acalabrutinib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
tyrosine kinase inhibitors 5260 1420477-60-6

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • acalabrutinib
  • ACP-196
  • calquence
Acalabrutinib is a small-molecule inhibitor of BTK. 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, an adhesion. In nonclinical studies, acalabrutinib inhibited BTK mediated activation of downstream signaling proteins CD86 and CD69 and inhibited malignant B-cell proliferation and survival.
  • Molecular weight: 465.52
  • Formula: C26H23N7O2
  • CLOGP: 2.05
  • LIPINSKI: 0
  • HAC: 9
  • HDO: 2
  • TPSA: 118.51
  • ALOGS: -4.63
  • ROTB: 5
  • Status: ONP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.20 g O

ADMET properties:

PropertyValueReference
S (Water solubility) 0.05 mg/mL Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Bocci G, Oprea TI, Benet LZ

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 2.159 High 0.88
caco2-efflux Caco-2 efflux ratio (BA/AB) 8.128 High 0.88
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 23.442 10^-6 cm/s High 0.88
dh-clint Dog hepatocyte intrinsic clearance 9.311 uL/min/10^6 cells High 0.88
dppb Dog plasma protein binding (% unbound) 34.110 % High 0.88
fcs-ppb Fetal calf serum protein binding (% unbound) 49.020 % High 0.88
herg hERG pIC50 4.789 pIC50 High 0.88
hh-clint Human hepatocyte intrinsic clearance 19.907 uL/min/10^6 cells High 0.88
hlm-clint Human liver microsomal intrinsic clearance 83.946 uL/min/mg protein High 0.88
hppb Human plasma protein binding (% unbound) 19.970 % High 0.88
kinase-safety-class ACVR2B,AURKA,BLK,BMX,BTK,CAMK2D,CSF1R,CSNK1G2,DDR1,EGFR,EIF2AK3,ERBB2,ERBB4,FGFR1,GAK,IRAK1,IRAK3,ITK,JAK3,KDR,LCK,LYN,MAP3K21,MAP4K2,MAPK10,MINK1,NTRK1,PDK1,PDK2,PDK4,RET,RIPK3,SRC,STK33,TNIK,YES1 36
kinase-selectivity-class BLK,BMX,BTK,EGFR,ERBB2,ERBB4 6
mdck-mdr1-bcrp-efflux MDCK-MDR1-BCRP efflux ratio 20.230 High 1
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 13.964 High 0.88
mh-clint Mouse hepatocyte intrinsic clearance 94.842 High 0.88
mppb Mouse plasma protein binding (% unbound) 20.710 High 0.88
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 44.978 High 0.88
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 46.950 % High 0.88
rat-kpuu-brain Rat brain Kpuu 0.018 % High 1
rh-clint Rat hepatocyte intrinsic clearance 100.693 uL/min/10^6 cells High 0.88
rh-fuinc Rat hepatocyte fraction unbound in incubation 76.180 % High 0.88
rppb Rat plasma protein binding (% unbound) 21.480 % High 0.88
solubility-dd Solubility at pH 7.4 in DMSO 193.197 uM High 0.88

Approvals:

DateAgencyCompanyOrphan
Jan. 22, 2021 PMDA ASTRAZENECA K.K.
Oct. 31, 2017 FDA ACERTA PHARMA BV
Nov. 5, 2020 EMA AstraZeneca AB

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Death 305.94 33.05 168 2027 456383 90169869
Malignant neoplasm progression 89.39 33.05 46 2149 106824 90519428
Disease progression 78.07 33.05 48 2147 156567 90469685
Lymphadenopathy 66.95 33.05 29 2166 45746 90580506
Mantle cell lymphoma recurrent 52.36 33.05 9 2186 399 90625853
Gastroenteritis bacterial 52.03 33.05 9 2186 414 90625838
Atrial fibrillation 37.98 33.05 29 2166 133582 90492670
Spontaneous haematoma 37.27 33.05 8 2187 1150 90625102
Haematoma 36.04 33.05 18 2177 39030 90587222
Lymphocytosis 34.47 33.05 9 2186 2988 90623264

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Death 685.35 23.26 448 3281 470737 42146869
Malignant neoplasm progression 98.61 23.26 79 3650 108321 42509285
Tumour lysis syndrome 65.36 23.26 34 3695 22197 42595409
COVID-19 57.13 23.26 60 3669 115888 42501718
Lymphocytosis 49.90 23.26 16 3713 3015 42614591
Cerebral aspergillosis 44.72 23.26 13 3716 1764 42615842
Atrial fibrillation 41.75 23.26 56 3673 139537 42478069
Babesiosis 39.84 23.26 8 3721 224 42617382
Lymphadenopathy 36.06 23.26 27 3702 33338 42584268
Ulcer haemorrhage 29.85 23.26 11 3718 3139 42614467
Chronic lymphocytic leukaemia recurrent 26.56 23.26 7 3722 661 42616945
Spontaneous haematoma 25.69 23.26 7 3722 751 42616855
Mantle cell lymphoma 25.02 23.26 8 3721 1492 42616114
Aspergillus infection 24.56 23.26 16 3713 15821 42601785

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Death 514.07 23.19 323 3979 698546 109886451
Malignant neoplasm progression 98.22 23.19 69 4233 174498 110410499
Atrial fibrillation 77.33 23.19 67 4235 229575 110355422
COVID-19 71.61 23.19 66 4236 244994 110340003
Tumour lysis syndrome 67.91 23.19 30 4272 30771 110554226
Lymphocytosis 62.32 23.19 18 4284 5393 110579604
Spontaneous haematoma 59.07 23.19 14 4288 1947 110583050
Cerebral aspergillosis 56.84 23.19 14 4288 2288 110582709
Lymphadenopathy 47.32 23.19 30 4272 63805 110521192
Gastroenteritis bacterial 46.03 23.19 9 4293 504 110584493
Haematoma 42.14 23.19 27 4275 58449 110526548
Aspergillus infection 41.02 23.19 20 4282 25596 110559401
Disease progression 36.24 23.19 46 4256 243988 110341009
Splenomegaly 32.97 23.19 17 4285 24481 110560516
Babesiosis 28.47 23.19 6 4296 489 110584508
White blood cell count abnormal 26.45 23.19 10 4292 6899 110578098
Nitrituria 24.17 23.19 3 4299 6 110584991
Mantle cell lymphoma recurrent 24.12 23.19 6 4296 1020 110583977

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01EL02 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
PROTEIN KINASE INHIBITORS
Bruton's tyrosine kinase (BTK) inhibitors
MeSH PA D000092004 Tyrosine Kinase Inhibitors
MeSH PA D000970 Antineoplastic Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D047428 Protein Kinase Inhibitors
FDA MoA N0000020001 Tyrosine Kinase Inhibitors
FDA EPC N0000175605 Kinase Inhibitor
CHEBI has role CHEBI:22587 antiviral agent
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:35842 antirheumatic drug
CHEBI has role CHEBI:68495 apoptosis inducer
CHEBI has role CHEBI:76617 EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor

Related Drugs by ATC class:

L01EL Bruton's tyrosine kinase (BTK) inhibitors 4 drugs
ibrutinibpirtobrutinibtirabrutinib hydrochloridezanubrutinib

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Chronic lymphocyticleukemia/small lymphocytic lymphoma indication 92814006
Mantle cell lymphoma indication 443487006




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 11.34 acidic
pKa2 3.25 Basic
pKa3 2.49 Basic
pKa4 1.5 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
100MG CALQUENCE ASTRAZENECA N210259 Oct. 31, 2017 RX CAPSULE ORAL 10239883 July 11, 2032 TREATMENT OF ADULT PATIENTS WITH CHRONIC LYMPHOCYTIC LEUKEMIA
100MG CALQUENCE ASTRAZENECA N210259 Oct. 31, 2017 RX CAPSULE ORAL 10239883 July 11, 2032 TREATMENT OF ADULT PATIENTS WITH PREVIOUSLY UNTREATED CHRONIC LYMPHOCYTIC LEUKEMIA IN COMBINATION WITH OBINUTUZUMAB
100MG CALQUENCE ASTRAZENECA N210259 Oct. 31, 2017 RX CAPSULE ORAL 9758524 July 11, 2032 TREATMENT OF ADULT PATIENTS WITH MANTLE CELL LYMPHOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
100MG CALQUENCE ASTRAZENECA N210259 Oct. 31, 2017 RX CAPSULE ORAL 9758524 July 11, 2032 TREATMENT OF ADULT PATIENTS WITH PREVIOUSLY UNTREATED MANTLE CELL LYMPHOMA WHO ARE INELIGIBLE FOR AUTOLOGOUS HEMATOPOIETIC STEM CELL TRANSPLANTATION IN COMBINATION WITH BENDAMUSTINE AND RITUXIMAB
100MG CALQUENCE ASTRAZENECA N210259 Oct. 31, 2017 RX CAPSULE ORAL 10272083 Jan. 21, 2035 TREATMENT OF ADULT PATIENTS WITH CHRONIC LYMPHOCYTIC LEUKEMIA BY ADMINISTERING 100MG OF ACALABRUTINIB TWICE DAILY
100MG CALQUENCE ASTRAZENECA N210259 Oct. 31, 2017 RX CAPSULE ORAL 10272083 Jan. 21, 2035 TREATMENT OF ADULT PATIENTS WITH CHRONIC LYMPHOCYTIC LEUKEMIA OR SMALL LYMPHOCYTIC LEUKEMIA BY ADMINISTERING 100 MG OF ACALABRUTINIB TWICE DAILY
100MG CALQUENCE ASTRAZENECA N210259 Oct. 31, 2017 RX CAPSULE ORAL 10272083 Jan. 21, 2035 TREATMENT OF ADULT PATIENTS WITH MANTLE CELL LYMPHOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY BY ADMINISTERING 100 MG OF ACALABRUTINIB TWICE DAILY
100MG CALQUENCE ASTRAZENECA N210259 Oct. 31, 2017 RX CAPSULE ORAL 10272083 Jan. 21, 2035 TREATMENT OF ADULT PATIENTS WITH PREVIOUSLY UNTREATED CHRONIC LYMPHOCYTIC LEUKEMIA BY ADMINISTERING 100 MG OF ACALABRUTINIB TWICE DAILY IN COMBINATION WITH OBINUTUZUMAB
100MG CALQUENCE ASTRAZENECA N210259 Oct. 31, 2017 RX CAPSULE ORAL 10272083 Jan. 21, 2035 TREATMENT OF ADULT PATIENTS WITH PREVIOUSLY UNTREATED CHRONIC LYMPHOCYTIC LEUKEMIA OR SMALL LYMPHOCYTIC LEUKEMIA IN COMBINATION WITH OBINUTUZUMAB BY ADMINISTERING 100 MG OF ACALABRUTINIB TWICE DAILY
100MG CALQUENCE ASTRAZENECA N210259 Oct. 31, 2017 RX CAPSULE ORAL 10272083 Jan. 21, 2035 TREATMENT OF ADULT PATIENTS WITH PREVIOUSLY UNTREATED MANTLE CELL LYMPHOMA WHO ARE INELIGIBLE FOR AUTOLOGOUS HEMATOPOIETIC STEM CELL TRANSPLANTATION BY ADMINISTERING 100 MG OF ACALABRUTINIB TWICE DAILY IN COMBINATION WITH BENDAMUSTINE AND RITUXIMAB
100MG CALQUENCE ASTRAZENECA N210259 Oct. 31, 2017 RX CAPSULE ORAL 10272083 Jan. 21, 2035 TREATMENT OF ADULT PATIENTS WITH PREVIOUSLY UNTREATED SMALL LYMPHOCYTIC LEUKEMIA BY ADMINISTERING 100 MG OF ACALABRUTINIB TWICE DAILY IN COMBINATION WITH OBINUTUZUMAB
100MG CALQUENCE ASTRAZENECA N210259 Oct. 31, 2017 RX CAPSULE ORAL 10272083 Jan. 21, 2035 TREATMENT OF ADULT PATIENTS WITH SMALL LYMPHOCYTIC LEUKEMIA BY ADMINISTERING 100MG OF ACALABRUTINIB TWICE DAILY
100MG CALQUENCE ASTRAZENECA N210259 Oct. 31, 2017 RX CAPSULE ORAL 11771696 Jan. 21, 2035 TREATMENT OF ADULT PATIENTS WITH PREVIOUSLY UNTREATED CHRONIC LYMPHOCYTIC LEUKEMIA BY ORALLY ADMINISTERING 100 MG OF ACALABRUTINIB TWICE DAILY IN COMBINATION WITH INTRAVENOUS ADMINISTRATION OF OBINUTUZUMAB
100MG CALQUENCE ASTRAZENECA N210259 Oct. 31, 2017 RX CAPSULE ORAL 11166951 Aug. 11, 2035 TREATMENT OF ADULT PATIENTS WITH PREVIOUSLY UNTREATED CHRONIC LYMPHOCYTIC LEUKEMIA BY ADMINISTERING 100 MG OF ACALABRUTINIB TWICE DAILY IN COMBINATION WITH VENETOCLAX
100MG CALQUENCE ASTRAZENECA N210259 Oct. 31, 2017 RX CAPSULE ORAL 11166951 Aug. 11, 2035 TREATMENT OF ADULT PATIENTS WITH PREVIOUSLY UNTREATED CHRONIC LYMPHOCYTIC LEUKEMIA IN COMBINATION WITH VENETOCLAX
100MG CALQUENCE ASTRAZENECA N210259 Oct. 31, 2017 RX CAPSULE ORAL 11166951 Aug. 11, 2035 TREATMENT OF ADULT PATIENTS WITH PREVIOUSLY UNTREATED CHRONIC LYMPHOCYTIC LEUKEMIA OR SMALL LYMPHOCYTIC LEUKEMIA BY ADMINISTERING 100 MG OF ACALABRUTINIB TWICE DAILY IN COMBINATION WITH VENETOCLAX
100MG CALQUENCE ASTRAZENECA N210259 Oct. 31, 2017 RX CAPSULE ORAL 11166951 Aug. 11, 2035 TREATMENT OF ADULT PATIENTS WITH PREVIOUSLY UNTREATED CHRONIC LYMPHOCYTIC LEUKEMIA OR SMALL LYMPHOCYTIC LEUKEMIA IN COMBINATION WITH VENETOCLAX
100MG CALQUENCE ASTRAZENECA N210259 Oct. 31, 2017 RX CAPSULE ORAL 11166951 Aug. 11, 2035 TREATMENT OF ADULT PATIENTS WITH PREVIOUSLY UNTREATED SMALL LYMPHOCYTIC LEUKEMIA BY ADMINISTERING 100 MG OF ACALABRUTINIB TWICE DAILY IN COMBINATION WITH VENETOCLAX
100MG CALQUENCE ASTRAZENECA N210259 Oct. 31, 2017 RX CAPSULE ORAL 11166951 Aug. 11, 2035 TREATMENT OF ADULT PATIENTS WITH PREVIOUSLY UNTREATED SMALL LYMPHOCYTIC LEUKEMIA IN COMBINATION WITH VENETOCLAX
100MG CALQUENCE ASTRAZENECA N210259 Oct. 31, 2017 RX CAPSULE ORAL 10167291 July 1, 2036 TREATMENT OF ADULT PATIENTS WITH CHRONIC LYMPHOCYTIC LEUKEMIA
100MG CALQUENCE ASTRAZENECA N210259 Oct. 31, 2017 RX CAPSULE ORAL 10167291 July 1, 2036 TREATMENT OF ADULT PATIENTS WITH CHRONIC LYMPHOCYTIC LEUKEMIA BY ADMINISTERING 100MG OF ACALABRUTINIB TWICE DAILY
100MG CALQUENCE ASTRAZENECA N210259 Oct. 31, 2017 RX CAPSULE ORAL 10167291 July 1, 2036 TREATMENT OF ADULT PATIENTS WITH CHRONIC LYMPHOCYTIC LEUKEMIA OR SMALL LYMPHOCYTIC LEUKEMIA
100MG CALQUENCE ASTRAZENECA N210259 Oct. 31, 2017 RX CAPSULE ORAL 10167291 July 1, 2036 TREATMENT OF ADULT PATIENTS WITH CHRONIC LYMPHOCYTIC LEUKEMIA OR SMALL LYMPHOCYTIC LEUKEMIA BY ADMINISTERING 100 MG OF ACALABRUTINIB TWICE DAILY
100MG CALQUENCE ASTRAZENECA N210259 Oct. 31, 2017 RX CAPSULE ORAL 10167291 July 1, 2036 TREATMENT OF ADULT PATIENTS WITH MANTLE CELL LYMPHOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
100MG CALQUENCE ASTRAZENECA N210259 Oct. 31, 2017 RX CAPSULE ORAL 10167291 July 1, 2036 TREATMENT OF ADULT PATIENTS WITH MANTLE CELL LYMPHOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY BY ADMINISTERING 100 MG OF ACALABRUTINIB TWICE DAILY
100MG CALQUENCE ASTRAZENECA N210259 Oct. 31, 2017 RX CAPSULE ORAL 10167291 July 1, 2036 TREATMENT OF ADULT PATIENTS WITH PREVIOUSLY UNTREATED CHRONIC LYMPHOCYTIC LEUKEMIA BY ADMINISTERING 100 MG OF ACALABRUTINIB TWICE DAILY IN COMBINATION WITH OBINUTUZUMAB
100MG CALQUENCE ASTRAZENECA N210259 Oct. 31, 2017 RX CAPSULE ORAL 10167291 July 1, 2036 TREATMENT OF ADULT PATIENTS WITH PREVIOUSLY UNTREATED CHRONIC LYMPHOCYTIC LEUKEMIA IN COMBINATION WITH OBINUTUZUMAB
100MG CALQUENCE ASTRAZENECA N210259 Oct. 31, 2017 RX CAPSULE ORAL 10167291 July 1, 2036 TREATMENT OF ADULT PATIENTS WITH PREVIOUSLY UNTREATED CHRONIC LYMPHOCYTIC LEUKEMIA OR SMALL LYMPHOCYTIC LEUKEMIA IN COMBINATION WITH OBINUTUZUMAB
100MG CALQUENCE ASTRAZENECA N210259 Oct. 31, 2017 RX CAPSULE ORAL 10167291 July 1, 2036 TREATMENT OF ADULT PATIENTS WITH PREVIOUSLY UNTREATED CHRONIC LYMPHOCYTIC LEUKEMIA OR SMALL LYMPHOCYTIC LEUKEMIA IN COMBINATION WITH OBINUTUZUMAB BY ADMINISTERING 100 MG OF ACALABRUTINIB TWICE DAILY
100MG CALQUENCE ASTRAZENECA N210259 Oct. 31, 2017 RX CAPSULE ORAL 10167291 July 1, 2036 TREATMENT OF ADULT PATIENTS WITH PREVIOUSLY UNTREATED MANTLE CELL LYMPHOMA WHO ARE INELIGIBLE FOR AUTOLOGOUS HEMATOPOIETIC STEM CELL TRANSPLANTATION BY ADMINISTERING 100 MG OF ACALABRUTINIB TWICE DAILY IN COMBINATION WITH BENDAMUSTINE AND RITUXIMAB
100MG CALQUENCE ASTRAZENECA N210259 Oct. 31, 2017 RX CAPSULE ORAL 10167291 July 1, 2036 TREATMENT OF ADULT PATIENTS WITH PREVIOUSLY UNTREATED SMALL LYMPHOCYTIC LEUKEMIA BY ADMINISTERING 100 MG OF ACALABRUTINIB TWICE DAILY IN COMBINATION WITH OBINUTUZUMAB
100MG CALQUENCE ASTRAZENECA N210259 Oct. 31, 2017 RX CAPSULE ORAL 10167291 July 1, 2036 TREATMENT OF ADULT PATIENTS WITH PREVIOUSLY UNTREATED SMALL LYMPHOCYTIC LEUKEMIA IN COMBINATION WITH OBINUTUZUMAB
100MG CALQUENCE ASTRAZENECA N210259 Oct. 31, 2017 RX CAPSULE ORAL 10167291 July 1, 2036 TREATMENT OF ADULT PATIENTS WITH SMALL LYMPHOCYTIC LEUKEMIA
100MG CALQUENCE ASTRAZENECA N210259 Oct. 31, 2017 RX CAPSULE ORAL 10167291 July 1, 2036 TREATMENT OF ADULT PATIENTS WITH SMALL LYMPHOCYTIC LEUKEMIA BY ADMINISTERING 100MG OF ACALABRUTINIB TWICE DAILY
100MG CALQUENCE ASTRAZENECA N210259 Oct. 31, 2017 RX CAPSULE ORAL 9796721 July 1, 2036 TREATMENT OF ADULT PATIENTS WITH CHRONIC LYMPHOCYTIC LEUKEMIA
100MG CALQUENCE ASTRAZENECA N210259 Oct. 31, 2017 RX CAPSULE ORAL 9796721 July 1, 2036 TREATMENT OF ADULT PATIENTS WITH CHRONIC LYMPHOCYTIC LEUKEMIA OR SMALL LYMPHOCYTIC LEUKEMIA
100MG CALQUENCE ASTRAZENECA N210259 Oct. 31, 2017 RX CAPSULE ORAL 9796721 July 1, 2036 TREATMENT OF ADULT PATIENTS WITH MANTLE CELL LYMPHOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
100MG CALQUENCE ASTRAZENECA N210259 Oct. 31, 2017 RX CAPSULE ORAL 9796721 July 1, 2036 TREATMENT OF ADULT PATIENTS WITH PREVIOUSLY UNTREATED CHRONIC LYMPHOCYTIC LEUKEMIA IN COMBINATION WITH OBINUTUZUMAB
100MG CALQUENCE ASTRAZENECA N210259 Oct. 31, 2017 RX CAPSULE ORAL 9796721 July 1, 2036 TREATMENT OF ADULT PATIENTS WITH PREVIOUSLY UNTREATED CHRONIC LYMPHOCYTIC LEUKEMIA OR SMALL LYMPHOCYTIC LEUKEMIA IN COMBINATION WITH OBINUTUZUMAB
100MG CALQUENCE ASTRAZENECA N210259 Oct. 31, 2017 RX CAPSULE ORAL 9796721 July 1, 2036 TREATMENT OF ADULT PATIENTS WITH PREVIOUSLY UNTREATED MANTLE CELL LYMPHOMA WHO ARE INELIGIBLE FOR AUTOLOGOUS HEMATOPOIETIC STEM CELL TRANSPLANTATION IN COMBINATION WITH BENDAMUSTINE AND RITUXIMAB
100MG CALQUENCE ASTRAZENECA N210259 Oct. 31, 2017 RX CAPSULE ORAL 9796721 July 1, 2036 TREATMENT OF ADULT PATIENTS WITH PREVIOUSLY UNTREATED SMALL LYMPHOCYTIC LEUKEMIA IN COMBINATION WITH OBINUTUZUMAB
100MG CALQUENCE ASTRAZENECA N210259 Oct. 31, 2017 RX CAPSULE ORAL 9796721 July 1, 2036 TREATMENT OF ADULT PATIENTS WITH SMALL LYMPHOCYTIC LEUKEMIA

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
100MG CALQUENCE ASTRAZENECA N210259 Oct. 31, 2017 RX CAPSULE ORAL Nov. 21, 2026 INDICATED FOR THE TREATMENT OF ADULT PATIENTS WITH CHRONIC LYMPHOCYTIC LEUKEMIA (CLL) OR SMALL LYMPHOCYTIC LYMPHOMA (SLL)
100MG CALQUENCE ASTRAZENECA N210259 Oct. 31, 2017 RX CAPSULE ORAL Jan. 16, 2028 IN COMBINATION WITH BENDAMUSTINE AND RITUXIMAB FOR THE TREATMENT OF ADULT PATIENTS WITH PREVIOUSLY UNTREATED MANTLE CELL LYMPHOMA (MCL) WHO ARE INELIGIBLE FOR AUTOLOGOUS HEMATOPOIETIC STEM CELL TRANSPLANTATION (HSCT)
100MG CALQUENCE ASTRAZENECA N210259 Oct. 31, 2017 RX CAPSULE ORAL Feb. 19, 2029 USE WITH VENETOCLAX AS A NEW COMBINATION REGIMEN FOR THE TREATMENT OFADULT PATIENTS WITH CHRONIC LYMPHOCYTIC LEUKEMIA OR SMALL LYMPHOCYTIC LYMPHOMA

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Tyrosine-protein kinase BTK Kinase INHIBITOR IC50 8.29 SCIENTIFIC LITERATURE DRUG LABEL
Epidermal growth factor receptor Kinase IC50 5.45 CHEMBL
Receptor tyrosine-protein kinase erbB-2 Kinase Kd 8.13 CHEMBL
Tyrosine-protein kinase Lyn Kinase INHIBITOR EC50 6 IUPHAR
Tyrosine-protein kinase ITK/TSK Kinase Kd 4.92 CHEMBL
Tyrosine-protein kinase Blk Kinase Kd 7.75 CHEMBL
Tyrosine-protein kinase JAK3 Kinase Kd 5.52 CHEMBL
Receptor tyrosine-protein kinase erbB-4 Kinase INHIBITOR IC50 7.80 SCIENTIFIC LITERATURE
Cytoplasmic tyrosine-protein kinase BMX Kinase INHIBITOR IC50 7.34 SCIENTIFIC LITERATURE
Tyrosine-protein kinase Tec Kinase INHIBITOR IC50 7.03 SCIENTIFIC LITERATURE
Tyrosine-protein kinase TXK Kinase INHIBITOR IC50 6.43 SCIENTIFIC LITERATURE
Platelet glycoprotein VI Membrane receptor IC50 5.92 CHEMBL

External reference:

IDSource
I42748ELQW UNII
4037065 VANDF
C4078312 UMLSCUI
CHEBI:167707 CHEBI
CHEMBL3707348 ChEMBL_ID
71226662 PUBCHEM_CID
DB11703 DRUGBANK_ID
CHEMBL4594293 ChEMBL_ID
D10893 KEGG_DRUG
10150 INN_ID
C000604908 MESH_SUPPLEMENTAL_RECORD_UI
8912 IUPHAR_LIGAND_ID
763037006 SNOMEDCT_US
763502000 SNOMEDCT_US
263870 MMSL
33203 MMSL
d08672 MMSL
017393 NDDF
1986808 RXNORM
I42748ELQW INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
CALQUENCE HUMAN PRESCRIPTION DRUG LABEL 1 0310-0512 CAPSULE, GELATIN COATED 100 mg ORAL NDA 25 sections
CALQUENCE HUMAN PRESCRIPTION DRUG LABEL 1 0310-3512 TABLET, FILM COATED 100 mg ORAL NDA 27 sections
CALQUENCE HUMAN PRESCRIPTION DRUG LABEL 1 0310-4513 TABLET, FILM COATED 100 mg ORAL NDA 27 sections