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Details

Stereochemistry ACHIRAL
Molecular Formula C45H50ClN7O7S
Molecular Weight 868.4419
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of VENETOCLAX

SMILES

CC1(C)CCC(=C(C1)c2ccc(cc2)Cl)CN3CCN(CC3)c4ccc(c(c4)Oc5cc-6ccnc6[nH]c5)C(=NS(=O)(=O)c7ccc(c(c7)N(=O)=O)NCC8CCOCC8)O

InChI

InChIKey=LQBVNQSMGBZMKD-UHFFFAOYSA-N
InChI=1S/C45H50ClN7O7S/c1-45(2)15-11-33(39(26-45)31-3-5-34(46)6-4-31)29-51-17-19-52(20-18-51)35-7-9-38(42(24-35)60-36-23-32-12-16-47-43(32)49-28-36)44(54)50-61(57,58)37-8-10-40(41(25-37)53(55)56)48-27-30-13-21-59-22-14-30/h3-10,12,16,23-25,28,30,48H,11,13-15,17-22,26-27,29H2,1-2H3,(H,47,49)(H,50,54)

HIDE SMILES / InChI

Molecular Formula C45H50ClN7O7S
Molecular Weight 868.4419
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Venetoclax (trade name Venclexta, also known as ABT-199) is a selective and orally bioavailable small-molecule inhibitor of BCL-2, an antiapoptotic protein. BCL-2 and its related proteins BCL-XL and MCL-1 bind to and sequester pro-apoptotic signals in the cell, causing a down-regulation of apoptosis. As an oncogene and an important regulator of apoptosis, BCL-2 overexpression therefore results in increased tumor cell survival and resistance to chemotherapy. FDA approved Venetoclax in April 2016 for the treatment of patients with chronic lymphocytic leukemia (CLL) with 17p deletion, as detected by an FDA approved test, who have received at least one prior therapy. Also this drug in phase 3 clinical trial in combination therapy for the treatment patients with refractory myeloma and Acute Myeloid Leukemia. Common side effects include neutropenia, nausea, anemia, diarrhea, upper respiratory tract infection. Major side effects include tumor lysis syndrome and severe neutropenia.

Approval Year

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
VENCLEXTA

Approved Use

VENCLEXTA is a BCL-2 inhibitor indicated for the treatment of patients with chronic lymphocytic leukemia (CLL) with 17p deletion, as detected by an FDA approved test, who have received at least one prior therapy. This indication is approved under accelerated approval based on overall response rate. Continued approval for this indication may be contingent upon verification and description of clinical benefit in a confirmatory trial.

Launch Date

1460332800000
Primary
Primary
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
2.1 μg/mL
400 mg 1 times / day steady-state, oral
dose: 400 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
VENETOCLAX plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: UNKNOWN
food status: LOW-FAT
1.43 μg/mL
400 mg 1 times / day multiple, oral
dose: 400 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
VENETOCLAX plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: HIGH-FAT
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
32.8 μg × h/mL
400 mg 1 times / day steady-state, oral
dose: 400 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
VENETOCLAX plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: UNKNOWN
food status: LOW-FAT
30.2 μg × h/mL
400 mg 1 times / day multiple, oral
dose: 400 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
VENETOCLAX plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: HIGH-FAT
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
14.1 h
400 mg 1 times / day multiple, oral
dose: 400 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
VENETOCLAX plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: HIGH-FAT
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
1%
400 mg 1 times / day steady-state, oral
dose: 400 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
VENETOCLAX plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: UNKNOWN
food status: LOW-FAT
Doses

Doses

DosePopulationAdverse events​
1200 mg 1 times / day steady, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: steady
Dose: 1200 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 25 - 86 years)
Health Status: unhealthy
Age Group: 66 years (range: 25 - 86 years)
Sex: M+F
Sources:
Disc. AE: Nausea, Diarrhea...
Other AEs: Nausea, Diarrhea...
AEs leading to
discontinuation/dose reduction:
Nausea (5 patients)
Diarrhea (4 patients)
Other AEs:
Nausea (grade 1-2, 53%)
Diarrhea (grade 1-2, 53%)
Diarrhea (grade 3-4, 2%)
Fatigue (grade 1-2, 49%)
Fatigue (grade 3-4, 6%)
Decreased appetite (grade 1-2, 29%)
Vomiting (grade 1-2, 24%)
Constipation (grade 1-2, 18%)
Headache (grade 1-2, 20%)
Anemia (grade 1-2, 10%)
Anemia (grade 3-4, 8%)
Cough (grade 1-2, 10%)
Neutropenia (grade 1-2, 12%)
Neutropenia (grade 3-4, 8%)
Back pain (grade 1-2, 16%)
Back pain (grade 3-4, 2%)
Upper respiratory tract infection (grade 1-2, 8%)
Sources:
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 29 - 85 years)
Health Status: unhealthy
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Sources:
Disc. AE: Neutropenia, Thrombocytopenia...
Other AEs: Neutropenia, Neutrophil count decreased...
AEs leading to
discontinuation/dose reduction:
Neutropenia (grade 3-4, 41%)
Thrombocytopenia (grade 3-4, 15%)
Febrile neutropenia (serious, 2%)
Anemia hemolytic autoimmune (serious, 2%)
Other AEs:
Neutropenia (all grades, > 20)
Neutrophil count decreased (all grades, 45%)
Neutrophil count decreased (grade 3-4, 41%)
Diarrhea (all grades, > 20)
Diarrhea (grade 3-4, <1%)
Nausea (grade 3-4, <1%)
Nausea (all grades, > 20)
Anemia (all grades, > 20)
Anemia (grade 3-4, 18%)
Hemoglobin decreased (all grades, 29%)
Hemoglobin decreased (grade 3-4, 18%)
Upper respiratory tract infection (all grades, > 20)
Thrombocytopenia (all grades, > 20)
Platelet count decreased (all grades, 22%)
Platelet count decreased (grade 3-4, 15%)
Fatigue (all grades, > 20)
Fatigue (grade 3-4, 2%)
Pneumonia (serious, 2%)
Pyrexia (serious, 2%)
Anemia (serious, 2%)
Tumor lysis syndrome (serious, 2%)
Vomiting (all grades, 15%)
Vomiting (grade 3-4, <1%)
Constipation (all grades, 14%)
Peripheral edema (all grades, 11%)
Peripheral edema (grade 3-4, <1%)
Upper respiratory tract infection (all grades, 22%)
Upper respiratory tract infection (grade 3-4, 1%)
Pneumonia (all grades, 8%)
Pneumonia (grade 3-4, 5%)
Hypokalemia (all grades, 12%)
Hypokalemia (grade 3-4, 4%)
Back pain (all grades, 10%)
Back pain (grade 3-4, <1%)
Headache (all grades, 15%)
Headache (grade 3-4, <1%)
Cough (all grades, 13%)
Sources:
600 mg 1 times / day steady, oral
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
DLT: Nausea, Abdominal pain...
Dose limiting toxicities:
Nausea (grade 3, 1 patient)
Abdominal pain (grade 2, 1 patient)
Vomiting (grade 3, 1 patient)
Epigastralgia (grade 3, 1 patient)
Sources:
AEs

AEs

AESignificanceDosePopulation
Diarrhea 4 patients
Disc. AE
1200 mg 1 times / day steady, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: steady
Dose: 1200 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 25 - 86 years)
Health Status: unhealthy
Age Group: 66 years (range: 25 - 86 years)
Sex: M+F
Sources:
Nausea 5 patients
Disc. AE
1200 mg 1 times / day steady, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: steady
Dose: 1200 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 25 - 86 years)
Health Status: unhealthy
Age Group: 66 years (range: 25 - 86 years)
Sex: M+F
Sources:
Anemia grade 1-2, 10%
1200 mg 1 times / day steady, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: steady
Dose: 1200 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 25 - 86 years)
Health Status: unhealthy
Age Group: 66 years (range: 25 - 86 years)
Sex: M+F
Sources:
Cough grade 1-2, 10%
1200 mg 1 times / day steady, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: steady
Dose: 1200 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 25 - 86 years)
Health Status: unhealthy
Age Group: 66 years (range: 25 - 86 years)
Sex: M+F
Sources:
Neutropenia grade 1-2, 12%
1200 mg 1 times / day steady, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: steady
Dose: 1200 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 25 - 86 years)
Health Status: unhealthy
Age Group: 66 years (range: 25 - 86 years)
Sex: M+F
Sources:
Back pain grade 1-2, 16%
1200 mg 1 times / day steady, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: steady
Dose: 1200 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 25 - 86 years)
Health Status: unhealthy
Age Group: 66 years (range: 25 - 86 years)
Sex: M+F
Sources:
Constipation grade 1-2, 18%
1200 mg 1 times / day steady, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: steady
Dose: 1200 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 25 - 86 years)
Health Status: unhealthy
Age Group: 66 years (range: 25 - 86 years)
Sex: M+F
Sources:
Headache grade 1-2, 20%
1200 mg 1 times / day steady, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: steady
Dose: 1200 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 25 - 86 years)
Health Status: unhealthy
Age Group: 66 years (range: 25 - 86 years)
Sex: M+F
Sources:
Vomiting grade 1-2, 24%
1200 mg 1 times / day steady, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: steady
Dose: 1200 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 25 - 86 years)
Health Status: unhealthy
Age Group: 66 years (range: 25 - 86 years)
Sex: M+F
Sources:
Decreased appetite grade 1-2, 29%
1200 mg 1 times / day steady, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: steady
Dose: 1200 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 25 - 86 years)
Health Status: unhealthy
Age Group: 66 years (range: 25 - 86 years)
Sex: M+F
Sources:
Fatigue grade 1-2, 49%
1200 mg 1 times / day steady, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: steady
Dose: 1200 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 25 - 86 years)
Health Status: unhealthy
Age Group: 66 years (range: 25 - 86 years)
Sex: M+F
Sources:
Diarrhea grade 1-2, 53%
1200 mg 1 times / day steady, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: steady
Dose: 1200 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 25 - 86 years)
Health Status: unhealthy
Age Group: 66 years (range: 25 - 86 years)
Sex: M+F
Sources:
Nausea grade 1-2, 53%
1200 mg 1 times / day steady, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: steady
Dose: 1200 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 25 - 86 years)
Health Status: unhealthy
Age Group: 66 years (range: 25 - 86 years)
Sex: M+F
Sources:
Upper respiratory tract infection grade 1-2, 8%
1200 mg 1 times / day steady, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: steady
Dose: 1200 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 25 - 86 years)
Health Status: unhealthy
Age Group: 66 years (range: 25 - 86 years)
Sex: M+F
Sources:
Back pain grade 3-4, 2%
1200 mg 1 times / day steady, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: steady
Dose: 1200 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 25 - 86 years)
Health Status: unhealthy
Age Group: 66 years (range: 25 - 86 years)
Sex: M+F
Sources:
Diarrhea grade 3-4, 2%
1200 mg 1 times / day steady, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: steady
Dose: 1200 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 25 - 86 years)
Health Status: unhealthy
Age Group: 66 years (range: 25 - 86 years)
Sex: M+F
Sources:
Fatigue grade 3-4, 6%
1200 mg 1 times / day steady, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: steady
Dose: 1200 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 25 - 86 years)
Health Status: unhealthy
Age Group: 66 years (range: 25 - 86 years)
Sex: M+F
Sources:
Anemia grade 3-4, 8%
1200 mg 1 times / day steady, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: steady
Dose: 1200 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 25 - 86 years)
Health Status: unhealthy
Age Group: 66 years (range: 25 - 86 years)
Sex: M+F
Sources:
Neutropenia grade 3-4, 8%
1200 mg 1 times / day steady, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: steady
Dose: 1200 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 25 - 86 years)
Health Status: unhealthy
Age Group: 66 years (range: 25 - 86 years)
Sex: M+F
Sources:
Back pain all grades, 10%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 29 - 85 years)
Health Status: unhealthy
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Sources:
Peripheral edema all grades, 11%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 29 - 85 years)
Health Status: unhealthy
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Sources:
Hypokalemia all grades, 12%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 29 - 85 years)
Health Status: unhealthy
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Sources:
Cough all grades, 13%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 29 - 85 years)
Health Status: unhealthy
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Sources:
Constipation all grades, 14%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 29 - 85 years)
Health Status: unhealthy
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Sources:
Headache all grades, 15%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 29 - 85 years)
Health Status: unhealthy
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Sources:
Vomiting all grades, 15%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 29 - 85 years)
Health Status: unhealthy
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Sources:
Platelet count decreased all grades, 22%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 29 - 85 years)
Health Status: unhealthy
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Sources:
Upper respiratory tract infection all grades, 22%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 29 - 85 years)
Health Status: unhealthy
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Sources:
Hemoglobin decreased all grades, 29%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 29 - 85 years)
Health Status: unhealthy
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Sources:
Neutrophil count decreased all grades, 45%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 29 - 85 years)
Health Status: unhealthy
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Sources:
Pneumonia all grades, 8%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 29 - 85 years)
Health Status: unhealthy
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Sources:
Anemia all grades, > 20
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 29 - 85 years)
Health Status: unhealthy
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Sources:
Diarrhea all grades, > 20
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 29 - 85 years)
Health Status: unhealthy
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Sources:
Fatigue all grades, > 20
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 29 - 85 years)
Health Status: unhealthy
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Sources:
Nausea all grades, > 20
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 29 - 85 years)
Health Status: unhealthy
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Sources:
Neutropenia all grades, > 20
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 29 - 85 years)
Health Status: unhealthy
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Sources:
Thrombocytopenia all grades, > 20
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 29 - 85 years)
Health Status: unhealthy
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Sources:
Upper respiratory tract infection all grades, > 20
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 29 - 85 years)
Health Status: unhealthy
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Sources:
Upper respiratory tract infection grade 3-4, 1%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 29 - 85 years)
Health Status: unhealthy
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Sources:
Platelet count decreased grade 3-4, 15%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 29 - 85 years)
Health Status: unhealthy
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Sources:
Thrombocytopenia grade 3-4, 15%
Disc. AE
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 29 - 85 years)
Health Status: unhealthy
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Sources:
Anemia grade 3-4, 18%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 29 - 85 years)
Health Status: unhealthy
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Sources:
Hemoglobin decreased grade 3-4, 18%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 29 - 85 years)
Health Status: unhealthy
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Sources:
Fatigue grade 3-4, 2%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 29 - 85 years)
Health Status: unhealthy
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Sources:
Hypokalemia grade 3-4, 4%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 29 - 85 years)
Health Status: unhealthy
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Sources:
Neutrophil count decreased grade 3-4, 41%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 29 - 85 years)
Health Status: unhealthy
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Sources:
Neutropenia grade 3-4, 41%
Disc. AE
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 29 - 85 years)
Health Status: unhealthy
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Sources:
Pneumonia grade 3-4, 5%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 29 - 85 years)
Health Status: unhealthy
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Sources:
Back pain grade 3-4, <1%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 29 - 85 years)
Health Status: unhealthy
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Sources:
Diarrhea grade 3-4, <1%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 29 - 85 years)
Health Status: unhealthy
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Sources:
Headache grade 3-4, <1%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 29 - 85 years)
Health Status: unhealthy
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Sources:
Nausea grade 3-4, <1%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 29 - 85 years)
Health Status: unhealthy
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Sources:
Peripheral edema grade 3-4, <1%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 29 - 85 years)
Health Status: unhealthy
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Sources:
Vomiting grade 3-4, <1%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 29 - 85 years)
Health Status: unhealthy
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Sources:
Anemia serious, 2%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 29 - 85 years)
Health Status: unhealthy
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Sources:
Pneumonia serious, 2%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 29 - 85 years)
Health Status: unhealthy
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Sources:
Pyrexia serious, 2%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 29 - 85 years)
Health Status: unhealthy
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Sources:
Tumor lysis syndrome serious, 2%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 29 - 85 years)
Health Status: unhealthy
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Sources:
Anemia hemolytic autoimmune serious, 2%
Disc. AE
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 29 - 85 years)
Health Status: unhealthy
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Sources:
Febrile neutropenia serious, 2%
Disc. AE
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, 66 years (range: 29 - 85 years)
Health Status: unhealthy
Age Group: 66 years (range: 29 - 85 years)
Sex: M+F
Sources:
Abdominal pain grade 2, 1 patient
DLT
600 mg 1 times / day steady, oral
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Epigastralgia grade 3, 1 patient
DLT
600 mg 1 times / day steady, oral
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Nausea grade 3, 1 patient
DLT
600 mg 1 times / day steady, oral
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Vomiting grade 3, 1 patient
DLT
600 mg 1 times / day steady, oral
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
no
no
no
no
yes [IC50 0.13 uM]
yes [IC50 0.14 uM]
yes [IC50 0.79 uM]
yes [IC50 0.82 uM]
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
major
yes (co-administration study)
Comment: Co-administration of ketoconazole (a strong CYP3A, P-gp and BCRP inhibitor) increased venetoclax Cmax and AUCX by 2.3- and 6.4-fold, respectively. Co-administration of moderate CYP3A4/5 inhibitors showed a smaller effect on venetoclax exposrue (40 to 60% increase in Cmax and AUCo-24)-
Page: 6
no
no
yes
yes
yes (co-administration study)
Comment: Venetoclax exposure also increased (Cmax t 106%, AUCX T 78%) after co-administration of single dose of rifampin, presumably due to the inhibition of P-gp by rifampin.
Page: 6
Tox targets

Tox targets

PubMed

PubMed

TitleDatePubMed
Bcl-2 gene promotes haemopoietic cell survival and cooperates with c-myc to immortalize pre-B cells.
1988 Sep 29
Potential roles of antisense oligonucleotides in cancer therapy. The example of Bcl-2 antisense oligonucleotides.
2002 Nov
Novel therapies for chronic lymphocytic leukemia.
2004 Jun
An inhibitor of Bcl-2 family proteins induces regression of solid tumours.
2005 Jun 2
Discovery of an orally bioavailable small molecule inhibitor of prosurvival B-cell lymphoma 2 proteins.
2008 Nov 13
The Bcl-xL inhibitor, ABT-737, efficiently induces apoptosis and suppresses growth of hepatoma cells in combination with sorafenib.
2010 Oct
ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets.
2013 Feb
Genomics and drug profiling of fatal TCF3-HLF-positive acute lymphoblastic leukemia identifies recurrent mutation patterns and therapeutic options.
2015 Sep
Patents

Sample Use Guides

Initiate therapy with VENCLEXTA (venetoclax) at 20 mg once daily for 7 days, followed by a weekly ramp-up dosing schedule to the recommended daily dose of 400 mg. VENCLEXTA tablets should be taken orally once daily with a meal and water.
Route of Administration: Oral
ABT-199 (Venetoclax) shows less sensitivity to Bcl-xL, Mcl-1 and Bcl-w with Ki of 48 nM, > 444 nM and 245 nM, respectively. ABT-199 potently inhibits FL5.12-Bcl-2 cells, RS4;11 cells with EC50 of 4 nM and 8 nM, while shows low activity against FL5. ABT-199 also induces apoptosis in CLL with an average EC50 of 3.0 nM.
Substance Class Chemical
Created
by admin
on Fri Jun 25 21:32:57 UTC 2021
Edited
by admin
on Fri Jun 25 21:32:57 UTC 2021
Record UNII
N54AIC43PW
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
VENETOCLAX
DASH   INN   USAN   WHO-DD  
USAN   INN  
Official Name English
RG7601
Code English
ABT-199
Code English
VENETOCLAX [INN]
Common Name English
VENCLEXTA
Brand Name English
VENETOCLAX [ORANGE BOOK]
Common Name English
VENETOCLAX [USAN]
Common Name English
4-(4-((2-(4-CHLOROPHENYL)-4,4-DIMETHYLCYCLOHEX-1-EN-1-YL)METHYL)PIPERAZIN-1-YL)-N-((3-NITRO-4-((TETRAHYDRO-2HPYRAN-4-YLMETHYL) AMINO)PHENYL)SULFONYL)-2-(1H-PYRROLO(2,3-B)PYRIDIN-5-YLOXY)BENZAMIDE
Common Name English
RG-7601
Code English
VENETOCLAX [MI]
Common Name English
BENZAMIDE, 4-(4-((2-(4-CHLOROPHENYL)-4,4-DIMETHYL-1-CYCLOHEXEN-1-YL)METHYL)-1-PIPERAZINYL)-N-((3-NITRO-4-(((TETRAHYDRO-2H-PYRAN-4-YL)METHYL)AMINO)PHENYL)SULFONYL)-2-(1H-PYRROLO(2,3-B)PYRIDIN-5-YLOXY)-
Common Name English
4-(4-((2-(4-CHLOROPHENYL)-4,4-DIMETHYLCYCLOHEX-1-EN-1-YL)METHYL)PIPERAZIN-1-YL)-N-((3-NITRO-4-((TETRAHYDRO-2H-PYRAN-4-YLMETHYL)AMINO)PHENYL)SULFONYL)-2-(1H-PYRROLO(2,3-B)PYRIDIN-5-YLOXY)BENZAMIDE
Systematic Name English
VENETOCLAX [WHO-DD]
Common Name English
GDC-0199
Code English
Classification Tree Code System Code
FDA ORPHAN DRUG 375612
Created by admin on Fri Jun 25 21:32:57 UTC 2021 , Edited by admin on Fri Jun 25 21:32:57 UTC 2021
FDA ORPHAN DRUG 780920
Created by admin on Fri Jun 25 21:32:57 UTC 2021 , Edited by admin on Fri Jun 25 21:32:57 UTC 2021
NDF-RT N0000192515
Created by admin on Fri Jun 25 21:32:57 UTC 2021 , Edited by admin on Fri Jun 25 21:32:57 UTC 2021
FDA ORPHAN DRUG 536116
Created by admin on Fri Jun 25 21:32:57 UTC 2021 , Edited by admin on Fri Jun 25 21:32:57 UTC 2021
EU-Orphan Drug EU/3/16/1617
Created by admin on Fri Jun 25 21:32:57 UTC 2021 , Edited by admin on Fri Jun 25 21:32:57 UTC 2021
FDA ORPHAN DRUG 664118
Created by admin on Fri Jun 25 21:32:57 UTC 2021 , Edited by admin on Fri Jun 25 21:32:57 UTC 2021
FDA ORPHAN DRUG 423814
Created by admin on Fri Jun 25 21:32:57 UTC 2021 , Edited by admin on Fri Jun 25 21:32:57 UTC 2021
FDA ORPHAN DRUG 506815
Created by admin on Fri Jun 25 21:32:57 UTC 2021 , Edited by admin on Fri Jun 25 21:32:57 UTC 2021
FDA ORPHAN DRUG 777520
Created by admin on Fri Jun 25 21:32:57 UTC 2021 , Edited by admin on Fri Jun 25 21:32:57 UTC 2021
NCI_THESAURUS C129824
Created by admin on Fri Jun 25 21:32:57 UTC 2021 , Edited by admin on Fri Jun 25 21:32:57 UTC 2021
WHO-ATC L01XX52
Created by admin on Fri Jun 25 21:32:57 UTC 2021 , Edited by admin on Fri Jun 25 21:32:57 UTC 2021
FDA ORPHAN DRUG 689119
Created by admin on Fri Jun 25 21:32:57 UTC 2021 , Edited by admin on Fri Jun 25 21:32:57 UTC 2021
FDA ORPHAN DRUG 600117
Created by admin on Fri Jun 25 21:32:57 UTC 2021 , Edited by admin on Fri Jun 25 21:32:57 UTC 2021
Code System Code Type Description
RXCUI
1747556
Created by admin on Fri Jun 25 21:32:57 UTC 2021 , Edited by admin on Fri Jun 25 21:32:57 UTC 2021
PRIMARY
NCI_THESAURUS
C103147
Created by admin on Fri Jun 25 21:32:57 UTC 2021 , Edited by admin on Fri Jun 25 21:32:57 UTC 2021
PRIMARY
EVMPD
SUB176260
Created by admin on Fri Jun 25 21:32:57 UTC 2021 , Edited by admin on Fri Jun 25 21:32:57 UTC 2021
PRIMARY
PUBCHEM
49846579
Created by admin on Fri Jun 25 21:32:57 UTC 2021 , Edited by admin on Fri Jun 25 21:32:57 UTC 2021
PRIMARY
WIKIPEDIA
Venetoclax
Created by admin on Fri Jun 25 21:32:57 UTC 2021 , Edited by admin on Fri Jun 25 21:32:57 UTC 2021
PRIMARY
DRUG CENTRAL
5133
Created by admin on Fri Jun 25 21:32:57 UTC 2021 , Edited by admin on Fri Jun 25 21:32:57 UTC 2021
PRIMARY
EPA CompTox
1257044-40-8
Created by admin on Fri Jun 25 21:32:57 UTC 2021 , Edited by admin on Fri Jun 25 21:32:57 UTC 2021
PRIMARY
FDA UNII
N54AIC43PW
Created by admin on Fri Jun 25 21:32:57 UTC 2021 , Edited by admin on Fri Jun 25 21:32:57 UTC 2021
PRIMARY
CAS
1257044-40-8
Created by admin on Fri Jun 25 21:32:57 UTC 2021 , Edited by admin on Fri Jun 25 21:32:57 UTC 2021
PRIMARY
NDF-RT
N0000009176
Created by admin on Fri Jun 25 21:32:57 UTC 2021 , Edited by admin on Fri Jun 25 21:32:57 UTC 2021
PRIMARY Increased Cellular Death [PE]
NDF-RT
N0000185503
Created by admin on Fri Jun 25 21:32:57 UTC 2021 , Edited by admin on Fri Jun 25 21:32:57 UTC 2021
PRIMARY P-Glycoprotein Inhibitors [MoA]
ChEMBL
CHEMBL3137309
Created by admin on Fri Jun 25 21:32:57 UTC 2021 , Edited by admin on Fri Jun 25 21:32:57 UTC 2021
PRIMARY
INN
9925
Created by admin on Fri Jun 25 21:32:57 UTC 2021 , Edited by admin on Fri Jun 25 21:32:57 UTC 2021
PRIMARY
DRUG BANK
DB11581
Created by admin on Fri Jun 25 21:32:57 UTC 2021 , Edited by admin on Fri Jun 25 21:32:57 UTC 2021
PRIMARY
MERCK INDEX
M11932
Created by admin on Fri Jun 25 21:32:57 UTC 2021 , Edited by admin on Fri Jun 25 21:32:57 UTC 2021
PRIMARY
Related Record Type Details
EXCRETED UNCHANGED
AMOUNT EXCRETED
FECAL
TARGET -> INHIBITOR
BINDING
Ki
METABOLIC ENZYME -> SUBSTRATE
TRANSPORTER -> INHIBITOR
IC50
TRANSPORTER -> SUBSTRATE
EFFLUX RATIO
TRANSPORTER -> INHIBITOR
INHIBITOR
IC50
TRANSPORTER -> SUBSTRATE
EFFLUX RATIO
BINDER->LIGAND
BINDING
METABOLIC ENZYME -> SUBSTRATE
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC
Tmax PHARMACOKINETIC ORAL ADMINISTRATION