Idelalisib

drug
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Also known as CAL-101GS-1101Gs-11cal-101ZydeligCAL-101 (GS-1101)CAL 101IdelalisibIdelalisibÊIdelalisibÂCal101

Summary

Idelalisib (CHEMBL2216870) is an approved small-molecule antineoplastic agent (ATC L01EM01) targeting PIK3CA, PIK3CB, and PIK3CD; indicated across 19 conditions including b-cell chronic lymphocytic leukemia and neoplasm; with CIViC clinical evidence for 1 variant-indication association (e.g. PIK3CA P471L in merkel cell carcinoma).

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: L01EM01
  • Targets: 4 (PIK3CA, PIK3CB, PIK3CD…)
  • Indications: 19 conditions
  • Clinical trials: 64
  • Precision-oncology evidence (CIViC): 1 variant–indication association
  • Chemistry: 415.4 Da · C22H18FN7O

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL2216870
NameIdelalisib
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID11625818
ChEBICHEBI:82701
ATCL01EM01
Molecular formulaC22H18FN7O
Molecular weight415.4
InChIKeyIFSDAJWBUCMOAH-HNNXBMFYSA-N

SMILES: CC[C@@H](C1=NC2=C(C(=CC=C2)F)C(=O)N1C3=CC=CC=C3)NC4=NC=NC5=C4NC=N5

IUPAC name: 5-fluoro-3-phenyl-2-[(1S)-1-(7H-purin-6-ylamino)propyl]quinazolin-4-one

ChEBI definition: A member of the class of quinazolines that is 5-fluoro-3-phenylquinazolin-4-one in which the hydrogen at position 2 is replaced by a (1S)-1-(3H-purin-6-ylamino)propyl group. used for for the treatment of refractory indolent non-Hodgkin’s lymphoma and relapsed chronic lymphocytic leukemia.

Pharmacological roles (ChEBI): antineoplastic agent, apoptosis inducer, EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor.

Also known as: CAL-101, GS-1101, Gs-11cal-101, Idelalisib, Zydelig, IDELALISIB, GS-11CAL-101, CAL-101 (GS-1101), CAL 101, ZYDELIG, idelalisib, Idelalisib; Zydelig

Patent coverage: 4,003 distinct patent families (10,163 SureChEMBL compound mentions), from 5 matched compound structure(s). One matched structure accounts for 9,090 (89%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

GeneTargetActionpAffinityCancer dependencyUniProt
PIK3CAphosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alphaInhibition6.0942.7%P42336
PIK3CBphosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit betaInhibition6.255%P42338
PIK3CDphosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit deltaInhibition8.66%O00329
PIK3CGphosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gammaInhibition7.050.7%P48736

Broader ChEMBL bioactivity targets: 18 (assay-derived). Sample: Phosphatidylinositol 3-kinase catalytic subunit type 3, PI3-kinase p110-alpha/p85-alpha, PI3-kinase p110-delta/p85-alpha, 5-hydroxytryptamine receptor 1A, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform, Prostaglandin G/H synthase 1, Mu-type opioid receptor, Sodium-dependent dopamine transporter, cGMP-inhibited 3’,5’-cyclic phosphodiesterase 3A, 3’,5’-cyclic-AMP phosphodiesterase 4D.

Bioactivity

ChEMBL activities: 168 potent at pChembl ≥ 5 of 172 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
PIK3CD9IC501nMCHEMBL_ACT_25038380
PIK3CD8.97IC501.08nMCHEMBL_ACT_23279989
PIK3CD8.92IC501.2nMCHEMBL_ACT_19242051
PIK3CD8.8IC501.6nMCHEMBL_ACT_18658752
PIK3CD8.8Ki1.58nMCHEMBL_ACT_29215579
PIK3CD8.74IC501.8nMCHEMBL_ACT_19174499
PIK3CD8.7IC502nMCHEMBL_ACT_16673471
PIK3CD8.7IC502nMCHEMBL_ACT_18077974
PIK3CD8.7IC502nMCHEMBL_ACT_18113972
PIK3CD8.7IC502nMCHEMBL_ACT_18952539
PIK3CD8.7IC502nMCHEMBL_ACT_19041449
PIK3CD8.7IC502nMCHEMBL_ACT_23296114
PIK3CD8.68IC502.1nMCHEMBL_ACT_19207806
PIK3CD8.6IC502.5nMCHEMBL_ACT_12645772
PIK3CD8.6IC502.5nMCHEMBL_ACT_14553166
PIK3CD8.6IC502.5nMCHEMBL_ACT_18197122
PIK3CD8.6IC502.5nMCHEMBL_ACT_18573179
PIK3CD8.6IC502.5nMCHEMBL_ACT_18578195
PIK3CD8.6IC502.5nMCHEMBL_ACT_19036837
PIK3CD8.6IC502.5nMCHEMBL_ACT_22885893
PIK3CD8.6IC502.5nMCHEMBL_ACT_23127306
PIK3CD8.6IC502.5nMCHEMBL_ACT_23258676
PIK3CD8.6IC502.5nMCHEMBL_ACT_24862055
PIK3CD8.6IC502.5nMCHEMBL_ACT_25892698
PIK3CD8.59IC502.56nMCHEMBL_ACT_29244756
PIK3CD8.57IC502.7nMCHEMBL_ACT_15166421
PIK3CD8.57IC502.7nMCHEMBL_ACT_18234615
PIK3CD8.57IC502.7nMCHEMBL_ACT_18578193
PIK3CD8.54IC502.9nMCHEMBL_ACT_25634111
PIK3CD8.52IC503nMCHEMBL_ACT_16490965

Target pathways

Aggregated over 4 target gene(s): PIK3CA, PIK3CB, PIK3CD, PIK3CG.

Top Reactome pathways

62 total, by targets touching each:

PathwayTargetsGenes
PIP3 activates AKT signaling4PIK3CA, PIK3CB, PIK3CD, PIK3CG
Synthesis of PIPs at the plasma membrane4PIK3CA, PIK3CB, PIK3CD, PIK3CG
Constitutive Signaling by Aberrant PI3K in Cancer4PIK3CA, PIK3CB, PIK3CD, PIK3CG
CD28 dependent PI3K/Akt signaling4PIK3CA, PIK3CB, PIK3CD, PIK3CG
PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling4PIK3CA, PIK3CB, PIK3CD, PIK3CG
Erythropoietin activates Phosphoinositide-3-kinase (PI3K)4PIK3CA, PIK3CB, PIK3CD, PIK3CG
Co-stimulation by ICOS4PIK3CA, PIK3CB, PIK3CD, PIK3CG
GPVI-mediated activation cascade3PIK3CA, PIK3CB, PIK3CG
Interleukin-3, Interleukin-5 and GM-CSF signaling3PIK3CA, PIK3CB, PIK3CD
RET signaling3PIK3CA, PIK3CB, PIK3CD
Interleukin receptor SHC signaling3PIK3CA, PIK3CB, PIK3CD
Regulation of signaling by CBL3PIK3CA, PIK3CB, PIK3CD
Signaling by CSF1 (M-CSF) in myeloid cells3PIK3CA, PIK3CB, PIK3CD
High laminar flow shear stress activates signaling by PIEZO1 and PECAM1:CDH5:KDR in endothelial cells3PIK3CA, PIK3CB, PIK3CD
PI3K Cascade2PIK3CA, PIK3CB
IRS-mediated signalling2PIK3CA, PIK3CB
Downstream signal transduction2PIK3CA, PIK3CB
PI3K/AKT activation2PIK3CA, PIK3CB
Signaling by ALK2PIK3CA, PIK3CB
Downstream TCR signaling2PIK3CA, PIK3CB
Role of phospholipids in phagocytosis2PIK3CA, PIK3CB
Tie2 Signaling2PIK3CA, PIK3CB
DAP12 signaling2PIK3CA, PIK3CB
Role of LAT2/NTAL/LAB on calcium mobilization2PIK3CA, PIK3CB
Nephrin family interactions2PIK3CA, PIK3CB
VEGFA-VEGFR2 Pathway2PIK3CA, PIK3CB
RAF/MAP kinase cascade2PIK3CA, PIK3CB
Signaling by PDGFRA transmembrane, juxtamembrane and kinase domain mutants2PIK3CA, PIK3CB
Signaling by PDGFRA extracellular domain mutants2PIK3CA, PIK3CB
Signaling by ALK fusions and activated point mutants2PIK3CA, PIK3CB

Dominant GO biological processes

GO termTargets
cell migration4
phosphatidylinositol-3-phosphate biosynthetic process4
phosphatidylinositol 3-kinase/protein kinase B signal transduction4
phosphatidylinositol phosphate biosynthetic process4
phosphatidylinositol-mediated signaling4
lipid metabolic process4
chemotaxis3
positive regulation of endothelial cell migration3
innate immune response3
angiogenesis2
platelet activation2
vascular endothelial growth factor signaling pathway2
T cell receptor signaling pathway2
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction2
negative regulation of fibroblast apoptotic process2

Indications & clinical

Indications

19 indications (5 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

IndicationTrial phaseMONDOEFO
B-cell chronic lymphocytic leukemia4MONDO:0004948EFO:0000095
neoplasm4MONDO:0005070EFO:0000616
neoplasm of mature B-cells4MONDO:0004949EFO:0000096
non-Hodgkin lymphoma4MONDO:0018908EFO:0005952
lymphoma3MONDO:0005062EFO:0000574
follicular lymphoma3MONDO:0018906MONDO:0018906
Hodgkins lymphoma2MONDO:0004952EFO:0000183
mantle cell lymphoma2MONDO:0018876EFO:1001469
diffuse large B-cell lymphoma2MONDO:0018905EFO:0000403
amyloidosis2MONDO:0019065EFO:1001875
Waldenstrom macroglobulinemia2MONDO:0100280EFO:0009441
allergic rhinitis1MONDO:0011786EFO:0005854
acute myeloid leukemia1MONDO:0018874EFO:0000222
plasma cell myeloma1MONDO:0009693EFO:0001378
acute lymphoblastic leukemia1MONDO:0004967EFO:0000220
primary myelofibrosis1MONDO:0009692MONDO:0044903
pancreatic ductal adenocarcinoma1MONDO:0005184MONDO:0005184

2 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 64.

Phase distribution

PhaseTrials
PHASE223
PHASE116
PHASE314
Not specified5
PHASE1/PHASE24
PHASE42

Top trials by phase / activity

NCTPhaseStatusTitle
NCT07218341PHASE4RECRUITINGA Study of Pirtobrutinib (LY3527727) in Participants With Chronic Lymphocytic Leukemia/Small Lymphocytic Lymphoma
NCT02739360PHASE4TERMINATEDRoll Over Study to Provide Idelalisib to Participants Previously Treated With the Investigational PI3Kδ Inhibitor, GS-9820
NCT02970318PHASE3ACTIVE_NOT_RECRUITINGA Study of Acalabrutinib vs Investigator’s Choice of Idelalisib Plus Rituximab or Bendamustine Plus Rituximab in R/R CLL
NCT04666038PHASE3ACTIVE_NOT_RECRUITINGStudy of LOXO-305 (Pirtobrutinib) Versus Investigator’s Choice (Idelalisib Plus Rituximab or Bendamustine Plus Rituximab) in Patients With Previously Treated Chronic Lymphocytic Leukemia (CLL)/Small Lymphocytic Lymphoma (SLL)
NCT06846671PHASE3RECRUITINGA Study of BGB-16673 Compared to Investigator’s Choice in Participants With Chronic Lymphocytic Leukemia or Small Lymphocytic Lymphoma Previously Exposed to Both Bruton Tyrosine Kinase (BTK) and B-cell Leukemia/Lymphoma 2 Protein (BCL2) Inhibitors
NCT07139873PHASE3RECRUITINGA Study of DZD8586 Versus Investigator’s Choice in r/r CLL/SLL (TAI-SHAN6)
NCT01539291PHASE3TERMINATEDExtension Study of Idelalisib in Participants With Chronic Lymphocytic Leukemia (CLL) Who Participated in GS-US-312-0116 (NCT01539512)
NCT01539512PHASE3COMPLETEDA Randomized, Double-Blind, Placebo-Controlled Study of Idelalisib in Combination With Rituximab for Previously Treated Chronic Lymphocytic Leukemia (CLL)
NCT01569295PHASE3COMPLETEDStudy Evaluating the Efficacy and Safety of Idelalisib in Combination With Bendamustine and Rituximab for Previously Treated Chronic Lymphocytic Leukemia (CLL) (Tugela )
NCT01659021PHASE3TERMINATEDEfficacy and Safety of Idelalisib in Combination With Ofatumumab for Previously Treated Chronic Lymphocytic Leukemia
NCT01732913PHASE3TERMINATEDEfficacy and Safety of Idelalisib (GS-1101) in Combination With Rituximab for Previously Treated Indolent Non-Hodgkin Lymphomas
NCT01732926PHASE3TERMINATEDEfficacy and Safety of Idelalisib (GS-1101) in Combination With Bendamustine and Rituximab for Previously Treated Indolent Non-Hodgkin Lymphomas
NCT01980875PHASE3TERMINATEDEfficacy and Safety of Idelalisib in Combination With Obinutuzumab Compared to Chlorambucil in Combination With Obinutuzumab for Previously Untreated Chronic Lymphocytic Leukemia
NCT01980888PHASE3TERMINATEDEfficacy and Safety of Idelalisib in Combination With Bendamustine and Rituximab in Adults With Previously Untreated Chronic Lymphocytic Leukemia
NCT02536300PHASE3TERMINATEDDose Optimization Study of Idelalisib in Follicular Lymphoma
NCT06205290PHASE3WITHDRAWNA Study to Compare the Efficacy and Safety of Lisocabtagene Maraleucel vs Investigator’s Choice Options in Adult Participants With Relapsed or Refractory Chronic Lymphocytic Leukemia or Small Lymphocytic Lymphoma, Whose Disease Has Failed Treatment With Both BTKi and BCL2i Therapies
NCT05725200PHASE2RECRUITINGStudy to Investigate Outcome of Individualized Treatment in Patients With Metastatic Colorectal Cancer
NCT06736990PHASE2ACTIVE_NOT_RECRUITINGA Phase 2 Study of CAL101 in Patients With Idiopathic Pulmonary Fibrosis
NCT01090414PHASE1/PHASE2TERMINATEDAn Extension Study for Subjects Who Are Deriving Benefit With Idelalisib (GS-1101; CAL-101) Following Completion of a Prior Idelalisib Study
NCT01203930PHASE2TERMINATEDA Study of Idelalisib and Rituximab in Elderly Patients With Untreated CLL or SLL
NCT01282424PHASE2COMPLETEDEfficacy and Safety Study of Idelalisib in Participants With Indolent B-Cell Non-Hodgkin Lymphomas
NCT01306643PHASE1/PHASE2COMPLETEDSafety and Efficacy Study of Idelalisib (GS-1101, CAL-101) in Patients With Previously Treated Low-grade Lymphoma
NCT01393106PHASE2COMPLETEDSafety and Efficacy of Idelalisib in Relapsed or Refractory Hodgkin Lymphoma
NCT01620216PHASE2TERMINATEDTargeted Therapy in Treating Patients With Relapsed or Refractory Acute Lymphoblastic Leukemia or Acute Myelogenous Leukemia
NCT01659047PHASE2WITHDRAWNA Phase 2, Single-Arm, Open-Label Study Evaluating the Efficacy and Safety of Single Agent GS 1101 (CAL 101) as Therapy for Previously Treated Chronic Lymphocytic Leukemia
NCT01796470PHASE2TERMINATEDEntospletinib in Combination With Idelalisib in Adults With Relapsed or Refractory Hematologic Malignancies
NCT02044822PHASE2TERMINATEDEfficacy and Safety of Idelalisib in Combination With Rituximab in Patients With Previously Untreated Chronic Lymphocytic Leukemia With 17p Deletion
NCT02135133PHASE2COMPLETEDA Study of Idelalisib (GS1101, CAL101) + Ofatumumab in Previously Untreated CLL/SLL
NCT02258529PHASE2TERMINATEDIdelalisib in Combination With Rituximab for Previously Untreated Follicular Lymphoma and Small Lymphocytic Lymphoma
NCT02332980PHASE2COMPLETEDPembrolizumab Alone or With Idelalisib or Ibrutinib in Treating Patients With Relapsed or Refractory Chronic Lymphocytic Leukemia or Other Low-Grade B-Cell Non-Hodgkin Lymphomas
NCT02439138PHASE2TERMINATEDStudy of Phosphatidylinositol-3-kinase (PI3K) Inhibitor Idelalisib (GS-1101) in Waldenström Macroglobulinemia
NCT02445131PHASE2COMPLETEDSequential Regimen of Bendamustine-Debulking Followed by CAL-101 and GA101-Induction and -Maintenance in CLL (CLL2-BCG)
NCT02590588PHASE2TERMINATEDIdelalisib for Immunoglobulin M (IgM)-Associated Primary (AL) Amyloidosis
NCT02639910PHASE2COMPLETEDStudy to Evaluate Safety and Preliminary Efficacy of Tafasitamab With Idelalisib or Venetoclax in R/R CLL/SLL Patients Pretreated With BTKi
NCT02662296PHASE2WITHDRAWNIbrutinib or Idelalisib in Treating Patients With Persistent or Relapsed Chronic Lymphocytic Leukemia, Small Lymphocytic Lymphoma, or Non-Hodgkin Lymphoma After Donor Stem Cell Transplant
NCT02962401PHASE2COMPLETEDEfficacity of Idelalisib and Obinutuzumab in Patient With Relapsed Refractory Waldenstrom’s Macroglobulinemia
NCT02968563PHASE2COMPLETEDStudy to Evaluate the Safety and Efficacy of the Combination of Tirabrutinib and Idelalisib With and Without Obinutuzumab in Adults With Relapsed or Refractory Chronic Lymphocytic Leukemia (CLL)
NCT03133221PHASE2COMPLETED1630GCC: Zydelig Maintenance in B-Cell Non-Hodgkin’s Lymphoma After Autologous Stem Cell Transplantation
NCT03257722PHASE1/PHASE2TERMINATEDPembrolizumab + Idelalisib for Lung Cancer Study
NCT03576443PHASE2COMPLETEDTrial of Idelalisib in Patients With Relapsed Diffuse Large B-cell Lymphoma

Clinical evidence (CIViC)

Variant × indication × effect (1 predictive associations from 1 curated evidence items):

VariantIndicationEffectTherapyLevelCIViC
PIK3CA P471LMerkel Cell CarcinomaSensitivity/ResponseIdelalisibCIViC CEID739

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

72 molecules share ≥1 primary target. Top 60 by shared-target count:

MoleculeSourceStatusShared targets
CRIZOTINIBChEMBL + PubChemPhase 4 (approved)PIK3CA, PIK3CB, PIK3CD, PIK3CG
INAVOLISIBChEMBL + PubChemPhase 4 (approved)PIK3CA, PIK3CB, PIK3CD, PIK3CG
ALPELISIBChEMBLPhase 4 (approved)PIK3CA, PIK3CB, PIK3CD, PIK3CG
COPANLISIBChEMBLPhase 4 (approved)PIK3CA, PIK3CB, PIK3CD, PIK3CG
DUVELISIBChEMBLPhase 4 (approved)PIK3CA, PIK3CB, PIK3CD, PIK3CG
LENIOLISIBChEMBLPhase 4 (approved)PIK3CA, PIK3CB, PIK3CD, PIK3CG
BUPARLISIBChEMBLPhase 3PIK3CA, PIK3CB, PIK3CD, PIK3CG
DACTOLISIBChEMBLPhase 3PIK3CA, PIK3CB, PIK3CD, PIK3CG
GEDATOLISIBChEMBLPhase 3PIK3CA, PIK3CB, PIK3CD, PIK3CG
LESTAURTINIBChEMBLPhase 3PIK3CA, PIK3CB, PIK3CD, PIK3CG
TASELISIBChEMBLPhase 3PIK3CA, PIK3CB, PIK3CD, PIK3CG
AMG-319ChEMBLPhase 2PIK3CA, PIK3CB, PIK3CD, PIK3CG
APITOLISIBChEMBLPhase 2PIK3CA, PIK3CB, PIK3CD, PIK3CG
AZD-6482ChEMBLPhase 2PIK3CA, PIK3CB, PIK3CD, PIK3CG
BGT-226 FREE BASEChEMBLPhase 2PIK3CA, PIK3CB, PIK3CD, PIK3CG
BIMIRALISIBChEMBLPhase 2PIK3CA, PIK3CB, PIK3CD, PIK3CG
EGANELISIBChEMBLPhase 2PIK3CA, PIK3CB, PIK3CD, PIK3CG
FIMEPINOSTATChEMBLPhase 2PIK3CA, PIK3CB, PIK3CD, PIK3CG
IZORLISIBChEMBLPhase 2PIK3CA, PIK3CB, PIK3CD, PIK3CG
NEMIRALISIBChEMBLPhase 2PIK3CA, PIK3CB, PIK3CD, PIK3CG
OMIPALISIBChEMBLPhase 2PIK3CA, PIK3CB, PIK3CD, PIK3CG
ONATASERTIBChEMBLPhase 2PIK3CA, PIK3CB, PIK3CD, PIK3CG
PAXALISIBChEMBLPhase 2PIK3CA, PIK3CB, PIK3CD, PIK3CG
PF-04691502ChEMBLPhase 2PIK3CA, PIK3CB, PIK3CD, PIK3CG
PICTILISIBChEMBLPhase 2PIK3CA, PIK3CB, PIK3CD, PIK3CG
PILARALISIBChEMBLPhase 2PIK3CA, PIK3CB, PIK3CD, PIK3CG
ROGINOLISIBChEMBLPhase 2PIK3CA, PIK3CB, PIK3CD, PIK3CG
SAMOTOLISIBChEMBLPhase 2PIK3CA, PIK3CB, PIK3CD, PIK3CG
SAPANISERTIBChEMBLPhase 2PIK3CA, PIK3CB, PIK3CD, PIK3CG
SERABELISIBChEMBLPhase 2PIK3CA, PIK3CB, PIK3CD, PIK3CG
TG100-115ChEMBLPhase 2PIK3CA, PIK3CB, PIK3CD, PIK3CG
VISTUSERTIBChEMBLPhase 2PIK3CA, PIK3CB, PIK3CD, PIK3CG
VOXTALISIBChEMBLPhase 2PIK3CA, PIK3CB, PIK3CD, PIK3CG
ZSTK-474ChEMBLPhase 2PIK3CA, PIK3CB, PIK3CD, PIK3CG
AfatinibPubChemApprovedPIK3CA, PIK3CB, PIK3CD, PIK3CG
PazopanibPubChemApprovedPIK3CA, PIK3CB, PIK3CD, PIK3CG
SelumetinibPubChemApprovedPIK3CA, PIK3CB, PIK3CD, PIK3CG
SUNITINIBChEMBLPhase 4 (approved)PIK3CA, PIK3CD, PIK3CG
DEZAPELISIBChEMBLPhase 2PIK3CB, PIK3CD, PIK3CG
QUISINOSTATChEMBLPhase 2PIK3CA, PIK3CB, PIK3CD
RISOVALISIBChEMBLPhase 2PIK3CA, PIK3CB, PIK3CD
SONOLISIBChEMBLPhase 2PIK3CA, PIK3CD, PIK3CG
GefitinibPubChemApprovedPIK3CB, PIK3CD, PIK3CG
DASATINIBChEMBLPhase 4 (approved)PIK3CA, PIK3CD
FEDRATINIBChEMBLPhase 4 (approved)PIK3CA, PIK3CG
UMBRALISIBChEMBLPhase 4 (approved)PIK3CD, PIK3CG
RESVERATROLChEMBLPhase 3PIK3CA, PIK3CB
ACALISIBChEMBLPhase 2PIK3CD, PIK3CG
AMDIZALISIBChEMBLPhase 2PIK3CD, PIK3CG
AZD-8154ChEMBLPhase 2PIK3CA, PIK3CD
BI-2536ChEMBLPhase 2PIK3CA, PIK3CD
GSK-2636771ChEMBLPhase 2PIK3CB, PIK3CD
OSI-027ChEMBLPhase 2PIK3CA, PIK3CG
SELETALISIBChEMBLPhase 2PIK3CD, PIK3CG
TENALISIBChEMBLPhase 2PIK3CD, PIK3CG
BELINOSTATChEMBLPhase 4 (approved)PIK3CA
CAFFEINEChEMBLPhase 4 (approved)PIK3CD
MIDOSTAURINChEMBLPhase 4 (approved)PIK3CA
ROMIDEPSINChEMBLPhase 4 (approved)PIK3CA
THEOPHYLLINEChEMBLPhase 4 (approved)PIK3CD