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Details

Stereochemistry ABSOLUTE
Molecular Formula C25H24N6O2
Molecular Weight 440.498
Optical Activity UNSPECIFIED
Defined Stereocenters 1 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of IBRUTINIB

SMILES

C=CC(=O)N1CCC[C@]([H])(C1)n2c3c(c(-c4ccc(cc4)Oc5ccccc5)n2)c(N)ncn3

InChI

InChIKey=XYFPWWZEPKGCCK-GOSISDBHSA-N
InChI=1S/C25H24N6O2/c1-2-21(32)30-14-6-7-18(15-30)31-25-22(24(26)27-16-28-25)23(29-31)17-10-12-20(13-11-17)33-19-8-4-3-5-9-19/h2-5,8-13,16,18H,1,6-7,14-15H2,(H2,26,27,28)/t18-/m1/s1

HIDE SMILES / InChI

Molecular Formula C25H24N6O2
Molecular Weight 440.498
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 1 / 1
E/Z Centers 0
Optical Activity UNSPECIFIED

Description
Curator's Comment:: http://www.ncbi.nlm.nih.gov/pubmed/?term=23425038

Ibrutinib is an orally bioavailable Bruton's tyrosine kinase (BTK) inhibitor indicated for the treatment of mantle cell lymphoma (MCL) patients that previously received at least one therapy. The drug was jointly developed by Janssen Biotech and Pharmacyclics. Ibrutinib selectively binds to Cys-481 residue in the allosteric inhibitory segment of BTK (TK/SH1 domain), and irreversibly blocks its enzymatic activity thus preventing B-cell activation and signaling, totally blocking the B-cell receptor and cytokine receptor pathways. This leads to an inhibition of the growth of malignant B cells that overexpress BTK. Apart from mantle cell lymphoma Ibrutinib is approved for the treatment of chronic lymphocytic leukemia and Waldenstrom Macroglobulinemia.

CNS Activity

Curator's Comment:: Ibrutinib penetration through the blood-brain barrier was confirmed using plasma and cerebrospinal fluid pharmacokinetic analyses. It has been shown that a low CSF-to-plasma ibrutinib concentration ratio (ranging from 1%-7%) was observed. Ibrutinib CSF distribution may rely on an active influx transport across the blood-brain barrier or a simple diffusion limited by the high plasma protein binding of ibrutinib.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Target ID: Q06187
Gene ID: 695
Gene Symbol: BTK
Target Organism: Homo sapiens (Human)
0.5 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
IMBRUVICA

Approved Use

Indicated for the treatment of patients with: Mantle cell lymphoma (MCL) who have received at least one prior therapy; chronic lymphocytic leukemia (CLL)/Small lymphocytic lymphoma (SLL); Waldenström's macroglobulinemia (WM).

Launch Date

1384300800000
Primary
IMBRUVICA

Approved Use

Indicated for the treatment of patients with: Mantle cell lymphoma (MCL) who have received at least one prior therapy; chronic lymphocytic leukemia (CLL)/Small lymphocytic lymphoma (SLL); Waldenström's macroglobulinemia (WM).

Launch Date

1384300800000
Primary
IMBRUVICA

Approved Use

Indicated for the treatment of patients with: Mantle cell lymphoma (MCL) who have received at least one prior therapy; chronic lymphocytic leukemia (CLL)/Small lymphocytic lymphoma (SLL); Waldenstrom Macroglobulinemia (WM).

Launch Date

1384300800000
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
38.5 ng/mL
420 mg single, oral
dose: 420 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
IBRUTINIB blood
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
51.7 ng/mL
420 mg single, oral
dose: 420 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
IBRUTINIB blood
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
147 ng/mL
420 mg single, oral
dose: 420 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
IBRUTINIB blood
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
120 ng/mL
420 mg single, oral
dose: 420 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
IBRUTINIB blood
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
236 ng × h/mL
420 mg single, oral
dose: 420 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
IBRUTINIB blood
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
485 ng × h/mL
420 mg single, oral
dose: 420 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
IBRUTINIB blood
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
6100 ng × h/mL
420 mg single, oral
dose: 420 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
IBRUTINIB blood
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
864 ng × h/mL
420 mg single, oral
dose: 420 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
IBRUTINIB blood
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
561.6 ng*h/mL
560 mg 1 times / day steady, oral
dose: 560 mg
route of administration: oral
experiment type: steady
co-administered:
IBRUTINIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
1285 ng*h/mL
560 mg 1 times / day multiple, oral
dose: 560 mg
route of administration: oral
experiment type: multiple
co-administered:
IBRUTINIB unknown
Homo sapiens
population: unhealthy
age:
sex:
food status:
1337 ng*h/mL
840 mg 1 times / day multiple, oral
dose: 840 mg
route of administration: oral
experiment type: multiple
co-administered:
IBRUTINIB unknown
Homo sapiens
population: unhealthy
age:
sex:
food status:
1485 ng*h/mL
560 mg 1 times / day multiple, oral
dose: 560 mg
route of administration: oral
experiment type: multiple
co-administered:
PCI-45227 unknown
Homo sapiens
population: unhealthy
age:
sex:
food status:
1671 ng*h/mL
840 mg 1 times / day multiple, oral
dose: 840 mg
route of administration: oral
experiment type: multiple
co-administered:
PCI-45227 unknown
Homo sapiens
population: unhealthy
age:
sex:
food status:
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
9.7 h
420 mg single, oral
dose: 420 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
IBRUTINIB blood
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
11 h
420 mg single, oral
dose: 420 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
IBRUTINIB blood
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
5.2 h
420 mg single, oral
dose: 420 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
IBRUTINIB blood
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
4.5 h
420 mg single, oral
dose: 420 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
IBRUTINIB blood
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
2.7%
IBRUTINIB plasma
Homo sapiens
Doses

Doses

DosePopulationAdverse events​
12.5 mg/kg 1 times / day steady, oral
Highest studied dose
Dose: 12.5 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 12.5 mg/kg, 1 times / day
Sources:
unhealthy, 65 years (range: 41-82 years)
Health Status: unhealthy
Age Group: 65 years (range: 41-82 years)
Sex: M+F
Sources:
Other AEs: Diarrhea, Nausea...
Other AEs:
Diarrhea (grade 1-2, 3 patients)
Nausea (grade 1-2, 2 patients)
Vomiting (grade 1-2, 2 patients)
Constipation (grade 1-2, 1 patient)
Decreased appetite (grade 1-2, 1 patient)
Dyspepsia (grade 1-2, 1 patient)
Fatigue (grade 1-2, 4 patients)
Headache (grade 1-2, 2 patients)
Muscle spasms (grade 1-2, 3 patients)
Myalgia (grade 1-2, 3 patients)
Pyrexia (grade 1-2, 2 patients)
Rash (grade 1-2, 1 patient)
Cough (grade 1-2, 3 patients)
Arthralgia (grade 1-2, 2 patients)
Edema (grade 1-2, 2 patients)
Sources:
8.3 mg/kg 1 times / day steady, oral
Dose: 8.3 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 8.3 mg/kg, 1 times / day
Sources:
unhealthy, 66 years (range: 41-82 years)
Health Status: unhealthy
Age Group: 66 years (range: 41-82 years)
Sex: M+F
Sources:
DLT: Hypersensitivity...
Dose limiting toxicities:
Hypersensitivity (grade 3, 1 patient)
Sources:
2.5 mg/kg 1 times / day steady, oral
Dose: 2.5 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 2.5 mg/kg, 1 times / day
Sources:
unhealthy, 67 years (range: 41-82 years)
Health Status: unhealthy
Age Group: 67 years (range: 41-82 years)
Sex: M+F
Sources:
DLT: Neutropenia...
Dose limiting toxicities:
Neutropenia (grade 2, 1 patient)
Sources:
420 mg 1 times / day steady, oral
Dose: 420 mg, 1 times / day
Route: oral
Route: steady
Dose: 420 mg, 1 times / day
Sources:
unhealthy, 67.0 years (range: 56–71 years)
Health Status: unhealthy
Age Group: 67.0 years (range: 56–71 years)
Sex: M+F
Sources:
DLT: Pneumonia, Sepsis...
Disc. AE: Stomatitis...
Dose limiting toxicities:
Pneumonia (grade 3)
Sepsis (grade 3)
AEs leading to
discontinuation/dose reduction:
Stomatitis (grade 3, 1 patient)
Sources:
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Disc. AE: Subdural hematoma, Neutropenia...
Other AEs: Diarrhea, Diarrhea...
AEs leading to
discontinuation/dose reduction:
Subdural hematoma (1.8%)
Neutropenia (grade 3-4, 29%)
Thrombocytopenia (grade 3-4, 17%)
Anemia (grade 3-4, 9%)
Other AEs:
Diarrhea (grade 1-2, 46%)
Diarrhea (grade 3-4, 5%)
Nausea (grade 1-2, 31%)
Constipation (grade 1-2, 25%)
Abdominal pain (grade 1-2, 19%)
Abdominal pain (grade 3-4, 5%)
Vomiting (grade 1-2, 23%)
Stomatitis (grade 1-2, 16%)
Stomatitis (grade 3-4, 1%)
Dyspepsia (grade 1-2, 11%)
Upper respiratory tract infection (grade 1-2, 34%)
Urinary tract infection (grade 1-2, 11%)
Urinary tract infection (grade 3-4, 3%)
Pneumonia (grade 1-2, 7%)
Pneumonia (grade 3-4, 7%)
Skin infection (grade 1-2, 9%)
Skin infection (grade 3-4, 5%)
Sinusitis (grade 1-2, 12%)
Sinusitis (grade 3-4, 1%)
Fatigue (grade 1-2, 36%)
Fatigue (grade 3-4, 5%)
Peripheral edema (grade 1-2, 32%)
Peripheral edema (grade 3-4, 3%)
Pyrexia (grade 1-2, 17%)
Pyrexia (grade 3-4, 1%)
Asthenia (grade 1-2, 11%)
Asthenia (grade 3-4, 3%)
Bruising (grade 1-2, 30%)
Rash (grade 1-2, 22%)
Rash (grade 3-4, 3%)
Petechiae (grade 1-2, 11%)
Musculoskeletal pain (grade 1-2, 36%)
Musculoskeletal pain (grade 3-4, 1%)
Muscle spasms (grade 1-2, 14%)
Arthralgia (grade 1-2, 11%)
Dyspnea (grade 1-2, 23%)
Dyspnea (grade 3-4, 4%)
Cough (grade 1-2, 19%)
Epistaxis (grade 1-2, 11%)
Decreased appetite (grade 1-2, 19%)
Decreased appetite (grade 3-4, 2%)
Dehydration (grade 1-2, 8%)
Dehydration (grade 3-4, 4%)
Dizziness (grade 1-2, 14%)
Headache (grade 1-2, 13%)
Platelets decreased (grade 1-2, 40%)
Platelets decreased (grade 3-4, 17%)
Neutrophil count decreased (grade 1-2, 18%)
Neutrophil count decreased (grade 3-4, 29%)
Hemoglobin decreased (grade 1-2, 32%)
Hemoglobin decreased (grade 3-4, 9%)
Hyperuricemia (15%)
Hemorrhage (grade 3, 5%)
Infection (grade 3, 25%)
Sources:
AEs

AEs

AESignificanceDosePopulation
Constipation grade 1-2, 1 patient
12.5 mg/kg 1 times / day steady, oral
Highest studied dose
Dose: 12.5 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 12.5 mg/kg, 1 times / day
Sources:
unhealthy, 65 years (range: 41-82 years)
Health Status: unhealthy
Age Group: 65 years (range: 41-82 years)
Sex: M+F
Sources:
Decreased appetite grade 1-2, 1 patient
12.5 mg/kg 1 times / day steady, oral
Highest studied dose
Dose: 12.5 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 12.5 mg/kg, 1 times / day
Sources:
unhealthy, 65 years (range: 41-82 years)
Health Status: unhealthy
Age Group: 65 years (range: 41-82 years)
Sex: M+F
Sources:
Dyspepsia grade 1-2, 1 patient
12.5 mg/kg 1 times / day steady, oral
Highest studied dose
Dose: 12.5 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 12.5 mg/kg, 1 times / day
Sources:
unhealthy, 65 years (range: 41-82 years)
Health Status: unhealthy
Age Group: 65 years (range: 41-82 years)
Sex: M+F
Sources:
Rash grade 1-2, 1 patient
12.5 mg/kg 1 times / day steady, oral
Highest studied dose
Dose: 12.5 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 12.5 mg/kg, 1 times / day
Sources:
unhealthy, 65 years (range: 41-82 years)
Health Status: unhealthy
Age Group: 65 years (range: 41-82 years)
Sex: M+F
Sources:
Arthralgia grade 1-2, 2 patients
12.5 mg/kg 1 times / day steady, oral
Highest studied dose
Dose: 12.5 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 12.5 mg/kg, 1 times / day
Sources:
unhealthy, 65 years (range: 41-82 years)
Health Status: unhealthy
Age Group: 65 years (range: 41-82 years)
Sex: M+F
Sources:
Edema grade 1-2, 2 patients
12.5 mg/kg 1 times / day steady, oral
Highest studied dose
Dose: 12.5 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 12.5 mg/kg, 1 times / day
Sources:
unhealthy, 65 years (range: 41-82 years)
Health Status: unhealthy
Age Group: 65 years (range: 41-82 years)
Sex: M+F
Sources:
Headache grade 1-2, 2 patients
12.5 mg/kg 1 times / day steady, oral
Highest studied dose
Dose: 12.5 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 12.5 mg/kg, 1 times / day
Sources:
unhealthy, 65 years (range: 41-82 years)
Health Status: unhealthy
Age Group: 65 years (range: 41-82 years)
Sex: M+F
Sources:
Nausea grade 1-2, 2 patients
12.5 mg/kg 1 times / day steady, oral
Highest studied dose
Dose: 12.5 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 12.5 mg/kg, 1 times / day
Sources:
unhealthy, 65 years (range: 41-82 years)
Health Status: unhealthy
Age Group: 65 years (range: 41-82 years)
Sex: M+F
Sources:
Pyrexia grade 1-2, 2 patients
12.5 mg/kg 1 times / day steady, oral
Highest studied dose
Dose: 12.5 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 12.5 mg/kg, 1 times / day
Sources:
unhealthy, 65 years (range: 41-82 years)
Health Status: unhealthy
Age Group: 65 years (range: 41-82 years)
Sex: M+F
Sources:
Vomiting grade 1-2, 2 patients
12.5 mg/kg 1 times / day steady, oral
Highest studied dose
Dose: 12.5 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 12.5 mg/kg, 1 times / day
Sources:
unhealthy, 65 years (range: 41-82 years)
Health Status: unhealthy
Age Group: 65 years (range: 41-82 years)
Sex: M+F
Sources:
Cough grade 1-2, 3 patients
12.5 mg/kg 1 times / day steady, oral
Highest studied dose
Dose: 12.5 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 12.5 mg/kg, 1 times / day
Sources:
unhealthy, 65 years (range: 41-82 years)
Health Status: unhealthy
Age Group: 65 years (range: 41-82 years)
Sex: M+F
Sources:
Diarrhea grade 1-2, 3 patients
12.5 mg/kg 1 times / day steady, oral
Highest studied dose
Dose: 12.5 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 12.5 mg/kg, 1 times / day
Sources:
unhealthy, 65 years (range: 41-82 years)
Health Status: unhealthy
Age Group: 65 years (range: 41-82 years)
Sex: M+F
Sources:
Muscle spasms grade 1-2, 3 patients
12.5 mg/kg 1 times / day steady, oral
Highest studied dose
Dose: 12.5 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 12.5 mg/kg, 1 times / day
Sources:
unhealthy, 65 years (range: 41-82 years)
Health Status: unhealthy
Age Group: 65 years (range: 41-82 years)
Sex: M+F
Sources:
Myalgia grade 1-2, 3 patients
12.5 mg/kg 1 times / day steady, oral
Highest studied dose
Dose: 12.5 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 12.5 mg/kg, 1 times / day
Sources:
unhealthy, 65 years (range: 41-82 years)
Health Status: unhealthy
Age Group: 65 years (range: 41-82 years)
Sex: M+F
Sources:
Fatigue grade 1-2, 4 patients
12.5 mg/kg 1 times / day steady, oral
Highest studied dose
Dose: 12.5 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 12.5 mg/kg, 1 times / day
Sources:
unhealthy, 65 years (range: 41-82 years)
Health Status: unhealthy
Age Group: 65 years (range: 41-82 years)
Sex: M+F
Sources:
Hypersensitivity grade 3, 1 patient
DLT
8.3 mg/kg 1 times / day steady, oral
Dose: 8.3 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 8.3 mg/kg, 1 times / day
Sources:
unhealthy, 66 years (range: 41-82 years)
Health Status: unhealthy
Age Group: 66 years (range: 41-82 years)
Sex: M+F
Sources:
Neutropenia grade 2, 1 patient
DLT, Disc. AE
2.5 mg/kg 1 times / day steady, oral
Dose: 2.5 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 2.5 mg/kg, 1 times / day
Sources:
unhealthy, 67 years (range: 41-82 years)
Health Status: unhealthy
Age Group: 67 years (range: 41-82 years)
Sex: M+F
Sources:
Stomatitis grade 3, 1 patient
Disc. AE
420 mg 1 times / day steady, oral
Dose: 420 mg, 1 times / day
Route: oral
Route: steady
Dose: 420 mg, 1 times / day
Sources:
unhealthy, 67.0 years (range: 56–71 years)
Health Status: unhealthy
Age Group: 67.0 years (range: 56–71 years)
Sex: M+F
Sources:
Pneumonia grade 3
DLT, Disc. AE
420 mg 1 times / day steady, oral
Dose: 420 mg, 1 times / day
Route: oral
Route: steady
Dose: 420 mg, 1 times / day
Sources:
unhealthy, 67.0 years (range: 56–71 years)
Health Status: unhealthy
Age Group: 67.0 years (range: 56–71 years)
Sex: M+F
Sources:
Sepsis grade 3
DLT, Disc. AE
420 mg 1 times / day steady, oral
Dose: 420 mg, 1 times / day
Route: oral
Route: steady
Dose: 420 mg, 1 times / day
Sources:
unhealthy, 67.0 years (range: 56–71 years)
Health Status: unhealthy
Age Group: 67.0 years (range: 56–71 years)
Sex: M+F
Sources:
Subdural hematoma 1.8%
Disc. AE
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Hyperuricemia 15%
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Arthralgia grade 1-2, 11%
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Asthenia grade 1-2, 11%
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Dyspepsia grade 1-2, 11%
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Epistaxis grade 1-2, 11%
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Petechiae grade 1-2, 11%
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Urinary tract infection grade 1-2, 11%
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Sinusitis grade 1-2, 12%
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Headache grade 1-2, 13%
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Dizziness grade 1-2, 14%
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Muscle spasms grade 1-2, 14%
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Stomatitis grade 1-2, 16%
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Pyrexia grade 1-2, 17%
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Neutrophil count decreased grade 1-2, 18%
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Abdominal pain grade 1-2, 19%
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Cough grade 1-2, 19%
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Decreased appetite grade 1-2, 19%
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Rash grade 1-2, 22%
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Dyspnea grade 1-2, 23%
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Vomiting grade 1-2, 23%
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Constipation grade 1-2, 25%
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Bruising grade 1-2, 30%
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Nausea grade 1-2, 31%
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Hemoglobin decreased grade 1-2, 32%
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Peripheral edema grade 1-2, 32%
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Upper respiratory tract infection grade 1-2, 34%
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Fatigue grade 1-2, 36%
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Musculoskeletal pain grade 1-2, 36%
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Platelets decreased grade 1-2, 40%
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Diarrhea grade 1-2, 46%
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Pneumonia grade 1-2, 7%
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Dehydration grade 1-2, 8%
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Skin infection grade 1-2, 9%
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Infection grade 3, 25%
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Hemorrhage grade 3, 5%
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Musculoskeletal pain grade 3-4, 1%
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Pyrexia grade 3-4, 1%
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Sinusitis grade 3-4, 1%
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Stomatitis grade 3-4, 1%
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Platelets decreased grade 3-4, 17%
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Thrombocytopenia grade 3-4, 17%
Disc. AE
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Decreased appetite grade 3-4, 2%
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Neutrophil count decreased grade 3-4, 29%
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Neutropenia grade 3-4, 29%
Disc. AE
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Asthenia grade 3-4, 3%
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Peripheral edema grade 3-4, 3%
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Rash grade 3-4, 3%
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Urinary tract infection grade 3-4, 3%
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Dehydration grade 3-4, 4%
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Dyspnea grade 3-4, 4%
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Abdominal pain grade 3-4, 5%
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Diarrhea grade 3-4, 5%
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Fatigue grade 3-4, 5%
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Skin infection grade 3-4, 5%
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Pneumonia grade 3-4, 7%
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Hemoglobin decreased grade 3-4, 9%
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
Anemia grade 3-4, 9%
Disc. AE
560 mg 1 times / day steady, oral
Recommended
Dose: 560 mg, 1 times / day
Route: oral
Route: steady
Dose: 560 mg, 1 times / day
Sources:
unhealthy, 68 years (range: 40 - 84 years)
Health Status: unhealthy
Age Group: 68 years (range: 40 - 84 years)
Sex: M+F
Sources:
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no [Ki 4.8 uM]
no
no
no
no
weak [Ki 10 uM]
weak [Ki 12 uM]
weak [Ki 12.5 uM]
weak [Ki 4.8 uM]
weak [Ki 5.9 uM]
weak [Ki 6.6 uM]
yes [IC50 4.9 uM]
yes
yes
yes
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
major
yes (co-administration study)
Comment: In a dedicated drug-interaction trial, concomitant ketoconazole (strong CYP3A4 inhibitor) increased ibrutinib Cmax 29-fold and AUC 24-fold.
Page: -
no [Ki >100 uM]
no
no
no
no
no
no
yes
yes
yes (pharmacogenomic study)
Comment: n the mass balance trial (n = 6), the mean ibrutinib and the active metabolite PCI-45227 AUCs were 10% and 29% higher, respectively in CYP2D6 poor metabolizers (PMs, N=2) compared with the mean AUCs in CYP2D6 extensive metabolizers (EMs, N=4).
Page: -
Tox targets

Tox targets

PubMed

PubMed

TitleDatePubMed
Discovery of selective irreversible inhibitors for Bruton's tyrosine kinase.
2007 Jan
Bruton's tyrosine kinase inhibitors: approaches to potent and selective inhibition, preclinical and clinical evaluation for inflammatory diseases and B cell malignancies.
2012 May 24
Ibrutinib: a novel Bruton's tyrosine kinase inhibitor with outstanding responses in patients with chronic lymphocytic leukemia.
2013 Aug
Targeting BTK with ibrutinib in relapsed chronic lymphocytic leukemia.
2013 Jul 4
Ibrutinib: a strong candidate for the future of mantle cell lymphoma treatment.
2013 Jun
Bruton tyrosine kinase inhibitor ibrutinib (PCI-32765).
2013 Nov
Blockade of oncogenic IκB kinase activity in diffuse large B-cell lymphoma by bromodomain and extraterminal domain protein inhibitors.
2014 Aug 5
Absorption, metabolism, and excretion of oral ¹⁴C radiolabeled ibrutinib: an open-label, phase I, single-dose study in healthy men.
2015 Feb
Ibrutinib in pretreated Waldenström's macroglobulinaemia.
2015 May
Ibrutinib: a review of its use in patients with mantle cell lymphoma or chronic lymphocytic leukaemia.
2015 May
Synergistic activity of BET protein antagonist-based combinations in mantle cell lymphoma cells sensitive or resistant to ibrutinib.
2015 Sep 24
Patents

Patents

Sample Use Guides

MCL: 560 mg taken orally once daily (four 140 mg capsules once daily); CLL/SLL and WM: 420 mg taken orally once daily (three 140 mg capsules once daily). Capsules should be taken orally with a glass of water.
Route of Administration: Oral
CLL-B cells were freshly isolated from the peripheral blood of the CLL patients before the initiation of ibrutinib therapy, cultured in vitro for 72 h in the presence or absence of ibrutinib, and analyzed with annexin V and 7AAD double staining. CLL cells were cultured alone in the presence or absence of various concentrations of ibrutinib from 0.01 to 10 uM.
Substance Class Chemical
Created
by admin
on Fri Jun 25 21:40:10 UTC 2021
Edited
by admin
on Fri Jun 25 21:40:10 UTC 2021
Record UNII
1X70OSD4VX
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
IBRUTINIB
DASH   INN   USAN   VANDF   WHO-DD  
INN   USAN  
Official Name English
PCI-32765
Code English
PCI-32765-00
Code English
IBRUTINIB [VANDF]
Common Name English
IMBRUVICA
Brand Name English
IBRUTINIB [WHO-DD]
Common Name English
IBRUTINIB [ORANGE BOOK]
Common Name English
2-PROPEN-1-ONE, 1-((3R)-3-(4-AMINO-3-(4-PHENOXYPHENYL)-1H-PYRAZOLO(3,4-D)PYRIMIDIN-1-YL)-1-PIPERIDINYL)-
Systematic Name English
IBRUTINIB [USAN]
Common Name English
IBRUTINIB [MI]
Common Name English
PC-32765
Code English
PCI 32765
Code English
1-((3R)-3-(4-AMINO-3-(4-PHENOXYPHENYL)-1H-PYRAZOLO(3,4-D)PYRIMIDIN-1-YL)PIPERIDIN-1- YL)PROP-2-EN-1-ONE
Systematic Name English
CRA-032765
Code English
IBRUTINIB [INN]
Common Name English
Classification Tree Code System Code
FDA ORPHAN DRUG 462314
Created by admin on Fri Jun 25 21:40:10 UTC 2021 , Edited by admin on Fri Jun 25 21:40:10 UTC 2021
FDA ORPHAN DRUG 574317
Created by admin on Fri Jun 25 21:40:10 UTC 2021 , Edited by admin on Fri Jun 25 21:40:10 UTC 2021
EMA ASSESSMENT REPORTS IMBRUVIA (AUTHORIZED: LYMPHOMA, MANTLE-CELL)
Created by admin on Fri Jun 25 21:40:10 UTC 2021 , Edited by admin on Fri Jun 25 21:40:10 UTC 2021
FDA ORPHAN DRUG 622317
Created by admin on Fri Jun 25 21:40:10 UTC 2021 , Edited by admin on Fri Jun 25 21:40:10 UTC 2021
FDA ORPHAN DRUG 409713
Created by admin on Fri Jun 25 21:40:10 UTC 2021 , Edited by admin on Fri Jun 25 21:40:10 UTC 2021
FDA ORPHAN DRUG 462214
Created by admin on Fri Jun 25 21:40:10 UTC 2021 , Edited by admin on Fri Jun 25 21:40:10 UTC 2021
FDA ORPHAN DRUG 444414
Created by admin on Fri Jun 25 21:40:10 UTC 2021 , Edited by admin on Fri Jun 25 21:40:10 UTC 2021
EMA ASSESSMENT REPORTS IMBRUVICA (AUTHORIZED: LEUKEMIA, LYMPHOCYTIC, CHRONIC, B-CELL)
Created by admin on Fri Jun 25 21:40:10 UTC 2021 , Edited by admin on Fri Jun 25 21:40:10 UTC 2021
FDA ORPHAN DRUG 407413
Created by admin on Fri Jun 25 21:40:10 UTC 2021 , Edited by admin on Fri Jun 25 21:40:10 UTC 2021
NCI_THESAURUS C124801
Created by admin on Fri Jun 25 21:40:11 UTC 2021 , Edited by admin on Fri Jun 25 21:40:11 UTC 2021
EU-Orphan Drug EU/3/13/1203
Created by admin on Fri Jun 25 21:40:10 UTC 2021 , Edited by admin on Fri Jun 25 21:40:10 UTC 2021
WHO-ATC L01XE27
Created by admin on Fri Jun 25 21:40:10 UTC 2021 , Edited by admin on Fri Jun 25 21:40:10 UTC 2021
FDA ORPHAN DRUG 395513
Created by admin on Fri Jun 25 21:40:10 UTC 2021 , Edited by admin on Fri Jun 25 21:40:10 UTC 2021
FDA ORPHAN DRUG 525616
Created by admin on Fri Jun 25 21:40:10 UTC 2021 , Edited by admin on Fri Jun 25 21:40:10 UTC 2021
FDA ORPHAN DRUG 383112
Created by admin on Fri Jun 25 21:40:10 UTC 2021 , Edited by admin on Fri Jun 25 21:40:10 UTC 2021
NDF-RT N0000175605
Created by admin on Fri Jun 25 21:40:11 UTC 2021 , Edited by admin on Fri Jun 25 21:40:11 UTC 2021
FDA ORPHAN DRUG 462114
Created by admin on Fri Jun 25 21:40:10 UTC 2021 , Edited by admin on Fri Jun 25 21:40:10 UTC 2021
FDA ORPHAN DRUG 366212
Created by admin on Fri Jun 25 21:40:10 UTC 2021 , Edited by admin on Fri Jun 25 21:40:10 UTC 2021
FDA ORPHAN DRUG 368012
Created by admin on Fri Jun 25 21:40:10 UTC 2021 , Edited by admin on Fri Jun 25 21:40:10 UTC 2021
FDA ORPHAN DRUG 397313
Created by admin on Fri Jun 25 21:40:10 UTC 2021 , Edited by admin on Fri Jun 25 21:40:10 UTC 2021
NCI_THESAURUS C129825
Created by admin on Fri Jun 25 21:40:11 UTC 2021 , Edited by admin on Fri Jun 25 21:40:11 UTC 2021
Code System Code Type Description
INN
9566
Created by admin on Fri Jun 25 21:40:10 UTC 2021 , Edited by admin on Fri Jun 25 21:40:10 UTC 2021
PRIMARY
EU-Orphan Drug
EU/3/12/984(POSITIVE)
Created by admin on Fri Jun 25 21:40:10 UTC 2021 , Edited by admin on Fri Jun 25 21:40:10 UTC 2021
PRIMARY On 26 April 2012, orphan designation (EU/3/12/984) was granted by the European Commission to Nexus Oncology Ltd, United Kingdom, for 1-[(3R)-3-[4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4 d]pyrimidin-1-yl]-1-piperidinyl]-2-propen-1-one for the treatment of chronic lymphocytic leukaemia. The sponsorship was transferred to Janssen-Cilag International N.V, Belgium, in January 2013.
DRUG BANK
DB09053
Created by admin on Fri Jun 25 21:40:10 UTC 2021 , Edited by admin on Fri Jun 25 21:40:10 UTC 2021
PRIMARY
FDA UNII
1X70OSD4VX
Created by admin on Fri Jun 25 21:40:10 UTC 2021 , Edited by admin on Fri Jun 25 21:40:10 UTC 2021
PRIMARY
MERCK INDEX
M11677
Created by admin on Fri Jun 25 21:40:11 UTC 2021 , Edited by admin on Fri Jun 25 21:40:11 UTC 2021
PRIMARY
LACTMED
Ibrutinib
Created by admin on Fri Jun 25 21:40:11 UTC 2021 , Edited by admin on Fri Jun 25 21:40:11 UTC 2021
PRIMARY
IUPHAR
6912
Created by admin on Fri Jun 25 21:40:10 UTC 2021 , Edited by admin on Fri Jun 25 21:40:10 UTC 2021
PRIMARY
ChEMBL
CHEMBL1873475
Created by admin on Fri Jun 25 21:40:10 UTC 2021 , Edited by admin on Fri Jun 25 21:40:10 UTC 2021
PRIMARY
NCI_THESAURUS
C81934
Created by admin on Fri Jun 25 21:40:11 UTC 2021 , Edited by admin on Fri Jun 25 21:40:11 UTC 2021
PRIMARY
DRUG CENTRAL
4810
Created by admin on Fri Jun 25 21:40:10 UTC 2021 , Edited by admin on Fri Jun 25 21:40:10 UTC 2021
PRIMARY
RXCUI
1442981
Created by admin on Fri Jun 25 21:40:11 UTC 2021 , Edited by admin on Fri Jun 25 21:40:11 UTC 2021
PRIMARY RxNorm
PUBCHEM
24821094
Created by admin on Fri Jun 25 21:40:11 UTC 2021 , Edited by admin on Fri Jun 25 21:40:11 UTC 2021
PRIMARY
EVMPD
SUB120863
Created by admin on Fri Jun 25 21:40:10 UTC 2021 , Edited by admin on Fri Jun 25 21:40:10 UTC 2021
PRIMARY
CAS
936563-96-1
Created by admin on Fri Jun 25 21:40:10 UTC 2021 , Edited by admin on Fri Jun 25 21:40:10 UTC 2021
PRIMARY
HSDB
8260
Created by admin on Fri Jun 25 21:40:10 UTC 2021 , Edited by admin on Fri Jun 25 21:40:10 UTC 2021
PRIMARY
Related Record Type Details
BINDER->LIGAND
BINDING
TARGET -> INHIBITOR RESISTANT
TARGET -> INHIBITOR
Binds to a cysteine residue (Cys-481) in the BTK active site
IRREVERSIBLE INHIBITOR
IC50
EXCRETED UNCHANGED
FECAL
ENANTIOMER -> ENANTIOMER
METABOLIC ENZYME -> SUBSTRATE
Related Record Type Details
METABOLITE -> PARENT
METABOLITE ACTIVE -> PARENT
Concentration higher than IBRUTINIB
MAJOR
PLASMA
METABOLITE -> PARENT
METABOLITE -> PARENT
METABOLITE ACTIVE -> PARENT
FECAL
Related Record Type Details
ACTIVE MOIETY
FECAL
Name Property Type Amount Referenced Substance Defining Parameters References
Volume of Distribution PHARMACOKINETIC
Biological Half-life PHARMACOKINETIC