than 3 hours past your usual dosing time, skip the missed dose and take your next dose of CALQUENCE at your regularly scheduled time. Do not take an extra dose to make up for a missed dose.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Capsules: 100 mg.

This medicine is available in fallowing brand namesː

• CALQUENCE

What side effects can this medication cause?

The most common side effects of this medicine include: Side effects are common, but usually mild-to-moderate in severity; they include:

• Myelosuppression,
• fatigue,
• diarrhea,
• nausea,
• vomiting,
• anorexia,
• constipation,
• peripheral edema,
• dyspnea,
• headache,
• arthralgia,
• myalgia,
• rash and
• fever. 

Uncommon, but potentially serious side effects include:

• severe bone marrow suppression,
• infections,
• bleeding,
• tumor lysis syndrome and
• renal toxicity.

CALQUENCE may cause serious side effects, including:

• Serious infections
• hemorrhage
• Decrease in blood cell counts
• Second primary cancers
• atrial fibrillation and atrial flutter

What special precautions should I follow?

• Acalabrutinib has not been associated with serum enzyme elevations during therapy or with cases of idiosyncratic acute liver injury, but has been linked to cases of reactivation of hepatitis B. 
• Fatal and serious infections, including opportunistic infections, have occurred in patients with hematologic malignancies treated with CALQUENCE. Consider prophylaxis in patients who are at increased risk for opportunistic infections. Monitor patients for signs and symptoms of infection and treat promptly.
• Fatal and serious hemorrhagic events have occurred in patients with hematologic malignancies treated with CALQUENCE. Consider the benefit-risk of withholding CALQUENCE for 3-7 days pre- and post-surgery depending upon the type of surgery and the risk of bleeding.
• Grade 3 or 4 cytopenias, including neutropenia (23%), anemia (8%), thrombocytopenia (7%), and lymphopenia (7%), developed in patients with hematologic malignancies treated with CALQUENCE. Monitor complete blood counts regularly during treatment. Interrupt treatment, reduce the dose, or discontinue treatment as warranted.
• Second primary malignancies, including skin cancers and other solid tumors, occurred in patients exposed to CALQUENCE. Advise patients to use sun protection.
• Grade 3 atrial fibrillation or flutter occurred in patients treated with CALQUENCE. Monitor for symptoms of arrhythmias and manage.

What to do in case of emergency/overdose?

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.

Can this medicine be used in pregnancy?

• 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.

Can this medicine be used in children?

• The safety and efficacy of CALQUENCE in pediatric patients have not been established.

What are the active and inactive ingredients in this medicine?

• Active ingredient: acalabrutinib
• Inactive ingredients: silicified microcrystalline cellulose, pregelatinized starch, magnesium stearate, and sodium starch glycolate.
• Capsule shell contains: gelatin, titanium dioxide, yellow iron oxide, FD&C Blue 2, and black ink.

Who manufactures and distributes this medicine?

Distributed by:

• AstraZeneca Pharmaceuticals LP, Wilmington, DE
• CALQUENCE is a registered trademark of the AstraZeneca group of companies.

What should I know about storage and disposal of this medication?

• Store CALQUENCE at room temperature between 68°F to 77°F (20°C to 25°C).
• Keep CALQUENCE and all medicines out of the reach of children.

• Dailymed label info on Acalabrutinib
• FDA Acalabrutinib

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