U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ABSOLUTE
Molecular Formula C22H17ClN6O
Molecular Weight 416.863
Optical Activity UNSPECIFIED
Defined Stereocenters 1 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of DUVELISIB

SMILES

C[C@H](NC1=NC=NC2=C1N=CN2)C3=CC4=C(C(Cl)=CC=C4)C(=O)N3C5=CC=CC=C5

InChI

InChIKey=SJVQHLPISAIATJ-ZDUSSCGKSA-N
InChI=1S/C22H17ClN6O/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)/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
1.5 μg/mL
25 mg 2 times / day steady-state, oral
dose: 25 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
DUVELISIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
1062 ng/mL
25 mg 2 times / day multiple, oral
dose: 25 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
DUVELISIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
7.9 μg × h/mL
25 mg 2 times / day steady-state, oral
dose: 25 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
DUVELISIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
7098.4 ng × h/mL
25 mg 2 times / day multiple, oral
dose: 25 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
DUVELISIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
4.7 h
25 mg 2 times / day steady-state, oral
dose: 25 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
DUVELISIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
6.8 h
25 mg 2 times / day multiple, oral
dose: 25 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
DUVELISIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
2%
25 mg 2 times / day steady-state, oral
dose: 25 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
DUVELISIB plasma
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)
Health Status: unhealthy
Age Group: 66.5 years (range: 25-86 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 66.5 years (range: 25-86 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 66.5 years (range: 25-86 years)
Sex: M+F
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:
unhealthy, 67 years (range: 30 - 90 years)
Health Status: unhealthy
Age Group: 67 years (range: 30 - 90 years)
Sex: M+F
Sources:
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:
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
Health Status: unhealthy
Age Group: 69 years (range: 39 - 90 years
Sex: M+F
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)
Health Status: unhealthy
Age Group: 70 years (range: 42-78)
Sex: M+F
Sources:
Other AEs: Neutropenia, ALT increased...
Other AEs:
Neutropenia (grade 3-4, 33.3%)
ALT increased (grade 3-4, 40%)
AST increased (grade 3-4, 13.3%)
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)
Health Status: unhealthy
Age Group: 66.5 years (range: 25-86 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 66.5 years (range: 25-86 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 66.5 years (range: 25-86 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 66.5 years (range: 25-86 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 66.5 years (range: 25-86 years)
Sex: M+F
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:
unhealthy, 67 years (range: 30 - 90 years)
Health Status: unhealthy
Age Group: 67 years (range: 30 - 90 years)
Sex: M+F
Sources:
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:
unhealthy, 67 years (range: 30 - 90 years)
Health Status: unhealthy
Age Group: 67 years (range: 30 - 90 years)
Sex: M+F
Sources:
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:
unhealthy, 67 years (range: 30 - 90 years)
Health Status: unhealthy
Age Group: 67 years (range: 30 - 90 years)
Sex: M+F
Sources:
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:
unhealthy, 67 years (range: 30 - 90 years)
Health Status: unhealthy
Age Group: 67 years (range: 30 - 90 years)
Sex: M+F
Sources:
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:
unhealthy, 67 years (range: 30 - 90 years)
Health Status: unhealthy
Age Group: 67 years (range: 30 - 90 years)
Sex: M+F
Sources:
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:
unhealthy, 67 years (range: 30 - 90 years)
Health Status: unhealthy
Age Group: 67 years (range: 30 - 90 years)
Sex: M+F
Sources:
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:
unhealthy, 67 years (range: 30 - 90 years)
Health Status: unhealthy
Age Group: 67 years (range: 30 - 90 years)
Sex: M+F
Sources:
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:
unhealthy, 67 years (range: 30 - 90 years)
Health Status: unhealthy
Age Group: 67 years (range: 30 - 90 years)
Sex: M+F
Sources:
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:
unhealthy, 67 years (range: 30 - 90 years)
Health Status: unhealthy
Age Group: 67 years (range: 30 - 90 years)
Sex: M+F
Sources:
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:
unhealthy, 67 years (range: 30 - 90 years)
Health Status: unhealthy
Age Group: 67 years (range: 30 - 90 years)
Sex: M+F
Sources:
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:
unhealthy, 67 years (range: 30 - 90 years)
Health Status: unhealthy
Age Group: 67 years (range: 30 - 90 years)
Sex: M+F
Sources:
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:
unhealthy, 67 years (range: 30 - 90 years)
Health Status: unhealthy
Age Group: 67 years (range: 30 - 90 years)
Sex: M+F
Sources:
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:
unhealthy, 67 years (range: 30 - 90 years)
Health Status: unhealthy
Age Group: 67 years (range: 30 - 90 years)
Sex: M+F
Sources:
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:
unhealthy, 67 years (range: 30 - 90 years)
Health Status: unhealthy
Age Group: 67 years (range: 30 - 90 years)
Sex: M+F
Sources:
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:
unhealthy, 67 years (range: 30 - 90 years)
Health Status: unhealthy
Age Group: 67 years (range: 30 - 90 years)
Sex: M+F
Sources:
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:
unhealthy, 67 years (range: 30 - 90 years)
Health Status: unhealthy
Age Group: 67 years (range: 30 - 90 years)
Sex: M+F
Sources:
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:
unhealthy, 67 years (range: 30 - 90 years)
Health Status: unhealthy
Age Group: 67 years (range: 30 - 90 years)
Sex: M+F
Sources:
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
Health Status: unhealthy
Age Group: 69 years (range: 39 - 90 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 69 years (range: 39 - 90 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 69 years (range: 39 - 90 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 69 years (range: 39 - 90 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 69 years (range: 39 - 90 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 69 years (range: 39 - 90 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 69 years (range: 39 - 90 years
Sex: M+F
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)
Health Status: unhealthy
Age Group: 70 years (range: 42-78)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 70 years (range: 42-78)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 70 years (range: 42-78)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 70 years (range: 42-78)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 70 years (range: 42-78)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 70 years (range: 42-78)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 70 years (range: 42-78)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 70 years (range: 42-78)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 70 years (range: 42-78)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 70 years (range: 42-78)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 70 years (range: 42-78)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 70 years (range: 42-78)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 70 years (range: 42-78)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 70 years (range: 42-78)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 70 years (range: 42-78)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 70 years (range: 42-78)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 70 years (range: 42-78)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 70 years (range: 42-78)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 70 years (range: 42-78)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 70 years (range: 42-78)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 70 years (range: 42-78)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 70 years (range: 42-78)
Sex: M+F
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
Targeting PI3Kδ and PI3Kγ signalling disrupts human AML survival and bone marrow stromal cell mediated protection.
2016-06-28
The phosphoinositide-3-kinase (PI3K)-delta and gamma inhibitor, IPI-145 (Duvelisib), overcomes signals from the PI3K/AKT/S6 pathway and promotes apoptosis in CLL.
2015-09
IPI-145 antagonizes intrinsic and extrinsic survival signals in chronic lymphocytic leukemia cells.
2014-12-04
PI3-kinase inhibitors in chronic lymphocytic leukemia.
2014-03
Novel phosphoinositide 3-kinase δ,γ inhibitor: potent anti-inflammatory effects and joint protection in models of rheumatoid arthritis.
2014-02
IPI-145 shows promise in CLL patients.
2014-02
PI3K-δ and PI3K-γ inhibition by IPI-145 abrogates immune responses and suppresses activity in autoimmune and inflammatory disease models.
2013-11-21
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 [INN]
Preferred Name English
DUVELISIB
INN   USAN   WHO-DD  
INN   USAN  
Official Name English
1(2H)-ISOQUINOLINONE, 8-CHLORO-2-PHENYL-3-((1S)-1-(9H-PURIN-6-YLAMINO)ETHYL)-
Systematic Name English
IPI-145
Code English
Duvelisib [WHO-DD]
Common Name English
(S)-3-(1-(9H-PURIN-6-YLAMINO)ETHYL)-8-CHLORO-2-PHENYLISOQUINOLIN-1(2H)-ONE
Systematic Name English
DUVELISIB [MI]
Common Name English
INK-1197
Code English
DUVELISIB [ORANGE BOOK]
Common Name English
DUVELISIB [USAN]
Common Name English
INK-1147
Code English
Classification Tree Code System Code
NCI_THESAURUS C2152
Created by admin on Mon Mar 31 20:58:20 GMT 2025 , Edited by admin on Mon Mar 31 20:58:20 GMT 2025
FDA ORPHAN DRUG 703019
Created by admin on Mon Mar 31 20:58:20 GMT 2025 , Edited by admin on Mon Mar 31 20:58:20 GMT 2025
FDA ORPHAN DRUG 399913
Created by admin on Mon Mar 31 20:58:20 GMT 2025 , Edited by admin on Mon Mar 31 20:58:20 GMT 2025
NCI_THESAURUS C129825
Created by admin on Mon Mar 31 20:58:20 GMT 2025 , Edited by admin on Mon Mar 31 20:58:20 GMT 2025
FDA ORPHAN DRUG 394413
Created by admin on Mon Mar 31 20:58:20 GMT 2025 , Edited by admin on Mon Mar 31 20:58:20 GMT 2025
EU-Orphan Drug EU/3/13/1125
Created by admin on Mon Mar 31 20:58:20 GMT 2025 , Edited by admin on Mon Mar 31 20:58:20 GMT 2025
Code System Code Type Description
DRUG BANK
DB11952
Created by admin on Mon Mar 31 20:58:20 GMT 2025 , Edited by admin on Mon Mar 31 20:58:20 GMT 2025
PRIMARY
PUBCHEM
50905713
Created by admin on Mon Mar 31 20:58:20 GMT 2025 , Edited by admin on Mon Mar 31 20:58:20 GMT 2025
PRIMARY
ChEMBL
CHEMBL3039502
Created by admin on Mon Mar 31 20:58:20 GMT 2025 , Edited by admin on Mon Mar 31 20:58:20 GMT 2025
PRIMARY
NCI_THESAURUS
C99225
Created by admin on Mon Mar 31 20:58:20 GMT 2025 , Edited by admin on Mon Mar 31 20:58:20 GMT 2025
PRIMARY
RXCUI
2058509
Created by admin on Mon Mar 31 20:58:20 GMT 2025 , Edited by admin on Mon Mar 31 20:58:20 GMT 2025
PRIMARY
MERCK INDEX
m12094
Created by admin on Mon Mar 31 20:58:20 GMT 2025 , Edited by admin on Mon Mar 31 20:58:20 GMT 2025
PRIMARY
USAN
AB-61
Created by admin on Mon Mar 31 20:58:20 GMT 2025 , Edited by admin on Mon Mar 31 20:58:20 GMT 2025
PRIMARY
DRUG CENTRAL
5296
Created by admin on Mon Mar 31 20:58:20 GMT 2025 , Edited by admin on Mon Mar 31 20:58:20 GMT 2025
PRIMARY
INN
9856
Created by admin on Mon Mar 31 20:58:20 GMT 2025 , Edited by admin on Mon Mar 31 20:58:20 GMT 2025
PRIMARY
DAILYMED
610V23S0JI
Created by admin on Mon Mar 31 20:58:20 GMT 2025 , Edited by admin on Mon Mar 31 20:58:20 GMT 2025
PRIMARY
WIKIPEDIA
Duvelisib
Created by admin on Mon Mar 31 20:58:20 GMT 2025 , Edited by admin on Mon Mar 31 20:58:20 GMT 2025
PRIMARY
LACTMED
Duvelisib
Created by admin on Mon Mar 31 20:58:20 GMT 2025 , Edited by admin on Mon Mar 31 20:58:20 GMT 2025
PRIMARY
EPA CompTox
DTXSID80152697
Created by admin on Mon Mar 31 20:58:20 GMT 2025 , Edited by admin on Mon Mar 31 20:58:20 GMT 2025
PRIMARY
CAS
1201438-56-3
Created by admin on Mon Mar 31 20:58:20 GMT 2025 , Edited by admin on Mon Mar 31 20:58:20 GMT 2025
PRIMARY
SMS_ID
100000166112
Created by admin on Mon Mar 31 20:58:20 GMT 2025 , Edited by admin on Mon Mar 31 20:58:20 GMT 2025
PRIMARY
FDA UNII
610V23S0JI
Created by admin on Mon Mar 31 20:58:20 GMT 2025 , Edited by admin on Mon Mar 31 20:58:20 GMT 2025
PRIMARY
EVMPD
SUB180102
Created by admin on Mon Mar 31 20:58:20 GMT 2025 , Edited by admin on Mon Mar 31 20:58:20 GMT 2025
PRIMARY