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This repository is under review for potential modification in compliance with Administration directives.

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=NC=NC2=C1N=CN2)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

Molecular Formula H2O
Molecular Weight 18.0153
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Molecular Formula C22H17ClN6O
Molecular Weight 416.863
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 1 / 1
E/Z Centers 0
Optical Activity UNSPECIFIED

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
PI3K-δ and PI3K-γ inhibition by IPI-145 abrogates immune responses and suppresses activity in autoimmune and inflammatory disease models.
2013 Nov 21
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 Sep
Targeting PI3Kδ and PI3Kγ signalling disrupts human AML survival and bone marrow stromal cell mediated protection.
2016 Jun 28
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
Substance Class Chemical
Created
by admin
on Tue Apr 01 23:32:37 GMT 2025
Edited
by admin
on Tue Apr 01 23:32:37 GMT 2025
Record UNII
4WD61MR063
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
DUVELISIB MONOHYDRATE
Common Name English
1(2H)-ISOQUINOLINONE, 8-CHLORO-2-PHENYL-3-((1S)-1-(9H-PURIN-6-YLAMINO)ETHYL)-, HYDRATE
Preferred 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 (1:1)
Systematic Name English
DUVELISIB HYDRATE [JAN]
Common Name English
Code System Code Type Description
FDA UNII
4WD61MR063
Created by admin on Tue Apr 01 23:32:37 GMT 2025 , Edited by admin on Tue Apr 01 23:32:37 GMT 2025
PRIMARY
SMS_ID
300000046370
Created by admin on Tue Apr 01 23:32:37 GMT 2025 , Edited by admin on Tue Apr 01 23:32:37 GMT 2025
PRIMARY
CAS
1386861-49-9
Created by admin on Tue Apr 01 23:32:37 GMT 2025 , Edited by admin on Tue Apr 01 23:32:37 GMT 2025
NON-SPECIFIC STOICHIOMETRY
MERCK INDEX
m12094
Created by admin on Tue Apr 01 23:32:37 GMT 2025 , Edited by admin on Tue Apr 01 23:32:37 GMT 2025
PRIMARY
PUBCHEM
137528190
Created by admin on Tue Apr 01 23:32:37 GMT 2025 , Edited by admin on Tue Apr 01 23:32:37 GMT 2025
PRIMARY
Related Record Type Details
PARENT -> SALT/SOLVATE
ANHYDROUS->SOLVATE