idelalisib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
phosphatidylinositol 3-kinase inhibitors, antineoplastics 4878 870281-82-6

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • CAL 101
  • idelalisib
  • zydelig
  • CAL-101
  • GS-1101
Idelalisib is an inhibitor of PI3K-delta kinase, which is expressed in normal and malignant B-cells. Idelalisib induced apoptosis and inhibited proliferation in cell lines derived from malignant B-cells and in primary tumor cells. Idelalisib inhibits several cell signaling pathways, including B-cell receptor (BCR) signaling and the CXCR4 and CXCR5 signaling, which are involved in trafficking and homing of B-cells to the lymph nodes and bone marrow.
  • Molecular weight: 415.43
  • Formula: C22H18FN7O
  • CLOGP: 3.32
  • LIPINSKI: 0
  • HAC: 8
  • HDO: 2
  • TPSA: 99.16
  • ALOGS: -4.22
  • ROTB: 5

  • Status: ONP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.30 g O

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
July 25, 2014 EMA
July 23, 2014 FDA GILEAD SCIENCES INC

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Disease progression 1165.24 31.11 380 3236 122378 63363028
Death 108.26 31.11 119 3497 374262 63111144
Pneumonitis 106.70 31.11 48 3568 35174 63450232
Off label use 97.31 31.11 152 3464 674310 62811096
Diarrhoea 94.69 31.11 155 3461 715211 62770195
Colitis 83.56 31.11 45 3571 48483 63436923
Neutropenia 74.95 31.11 69 3547 174936 63310470
Cytomegalovirus infection 74.57 31.11 32 3584 20920 63464486
Non-small cell lung cancer 67.33 31.11 19 3597 3576 63481830
Chronic lymphocytic leukaemia recurrent 49.29 31.11 9 3607 235 63485171
Chronic lymphocytic leukaemia refractory 47.52 31.11 7 3609 44 63485362
Pneumonia 45.80 31.11 88 3528 456679 63028727
Lymph node palpable 42.08 31.11 7 3609 104 63485302
Pseudolymphoma 40.78 31.11 9 3607 620 63484786
Progressive multifocal leukoencephalopathy 40.26 31.11 18 3598 12953 63472453
Lung disorder 39.86 31.11 31 3585 62230 63423176
Dehydration 39.58 31.11 49 3567 173305 63312101
B-cell lymphoma recurrent 38.67 31.11 8 3608 405 63485001
Neutropenic infection 38.65 31.11 10 3606 1357 63484049
Nonspecific reaction 37.92 31.11 11 3605 2281 63483125
Blood disorder 36.70 31.11 14 3602 6757 63478649
Pyrexia 35.81 31.11 81 3535 470397 63015009
Respiratory failure 35.64 31.11 36 3580 101822 63383584
B-cell lymphoma refractory 35.42 31.11 6 3610 100 63485306
Transaminases increased 32.59 31.11 21 3595 31346 63454060
Febrile neutropenia 31.15 31.11 36 3580 118413 63366993

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Disease progression 1460.87 27.92 581 5471 107496 34843383
Diarrhoea 205.92 27.92 291 5761 389621 34561258
Pneumonitis 190.22 27.92 100 5952 33778 34917101
Colitis 174.59 27.92 98 5954 37652 34913227
Pneumonia 85.68 27.92 191 5861 362436 34588443
Death 84.54 27.92 201 5851 397848 34553031
Chronic lymphocytic leukaemia recurrent 76.23 27.92 17 6035 393 34950486
Off label use 62.62 27.92 186 5866 419338 34531541
Pyrexia 58.76 27.92 157 5895 332856 34618023
Lymphocytosis 52.75 27.92 19 6033 2558 34948321
Dehydration 50.80 27.92 85 5967 129884 34820995
Neutropenia 49.03 27.92 93 5959 156685 34794194
Lung disorder 45.80 27.92 42 6010 34654 34916225
Pneumocystis jirovecii infection 43.69 27.92 15 6037 1755 34949124
Lymphoma transformation 43.46 27.92 10 6042 267 34950612
Electrolyte imbalance 37.48 27.92 26 6026 14386 34936493
Febrile neutropenia 33.04 27.92 73 5979 136776 34814103
Cytomegalovirus colitis 30.33 27.92 13 6039 2771 34948108
Respiratory tract infection 30.25 27.92 26 6026 19686 34931193
Dermatitis exfoliative 29.97 27.92 17 6035 6622 34944257
Hepatocellular injury 29.51 27.92 27 6025 22184 34928695

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Disease progression 2192.04 25.88 796 7858 183566 79552168
Colitis 228.06 25.88 125 8529 73182 79662552
Pneumonitis 226.62 25.88 117 8537 60743 79674991
Diarrhoea 225.40 25.88 366 8288 880123 78855611
Death 178.71 25.88 260 8394 566254 79169480
Pneumonia 118.55 25.88 236 8418 660010 79075724
Off label use 104.64 25.88 272 8382 906943 78828791
Neutropenia 97.47 25.88 137 8517 287573 79448161
Dehydration 95.91 25.88 126 8528 248061 79487673
Pyrexia 91.23 25.88 216 8438 678493 79057241
Febrile neutropenia 59.62 25.88 97 8557 230902 79504832
Electrolyte imbalance 57.69 25.88 38 8616 30843 79704891
Cytomegalovirus infection 55.34 25.88 42 8612 42602 79693132
Chronic lymphocytic leukaemia recurrent 54.94 25.88 13 8641 635 79735099
Progressive multifocal leukoencephalopathy 52.80 25.88 31 8623 20569 79715165
Chronic lymphocytic leukaemia refractory 49.42 25.88 9 8645 117 79735617
Pneumocystis jirovecii pneumonia 48.90 25.88 35 8619 32473 79703261
Respiratory tract infection 48.36 25.88 41 8613 48648 79687086
Pneumocystis jirovecii infection 47.22 25.88 16 8638 2878 79732856
Cytomegalovirus colitis 46.73 25.88 18 8636 4667 79731067
Lymphoma transformation 46.36 25.88 10 8644 320 79735414
Lung disorder 46.03 25.88 50 8604 80507 79655227
Headache 45.72 25.88 8 8646 653764 79081970
Lymphocytosis 43.16 25.88 17 8637 4676 79731058
Non-small cell lung cancer 41.41 25.88 18 8636 6342 79729392
Sepsis 39.52 25.88 89 8565 269339 79466395
Lymph node palpable 34.35 25.88 7 8647 169 79735565
Tumour lysis syndrome 34.23 25.88 25 8629 23914 79711820
Mixed dementia 30.84 25.88 7 8647 284 79735450
Nonspecific reaction 29.87 25.88 11 8643 2521 79733213
Pain 29.76 25.88 20 8634 703782 79031952
Pseudolymphoma 29.22 25.88 9 8645 1196 79734538
Respiratory failure 29.03 25.88 62 8592 180849 79554885
Pain in extremity 28.90 25.88 3 8651 364535 79371199
Blood disorder 28.15 25.88 15 8639 8258 79727476
Dermatitis exfoliative 26.97 25.88 16 8638 10813 79724921
Hypogammaglobulinaemia 26.80 25.88 17 8637 12934 79722800
Lymphadenitis viral 26.67 25.88 5 8649 77 79735657
Neutropenic infection 26.64 25.88 10 8644 2417 79733317
Borrelia infection 26.26 25.88 6 8648 251 79735483
Hepatocellular injury 26.24 25.88 29 8625 47564 79688170
Transaminases increased 25.92 25.88 30 8624 51713 79684021

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01EM01 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
PROTEIN KINASE INHIBITORS
Phosphatidylinositol-3-kinase (Pi3K) inhibitors
FDA MoA N0000175082 Kinase Inhibitors
MeSH PA D000970 Antineoplastic Agents
MeSH PA D004791 Enzyme Inhibitors
FDA EPC N0000175605 Kinase Inhibitor
FDA MoA N0000190114 Cytochrome P450 3A Inhibitors
CHEBI has role CHEBI:35610 antineoplastic agents
CHEBI has role CHEBI:50914 PI(3)K inhibitor
CHEBI has role CHEBI:68495 Type I cell-death inducers

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Chronic lymphoid leukemia, disease indication 92814006
Malignant lymphoma - small lymphocytic indication 302841002
Follicular non-Hodgkin's lymphoma indication 308121000
Toxic epidermal necrolysis due to drug contraindication 402744003




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 10.29 acidic
pKa2 4.22 Basic
pKa3 2.56 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
100MG ZYDELIG GILEAD SCIENCES INC N205858 July 23, 2014 RX TABLET ORAL 8980901 May 12, 2025 FOR THE TREATMENT OF PATIENTS WITH CLL, FL, OR SLL
100MG ZYDELIG GILEAD SCIENCES INC N205858 July 23, 2014 RX TABLET ORAL 9149477 May 12, 2025 INHIBITION ON PI3K KINASE
150MG ZYDELIG GILEAD SCIENCES INC N205858 July 23, 2014 RX TABLET ORAL 8980901 May 12, 2025 FOR THE TREATMENT OF PATIENTS WITH CLL, FL, OR SLL
150MG ZYDELIG GILEAD SCIENCES INC N205858 July 23, 2014 RX TABLET ORAL 9149477 May 12, 2025 INHIBITION ON PI3K KINASE
100MG ZYDELIG GILEAD SCIENCES INC N205858 July 23, 2014 RX TABLET ORAL RE44599 July 21, 2025 FOR THE TREATMENT OF PATIENTS WITH CLL, FL, OR SLL
100MG ZYDELIG GILEAD SCIENCES INC N205858 July 23, 2014 RX TABLET ORAL RE44599 July 21, 2025 FOR THE TREATMENT OF PATIENTS WITH RELAPSED FOLLICULAR B-CELL NON-HODGKIN LYMPHOMA OR [RELAPSED] SMALL LYMPHOCYTIC LYMPHOMA
150MG ZYDELIG GILEAD SCIENCES INC N205858 July 23, 2014 RX TABLET ORAL RE44599 July 21, 2025 FOR THE TREATMENT OF PATIENTS WITH CLL, FL, OR SLL
150MG ZYDELIG GILEAD SCIENCES INC N205858 July 23, 2014 RX TABLET ORAL RE44599 July 21, 2025 FOR THE TREATMENT OF PATIENTS WITH RELAPSED FOLLICULAR B-CELL NON-HODGKIN LYMPHOMA OR [RELAPSED] SMALL LYMPHOCYTIC LYMPHOMA
100MG ZYDELIG GILEAD SCIENCES INC N205858 July 23, 2014 RX TABLET ORAL 9492449 March 11, 2030 IN COMBINATION WITH RITUXIMAB, FOR THE TREATMENT OF PATIENTS WITH RELAPSED CHRONIC LYMPHOCYTIC LEUKEMIA (CLL)
150MG ZYDELIG GILEAD SCIENCES INC N205858 July 23, 2014 RX TABLET ORAL 9492449 March 11, 2030 IN COMBINATION WITH RITUXIMAB, FOR THE TREATMENT OF PATIENTS WITH RELAPSED CHRONIC LYMPHOCYTIC LEUKEMIA (CLL)
100MG ZYDELIG GILEAD SCIENCES INC N205858 July 23, 2014 RX TABLET ORAL 8865730 March 5, 2033 FOR THE TREATMENT OF PATIENTS WITH CLL, FL, OR SLL
150MG ZYDELIG GILEAD SCIENCES INC N205858 July 23, 2014 RX TABLET ORAL 8865730 March 5, 2033 FOR THE TREATMENT OF PATIENTS WITH CLL, FL, OR SLL

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform Kinase INHIBITOR IC50 8.60 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
DNA-dependent protein kinase catalytic subunit Kinase IC50 5.17 CHEMBL
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform Kinase IC50 6.25 SCIENTIFIC LITERATURE
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform Kinase IC50 6.09 SCIENTIFIC LITERATURE
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Kinase IC50 7.05 SCIENTIFIC LITERATURE
Phosphatidylinositol 3-kinase catalytic subunit type 3 Kinase IC50 5.36 CHEMBL
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Kinase IC50 5.88 CHEMBL

External reference:

IDSource
D10560 KEGG_DRUG
4033559 VUID
N0000190926 NUI
4033559 VANDF
CHEBI:82701 CHEBI
40L PDB_CHEM_ID
CHEMBL2216870 ChEMBL_ID
C552946 MESH_SUPPLEMENTAL_RECORD_UI
6741 IUPHAR_LIGAND_ID
DB09054 DRUGBANK_ID
1544460 RXNORM
226727 MMSL
30429 MMSL
d08273 MMSL
015626 NDDF
709283009 SNOMEDCT_US
710278000 SNOMEDCT_US
C2698692 UMLSCUI
9624 INN_ID
11625818 PUBCHEM_CID
YG57I8T5M0 UNII

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Zydelig HUMAN PRESCRIPTION DRUG LABEL 1 61958-1701 TABLET, FILM COATED 100 mg ORAL NDA 33 sections
Zydelig HUMAN PRESCRIPTION DRUG LABEL 1 61958-1701 TABLET, FILM COATED 100 mg ORAL NDA 33 sections
Zydelig HUMAN PRESCRIPTION DRUG LABEL 1 61958-1702 TABLET, FILM COATED 150 mg ORAL NDA 33 sections
Zydelig HUMAN PRESCRIPTION DRUG LABEL 1 61958-1702 TABLET, FILM COATED 150 mg ORAL NDA 33 sections