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Details

Stereochemistry ABSOLUTE
Molecular Formula C22H18FN7O
Molecular Weight 415.423
Optical Activity UNSPECIFIED
Defined Stereocenters 1 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of IDELALISIB

SMILES

CC[C@H](NC1=C2N=CNC2=NC=N1)C3=NC4=C(C(=O)N3C5=CC=CC=C5)C(F)=CC=C4

InChI

InChIKey=IFSDAJWBUCMOAH-HNNXBMFYSA-N
InChI=1S/C22H18FN7O/c1-2-15(28-20-18-19(25-11-24-18)26-12-27-20)21-29-16-10-6-9-14(23)17(16)22(31)30(21)13-7-4-3-5-8-13/h3-12,15H,2H2,1H3,(H2,24,25,26,27,28)/t15-/m0/s1

HIDE SMILES / InChI

Description
Curator's Comment: description was created based on several sources, including http://link.springer.com/article/10.1007/s40265-014-0285-6

Idelalisib is a first-in-class selective inhibitor of adenosine-5'-triphosphate (ATP) binding to PI3Kdelta kinase, resulting in inhibition of the P13K signalling pathway in malignant B cells. The compound is approved for the treatment of several types of blood cancer. Idelalisib is intended to be used in combination with rituximab as second or subsequent line therapy for the treatment of chronic lymphocytic leukaemia. The drug may cause fatal and/or severe diarrhea or colitis, hepatotoxicity, pneumonitis and intestinal perforation.

CNS Activity

Curator's Comment: Ibrutinib can cross the blood-brain barrier (1–7% of the dose found in cerebral spinal fluid).

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
2.5 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
ZYDELIG

Approved Use

Indicated for the treatment of patients with: 1) relapsed chronic lymphocytic leukemia (CLL), in combination with rituximab, in patients for whom rituximab alone would be considered appropriate therapy due to other co-morbidities; 2) relapsed follicular B-cell non-Hodgkin lymphoma (FL) in patients who have received at least two prior systemic therapies; 3) relapsed small lymphocytic lymphoma (SLL) in patients who have received at least two prior systemic therapies.

Launch Date

2014
Primary
ZYDELIG

Approved Use

Indicated for the treatment of patients with: 1) relapsed chronic lymphocytic leukemia (CLL), in combination with rituximab, in patients for whom rituximab alone would be considered appropriate therapy due to other co-morbidities; 2) relapsed follicular B-cell non-Hodgkin lymphoma (FL) in patients who have received at least two prior systemic therapies; 3) relapsed small lymphocytic lymphoma (SLL) in patients who have received at least two prior systemic therapies.

Launch Date

2014
Primary
ZYDELIG

Approved Use

Indicated for the treatment of patients with: 1) relapsed chronic lymphocytic leukemia (CLL), in combination with rituximab, in patients for whom rituximab alone would be considered appropriate therapy due to other co-morbidities; 2) relapsed follicular B-cell non-Hodgkin lymphoma (FL) in patients who have received at least two prior systemic therapies; 3) relapsed small lymphocytic lymphoma (SLL) in patients who have received at least two prior systemic therapies.

Launch Date

2014
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
1.953 ng/mL
150 mg 2 times / day steady-state, oral
dose: 150 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
IDELALISIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
2647.5 ng/mL
150 mg single, oral
dose: 150 mg
route of administration: oral
experiment type: single
co-administered:
IDELALISIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
2258.8 ng/mL
150 mg 2 times / day multiple, oral
dose: 150 mg
route of administration: oral
experiment type: multiple
co-administered:
IDELALISIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
10.439 ng × h/mL
150 mg 2 times / day steady-state, oral
dose: 150 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
IDELALISIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
9094.76 ng*h/mL
150 mg single, oral
dose: 150 mg
route of administration: oral
experiment type: single
co-administered:
IDELALISIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
9293.39 ng*h/mL
150 mg 2 times / day multiple, oral
dose: 150 mg
route of administration: oral
experiment type: multiple
co-administered:
IDELALISIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
8.2 h
150 mg 2 times / day steady-state, oral
dose: 150 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
IDELALISIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
350 mg 2 times / day multiple, oral
Highest studied dose
Dose: 350 mg, 2 times / day
Route: oral
Route: multiple
Dose: 350 mg, 2 times / day
Sources:
unhealthy, 64 years (range: 32-91 years)
n = 4
Health Status: unhealthy
Condition: non-Hodgkin lymphoma
Age Group: 64 years (range: 32-91 years)
Sex: M+F
Population Size: 4
Sources:
Other AEs: Diarrhea, Pneumonia...
Other AEs:
Diarrhea (grade 3, 25%)
Pneumonia (grade 3, 25%)
Edema peripheral (grade 3, 25%)
AST increased (grade 3, 50%)
ALT increased (grade 3, 50%)
Absolute neutrophil count decreased (grade 3, 50%)
Platelets decreased (grade 3, 50%)
Vomiting (all grades, 25%)
Rash (all grades, 25%)
Chills (all grades, 25%)
Fatigue (all grades, 25%)
Constipation (all grades, 25%)
Nausea (all grades, 25%)
Insomnia (all grades, 25%)
Edema peripheral (all grades, 25%)
Arterial pressure NOS increased (all grades, 25%)
Bilirubin increased (all grades, 25%)
Glucose increased (all grades, 25%)
Glucose decreased (all grades, 25%)
Hemoglobin decreased (all grades, 25%)
Pyrexia (all grades, 25%)
Night sweats (all grades, 25%)
Sources:
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
unhealthy, 71 years (range: 47 - 92 years)
n = 110
Health Status: unhealthy
Condition: Relapsed Chronic Lymphocytic Leukemia
Age Group: 71 years (range: 47 - 92 years)
Sex: M+F
Population Size: 110
Sources:
Disc. AE: Hepatotoxicity, Diarrhea...
AEs leading to
discontinuation/dose reduction:
Hepatotoxicity (10%)
Diarrhea (10%)
Colitis (10%)
Transaminases increased (15%)
Diarrhea (15%)
Colitis (15%)
Rash (15%)
Sources:
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sources:
Other AEs: Hepatotoxicity, Diarrhea...
Other AEs:
Hepatotoxicity (serious|grade 5, 14%)
Diarrhea (serious|grade 5, 14%)
Colitis (serious|grade 5, 14%)
Pneumonitis (serious|grade 5)
Sources:
AEs

AEs

AESignificanceDosePopulation
Arterial pressure NOS increased all grades, 25%
350 mg 2 times / day multiple, oral
Highest studied dose
Dose: 350 mg, 2 times / day
Route: oral
Route: multiple
Dose: 350 mg, 2 times / day
Sources:
unhealthy, 64 years (range: 32-91 years)
n = 4
Health Status: unhealthy
Condition: non-Hodgkin lymphoma
Age Group: 64 years (range: 32-91 years)
Sex: M+F
Population Size: 4
Sources:
Bilirubin increased all grades, 25%
350 mg 2 times / day multiple, oral
Highest studied dose
Dose: 350 mg, 2 times / day
Route: oral
Route: multiple
Dose: 350 mg, 2 times / day
Sources:
unhealthy, 64 years (range: 32-91 years)
n = 4
Health Status: unhealthy
Condition: non-Hodgkin lymphoma
Age Group: 64 years (range: 32-91 years)
Sex: M+F
Population Size: 4
Sources:
Chills all grades, 25%
350 mg 2 times / day multiple, oral
Highest studied dose
Dose: 350 mg, 2 times / day
Route: oral
Route: multiple
Dose: 350 mg, 2 times / day
Sources:
unhealthy, 64 years (range: 32-91 years)
n = 4
Health Status: unhealthy
Condition: non-Hodgkin lymphoma
Age Group: 64 years (range: 32-91 years)
Sex: M+F
Population Size: 4
Sources:
Constipation all grades, 25%
350 mg 2 times / day multiple, oral
Highest studied dose
Dose: 350 mg, 2 times / day
Route: oral
Route: multiple
Dose: 350 mg, 2 times / day
Sources:
unhealthy, 64 years (range: 32-91 years)
n = 4
Health Status: unhealthy
Condition: non-Hodgkin lymphoma
Age Group: 64 years (range: 32-91 years)
Sex: M+F
Population Size: 4
Sources:
Edema peripheral all grades, 25%
350 mg 2 times / day multiple, oral
Highest studied dose
Dose: 350 mg, 2 times / day
Route: oral
Route: multiple
Dose: 350 mg, 2 times / day
Sources:
unhealthy, 64 years (range: 32-91 years)
n = 4
Health Status: unhealthy
Condition: non-Hodgkin lymphoma
Age Group: 64 years (range: 32-91 years)
Sex: M+F
Population Size: 4
Sources:
Fatigue all grades, 25%
350 mg 2 times / day multiple, oral
Highest studied dose
Dose: 350 mg, 2 times / day
Route: oral
Route: multiple
Dose: 350 mg, 2 times / day
Sources:
unhealthy, 64 years (range: 32-91 years)
n = 4
Health Status: unhealthy
Condition: non-Hodgkin lymphoma
Age Group: 64 years (range: 32-91 years)
Sex: M+F
Population Size: 4
Sources:
Glucose decreased all grades, 25%
350 mg 2 times / day multiple, oral
Highest studied dose
Dose: 350 mg, 2 times / day
Route: oral
Route: multiple
Dose: 350 mg, 2 times / day
Sources:
unhealthy, 64 years (range: 32-91 years)
n = 4
Health Status: unhealthy
Condition: non-Hodgkin lymphoma
Age Group: 64 years (range: 32-91 years)
Sex: M+F
Population Size: 4
Sources:
Glucose increased all grades, 25%
350 mg 2 times / day multiple, oral
Highest studied dose
Dose: 350 mg, 2 times / day
Route: oral
Route: multiple
Dose: 350 mg, 2 times / day
Sources:
unhealthy, 64 years (range: 32-91 years)
n = 4
Health Status: unhealthy
Condition: non-Hodgkin lymphoma
Age Group: 64 years (range: 32-91 years)
Sex: M+F
Population Size: 4
Sources:
Hemoglobin decreased all grades, 25%
350 mg 2 times / day multiple, oral
Highest studied dose
Dose: 350 mg, 2 times / day
Route: oral
Route: multiple
Dose: 350 mg, 2 times / day
Sources:
unhealthy, 64 years (range: 32-91 years)
n = 4
Health Status: unhealthy
Condition: non-Hodgkin lymphoma
Age Group: 64 years (range: 32-91 years)
Sex: M+F
Population Size: 4
Sources:
Insomnia all grades, 25%
350 mg 2 times / day multiple, oral
Highest studied dose
Dose: 350 mg, 2 times / day
Route: oral
Route: multiple
Dose: 350 mg, 2 times / day
Sources:
unhealthy, 64 years (range: 32-91 years)
n = 4
Health Status: unhealthy
Condition: non-Hodgkin lymphoma
Age Group: 64 years (range: 32-91 years)
Sex: M+F
Population Size: 4
Sources:
Nausea all grades, 25%
350 mg 2 times / day multiple, oral
Highest studied dose
Dose: 350 mg, 2 times / day
Route: oral
Route: multiple
Dose: 350 mg, 2 times / day
Sources:
unhealthy, 64 years (range: 32-91 years)
n = 4
Health Status: unhealthy
Condition: non-Hodgkin lymphoma
Age Group: 64 years (range: 32-91 years)
Sex: M+F
Population Size: 4
Sources:
Night sweats all grades, 25%
350 mg 2 times / day multiple, oral
Highest studied dose
Dose: 350 mg, 2 times / day
Route: oral
Route: multiple
Dose: 350 mg, 2 times / day
Sources:
unhealthy, 64 years (range: 32-91 years)
n = 4
Health Status: unhealthy
Condition: non-Hodgkin lymphoma
Age Group: 64 years (range: 32-91 years)
Sex: M+F
Population Size: 4
Sources:
Pyrexia all grades, 25%
350 mg 2 times / day multiple, oral
Highest studied dose
Dose: 350 mg, 2 times / day
Route: oral
Route: multiple
Dose: 350 mg, 2 times / day
Sources:
unhealthy, 64 years (range: 32-91 years)
n = 4
Health Status: unhealthy
Condition: non-Hodgkin lymphoma
Age Group: 64 years (range: 32-91 years)
Sex: M+F
Population Size: 4
Sources:
Rash all grades, 25%
350 mg 2 times / day multiple, oral
Highest studied dose
Dose: 350 mg, 2 times / day
Route: oral
Route: multiple
Dose: 350 mg, 2 times / day
Sources:
unhealthy, 64 years (range: 32-91 years)
n = 4
Health Status: unhealthy
Condition: non-Hodgkin lymphoma
Age Group: 64 years (range: 32-91 years)
Sex: M+F
Population Size: 4
Sources:
Vomiting all grades, 25%
350 mg 2 times / day multiple, oral
Highest studied dose
Dose: 350 mg, 2 times / day
Route: oral
Route: multiple
Dose: 350 mg, 2 times / day
Sources:
unhealthy, 64 years (range: 32-91 years)
n = 4
Health Status: unhealthy
Condition: non-Hodgkin lymphoma
Age Group: 64 years (range: 32-91 years)
Sex: M+F
Population Size: 4
Sources:
Diarrhea grade 3, 25%
350 mg 2 times / day multiple, oral
Highest studied dose
Dose: 350 mg, 2 times / day
Route: oral
Route: multiple
Dose: 350 mg, 2 times / day
Sources:
unhealthy, 64 years (range: 32-91 years)
n = 4
Health Status: unhealthy
Condition: non-Hodgkin lymphoma
Age Group: 64 years (range: 32-91 years)
Sex: M+F
Population Size: 4
Sources:
Edema peripheral grade 3, 25%
350 mg 2 times / day multiple, oral
Highest studied dose
Dose: 350 mg, 2 times / day
Route: oral
Route: multiple
Dose: 350 mg, 2 times / day
Sources:
unhealthy, 64 years (range: 32-91 years)
n = 4
Health Status: unhealthy
Condition: non-Hodgkin lymphoma
Age Group: 64 years (range: 32-91 years)
Sex: M+F
Population Size: 4
Sources:
Pneumonia grade 3, 25%
350 mg 2 times / day multiple, oral
Highest studied dose
Dose: 350 mg, 2 times / day
Route: oral
Route: multiple
Dose: 350 mg, 2 times / day
Sources:
unhealthy, 64 years (range: 32-91 years)
n = 4
Health Status: unhealthy
Condition: non-Hodgkin lymphoma
Age Group: 64 years (range: 32-91 years)
Sex: M+F
Population Size: 4
Sources:
ALT increased grade 3, 50%
350 mg 2 times / day multiple, oral
Highest studied dose
Dose: 350 mg, 2 times / day
Route: oral
Route: multiple
Dose: 350 mg, 2 times / day
Sources:
unhealthy, 64 years (range: 32-91 years)
n = 4
Health Status: unhealthy
Condition: non-Hodgkin lymphoma
Age Group: 64 years (range: 32-91 years)
Sex: M+F
Population Size: 4
Sources:
AST increased grade 3, 50%
350 mg 2 times / day multiple, oral
Highest studied dose
Dose: 350 mg, 2 times / day
Route: oral
Route: multiple
Dose: 350 mg, 2 times / day
Sources:
unhealthy, 64 years (range: 32-91 years)
n = 4
Health Status: unhealthy
Condition: non-Hodgkin lymphoma
Age Group: 64 years (range: 32-91 years)
Sex: M+F
Population Size: 4
Sources:
Absolute neutrophil count decreased grade 3, 50%
350 mg 2 times / day multiple, oral
Highest studied dose
Dose: 350 mg, 2 times / day
Route: oral
Route: multiple
Dose: 350 mg, 2 times / day
Sources:
unhealthy, 64 years (range: 32-91 years)
n = 4
Health Status: unhealthy
Condition: non-Hodgkin lymphoma
Age Group: 64 years (range: 32-91 years)
Sex: M+F
Population Size: 4
Sources:
Platelets decreased grade 3, 50%
350 mg 2 times / day multiple, oral
Highest studied dose
Dose: 350 mg, 2 times / day
Route: oral
Route: multiple
Dose: 350 mg, 2 times / day
Sources:
unhealthy, 64 years (range: 32-91 years)
n = 4
Health Status: unhealthy
Condition: non-Hodgkin lymphoma
Age Group: 64 years (range: 32-91 years)
Sex: M+F
Population Size: 4
Sources:
Colitis 10%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
unhealthy, 71 years (range: 47 - 92 years)
n = 110
Health Status: unhealthy
Condition: Relapsed Chronic Lymphocytic Leukemia
Age Group: 71 years (range: 47 - 92 years)
Sex: M+F
Population Size: 110
Sources:
Diarrhea 10%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
unhealthy, 71 years (range: 47 - 92 years)
n = 110
Health Status: unhealthy
Condition: Relapsed Chronic Lymphocytic Leukemia
Age Group: 71 years (range: 47 - 92 years)
Sex: M+F
Population Size: 110
Sources:
Hepatotoxicity 10%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
unhealthy, 71 years (range: 47 - 92 years)
n = 110
Health Status: unhealthy
Condition: Relapsed Chronic Lymphocytic Leukemia
Age Group: 71 years (range: 47 - 92 years)
Sex: M+F
Population Size: 110
Sources:
Colitis 15%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
unhealthy, 71 years (range: 47 - 92 years)
n = 110
Health Status: unhealthy
Condition: Relapsed Chronic Lymphocytic Leukemia
Age Group: 71 years (range: 47 - 92 years)
Sex: M+F
Population Size: 110
Sources:
Diarrhea 15%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
unhealthy, 71 years (range: 47 - 92 years)
n = 110
Health Status: unhealthy
Condition: Relapsed Chronic Lymphocytic Leukemia
Age Group: 71 years (range: 47 - 92 years)
Sex: M+F
Population Size: 110
Sources:
Rash 15%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
unhealthy, 71 years (range: 47 - 92 years)
n = 110
Health Status: unhealthy
Condition: Relapsed Chronic Lymphocytic Leukemia
Age Group: 71 years (range: 47 - 92 years)
Sex: M+F
Population Size: 110
Sources:
Transaminases increased 15%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
unhealthy, 71 years (range: 47 - 92 years)
n = 110
Health Status: unhealthy
Condition: Relapsed Chronic Lymphocytic Leukemia
Age Group: 71 years (range: 47 - 92 years)
Sex: M+F
Population Size: 110
Sources:
Pneumonitis serious|grade 5
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sources:
Colitis serious|grade 5, 14%
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sources:
Diarrhea serious|grade 5, 14%
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sources:
Hepatotoxicity serious|grade 5, 14%
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sources:
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no [IC50 >10 uM]
no [IC50 >10 uM]
no [IC50 >10 uM]
no [IC50 >100 uM]
no [IC50 >100 uM]
no [IC50 >100 uM]
no [IC50 >100 uM]
no [IC50 >100 uM]
no [IC50 >100 uM]
no [IC50 >100 uM]
no [IC50 >100 uM]
no [IC50 >100 uM]
no [IC50 >100 uM]
no [IC50 >25 uM]
no
no
no
yes [IC50 10 uM]
no (co-administration study)
Comment: No changes in exposure to rosuvastatin (OAT1B1 and OATP1B3) or digoxin (P-gp) were observed.
Page: 7.0
yes [IC50 22 uM]
yes [IC50 26 uM]
yes [IC50 36 uM]
yes [IC50 39.8 uM]
yes [IC50 42 uM]
yes [IC50 44 uM]
yes (co-administration study)
Comment: Idelalisib increased midazolam AUC by 5.4-fold; therefore, idelalisib should not be coadministered with sensitive CYP3A substrates.
Page: 7.0
yes [IC50 5.1 uM]
yes [IC50 50 uM]
yes [IC50 60.4 uM]
yes [IC50 7 uM]
no (co-administration study)
Comment: No changes in exposure to rosuvastatin (OAT1B1 and OATP1B3) or digoxin (P-gp) were observed.
Page: 7.0
yes [IC50 76 uM]
yes (co-administration study)
Comment: Relatively few patients were coadministered CYP2C8, CYP2C9 or UGT1A1 substrates, but about 30% of patients enrolled in NHL and CLL trials were coadministered sensitive CYP2C19 substrates, including lansoprazole and omeprazole. The incidence of diarrhea and rash were higher in patients taking PPI (Section 2.1.1). These adverse events are associated with both PPI (1% to 4%) [PMC2014999] and idelalisib. The exposure to idelalisib is similar in patients taking ARA as compared to patients not taking these agents. Overlapping adverse events or an increased exposure to PPI (CYP2C19 substrates) could explain the increased incidence of adverse events.
Page: 7.0
yes [IC50 8 uM]
no (co-administration study)
Comment: No changes in exposure to rosuvastatin (OAT1B1 and OATP1B3) or digoxin (P-gp) were observed.
Page: 7.0
yes [IC50 90.7 uM]
yes
yes
yes
yes
yes
yes
yes
yes
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
no
no
no
yes
yes
yes
yes
yes
yes
yes
yes (co-administration study)
Comment: Rifampin decreased idelalisib AUC by 75%
Page: 7.0
Tox targets

Tox targets

PubMed

PubMed

TitleDatePubMed
CAL-101, a p110delta selective phosphatidylinositol-3-kinase inhibitor for the treatment of B-cell malignancies, inhibits PI3K signaling and cellular viability.
2011 Jan 13
The PI3-kinase delta inhibitor idelalisib (GS-1101) targets integrin-mediated adhesion of chronic lymphocytic leukemia (CLL) cell to endothelial and marrow stromal cells.
2013
Simultaneous inhibition of pan-phosphatidylinositol-3-kinases and MEK as a potential therapeutic strategy in peripheral T-cell lymphomas.
2013 Jan
Induction of prolonged early G1 arrest by CDK4/CDK6 inhibition reprograms lymphoma cells for durable PI3Kδ inhibition through PIK3IP1.
2013 Jun 15
Idelalisib and rituximab in relapsed chronic lymphocytic leukemia.
2014 Mar 13
Idelalisib, an inhibitor of phosphatidylinositol 3-kinase p110δ, for relapsed/refractory chronic lymphocytic leukemia.
2014 May 29
Idelalisib, a selective inhibitor of phosphatidylinositol 3-kinase-δ, as therapy for previously treated indolent non-Hodgkin lymphoma.
2014 May 29
Clinical drug interaction profile of idelalisib in healthy subjects.
2015 Aug
Patents

Sample Use Guides

The recommended dose is 150 mg taken orally, twice daily
Route of Administration: Oral
Treatment of primary CLL cells (n =14) co-cultured with HS5 stromal cells with 100 nM idelalisib results in decreased AKT phosphorylation and inhibition of BCR mediated signaling pathways.
Name Type Language
IDELALISIB
DASH   INN   USAN   VANDF   WHO-DD  
INN   USAN  
Official Name English
CAL-101
Code English
GS-1101
Code English
4(3H)-QUINAZOLINONE, 5-FLUORO-3-PHENYL-2-((1S)-1-(1H-PURIN-6-YLAMINO)PROPYL)-
Systematic Name English
ZYDELIG
Brand Name English
IDELALISIB [JAN]
Common Name English
idelalisib [INN]
Common Name English
IDELALISIB [ORANGE BOOK]
Common Name English
5-FLUORO-3-PHENYL-2-((S)-1-(9H-PURIN-6-YLAMINO)-PROPYL)-3H-QUINAZOLIN-4-ONE
Systematic Name English
IDELALISIB [VANDF]
Common Name English
IDELALISIB [MI]
Common Name English
4(3H)-QUINAZOLINONE, 5-FLUORO-3-PHENYL-2-((1S)-1-(9H-PURIN-6-YLAMINO)PROPYL)-
Systematic Name English
Idelalisib [WHO-DD]
Common Name English
IDELALISIB [USAN]
Common Name English
Classification Tree Code System Code
FDA ORPHAN DRUG 405913
Created by admin on Sat Dec 16 01:29:15 GMT 2023 , Edited by admin on Sat Dec 16 01:29:15 GMT 2023
EMA ASSESSMENT REPORTS ZYDELIG (AUTHORIZED: LYMPHOMA, NON-HODGKIN)
Created by admin on Sat Dec 16 01:29:15 GMT 2023 , Edited by admin on Sat Dec 16 01:29:15 GMT 2023
NCI_THESAURUS C129825
Created by admin on Sat Dec 16 01:29:15 GMT 2023 , Edited by admin on Sat Dec 16 01:29:15 GMT 2023
FDA ORPHAN DRUG 405813
Created by admin on Sat Dec 16 01:29:15 GMT 2023 , Edited by admin on Sat Dec 16 01:29:15 GMT 2023
WHO-ATC L01XX47
Created by admin on Sat Dec 16 01:29:15 GMT 2023 , Edited by admin on Sat Dec 16 01:29:15 GMT 2023
NDF-RT N0000175605
Created by admin on Sat Dec 16 01:29:15 GMT 2023 , Edited by admin on Sat Dec 16 01:29:15 GMT 2023
FDA ORPHAN DRUG 405613
Created by admin on Sat Dec 16 01:29:15 GMT 2023 , Edited by admin on Sat Dec 16 01:29:15 GMT 2023
FDA ORPHAN DRUG 412613
Created by admin on Sat Dec 16 01:29:15 GMT 2023 , Edited by admin on Sat Dec 16 01:29:15 GMT 2023
EMA ASSESSMENT REPORTS ZYDELIG (AUTHORIZED: LEUKEMIA, LYMPHOCYTIC, CHRONIC, B-CELL)
Created by admin on Sat Dec 16 01:29:15 GMT 2023 , Edited by admin on Sat Dec 16 01:29:15 GMT 2023
FDA ORPHAN DRUG 405713
Created by admin on Sat Dec 16 01:29:15 GMT 2023 , Edited by admin on Sat Dec 16 01:29:15 GMT 2023
EU-Orphan Drug EU/3/13/1160
Created by admin on Sat Dec 16 01:29:15 GMT 2023 , Edited by admin on Sat Dec 16 01:29:15 GMT 2023
FDA ORPHAN DRUG 347511
Created by admin on Sat Dec 16 01:29:15 GMT 2023 , Edited by admin on Sat Dec 16 01:29:15 GMT 2023
NCI_THESAURUS C2152
Created by admin on Sat Dec 16 01:29:15 GMT 2023 , Edited by admin on Sat Dec 16 01:29:15 GMT 2023
FDA ORPHAN DRUG 412513
Created by admin on Sat Dec 16 01:29:15 GMT 2023 , Edited by admin on Sat Dec 16 01:29:15 GMT 2023
Code System Code Type Description
DRUG BANK
DB09054
Created by admin on Sat Dec 16 01:29:15 GMT 2023 , Edited by admin on Sat Dec 16 01:29:15 GMT 2023
PRIMARY
NDF-RT
N0000175082
Created by admin on Sat Dec 16 01:29:15 GMT 2023 , Edited by admin on Sat Dec 16 01:29:15 GMT 2023
PRIMARY Kinase Inhibitors [MoA]
SMS_ID
100000151771
Created by admin on Sat Dec 16 01:29:15 GMT 2023 , Edited by admin on Sat Dec 16 01:29:15 GMT 2023
PRIMARY
RXCUI
1544460
Created by admin on Sat Dec 16 01:29:15 GMT 2023 , Edited by admin on Sat Dec 16 01:29:15 GMT 2023
PRIMARY RxNorm
LACTMED
Idelalisib
Created by admin on Sat Dec 16 01:29:15 GMT 2023 , Edited by admin on Sat Dec 16 01:29:15 GMT 2023
PRIMARY
MERCK INDEX
m11752
Created by admin on Sat Dec 16 01:29:15 GMT 2023 , Edited by admin on Sat Dec 16 01:29:15 GMT 2023
PRIMARY
EVMPD
SUB126168
Created by admin on Sat Dec 16 01:29:15 GMT 2023 , Edited by admin on Sat Dec 16 01:29:15 GMT 2023
PRIMARY
CAS
870281-82-6
Created by admin on Sat Dec 16 01:29:15 GMT 2023 , Edited by admin on Sat Dec 16 01:29:15 GMT 2023
PRIMARY
CHEBI
82701
Created by admin on Sat Dec 16 01:29:15 GMT 2023 , Edited by admin on Sat Dec 16 01:29:15 GMT 2023
PRIMARY
EPA CompTox
DTXSID701007266
Created by admin on Sat Dec 16 01:29:15 GMT 2023 , Edited by admin on Sat Dec 16 01:29:15 GMT 2023
PRIMARY
NDF-RT
N0000190114
Created by admin on Sat Dec 16 01:29:15 GMT 2023 , Edited by admin on Sat Dec 16 01:29:15 GMT 2023
PRIMARY Cytochrome P450 3A Inhibitors [MoA]
NCI_THESAURUS
C78825
Created by admin on Sat Dec 16 01:29:15 GMT 2023 , Edited by admin on Sat Dec 16 01:29:15 GMT 2023
PRIMARY
WIKIPEDIA
Idelalisib
Created by admin on Sat Dec 16 01:29:15 GMT 2023 , Edited by admin on Sat Dec 16 01:29:15 GMT 2023
PRIMARY
IUPHAR
6741
Created by admin on Sat Dec 16 01:29:15 GMT 2023 , Edited by admin on Sat Dec 16 01:29:15 GMT 2023
PRIMARY
DAILYMED
YG57I8T5M0
Created by admin on Sat Dec 16 01:29:15 GMT 2023 , Edited by admin on Sat Dec 16 01:29:15 GMT 2023
PRIMARY
FDA UNII
YG57I8T5M0
Created by admin on Sat Dec 16 01:29:15 GMT 2023 , Edited by admin on Sat Dec 16 01:29:15 GMT 2023
PRIMARY
DRUG CENTRAL
4878
Created by admin on Sat Dec 16 01:29:15 GMT 2023 , Edited by admin on Sat Dec 16 01:29:15 GMT 2023
PRIMARY
INN
9624
Created by admin on Sat Dec 16 01:29:15 GMT 2023 , Edited by admin on Sat Dec 16 01:29:15 GMT 2023
PRIMARY
ChEMBL
CHEMBL2216870
Created by admin on Sat Dec 16 01:29:15 GMT 2023 , Edited by admin on Sat Dec 16 01:29:15 GMT 2023
PRIMARY
USAN
AB-74
Created by admin on Sat Dec 16 01:29:15 GMT 2023 , Edited by admin on Sat Dec 16 01:29:15 GMT 2023
PRIMARY
PUBCHEM
11625818
Created by admin on Sat Dec 16 01:29:15 GMT 2023 , Edited by admin on Sat Dec 16 01:29:15 GMT 2023
PRIMARY
NCI_THESAURUS
C78825
Created by admin on Sat Dec 16 01:29:15 GMT 2023 , Edited by admin on Sat Dec 16 01:29:15 GMT 2023
PRIMARY