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Acalabrutinib

Generic Name
Acalabrutinib
Brand Names
Calquence
Drug Type
Small Molecule
Chemical Formula
C26H23N7O2
CAS Number
1420477-60-6
Unique Ingredient Identifier
I42748ELQW

Overview

To date, acalabrutinib has been used in trials studying the treatment of B-All, myelofibrosis, ovarian cancer, multiple myeloma, and Hodgkin lymphoma, among others. As of October 31, 2017 the FDA approved Astra Zeneca's orally administered Calquence (acalabrutinib, capsules). This Bruton tyrosine kinase (BTK) inhibitor indicated for the treatment of chronic lymphocytic leukemia, small lymphocytic lymphoma, and in adult patients with Mantle cell lymphoma (MCL) who have already received at least one prior therapy. In August 2022, the FDA approved a new tablet formulation of Calquence, enabling the co-administration of this drug with proton pump inhibitors (PPIs). Unlike Calquence capsules, the co-administration of Calquence tablets and PPIs does not have an effect in the pharmacokinetics of acalabrutinib. Also known as ACP-196, acalabrutinib is also considered a second generation BTK inhibitor because it was rationally designed to be more potent and selective than ibrutinib, theoretically expected to demonstrate fewer adverse effects owing to minimized bystander effects on targets other than BTK. Nevertheless, acalabrutinib was approved under the FDA's accelerated approval pathway, which is based upon overall response rate and faciliates earlier approval of medicines that treat serious conditions or/and that fill an unmet medical need based on a surrogate endpoint. Continued approval for acalabrutinib's currently accepted indication may subsequently be contingent upon ongoing verification and description of clinical benefit in confimatory trials. Furthermore, the FDA granted this medication Priority Review and Breakthrough Therapy designations. It also received Orphan Drug designation, which provides incentives to assist and encourage the development of drugs for rare diseases. At this time, more than 35 clinical trials across 40 countries with more than 2500 patients are underway or have been completed with regards to further research into better understanding and expanding the therapeutic uses of acalabrutinib .

Indication

Acalabrutinib is currently indicated for the treatment of adult patients with Mantle Cell Lymphoma (MCL) who have received at least one prior therapy. It has also been recently approved for chronic lymphocytic leukemia and small lymphocytic lymphoma.

Associated Conditions

  • Chronic Lymphocytic Leukemia
  • Mantle Cell Lymphoma (MCL)
  • Small Lymphocytic Lymphoma

Research Report

Published: Jul 24, 2025

Acalabrutinib (Calquence): A Comprehensive Monograph on a Second-Generation BTK Inhibitor in Hematologic Malignancies

1.0 Introduction and Overview

Acalabrutinib represents a significant advancement in the targeted therapy of B-cell malignancies, embodying the principles of rational drug design to enhance the therapeutic window of its class. Marketed by AstraZeneca under the brand name Calquence, acalabrutinib is a second-generation, highly selective, and potent irreversible inhibitor of Bruton's tyrosine kinase (BTK).[1] BTK is an indispensable enzyme within the B-cell receptor (BCR) signaling pathway, a cascade that is fundamental to the proliferation, trafficking, and survival of both normal and malignant B-lymphocytes.[4] The clinical validation of BTK as a therapeutic target was firmly established by the first-in-class inhibitor, ibrutinib. However, the clinical utility of ibrutinib, while transformative, was frequently constrained by off-target toxicities stemming from its inhibition of other structurally related kinases, such as those in the TEC and EGFR families.[2] These off-target effects are associated with notable adverse events, including bleeding, atrial fibrillation, severe diarrhea, and skin rash, which can lead to dose reductions or treatment discontinuation.[2]

In this context, acalabrutinib (also known as ACP-196) was deliberately engineered to overcome these limitations. Its molecular structure was optimized for high potency and specificity for BTK, with the explicit goal of minimizing interaction with other kinases to theoretically reduce off-target adverse effects and improve overall tolerability.[1] This design philosophy—improving safety without compromising efficacy—is the central tenet of acalabrutinib's clinical development and its primary differentiator in the therapeutic landscape.

Continue reading the full research report

Clinical Trials

Title
Posted
Study ID
Phase
Status
Sponsor
2025/07/06
Not Applicable
Not yet recruiting
Inhye Ahn
2025/06/17
Phase 2
Not yet recruiting
2025/06/11
Phase 2
Not yet recruiting
Zulfa Omer
2025/02/26
Phase 2
Recruiting
Sun Yat-sen University
2025/02/21
Phase 2
Withdrawn
2025/01/03
Phase 2
Recruiting
2024/10/22
Phase 4
Recruiting
2024/08/21
Phase 1/2
Recruiting
2024/06/04
Phase 2
Not yet recruiting
2024/05/24
Phase 2/3
Recruiting

FDA Drug Approvals

Approved Product
Manufacturer
NDC Code
Route
Strength
Effective Date
AstraZeneca Pharmaceuticals LP
0310-0512
ORAL
100 mg in 1 1
3/23/2022
AstraZeneca Pharmaceuticals LP
0310-3512
ORAL
100 mg in 1 1
8/4/2022

EMA Drug Approvals

Approved Product
Authorization Holder
Status
Issued Date
Authorised
11/5/2020
Authorised
11/5/2020
Authorised
11/5/2020
Authorised
11/5/2020

HSA Drug Approvals

Approved Product
Manufacturer
Approval Number
Dosage Form
Strength
Approval Date
CALQUENCE FILM-COATED TABLET 100MG
SIN16875P
TABLET, FILM COATED
100mg
9/29/2023
CALQUENCE HARD CAPSULES 100MG
SIN15753P
CAPSULE
100mg
7/25/2019

NMPA Drug Approvals

Approved Product
Company
Approval Number
Drug Type
Dosage Form
Approval Date
No NMPA approvals found for this drug.

PPB Drug Approvals

Approved Product
Registration No.
Company
Licence No.
Strength
Registration Date
No PPB approvals found for this drug.

TGA Drug Approvals

Approved Product
ARTG ID
Sponsor
Registration Type
Status
Registration Date
CALQUENCE acalabrutinib 100 mg capsule blister pack
321419
Medicine
A
11/21/2019
CALQUENCE acalabrutinib (as maleate) 100 mg film-coated tablet blister pack
377410
Medicine
A
10/13/2022

Health Canada Drug Approvals

Approved Product
Company
DIN
Dosage Form
Strength
Market Date
CALQUENCE
astrazeneca canada inc
02491788
Capsule - Oral
100 MG
10/2/2019

CIMA AEMPS Drug Approvals

Approved Product
Company
Registration Number
Pharmaceutical Form
Prescription Type
Status
CALQUENCE 100 MG CAPSULAS DURAS
1201479002
CÁPSULA DURA
Diagnóstico Hospitalario
Not Commercialized

Philippines FDA Drug Approvals

Approved Product
Company
License Number
Dosage Form
Strength
Approval Date
No Philippines FDA approvals found for this drug.

Saudi SFDA Drug Approvals

Approved Product
Company
License Number
Dosage Form
Strength
Approval Date
No Saudi SFDA approvals found for this drug.

Malaysia NPRA Drug Approvals

Approved Product
Company
Registration Number
Dosage Form
Strength
Approval Date
No Malaysia NPRA approvals found for this drug.

UK EMC Drug Information

Medicine Name
MA Holder
MA Number
Pharmaceutical Form
Active Ingredient
Authorization Date
No UK EMC drug information found for this drug.

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