Acalabrutinib
Highest phase reached
Approved
Drug type
Small molecule
First approval year
2017
- First approval year
- 2017
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Acalabrutinib
- Molecular weight
- 465.52
- Structure (SMILES)
- CC#CC(=O)N1CCC[C@H]1c1nc(-c2ccc(C(=O)Nc3ccccn3)cc2)c2c(N)nccn12
- acalabrutinib
- Acalabrutinib
- Acalabrutinib [INN]
- Acalabrutinib [JAN]
- Acalabrutinib [MI]
- Acalabrutinib [ORANGE BOOK]
- Acalabrutinib [USAN]
- Acalabrutinib [WHO-DD]
- acalabrutinib inn
- acalabrutinib jan
- acalabrutinib mi
- acalabrutinib orange book
- acalabrutinib usan
- acalabrutinib who dd
- acalabrutininb acp 196
- acp 196
- Acp-196
- ACP-196
- ATC classification codes
- L01EL02
Sources for recorded values
- CAS registry numbers
- 1420477-60-6
- ChEMBL ID
- CHEMBL3707348
- InChIKey
- WDENQIQQYWYTPO-IBGZPJMESA-N
- PubChem compound IDs
- 71226662
- RxNorm IDs (RxCUI)
- 1986808
- FDA ingredient codes (UNII)
- I42748ELQW
- Applicant
- ASTRAZENECA
- Approval date
- 31 Oct 2017
- Application number
- NDA210259
- Status
- Authorised
- Status date
- 5 Nov 2020
- Authorisation date
- 5 Nov 2020
- Approved indications
- Calquence as monotherapy or in combination with obinutuzumab is indicated for the treatment of adult patients with previously untreated chronic lymphocytic leukaemia (CLL).Calquence in combination with venetoclax with or without obinutuzumab is indicated for the treatment of adult patients with previously untreated chronic lymphocytic leukaemia (CLL).Calquence as monotherapy is indicated for the treatment of adult patients with chronic lymphocytic leukaemia (CLL) who have received at least one prior therapy.Calquence in combination with bendamustine and rituximab (BR) is indicated for the treatment of adult patients with previously untreated mantle cell lymphoma (MCL) who are not eligible for autologous stem cell transplant (ASCT).Calquence as monotherapy is indicated for the treatment of adult patients with relapsed or refractory mantle cell lymphoma (MCL) not previously treated with a BTK inhibitor.
- Product number
- EMEA/H/C/005299
- Authorisation holder
- AstraZeneca AB
- Priority medicines scheme
- No
- Generic
- No
- Biosimilar
- No
- Generic medicines
- 0
- Biosimilar medicines
- 0
- Advanced therapy
- No
- Conditional approval
- No
- Additional monitoring
- No
- Accelerated assessment
- No
- Exceptional circumstances
- No
Therapeutic areas
- Leukemia, Lymphocytic, Chronic, B-Cell
European medicines record
- Patents
- 9
- Designations
- 6
- Earliest recorded loss of exclusivity
- 1 Jul 2036
- First in class
- No
- Fast track
- No
- Breakthrough designation
- Yes
- Orphan designation
- No
- Priority review
- Yes
- Orphan exclusivity
- No
- Accelerated approval
- Yes
- Availability
- Prescription only
- United States (FDA)
- Approved
- European Union (EMA)
- Authorised
- Pharmacology name
- acalabrutinib
- Type
- Synthetic organic
- Drug name stem
- -tinib
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- Oral
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- epidermal growth factor receptor
- Gene symbol
- EGFR
- Protein identifier
- P00533
- Median affinity
- 6
- Affinity units
- pIC50
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- erb-b2 receptor tyrosine kinase 2
- Gene symbol
- ERBB2
- Protein identifier
- P04626
- Median affinity
- 6
- Affinity units
- pIC50
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- LCK proto-oncogene, Src family tyrosine kinase
- Gene symbol
- LCK
- Protein identifier
- P06239
- Median affinity
- 6
- Affinity units
- pEC50
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- FYN proto-oncogene, Src family tyrosine kinase
- Gene symbol
- FYN
- Protein identifier
- P06241
- Median affinity
- 6
- Affinity units
- pEC50
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- LYN proto-oncogene, Src family tyrosine kinase
- Gene symbol
- LYN
- Protein identifier
- P07948
- Median affinity
- 6
- Affinity units
- pEC50
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- LYN proto-oncogene, Src family tyrosine kinase
- Gene symbol
- LYN
- Protein identifier
- P07948
- Median affinity
- 6
- Affinity units
- pIC50
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- SRC proto-oncogene, non-receptor tyrosine kinase
- Gene symbol
- SRC
- Protein identifier
- P12931
- Median affinity
- 6
- Affinity units
- pEC50
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- tec protein tyrosine kinase
- Gene symbol
- TEC
- Protein identifier
- P42680
- Median affinity
- 7.03
- Affinity units
- pIC50
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- TXK tyrosine kinase
- Gene symbol
- TXK
- Protein identifier
- P42681
- Median affinity
- 6.43
- Affinity units
- pIC50
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- BLK proto-oncogene, Src family tyrosine kinase
- Gene symbol
- BLK
- Protein identifier
- P51451
- Median affinity
- 6
- Affinity units
- pIC50
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- BMX non-receptor tyrosine kinase
- Gene symbol
- BMX
- Protein identifier
- P51813
- Median affinity
- 7.34
- Affinity units
- pIC50
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- Janus kinase 3
- Gene symbol
- JAK3
- Protein identifier
- P52333
- Median affinity
- 6
- Affinity units
- pIC50
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- Bruton tyrosine kinase
- Gene symbol
- BTK
- Protein identifier
- Q06187
- Median affinity
- 8
- Affinity units
- pEC50
- Primary target
- Yes
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- Bruton tyrosine kinase
- Gene symbol
- BTK
- Protein identifier
- Q06187
- Median affinity
- 8.29
- Affinity units
- pIC50
- Primary target
- Yes
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- IL2 inducible T cell kinase
- Gene symbol
- ITK
- Protein identifier
- Q08881
- Median affinity
- 6
- Affinity units
- pIC50
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- erb-b2 receptor tyrosine kinase 4
- Gene symbol
- ERBB4
- Protein identifier
- Q15303
- Median affinity
- 7.8
- Affinity units
- pIC50
- Mechanism
- Tyrosine-protein kinase BTK inhibitor
- Action type
- Inhibitor
- Target
- Tyrosine-protein kinase BTK
- Protein identifier
- Q06187
Open Targets mechanisms
- Mechanism
- Tyrosine-protein kinase BTK inhibitor
- Action type
- Inhibitor
- Target
- Tyrosine-protein kinase BTK
- Action type
- Inhibitor
- Gene symbol
- LYN
- Protein identifier
- P07948
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Inhibitor
- Gene symbol
- TEC
- Protein identifier
- P42680
- Organism
- Homo sapiens
- Target development level
- Chemical evidence
- Action type
- Inhibitor
- Gene symbol
- TXK
- Protein identifier
- P42681
- Organism
- Homo sapiens
- Target development level
- Chemical evidence
- Action type
- Inhibitor
- Gene symbol
- BMX
- Protein identifier
- P51813
- Organism
- Homo sapiens
- Target development level
- Chemical evidence
- Action type
- Inhibitor
- Gene symbol
- BTK
- Protein identifier
- Q06187
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Inhibitor
- Gene symbol
- ERBB4
- Protein identifier
- Q15303
- Organism
- Homo sapiens
- Target development level
- Clinical
- Condition
- Leukemia, Lymphocytic, Chronic, B-Cell
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000095
- Subject identifier
- D015451
- Condition
- Carcinoma, Squamous Cell
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000181
- Subject identifier
- D002294
- Condition
- Lymphoma, Large B-Cell, Diffuse
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000403
- Subject identifier
- D016403
- Condition
- Glioblastoma
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000519
- Subject identifier
- D005909
- Condition
- Leukemia
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000565
- Subject identifier
- D007938
- Condition
- Lymphoma
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000574
- Subject identifier
- D008223
- Condition
- Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000616
- Subject identifier
- D009369
- Condition
- Arthritis, Rheumatoid
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000685
- Subject identifier
- D001172
- Condition
- Multiple Myeloma
- Highest recorded phase
- 1
- Condition identifier
- EFO:0001378
- Subject identifier
- D009101
- Condition
- Pancreatic Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0002618
- Subject identifier
- D010190
- Condition
- Carcinoma, Non-Small-Cell Lung
- Highest recorded phase
- 2
- Condition identifier
- EFO:0003060
- Subject identifier
- D002289
- Condition
- Communicable Diseases
- Highest recorded phase
- 1
- Condition identifier
- EFO:0005741
- Subject identifier
- D003141
- Condition
- Lymphoma, Non-Hodgkin
- Highest recorded phase
- 2
- Condition identifier
- EFO:0005952
- Subject identifier
- D008228
- Condition
- Waldenstrom Macroglobulinemia
- Highest recorded phase
- 2
- Condition identifier
- EFO:0009441
- Subject identifier
- D008258
- Condition
- Lymphoma, B-Cell, Marginal Zone
- Highest recorded phase
- 2
- Condition identifier
- EFO:1000630
- Subject identifier
- D018442
- Condition
- Lymphoma, Mantle-Cell
- Highest recorded phase
- 4
- Condition identifier
- EFO:1001469
- Subject identifier
- D020522
- Condition
- Food Hypersensitivity
- Highest recorded phase
- 2
- Condition identifier
- EFO:1001890
- Subject identifier
- D005512
- Condition
- Leukemia, Prolymphocytic
- Highest recorded phase
- 1
- Condition identifier
- MONDO:0001023
- Subject identifier
- D015463
- Condition
- Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- MONDO:0004992
- Subject identifier
- D009369
- Condition
- Ovarian Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0008170
- Subject identifier
- D010051
- Condition
- Lymphoma, Follicular
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0018906
- Subject identifier
- D008224
- Condition
- Bronchiolitis Obliterans Syndrome
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0020547
- Subject identifier
- D000092122
- Condition
- Hematologic Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0044881
- Subject identifier
- D019337
- Condition
- Severe Acute Respiratory Syndrome
- Highest recorded phase
- 3
- Condition identifier
- MONDO:0100096
- Subject identifier
- D045169
- Condition identifier
- EFO_0000095
- Condition identifier
- EFO_0000181
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000403
- Highest recorded phase
- 3
- Condition identifier
- EFO_0000519
- Condition identifier
- EFO_0000616
- Condition identifier
- EFO_0000685
- Highest recorded phase
- 2
- Condition identifier
- EFO_0001378
- Highest recorded phase
- 1
- Condition identifier
- EFO_0002618
- Highest recorded phase
- 2
- Condition identifier
- EFO_0003060
- Highest recorded phase
- 2
- Condition identifier
- EFO_0005741
- Highest recorded phase
- 1
- Condition identifier
- EFO_0005952
- Highest recorded phase
- 2
- Condition identifier
- EFO_0009441
- Highest recorded phase
- 2
- Condition identifier
- EFO_1000157
- Highest recorded phase
- 2
- Condition identifier
- EFO_1000630
- Highest recorded phase
- 2
- Condition identifier
- EFO_1001469
- Condition identifier
- EFO_1001890
- Highest recorded phase
- 2
- Condition identifier
- HP_0001399
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0001023
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0002083
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0002571
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0003864
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0004355
- Condition identifier
- MONDO_0004355
- Highest recorded phase
- 4
- Condition identifier
- MONDO_0004948
- Highest recorded phase
- 4
- Condition identifier
- MONDO_0004949
- Highest recorded phase
- 2
And 30 more, listed on the interactive page.
- Event
- acquired gene mutation
- Reports
- 3
- Reporting signal score
- 8.93199
- Event
- aplastic anaemia
- Reports
- 4
- Reporting signal score
- 8.17512
- Event
- atrial fibrillation
- Reports
- 20
- Reporting signal score
- 19.6057
- Event
- chronic lymphocytic leukaemia recurrent
- Reports
- 3
- Reporting signal score
- 10.0936
- Event
- covid-19
- Reports
- 12
- Reporting signal score
- 12.9144
- Event
- disease progression
- Reports
- 15
- Reporting signal score
- 10.4223
- Event
- drug resistance
- Reports
- 15
- Reporting signal score
- 25.3332
- Event
- febrile neutropenia
- Reports
- 17
- Reporting signal score
- 16.6993
- Event
- haemoglobin abnormal
- Reports
- 4
- Reporting signal score
- 8.28638
- Event
- leukocytosis
- Reports
- 9
- Reporting signal score
- 13.1824
- Event
- leukostasis syndrome
- Reports
- 2
- Reporting signal score
- 10.1047
- Event
- lymphocytosis
- Reports
- 5
- Reporting signal score
- 14.2417
- Event
- malignant neoplasm progression
- Reports
- 24
- Reporting signal score
- 34.1039
- Event
- myelodysplastic syndrome
- Reports
- 6
- Reporting signal score
- 8.9817
- Event
- pseudomonal bacteraemia
- Reports
- 3
- Reporting signal score
- 11.7313
- Event
- richter's syndrome
- Reports
- 3
- Reporting signal score
- 11.432
- Event
- sars-cov-2 test negative
- Reports
- 2
- Reporting signal score
- 8.39067
- Event
- tumour lysis syndrome
- Reports
- 6
- Reporting signal score
- 12.0296
- Event
- white blood cell count abnormal
- Reports
- 5
- Reporting signal score
- 11.6569
- NCT02112526
- NCT03205046
- NCT03527147
- NCT03736616
- NCT04002947
- NCT04257578
- NCT04529772
- NCT04546620
- NCT04604067
- NCT04978584
- NCT05820841
- NCT05952024
- NCT06441097
- NCT02157324
- NCT02296918
- NCT02337829
- NCT02475681
- NCT02477696
- NCT02717611
- NCT02970318
- NCT03128879
- NCT03328273
- NCT03492125
- NCT03516617
- NCT03580928
And 73 more, listed on the interactive page.
- Dose
- 100 mg
- Route
- Oral
- How often
- Every 12 hours
- Swallow whole with water
- With or without food
- Hydrogen bond acceptors
- 7
- Hydrogen bond donors
- 2
- Polar surface area
- 118.51
- Calculated partition coefficient (ALogP)
- 3.31
- Calculated partition coefficient (XLogP)
- 3
- Prodrug
- No
- Chirality
- Single enantiomer
- Inorganic
- No
- Rule-of-five violations
- 0
- Rotatable bonds
- 4
- Heavy atoms
- 35
- Molecular formula
- C26H23N7O2
- Monoisotopic mass
- 465.19132300
- Natural product
- Yes
- 0310-0512
- 0310-3512
- 0310-4513
- Recorded assays
- 1,092
- Active assays
- 98
- Confirmatory
- Other
- Screening
- Tyrosine Kinase Inhibitors
- Antineoplastic Agents
Related records
Trials (153)
- A Combination of Acalabrutinib With R-CHOP for Patient Diffuse Large B-cell Lymphoma (DLBCL)
- A Combination of Acalabrutinib With R-CHOP in Subjects With Previously Untreated Non-GCB DLBCL (ACE-LY-312)
- A Comparison of Three Chemotherapy Regimens for the Treatment of Patients With Newly Diagnosed Mantle Cell Lymphoma
- A Phase 1 Study of Acalabrutinib in Japanese Adult Patients With Advanced B-cell Malignancies
- A Phase 1b/2, Multicenter, Open-label Study of ACP-196 in Subjects With Recurrent Glioblastoma Multiforme (GBM)
- A Phase-3-trial of Acalabrutinib, Obinutuzumab & Venetoclax Compared to Obinutuzumab and Venetoclax in Previously Untreated Patients With High Risk CLL
- A Pilot "Window-3" Study of Acalabrutinib Plus Rituximab Followed by Brexucabtagene Autoleucel Therapy in Patients With Previously Untreated High-risk Mantle Cell Lymphoma
- A Pilot Study of Acalabrutinib in Relapsed/Refractory Primary and Secondary CNS Lymphomas
- A Randomized Phase II Study Of Bruton Tyrosine Kinase Inhibitor With Or Without Venetoclax In Veterans With Chronic Lymphocytic Leukemia (CLL)/Small Lymphocytic Lymphoma (SLL)
- A Single Arm Study of Acalabrutinib Conbimed With Obinutuzumab in Chinese Patients With Previously Untreated CLL
- A Study in Healthy Subjects to Assess Bioavailability (Proportion of a Drug Which Enters the Circulation to Have an Active Effect) of Acalabrutinib Tablet and Protonpump Inhibitor Effect (Members of a Class of Medications That Inhibits in Gastric Acid Production) for Rabeprazole
- A Study of Acalabrutinib and Vistusertib in Subjects With Relapsed/Refractory B-cell Malignancies
- A Study of Acalabrutinib in Combination With Rituximab + (Bendamustine or Venetoclax) in Subjects With MCL
- A Study of Acalabrutinib in Combination With Rituximab Versus Ibrutinib Versus Acalabrutinib in Subjects With Relapsed or Refractory Mantle Cell Lymphoma
- A Study of Acalabrutinib Plus Venetoclax and Rituximab in Participants With Treatment Naïve Mantle Cell Lymphoma
- A Study of Acalabrutinib Plus Venetoclax Versus Venetoclax Plus Obinutuzumab in Previously Untreated Chronic Lymphocytic Leukemia or Small Lymphocytic Lymphoma
- A Study of Acalabrutinib Suspension to Evaluate Relative Bioavailability and Proton-pump Inhibitor Effect in Healthy Volunteers
- A Study of Acalabrutinib vs Investigator's Choice of Idelalisib Plus Rituximab or Bendamustine Plus Rituximab in R/R CLL
- A Study of ACP-196 (Acalabrutinib) in Subjects With Relapsed/Refractory CLL and Intolerant of Ibrutinib Therapy
- A Study of AZD0486 Monotherapy or in Combination With Other Anti-Cancer Agents for Mature B-Cell Malignancies
Approved for (5)
- B-cell chronic lymphocytic leukemia
- Cancer
- Childhood leukemia
- Mantle cell lymphoma
- Neoplasm
In development for (36)
- Autoimmune hemolytic anemia Phase 2
- B-cell non-Hodgkin lymphoma Phase 1
- Chronic graft versus host disease Phase 2
- Chronic lymphocytic leukemia/small lymphocytic lymphoma Phase 2
- COVID-19 Phase 3
- Diffuse large B-cell lymphoma Phase 3
- Exocrine pancreatic carcinoma Phase 2
- Follicular lymphoma Phase 2
- Food allergy Phase 2
- Glioblastoma Phase 1
- Graft versus host disease Phase 2
- Head and neck squamous cell carcinoma Phase 2
- Hematopoietic and lymphoid cell neoplasm Phase 2
- Infectious disease Phase 1
- Leukemia Phase 1
- Lymphoid leukemia Phase 2
- Lymphoma Phase 1
- Malignant pancreatic neoplasm Phase 2
- Marginal zone lymphoma Phase 2
- Myelofibrosis Phase 1