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Details

Stereochemistry ABSOLUTE
Molecular Formula C22H17ClN6O.H2O
Molecular Weight 434.878
Optical Activity UNSPECIFIED
Defined Stereocenters 1 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of DUVELISIB MONOHYDRATE

SMILES

O.C[C@H](NC1=C2N=CNC2=NC=N1)C3=CC4=C(C(Cl)=CC=C4)C(=O)N3C5=CC=CC=C5

InChI

InChIKey=FQLHRUBTGKTKPZ-ZOWNYOTGSA-N
InChI=1S/C22H17ClN6O.H2O/c1-13(28-21-19-20(25-11-24-19)26-12-27-21)17-10-14-6-5-9-16(23)18(14)22(30)29(17)15-7-3-2-4-8-15;/h2-13H,1H3,(H2,24,25,26,27,28);1H2/t13-;/m0./s1

HIDE SMILES / InChI

Description
Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/24211136

Duvelisib (IPI-145), is an orally available, small-molecule, selective dual inhibitor of phosphatidylinositol 3 kinase (PI3K) δ and γ isoforms originated by Intellikine (owned by Takeda) and developed by Infinity Pharmaceuticals. Orally administered duvelisib was rapidly absorbed, with a dose-proportional increase in exposure. The compound produced a half-life of approximately 7-12 hours, following 14 days of dosing. Duvelisib exerts profound effects on adaptive and innate immunity by inhibiting B and T cell proliferation, blocking neutrophil migration, and inhibiting basophil activation. Duvelisib blockade of PI3K-δ and PI3K-γ potentially lead to significant therapeutic effects in multiple inflammatory, autoimmune, and hematologic diseases. The molecule is in phase III development as a combination therapy for patients with haematological malignancies such as chronic lymphocytic leukemia and follicular lymphoma.

Originator

Curator's Comment: # Intellikine (owned by Takeda)

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
2.5 nM [IC50]
27.0 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
COPIKTRA

Approved Use

COPIKTRA is a kinase inhibitor indicated for the treatment of adult patients with: • Relapsed or refractory chronic lymphocytic leukemia (CLL) or small lymphocytic lymphoma (SLL) after at least two prior therapies. • Relapsed or refractory follicular lymphoma (FL) after at least two prior systemic therapies.

Launch Date

2018
Primary
COPIKTRA

Approved Use

COPIKTRA is a kinase inhibitor indicated for the treatment of adult patients with: • Relapsed or refractory chronic lymphocytic leukemia (CLL) or small lymphocytic lymphoma (SLL) after at least two prior therapies. • Relapsed or refractory follicular lymphoma (FL) after at least two prior systemic therapies.

Launch Date

2018
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
1062 ng/mL
50 mg single, oral
dose: 50 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
DUVELISIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
1.5 μg/mL
50 mg 2 times / day steady-state, oral
dose: 50 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
DUVELISIB unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
7098.4 ng × h/mL
50 mg single, oral
dose: 50 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
DUVELISIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
7.9 μg × h/mL
50 mg 2 times / day steady-state, oral
dose: 50 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
DUVELISIB unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
6.8 h
50 mg single, oral
dose: 50 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
DUVELISIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
4.7 h
50 mg 2 times / day steady-state, oral
dose: 50 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
DUVELISIB unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
100 mg 2 times / day steady, oral
Highest studied dose
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
unhealthy, 66.5 years (range: 25-86 years)
n = 2
Health Status: unhealthy
Age Group: 66.5 years (range: 25-86 years)
Sex: M+F
Population Size: 2
Sources:
DLT: Alanine aminotransferase increase, Aspartate aminotransferase increased...
Dose limiting toxicities:
Alanine aminotransferase increase (grade 3, 1 patient)
Aspartate aminotransferase increased (grade 3, 1 patient)
Rash (grade 3, 1 patient)
Sources:
75 mg 2 times / day steady, oral
MTD
Dose: 75 mg, 2 times / day
Route: oral
Route: steady
Dose: 75 mg, 2 times / day
Sources:
unhealthy, 66.5 years (range: 25-86 years)
n = 6
Health Status: unhealthy
Age Group: 66.5 years (range: 25-86 years)
Sex: M+F
Population Size: 6
Sources:
DLT: Cellulitis...
Dose limiting toxicities:
Cellulitis (grade 3, 1 patient)
Sources:
15 mg 2 times / day steady, oral
Dose: 15 mg, 2 times / day
Route: oral
Route: steady
Dose: 15 mg, 2 times / day
Sources:
unhealthy, 66.5 years (range: 25-86 years)
n = 7
Health Status: unhealthy
Age Group: 66.5 years (range: 25-86 years)
Sex: M+F
Population Size: 7
Sources:
DLT: Neutropenia...
Dose limiting toxicities:
Neutropenia (grade 4, 1 patient)
Sources:
25 mg 2 times / day steady, oral
Recommended
Dose: 25 mg, 2 times / day
Route: oral
Route: steady
Dose: 25 mg, 2 times / day
Sources: Page: p. 137
unhealthy, 67 years (range: 30 - 90 years)
n = 442
Health Status: unhealthy
Condition: Hematologic Malignancies
Age Group: 67 years (range: 30 - 90 years)
Sex: M+F
Population Size: 442
Sources: Page: p. 137
Disc. AE: Transaminases increased, Sepsis...
AEs leading to
discontinuation/dose reduction:
Transaminases increased (1%)
Sepsis (1%)
Transaminases increased (4%)
Neutropenia (3%)
Febrile neutropenia (2%)
Lipase increased (1%)
Diarrhea (19%)
Colitis (19%)
Rash (8%)
Pneumonia (10%)
Neutropenia (8%)
Transaminases increased (6%)
Pyrexia (4%)
Anemia (3%)
Febrile neutropenia (3%)
Lipase increased (3%)
Thrombocytopenia (3%)
Sources: Page: p. 137
25 mg 2 times / day steady, oral
Recommended
Dose: 25 mg, 2 times / day
Route: oral
Route: steady
Dose: 25 mg, 2 times / day
Sources:
unhealthy, 69 years (range: 39 - 90 years
n = 158
Health Status: unhealthy
Condition: CLL or SLL
Age Group: 69 years (range: 39 - 90 years
Sex: M+F
Population Size: 158
Sources:
Disc. AE: Diarrhea, Colitis...
AEs leading to
discontinuation/dose reduction:
Diarrhea (36%)
Colitis (36%)
Infection (36%)
Rash (36%)
Diarrhea (29%)
Colitis (29%)
Rash (29%)
Sources:
75 mg 2 times / day steady, oral
MTD
Dose: 75 mg, 2 times / day
Route: oral
Route: steady
Dose: 75 mg, 2 times / day
Sources:
unhealthy, 70 years (range: 42-78)
n = 15
Health Status: unhealthy
Age Group: 70 years (range: 42-78)
Sex: M+F
Population Size: 15
Sources:
Other AEs: ALT increased, AST increased...
Other AEs:
ALT increased (grade 3-4, 40%)
AST increased (grade 3-4, 13.3%)
Neutropenia (grade 3-4, 33.3%)
Anemia (grade 3, 13.3%)
Diarrhea (grade 3, 33.3%)
Pyrexia (grade 3, 6.7%)
Nausea (grade 3, 6.7%)
Rash maculo-papular (grade 3, 13.3%)
Thrombocytopenia (grade 1-2, 13.3%)
Fatigue (grade 1-2, 46.7%)
Cough (grade 1-2, 46.7%)
Headache (grade 1-2, 26.7%)
Decreased appetite (grade 1-2, 26.7%)
Dyspnoea (grade 1-2, 40%)
Rash (grade 1-2, 26.7%)
Upper respiratory tract infection (grade 1-2, 13.3%)
Vomiting (grade 1-2, 6.7%)
Chills (grade 1-2, 13.3%)
Myalgia (grade 1-2, 26.7%)
Edema peripheral (grade 1-2, 26.7%)
Oropharyngeal pain (grade 1-2, 20%)
Stomatitis (grade 1-2, 26.7%)
Sources:
25 mg 2 times / day steady, oral
Recommended
Dose: 25 mg, 2 times / day
Route: oral
Route: steady
Dose: 25 mg, 2 times / day
Sources:
unhealthy
Other AEs: Infection, Diarrhea...
Other AEs:
Infection (grade 5|serious, 31%)
Diarrhea (grade 5|serious, 18%)
Colitis (grade 5|serious, 18%)
Epidermal and dermal conditions (grade 5|serious, 5%)
Pneumonitis (grade 5|serious, 5%)
Sources:
AEs

AEs

AESignificanceDosePopulation
Alanine aminotransferase increase grade 3, 1 patient
DLT
100 mg 2 times / day steady, oral
Highest studied dose
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
unhealthy, 66.5 years (range: 25-86 years)
n = 2
Health Status: unhealthy
Age Group: 66.5 years (range: 25-86 years)
Sex: M+F
Population Size: 2
Sources:
Aspartate aminotransferase increased grade 3, 1 patient
DLT
100 mg 2 times / day steady, oral
Highest studied dose
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
unhealthy, 66.5 years (range: 25-86 years)
n = 2
Health Status: unhealthy
Age Group: 66.5 years (range: 25-86 years)
Sex: M+F
Population Size: 2
Sources:
Rash grade 3, 1 patient
DLT
100 mg 2 times / day steady, oral
Highest studied dose
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
unhealthy, 66.5 years (range: 25-86 years)
n = 2
Health Status: unhealthy
Age Group: 66.5 years (range: 25-86 years)
Sex: M+F
Population Size: 2
Sources:
Cellulitis grade 3, 1 patient
DLT
75 mg 2 times / day steady, oral
MTD
Dose: 75 mg, 2 times / day
Route: oral
Route: steady
Dose: 75 mg, 2 times / day
Sources:
unhealthy, 66.5 years (range: 25-86 years)
n = 6
Health Status: unhealthy
Age Group: 66.5 years (range: 25-86 years)
Sex: M+F
Population Size: 6
Sources:
Neutropenia grade 4, 1 patient
DLT
15 mg 2 times / day steady, oral
Dose: 15 mg, 2 times / day
Route: oral
Route: steady
Dose: 15 mg, 2 times / day
Sources:
unhealthy, 66.5 years (range: 25-86 years)
n = 7
Health Status: unhealthy
Age Group: 66.5 years (range: 25-86 years)
Sex: M+F
Population Size: 7
Sources:
Lipase increased 1%
Disc. AE
25 mg 2 times / day steady, oral
Recommended
Dose: 25 mg, 2 times / day
Route: oral
Route: steady
Dose: 25 mg, 2 times / day
Sources: Page: p. 137
unhealthy, 67 years (range: 30 - 90 years)
n = 442
Health Status: unhealthy
Condition: Hematologic Malignancies
Age Group: 67 years (range: 30 - 90 years)
Sex: M+F
Population Size: 442
Sources: Page: p. 137
Sepsis 1%
Disc. AE
25 mg 2 times / day steady, oral
Recommended
Dose: 25 mg, 2 times / day
Route: oral
Route: steady
Dose: 25 mg, 2 times / day
Sources: Page: p. 137
unhealthy, 67 years (range: 30 - 90 years)
n = 442
Health Status: unhealthy
Condition: Hematologic Malignancies
Age Group: 67 years (range: 30 - 90 years)
Sex: M+F
Population Size: 442
Sources: Page: p. 137
Transaminases increased 1%
Disc. AE
25 mg 2 times / day steady, oral
Recommended
Dose: 25 mg, 2 times / day
Route: oral
Route: steady
Dose: 25 mg, 2 times / day
Sources: Page: p. 137
unhealthy, 67 years (range: 30 - 90 years)
n = 442
Health Status: unhealthy
Condition: Hematologic Malignancies
Age Group: 67 years (range: 30 - 90 years)
Sex: M+F
Population Size: 442
Sources: Page: p. 137
Pneumonia 10%
Disc. AE
25 mg 2 times / day steady, oral
Recommended
Dose: 25 mg, 2 times / day
Route: oral
Route: steady
Dose: 25 mg, 2 times / day
Sources: Page: p. 137
unhealthy, 67 years (range: 30 - 90 years)
n = 442
Health Status: unhealthy
Condition: Hematologic Malignancies
Age Group: 67 years (range: 30 - 90 years)
Sex: M+F
Population Size: 442
Sources: Page: p. 137
Colitis 19%
Disc. AE
25 mg 2 times / day steady, oral
Recommended
Dose: 25 mg, 2 times / day
Route: oral
Route: steady
Dose: 25 mg, 2 times / day
Sources: Page: p. 137
unhealthy, 67 years (range: 30 - 90 years)
n = 442
Health Status: unhealthy
Condition: Hematologic Malignancies
Age Group: 67 years (range: 30 - 90 years)
Sex: M+F
Population Size: 442
Sources: Page: p. 137
Diarrhea 19%
Disc. AE
25 mg 2 times / day steady, oral
Recommended
Dose: 25 mg, 2 times / day
Route: oral
Route: steady
Dose: 25 mg, 2 times / day
Sources: Page: p. 137
unhealthy, 67 years (range: 30 - 90 years)
n = 442
Health Status: unhealthy
Condition: Hematologic Malignancies
Age Group: 67 years (range: 30 - 90 years)
Sex: M+F
Population Size: 442
Sources: Page: p. 137
Febrile neutropenia 2%
Disc. AE
25 mg 2 times / day steady, oral
Recommended
Dose: 25 mg, 2 times / day
Route: oral
Route: steady
Dose: 25 mg, 2 times / day
Sources: Page: p. 137
unhealthy, 67 years (range: 30 - 90 years)
n = 442
Health Status: unhealthy
Condition: Hematologic Malignancies
Age Group: 67 years (range: 30 - 90 years)
Sex: M+F
Population Size: 442
Sources: Page: p. 137
Anemia 3%
Disc. AE
25 mg 2 times / day steady, oral
Recommended
Dose: 25 mg, 2 times / day
Route: oral
Route: steady
Dose: 25 mg, 2 times / day
Sources: Page: p. 137
unhealthy, 67 years (range: 30 - 90 years)
n = 442
Health Status: unhealthy
Condition: Hematologic Malignancies
Age Group: 67 years (range: 30 - 90 years)
Sex: M+F
Population Size: 442
Sources: Page: p. 137
Febrile neutropenia 3%
Disc. AE
25 mg 2 times / day steady, oral
Recommended
Dose: 25 mg, 2 times / day
Route: oral
Route: steady
Dose: 25 mg, 2 times / day
Sources: Page: p. 137
unhealthy, 67 years (range: 30 - 90 years)
n = 442
Health Status: unhealthy
Condition: Hematologic Malignancies
Age Group: 67 years (range: 30 - 90 years)
Sex: M+F
Population Size: 442
Sources: Page: p. 137
Lipase increased 3%
Disc. AE
25 mg 2 times / day steady, oral
Recommended
Dose: 25 mg, 2 times / day
Route: oral
Route: steady
Dose: 25 mg, 2 times / day
Sources: Page: p. 137
unhealthy, 67 years (range: 30 - 90 years)
n = 442
Health Status: unhealthy
Condition: Hematologic Malignancies
Age Group: 67 years (range: 30 - 90 years)
Sex: M+F
Population Size: 442
Sources: Page: p. 137
Neutropenia 3%
Disc. AE
25 mg 2 times / day steady, oral
Recommended
Dose: 25 mg, 2 times / day
Route: oral
Route: steady
Dose: 25 mg, 2 times / day
Sources: Page: p. 137
unhealthy, 67 years (range: 30 - 90 years)
n = 442
Health Status: unhealthy
Condition: Hematologic Malignancies
Age Group: 67 years (range: 30 - 90 years)
Sex: M+F
Population Size: 442
Sources: Page: p. 137
Thrombocytopenia 3%
Disc. AE
25 mg 2 times / day steady, oral
Recommended
Dose: 25 mg, 2 times / day
Route: oral
Route: steady
Dose: 25 mg, 2 times / day
Sources: Page: p. 137
unhealthy, 67 years (range: 30 - 90 years)
n = 442
Health Status: unhealthy
Condition: Hematologic Malignancies
Age Group: 67 years (range: 30 - 90 years)
Sex: M+F
Population Size: 442
Sources: Page: p. 137
Pyrexia 4%
Disc. AE
25 mg 2 times / day steady, oral
Recommended
Dose: 25 mg, 2 times / day
Route: oral
Route: steady
Dose: 25 mg, 2 times / day
Sources: Page: p. 137
unhealthy, 67 years (range: 30 - 90 years)
n = 442
Health Status: unhealthy
Condition: Hematologic Malignancies
Age Group: 67 years (range: 30 - 90 years)
Sex: M+F
Population Size: 442
Sources: Page: p. 137
Transaminases increased 4%
Disc. AE
25 mg 2 times / day steady, oral
Recommended
Dose: 25 mg, 2 times / day
Route: oral
Route: steady
Dose: 25 mg, 2 times / day
Sources: Page: p. 137
unhealthy, 67 years (range: 30 - 90 years)
n = 442
Health Status: unhealthy
Condition: Hematologic Malignancies
Age Group: 67 years (range: 30 - 90 years)
Sex: M+F
Population Size: 442
Sources: Page: p. 137
Transaminases increased 6%
Disc. AE
25 mg 2 times / day steady, oral
Recommended
Dose: 25 mg, 2 times / day
Route: oral
Route: steady
Dose: 25 mg, 2 times / day
Sources: Page: p. 137
unhealthy, 67 years (range: 30 - 90 years)
n = 442
Health Status: unhealthy
Condition: Hematologic Malignancies
Age Group: 67 years (range: 30 - 90 years)
Sex: M+F
Population Size: 442
Sources: Page: p. 137
Neutropenia 8%
Disc. AE
25 mg 2 times / day steady, oral
Recommended
Dose: 25 mg, 2 times / day
Route: oral
Route: steady
Dose: 25 mg, 2 times / day
Sources: Page: p. 137
unhealthy, 67 years (range: 30 - 90 years)
n = 442
Health Status: unhealthy
Condition: Hematologic Malignancies
Age Group: 67 years (range: 30 - 90 years)
Sex: M+F
Population Size: 442
Sources: Page: p. 137
Rash 8%
Disc. AE
25 mg 2 times / day steady, oral
Recommended
Dose: 25 mg, 2 times / day
Route: oral
Route: steady
Dose: 25 mg, 2 times / day
Sources: Page: p. 137
unhealthy, 67 years (range: 30 - 90 years)
n = 442
Health Status: unhealthy
Condition: Hematologic Malignancies
Age Group: 67 years (range: 30 - 90 years)
Sex: M+F
Population Size: 442
Sources: Page: p. 137
Colitis 29%
Disc. AE
25 mg 2 times / day steady, oral
Recommended
Dose: 25 mg, 2 times / day
Route: oral
Route: steady
Dose: 25 mg, 2 times / day
Sources:
unhealthy, 69 years (range: 39 - 90 years
n = 158
Health Status: unhealthy
Condition: CLL or SLL
Age Group: 69 years (range: 39 - 90 years
Sex: M+F
Population Size: 158
Sources:
Diarrhea 29%
Disc. AE
25 mg 2 times / day steady, oral
Recommended
Dose: 25 mg, 2 times / day
Route: oral
Route: steady
Dose: 25 mg, 2 times / day
Sources:
unhealthy, 69 years (range: 39 - 90 years
n = 158
Health Status: unhealthy
Condition: CLL or SLL
Age Group: 69 years (range: 39 - 90 years
Sex: M+F
Population Size: 158
Sources:
Rash 29%
Disc. AE
25 mg 2 times / day steady, oral
Recommended
Dose: 25 mg, 2 times / day
Route: oral
Route: steady
Dose: 25 mg, 2 times / day
Sources:
unhealthy, 69 years (range: 39 - 90 years
n = 158
Health Status: unhealthy
Condition: CLL or SLL
Age Group: 69 years (range: 39 - 90 years
Sex: M+F
Population Size: 158
Sources:
Colitis 36%
Disc. AE
25 mg 2 times / day steady, oral
Recommended
Dose: 25 mg, 2 times / day
Route: oral
Route: steady
Dose: 25 mg, 2 times / day
Sources:
unhealthy, 69 years (range: 39 - 90 years
n = 158
Health Status: unhealthy
Condition: CLL or SLL
Age Group: 69 years (range: 39 - 90 years
Sex: M+F
Population Size: 158
Sources:
Diarrhea 36%
Disc. AE
25 mg 2 times / day steady, oral
Recommended
Dose: 25 mg, 2 times / day
Route: oral
Route: steady
Dose: 25 mg, 2 times / day
Sources:
unhealthy, 69 years (range: 39 - 90 years
n = 158
Health Status: unhealthy
Condition: CLL or SLL
Age Group: 69 years (range: 39 - 90 years
Sex: M+F
Population Size: 158
Sources:
Infection 36%
Disc. AE
25 mg 2 times / day steady, oral
Recommended
Dose: 25 mg, 2 times / day
Route: oral
Route: steady
Dose: 25 mg, 2 times / day
Sources:
unhealthy, 69 years (range: 39 - 90 years
n = 158
Health Status: unhealthy
Condition: CLL or SLL
Age Group: 69 years (range: 39 - 90 years
Sex: M+F
Population Size: 158
Sources:
Rash 36%
Disc. AE
25 mg 2 times / day steady, oral
Recommended
Dose: 25 mg, 2 times / day
Route: oral
Route: steady
Dose: 25 mg, 2 times / day
Sources:
unhealthy, 69 years (range: 39 - 90 years
n = 158
Health Status: unhealthy
Condition: CLL or SLL
Age Group: 69 years (range: 39 - 90 years
Sex: M+F
Population Size: 158
Sources:
Chills grade 1-2, 13.3%
75 mg 2 times / day steady, oral
MTD
Dose: 75 mg, 2 times / day
Route: oral
Route: steady
Dose: 75 mg, 2 times / day
Sources:
unhealthy, 70 years (range: 42-78)
n = 15
Health Status: unhealthy
Age Group: 70 years (range: 42-78)
Sex: M+F
Population Size: 15
Sources:
Thrombocytopenia grade 1-2, 13.3%
75 mg 2 times / day steady, oral
MTD
Dose: 75 mg, 2 times / day
Route: oral
Route: steady
Dose: 75 mg, 2 times / day
Sources:
unhealthy, 70 years (range: 42-78)
n = 15
Health Status: unhealthy
Age Group: 70 years (range: 42-78)
Sex: M+F
Population Size: 15
Sources:
Upper respiratory tract infection grade 1-2, 13.3%
75 mg 2 times / day steady, oral
MTD
Dose: 75 mg, 2 times / day
Route: oral
Route: steady
Dose: 75 mg, 2 times / day
Sources:
unhealthy, 70 years (range: 42-78)
n = 15
Health Status: unhealthy
Age Group: 70 years (range: 42-78)
Sex: M+F
Population Size: 15
Sources:
Oropharyngeal pain grade 1-2, 20%
75 mg 2 times / day steady, oral
MTD
Dose: 75 mg, 2 times / day
Route: oral
Route: steady
Dose: 75 mg, 2 times / day
Sources:
unhealthy, 70 years (range: 42-78)
n = 15
Health Status: unhealthy
Age Group: 70 years (range: 42-78)
Sex: M+F
Population Size: 15
Sources:
Decreased appetite grade 1-2, 26.7%
75 mg 2 times / day steady, oral
MTD
Dose: 75 mg, 2 times / day
Route: oral
Route: steady
Dose: 75 mg, 2 times / day
Sources:
unhealthy, 70 years (range: 42-78)
n = 15
Health Status: unhealthy
Age Group: 70 years (range: 42-78)
Sex: M+F
Population Size: 15
Sources:
Edema peripheral grade 1-2, 26.7%
75 mg 2 times / day steady, oral
MTD
Dose: 75 mg, 2 times / day
Route: oral
Route: steady
Dose: 75 mg, 2 times / day
Sources:
unhealthy, 70 years (range: 42-78)
n = 15
Health Status: unhealthy
Age Group: 70 years (range: 42-78)
Sex: M+F
Population Size: 15
Sources:
Headache grade 1-2, 26.7%
75 mg 2 times / day steady, oral
MTD
Dose: 75 mg, 2 times / day
Route: oral
Route: steady
Dose: 75 mg, 2 times / day
Sources:
unhealthy, 70 years (range: 42-78)
n = 15
Health Status: unhealthy
Age Group: 70 years (range: 42-78)
Sex: M+F
Population Size: 15
Sources:
Myalgia grade 1-2, 26.7%
75 mg 2 times / day steady, oral
MTD
Dose: 75 mg, 2 times / day
Route: oral
Route: steady
Dose: 75 mg, 2 times / day
Sources:
unhealthy, 70 years (range: 42-78)
n = 15
Health Status: unhealthy
Age Group: 70 years (range: 42-78)
Sex: M+F
Population Size: 15
Sources:
Rash grade 1-2, 26.7%
75 mg 2 times / day steady, oral
MTD
Dose: 75 mg, 2 times / day
Route: oral
Route: steady
Dose: 75 mg, 2 times / day
Sources:
unhealthy, 70 years (range: 42-78)
n = 15
Health Status: unhealthy
Age Group: 70 years (range: 42-78)
Sex: M+F
Population Size: 15
Sources:
Stomatitis grade 1-2, 26.7%
75 mg 2 times / day steady, oral
MTD
Dose: 75 mg, 2 times / day
Route: oral
Route: steady
Dose: 75 mg, 2 times / day
Sources:
unhealthy, 70 years (range: 42-78)
n = 15
Health Status: unhealthy
Age Group: 70 years (range: 42-78)
Sex: M+F
Population Size: 15
Sources:
Dyspnoea grade 1-2, 40%
75 mg 2 times / day steady, oral
MTD
Dose: 75 mg, 2 times / day
Route: oral
Route: steady
Dose: 75 mg, 2 times / day
Sources:
unhealthy, 70 years (range: 42-78)
n = 15
Health Status: unhealthy
Age Group: 70 years (range: 42-78)
Sex: M+F
Population Size: 15
Sources:
Cough grade 1-2, 46.7%
75 mg 2 times / day steady, oral
MTD
Dose: 75 mg, 2 times / day
Route: oral
Route: steady
Dose: 75 mg, 2 times / day
Sources:
unhealthy, 70 years (range: 42-78)
n = 15
Health Status: unhealthy
Age Group: 70 years (range: 42-78)
Sex: M+F
Population Size: 15
Sources:
Fatigue grade 1-2, 46.7%
75 mg 2 times / day steady, oral
MTD
Dose: 75 mg, 2 times / day
Route: oral
Route: steady
Dose: 75 mg, 2 times / day
Sources:
unhealthy, 70 years (range: 42-78)
n = 15
Health Status: unhealthy
Age Group: 70 years (range: 42-78)
Sex: M+F
Population Size: 15
Sources:
Vomiting grade 1-2, 6.7%
75 mg 2 times / day steady, oral
MTD
Dose: 75 mg, 2 times / day
Route: oral
Route: steady
Dose: 75 mg, 2 times / day
Sources:
unhealthy, 70 years (range: 42-78)
n = 15
Health Status: unhealthy
Age Group: 70 years (range: 42-78)
Sex: M+F
Population Size: 15
Sources:
Anemia grade 3, 13.3%
75 mg 2 times / day steady, oral
MTD
Dose: 75 mg, 2 times / day
Route: oral
Route: steady
Dose: 75 mg, 2 times / day
Sources:
unhealthy, 70 years (range: 42-78)
n = 15
Health Status: unhealthy
Age Group: 70 years (range: 42-78)
Sex: M+F
Population Size: 15
Sources:
Rash maculo-papular grade 3, 13.3%
75 mg 2 times / day steady, oral
MTD
Dose: 75 mg, 2 times / day
Route: oral
Route: steady
Dose: 75 mg, 2 times / day
Sources:
unhealthy, 70 years (range: 42-78)
n = 15
Health Status: unhealthy
Age Group: 70 years (range: 42-78)
Sex: M+F
Population Size: 15
Sources:
Diarrhea grade 3, 33.3%
75 mg 2 times / day steady, oral
MTD
Dose: 75 mg, 2 times / day
Route: oral
Route: steady
Dose: 75 mg, 2 times / day
Sources:
unhealthy, 70 years (range: 42-78)
n = 15
Health Status: unhealthy
Age Group: 70 years (range: 42-78)
Sex: M+F
Population Size: 15
Sources:
Nausea grade 3, 6.7%
75 mg 2 times / day steady, oral
MTD
Dose: 75 mg, 2 times / day
Route: oral
Route: steady
Dose: 75 mg, 2 times / day
Sources:
unhealthy, 70 years (range: 42-78)
n = 15
Health Status: unhealthy
Age Group: 70 years (range: 42-78)
Sex: M+F
Population Size: 15
Sources:
Pyrexia grade 3, 6.7%
75 mg 2 times / day steady, oral
MTD
Dose: 75 mg, 2 times / day
Route: oral
Route: steady
Dose: 75 mg, 2 times / day
Sources:
unhealthy, 70 years (range: 42-78)
n = 15
Health Status: unhealthy
Age Group: 70 years (range: 42-78)
Sex: M+F
Population Size: 15
Sources:
AST increased grade 3-4, 13.3%
75 mg 2 times / day steady, oral
MTD
Dose: 75 mg, 2 times / day
Route: oral
Route: steady
Dose: 75 mg, 2 times / day
Sources:
unhealthy, 70 years (range: 42-78)
n = 15
Health Status: unhealthy
Age Group: 70 years (range: 42-78)
Sex: M+F
Population Size: 15
Sources:
Neutropenia grade 3-4, 33.3%
75 mg 2 times / day steady, oral
MTD
Dose: 75 mg, 2 times / day
Route: oral
Route: steady
Dose: 75 mg, 2 times / day
Sources:
unhealthy, 70 years (range: 42-78)
n = 15
Health Status: unhealthy
Age Group: 70 years (range: 42-78)
Sex: M+F
Population Size: 15
Sources:
ALT increased grade 3-4, 40%
75 mg 2 times / day steady, oral
MTD
Dose: 75 mg, 2 times / day
Route: oral
Route: steady
Dose: 75 mg, 2 times / day
Sources:
unhealthy, 70 years (range: 42-78)
n = 15
Health Status: unhealthy
Age Group: 70 years (range: 42-78)
Sex: M+F
Population Size: 15
Sources:
Colitis grade 5|serious, 18%
25 mg 2 times / day steady, oral
Recommended
Dose: 25 mg, 2 times / day
Route: oral
Route: steady
Dose: 25 mg, 2 times / day
Sources:
unhealthy
Diarrhea grade 5|serious, 18%
25 mg 2 times / day steady, oral
Recommended
Dose: 25 mg, 2 times / day
Route: oral
Route: steady
Dose: 25 mg, 2 times / day
Sources:
unhealthy
Infection grade 5|serious, 31%
25 mg 2 times / day steady, oral
Recommended
Dose: 25 mg, 2 times / day
Route: oral
Route: steady
Dose: 25 mg, 2 times / day
Sources:
unhealthy
Epidermal and dermal conditions grade 5|serious, 5%
25 mg 2 times / day steady, oral
Recommended
Dose: 25 mg, 2 times / day
Route: oral
Route: steady
Dose: 25 mg, 2 times / day
Sources:
unhealthy
Pneumonitis grade 5|serious, 5%
25 mg 2 times / day steady, oral
Recommended
Dose: 25 mg, 2 times / day
Route: oral
Route: steady
Dose: 25 mg, 2 times / day
Sources:
unhealthy
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
no
no
no
no
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes (co-administration study)
Comment: In a dedicated drug-interaction trial in healthy subjects, midazolam (a CYP3A4 substrate) single dose Cmax and AUC were increased by 120% and 330% respectively, when co-administered with duvelisib (
Page: 64.0
yes
yes (co-administration study)
Comment: In a dedicated drug-interaction trial in healthy subjects, midazolam (a CYP3A4 substrate) single dose Cmax and AUC were increased by 120% and 330% respectively, when co-administered with duvelisib (
Page: 64.0
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
no
yes
yes
yes
yes (co-administration study)
Comment: In a dedicated drug-interaction trial in healthy subjects (N=16), concomitant ketoconazole (a strong CYP3A4 inhibitor and P-gp inhibitor) increased duvelisib Cmax and AUC by 66% and 295% respectively
Page: 39.0
Tox targets
Sourcing

Sourcing

Vendor/AggregatorIDURL
PubMed

PubMed

TitleDatePubMed
PI3-kinase inhibitors in chronic lymphocytic leukemia.
2014 Mar
Patents

Sample Use Guides

25-75 mg twice daily for five to 28 days
Route of Administration: Oral
0.25 to 5 uM IPI-145 exhibited concentration- and time-dependent induction of cytotoxicity in primary chronic lymphocytic leukemia cells
Name Type Language
DUVELISIB MONOHYDRATE
Common Name English
DUVELISIB HYDRATE [MI]
Common Name English
DUVELISIB HYDRATE
Common Name English
COPIKTRA
Brand Name English
Duvelisib monohydrate [WHO-DD]
Common Name English
1(2H)-ISOQUINOLINONE, 8-CHLORO-2-PHENYL-3-((1S)-1-(9H-PURIN-6-YLAMINO)ETHYL)-, HYDRATE
Systematic Name English
1(2H)-ISOQUINOLINONE, 8-CHLORO-2-PHENYL-3-((1S)-1-(9H-PURIN-6-YLAMINO)ETHYL)-, HYDRATE (1:1)
Systematic Name English
DUVELISIB HYDRATE [JAN]
Common Name English
Code System Code Type Description
FDA UNII
4WD61MR063
Created by admin on Sat Dec 16 14:24:27 GMT 2023 , Edited by admin on Sat Dec 16 14:24:27 GMT 2023
PRIMARY
SMS_ID
300000046370
Created by admin on Sat Dec 16 14:24:27 GMT 2023 , Edited by admin on Sat Dec 16 14:24:27 GMT 2023
PRIMARY
CAS
1386861-49-9
Created by admin on Sat Dec 16 14:24:27 GMT 2023 , Edited by admin on Sat Dec 16 14:24:27 GMT 2023
NON-SPECIFIC STOICHIOMETRY
MERCK INDEX
m12094
Created by admin on Sat Dec 16 14:24:27 GMT 2023 , Edited by admin on Sat Dec 16 14:24:27 GMT 2023
PRIMARY
PUBCHEM
137528190
Created by admin on Sat Dec 16 14:24:27 GMT 2023 , Edited by admin on Sat Dec 16 14:24:27 GMT 2023
PRIMARY