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acalabrutinib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| tyrosine kinase inhibitors | 5260 | 1420477-60-6 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
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.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.20 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| 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):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| 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:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| 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 term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients 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 term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients 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 term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients 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:
| Source | Code | Description |
|---|---|---|
| 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
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| 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 level | Dissociation constant | Type (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 strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent 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 strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 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:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA 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:
| ID | Source |
|---|---|
| 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:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| 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 |