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Details

Stereochemistry ABSOLUTE
Molecular Formula C22H18FN7O
Molecular Weight 415.4239
Optical Activity UNSPECIFIED
Defined Stereocenters 1 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of IDELALISIB

SMILES

CC[C@@]([H])(c1nc2cccc(c2c(=O)n1-c3ccccc3)F)Nc4c5c([nH]cn5)ncn4

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

Molecular Formula C22H18FN7O
Molecular Weight 415.4239
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 1 / 1
E/Z Centers 0
Optical Activity UNSPECIFIED

Description
Curator's Comment:: 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

TargetsConditions

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

1406073600000
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

1406073600000
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

1406073600000
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)
Health Status: unhealthy
Age Group: 64 years (range: 32-91 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 71 years (range: 47 - 92 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 64 years (range: 32-91 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 64 years (range: 32-91 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 64 years (range: 32-91 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 64 years (range: 32-91 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 64 years (range: 32-91 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 64 years (range: 32-91 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 64 years (range: 32-91 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 64 years (range: 32-91 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 64 years (range: 32-91 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 64 years (range: 32-91 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 64 years (range: 32-91 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 64 years (range: 32-91 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 64 years (range: 32-91 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 64 years (range: 32-91 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 64 years (range: 32-91 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 64 years (range: 32-91 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 64 years (range: 32-91 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 64 years (range: 32-91 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 64 years (range: 32-91 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 64 years (range: 32-91 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 64 years (range: 32-91 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 64 years (range: 32-91 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 71 years (range: 47 - 92 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 71 years (range: 47 - 92 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 71 years (range: 47 - 92 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 71 years (range: 47 - 92 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 71 years (range: 47 - 92 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 71 years (range: 47 - 92 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 71 years (range: 47 - 92 years)
Sex: M+F
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
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
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
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
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
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
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.
Substance Class Chemical
Created
by admin
on Sat Jun 26 11:14:23 UTC 2021
Edited
by admin
on Sat Jun 26 11:14:23 UTC 2021
Record UNII
YG57I8T5M0
Record Status Validated (UNII)
Record Version
  • Download
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 [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
IDELALISIB [WHO-DD]
Common Name English
4(3H)-QUINAZOLINONE, 5-FLUORO-3-PHENYL-2-((1S)-1-(9H-PURIN-6-YLAMINO)PROPYL)-
Systematic Name English
IDELALISIB [USAN]
Common Name English
Classification Tree Code System Code
FDA ORPHAN DRUG 405913
Created by admin on Sat Jun 26 11:14:24 UTC 2021 , Edited by admin on Sat Jun 26 11:14:24 UTC 2021
EMA ASSESSMENT REPORTS ZYDELIG (AUTHORIZED: LYMPHOMA, NON-HODGKIN)
Created by admin on Sat Jun 26 11:14:24 UTC 2021 , Edited by admin on Sat Jun 26 11:14:24 UTC 2021
NCI_THESAURUS C129825
Created by admin on Sat Jun 26 11:14:24 UTC 2021 , Edited by admin on Sat Jun 26 11:14:24 UTC 2021
FDA ORPHAN DRUG 405813
Created by admin on Sat Jun 26 11:14:24 UTC 2021 , Edited by admin on Sat Jun 26 11:14:24 UTC 2021
WHO-ATC L01XX47
Created by admin on Sat Jun 26 11:14:24 UTC 2021 , Edited by admin on Sat Jun 26 11:14:24 UTC 2021
NDF-RT N0000175605
Created by admin on Sat Jun 26 11:14:24 UTC 2021 , Edited by admin on Sat Jun 26 11:14:24 UTC 2021
FDA ORPHAN DRUG 405613
Created by admin on Sat Jun 26 11:14:24 UTC 2021 , Edited by admin on Sat Jun 26 11:14:24 UTC 2021
FDA ORPHAN DRUG 412613
Created by admin on Sat Jun 26 11:14:24 UTC 2021 , Edited by admin on Sat Jun 26 11:14:24 UTC 2021
EMA ASSESSMENT REPORTS ZYDELIG (AUTHORIZED: LEUKEMIA, LYMPHOCYTIC, CHRONIC, B-CELL)
Created by admin on Sat Jun 26 11:14:24 UTC 2021 , Edited by admin on Sat Jun 26 11:14:24 UTC 2021
FDA ORPHAN DRUG 405713
Created by admin on Sat Jun 26 11:14:24 UTC 2021 , Edited by admin on Sat Jun 26 11:14:24 UTC 2021
EU-Orphan Drug EU/3/13/1160
Created by admin on Sat Jun 26 11:14:24 UTC 2021 , Edited by admin on Sat Jun 26 11:14:24 UTC 2021
FDA ORPHAN DRUG 347511
Created by admin on Sat Jun 26 11:14:24 UTC 2021 , Edited by admin on Sat Jun 26 11:14:24 UTC 2021
NCI_THESAURUS C2152
Created by admin on Sat Jun 26 11:14:24 UTC 2021 , Edited by admin on Sat Jun 26 11:14:24 UTC 2021
FDA ORPHAN DRUG 412513
Created by admin on Sat Jun 26 11:14:24 UTC 2021 , Edited by admin on Sat Jun 26 11:14:24 UTC 2021
Code System Code Type Description
DRUG BANK
DB09054
Created by admin on Sat Jun 26 11:14:24 UTC 2021 , Edited by admin on Sat Jun 26 11:14:24 UTC 2021
PRIMARY
NDF-RT
N0000175082
Created by admin on Sat Jun 26 11:14:24 UTC 2021 , Edited by admin on Sat Jun 26 11:14:24 UTC 2021
PRIMARY Kinase Inhibitors [MoA]
RXCUI
1544460
Created by admin on Sat Jun 26 11:14:24 UTC 2021 , Edited by admin on Sat Jun 26 11:14:24 UTC 2021
PRIMARY RxNorm
LACTMED
Idelalisib
Created by admin on Sat Jun 26 11:14:24 UTC 2021 , Edited by admin on Sat Jun 26 11:14:24 UTC 2021
PRIMARY
MERCK INDEX
M11752
Created by admin on Sat Jun 26 11:14:24 UTC 2021 , Edited by admin on Sat Jun 26 11:14:24 UTC 2021
PRIMARY
EVMPD
SUB126168
Created by admin on Sat Jun 26 11:14:24 UTC 2021 , Edited by admin on Sat Jun 26 11:14:24 UTC 2021
PRIMARY
CAS
870281-82-6
Created by admin on Sat Jun 26 11:14:24 UTC 2021 , Edited by admin on Sat Jun 26 11:14:24 UTC 2021
PRIMARY
NDF-RT
N0000190114
Created by admin on Sat Jun 26 11:14:24 UTC 2021 , Edited by admin on Sat Jun 26 11:14:24 UTC 2021
PRIMARY Cytochrome P450 3A Inhibitors [MoA]
NCI_THESAURUS
C78825
Created by admin on Sat Jun 26 11:14:24 UTC 2021 , Edited by admin on Sat Jun 26 11:14:24 UTC 2021
PRIMARY
WIKIPEDIA
Idelalisib
Created by admin on Sat Jun 26 11:14:24 UTC 2021 , Edited by admin on Sat Jun 26 11:14:24 UTC 2021
PRIMARY
IUPHAR
6741
Created by admin on Sat Jun 26 11:14:24 UTC 2021 , Edited by admin on Sat Jun 26 11:14:24 UTC 2021
PRIMARY
FDA UNII
YG57I8T5M0
Created by admin on Sat Jun 26 11:14:24 UTC 2021 , Edited by admin on Sat Jun 26 11:14:24 UTC 2021
PRIMARY
DRUG CENTRAL
4878
Created by admin on Sat Jun 26 11:14:24 UTC 2021 , Edited by admin on Sat Jun 26 11:14:24 UTC 2021
PRIMARY
INN
9624
Created by admin on Sat Jun 26 11:14:24 UTC 2021 , Edited by admin on Sat Jun 26 11:14:24 UTC 2021
PRIMARY
ChEMBL
CHEMBL2216870
Created by admin on Sat Jun 26 11:14:24 UTC 2021 , Edited by admin on Sat Jun 26 11:14:24 UTC 2021
PRIMARY
PUBCHEM
11625818
Created by admin on Sat Jun 26 11:14:24 UTC 2021 , Edited by admin on Sat Jun 26 11:14:24 UTC 2021
PRIMARY
NCI_THESAURUS
C78825
Created by admin on Sat Jun 26 11:14:24 UTC 2021 , Edited by admin on Sat Jun 26 11:14:24 UTC 2021
PRIMARY
Related Record Type Details
METABOLIC ENZYME -> SUBSTRATE
TRANSPORTER -> INHIBITOR
TRANSPORTER -> SUBSTRATE
BINDER->LIGAND
BINDING
TARGET->WEAK INHIBITOR
TRANSPORTER -> SUBSTRATE
METABOLIC ENZYME -> SUBSTRATE
METABOLIC ENZYME -> SUBSTRATE
METABOLIC ENZYME -> INHIBITOR
IN VITRO
TRANSPORTER -> INHIBITOR
METABOLIC ENZYME -> INHIBITOR
IN VITRO
METABOLIC ENZYME -> INHIBITOR
INN VITRO
TRANSPORTER -> INHIBITOR
METABOLIC ENZYME -> INHIBITOR
IN VITRO
TARGET -> INHIBITOR
IC50
Related Record Type Details
METABOLITE INACTIVE -> PARENT
MAJOR
PLASMA
METABOLITE INACTIVE -> PARENT
MAJOR
PLASMA
METABOLITE INACTIVE -> PARENT
MAJOR
PLASMA
METABOLITE INACTIVE -> PARENT
MAJOR
PLASMA
METABOLITE -> PARENT
METABOLITE -> PARENT
METABOLITE INACTIVE -> PARENT
MAJOR
PLASMA
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
blood-to-plasma ratio PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC
Tmax PHARMACOKINETIC