Copanlisib

drug
On this page

Also known as Copanilisib

Summary

Copanlisib (CHEMBL3218576) is an approved small-molecule EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor (ATC L01EM02) targeting MTOR, PIK3CA, and PIK3CB; indicated across 20 conditions including neoplasm and non-hodgkin lymphoma; with CIViC clinical evidence for 2 variant-indication associations (e.g. PIK3CA Mutation in cancer).

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: L01EM02
  • Targets: 5 (MTOR, PIK3CA, PIK3CB…)
  • Indications: 20 conditions
  • Clinical trials: 57
  • Precision-oncology evidence (CIViC): 2 variant–indication associations
  • Chemistry: 480.5 Da · C23H28N8O4

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL3218576
NameCopanlisib
TypeSmall molecule
Max phase4
FDA approvedno
PubChem CID135565596
ChEBICHEBI:173077
ATCL01EM02
Molecular formulaC23H28N8O4
Molecular weight480.5
InChIKeyMWYDSXOGIBMAET-UHFFFAOYSA-N

SMILES: COC1=C(C=CC2=C3NCCN3C(=NC(=O)C4=CN=C(N=C4)N)N=C21)OCCCN5CCOCC5

IUPAC name: 2-amino-N-[7-methoxy-8-(3-morpholin-4-ylpropoxy)-2,3-dihydro-1H-imidazo[1,2-c]quinazolin-5-ylidene]pyrimidine-5-carboxamide

ChEBI definition: An imidazoquinazoline that is 2,3-dihydroimidazo[1,2-c]quinazoline substituted by (2-aminopyrimidine-5-carbonyl)amino, methoxy, and 3-(morpholin-4-yl)propoxy groups at positions 5, 7 and 8, respectively. It is a intravenous pan-class I PI3K inhibitor used for the treatment of relapsed follicular lymphoma in patients who have received at least 2 prior systemic therapies.

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

Also known as: Copanlisib, COPANLISIB, copanlisib, Copanilisib

Parent form; salt/anhydrous children: CHEMBL3545068

Patent coverage: 1,789 distinct patent families (4,529 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 4,465 (99%) 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
MTORmechanistic target of rapamycin kinaseInhibition7.3598.3% (common-essential)P42345
PIK3CAphosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alphaInhibition9.342.7%P42336
PIK3CBphosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit betaInhibition8.435%P42338
PIK3CDphosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit deltaInhibition9.156%O00329
PIK3CGphosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gammaInhibition8.190.7%P48736

Broader ChEMBL bioactivity targets: 10 (assay-derived). Sample: Muscarinic acetylcholine receptor M2, PI3-kinase p110-alpha/p85-alpha, PI3-kinase p110-delta/p85-alpha, Serine/threonine-protein kinase mTOR, PI3K p110 beta/p85 alpha, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform, Ras-related protein Rab-27A.

Bioactivity

ChEMBL activities: 37 potent at pChembl ≥ 5 of 37 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
PIK3R19.96IC500.11nMCHEMBL_ACT_19060780
PIK3CA9.96IC500.11nMCHEMBL_ACT_25593613
PIK3CD9.74IC500.18nMCHEMBL_ACT_19060853
PIK3CD9.74IC500.18nMCHEMBL_ACT_25593650
PIK3CA9.3IC500.5nMCHEMBL_ACT_16801263
PIK3CA9.3IC500.5nMCHEMBL_ACT_19139825
PIK3CA9.3IC500.5nMCHEMBL_ACT_19214491
PIK3CA9.3IC500.5nMCHEMBL_ACT_25556607
PIK3CA9.3IC500.5nMCHEMBL_ACT_29092034
PIK3CD9.15IC500.7nMCHEMBL_ACT_16801260
PIK3CG9.15IC500.7nMCHEMBL_ACT_19139830
PIK3CG9.15IC500.7nMCHEMBL_ACT_25556626
PIK3CG9.15IC500.7nMCHEMBL_ACT_29092037
PIK3CA8.85IC501.42nMCHEMBL_ACT_25892641
PIK3CG8.78IC501.68nMCHEMBL_ACT_19060851
PIK3CG8.78IC501.68nMCHEMBL_ACT_25593647
PIK3CD8.76IC501.72nMCHEMBL_ACT_25892657
PIK3CB8.43IC503.7nMCHEMBL_ACT_16801262
PIK3CB8.43IC503.7nMCHEMBL_ACT_19139824
PIK3CB8.43IC503.7nMCHEMBL_ACT_19214493
PIK3CB8.43IC503.7nMCHEMBL_ACT_25556617
PIK3CB8.43IC503.7nMCHEMBL_ACT_29092035
PIK3R18.34IC504.57nMCHEMBL_ACT_19060849
PIK3CB8.34IC504.57nMCHEMBL_ACT_25593644
PIK3CG8.19IC506.4nMCHEMBL_ACT_16801261
PIK3CD8.19IC506.4nMCHEMBL_ACT_19139820
PIK3CG8.19IC506.4nMCHEMBL_ACT_19214494
PIK3CD8.19IC506.4nMCHEMBL_ACT_25556641
PIK3CD8.19IC506.4nMCHEMBL_ACT_29092036
PIK3CB8.04IC509.12nMCHEMBL_ACT_25892645

Target pathways

Aggregated over 5 target gene(s): MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG.

Top Reactome pathways

99 total, by targets touching each:

PathwayTargetsGenes
PIP3 activates AKT signaling5MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG
CD28 dependent PI3K/Akt signaling5MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG
Synthesis of PIPs at the plasma membrane4PIK3CA, PIK3CB, PIK3CD, PIK3CG
Constitutive Signaling by Aberrant PI3K in Cancer4PIK3CA, PIK3CB, PIK3CD, PIK3CG
PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling4PIK3CA, PIK3CB, PIK3CD, PIK3CG
Erythropoietin activates Phosphoinositide-3-kinase (PI3K)4PIK3CA, PIK3CB, PIK3CD, PIK3CG
High laminar flow shear stress activates signaling by PIEZO1 and PECAM1:CDH5:KDR in endothelial cells4MTOR, PIK3CA, PIK3CB, PIK3CD
Co-stimulation by ICOS4PIK3CA, PIK3CB, PIK3CD, PIK3CG
GPVI-mediated activation cascade3PIK3CA, PIK3CB, PIK3CG
VEGFA-VEGFR2 Pathway3MTOR, PIK3CA, PIK3CB
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
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
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
phosphatidylinositol 3-kinase/protein kinase B signal transduction5
cell migration4
phosphatidylinositol-3-phosphate biosynthetic process4
phosphatidylinositol phosphate biosynthetic process4
phosphatidylinositol-mediated signaling4
lipid metabolic process4
inflammatory response3
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction3
chemotaxis3
positive regulation of endothelial cell migration3
innate immune response3
positive regulation of lamellipodium assembly2
negative regulation of macroautophagy2
T cell costimulation2
cellular response to insulin stimulus2

Indications & clinical

Indications

20 indications (1 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
neoplasm4MONDO:0005070EFO:0000616
non-Hodgkin lymphoma3MONDO:0018908EFO:0005952
mantle cell lymphoma2MONDO:0018876EFO:1001469
diffuse large B-cell lymphoma2MONDO:0018905EFO:0000403
breast carcinoma2MONDO:0004989EFO:0000305
gallbladder neoplasm2MONDO:0021253EFO:0004606
cholangiocarcinoma2MONDO:0019087EFO:0005221
B-cell chronic lymphocytic leukemia2MONDO:0004948EFO:0000095
breast neoplasm2MONDO:0021100MONDO:0007254
follicular lymphoma2MONDO:0018906MONDO:0018906
uterine corpus cancer2MONDO:0006003EFO:0007532
marginal zone lymphoma2MONDO:0017604EFO:1000630
lymphoma1MONDO:0005062EFO:0000574
squamous cell carcinoma1MONDO:0005096EFO:0000707
colonic neoplasm1MONDO:0005401MONDO:0021063
non-small cell lung carcinoma1MONDO:0005233EFO:0003060
kidney failure1MONDO:0001106HP:0000083
urothelial carcinoma1MONDO:0040679EFO:0008528
acute lymphoblastic leukemia0MONDO:0004967EFO:0000220

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

Clinical trials

Total trials: 57.

Phase distribution

PhaseTrials
PHASE124
PHASE216
PHASE1/PHASE214
PHASE31
EARLY_PHASE11
Not specified1

Top trials by phase / activity

NCTPhaseStatusTitle
NCT02626455PHASE3TERMINATEDStudy of Copanlisib in Combination With Standard Immunochemotherapy in Relapsed Indolent Non-Hodgkin’s Lymphoma (iNHL)
NCT02465060PHASE2ACTIVE_NOT_RECRUITINGTargeted Therapy Directed by Genetic Testing in Treating Patients With Advanced Refractory Solid Tumors, Lymphomas, or Multiple Myeloma (The MATCH Screening Trial)
NCT03474744PHASE2ACTIVE_NOT_RECRUITINGCopanlisib and Rituximab in Marginal Zone Lymphoma Patients
NCT03789240PHASE2ACTIVE_NOT_RECRUITINGResponse-Adapted Therapy With Copanlisib and Rituximab in Untreated Follicular Lymphoma
NCT04253262PHASE1/PHASE2ACTIVE_NOT_RECRUITINGA Study of Copanlisib Combined With Rucaparib in Patients With Metastatic Castration-resistant Prostate Cancer
NCT04572763PHASE1/PHASE2ACTIVE_NOT_RECRUITINGCopanlisib Plus Venetoclax in R/R DLBCL
NCT06360588PHASE2ACTIVE_NOT_RECRUITINGTesting Copanlisib as Potentially Targeting Treatment in Cancers With PTEN Loss (MATCH - Subprotocol Z1G)
NCT06400238PHASE2ACTIVE_NOT_RECRUITINGTesting Copanlisib as Potentially Targeting Treatment in Cancers With PTEN Expression (MATCH - Subprotocol Z1H)
NCT02342665PHASE1/PHASE2COMPLETEDJapanese Phase Ib/II Copanlisib in Relapsed, Indolent B-cell NHL
NCT02455297PHASE2TERMINATEDPhase IIa Study of Copanlisib in Relapsed or Refractory Mantle Cell Lymphoma (MCL)
NCT02535247PHASE1/PHASE2TERMINATEDStudy of MK-3475 Alone or in Combination With Copanlisib in Relapsed or Refractory NK and T-cell Non-Hodgkin Lymphoma
NCT02631590PHASE2COMPLETEDCopanlisib (BAY 80-6946) in Combination With Gemcitabine and Cisplatin in Advanced Cholangiocarcinoma
NCT02728258PHASE2COMPLETEDCopanlisib in Treating Patients With Persistent or Recurrent Endometrial Cancer
NCT02822482PHASE1/PHASE2TERMINATEDCopanlisib in Association With Cetuximab in Patients With Recurrent and/or Metastatic Head and Neck Squamous Cell Carcinomas Harboring a PI3KCA Mutation/Amplification and/or a PTEN Loss
NCT03052933PHASE1/PHASE2COMPLETEDCopanlisib and Gemcitabine in Relapsed/Refractory PTCL
NCT03377101PHASE2WITHDRAWNFulvestrant and Palbociclib With or Without Copanlisib in Treating Patients With Hormone Receptor Positive, HER2 Negative, Stage IV Breast Cancer
NCT03458728PHASE1/PHASE2TERMINATEDSafety, Tolerability, Efficacy and Pharmacokinetics of Copanlisib in Pediatric Patients
NCT03581942PHASE1/PHASE2COMPLETEDCopanlisib With Ibrutinib for Patients With Recurrent/ Refractory Primary Central Nervous System Lymphoma (PCNSL)
NCT03711058PHASE1/PHASE2COMPLETEDStudy of PI3Kinase Inhibition (Copanlisib) and Anti-PD-1 Antibody Nivolumab in Relapsed/Refractory Solid Tumors With Expansions in Mismatch-repair Proficient (MSS) Colorectal Cancer
NCT03803761PHASE1/PHASE2WITHDRAWNA Study of a New Drug Combination, Copanlisib and Fulvestrant, in Advanced Breast Cancer
NCT03877055PHASE1/PHASE2COMPLETEDA Study of Copanlisib and Ibrutinib in Mantle Cell Lymphoma
NCT04108858PHASE1/PHASE2TERMINATEDTesting the Addition of an Anti-cancer Drug, Copanlisib, to the Usual Maintenance Treatment (Trastuzumab and Pertuzumab) After Initial Chemotherapy in a Phase Ib/II Trial for Advanced HER2 Positive Breast Cancer
NCT04155840PHASE2TERMINATEDBendamustine and Rituximab in Combination With Copanlisib for the Treatment of Chronic Lymphocytic Leukemia or Small Lymphocytic Lymphoma
NCT04263584PHASE2UNKNOWNCopanlisib in Combination With Rituximab and CHOP Chemotherapy in Patients With Previously Untreated DLBCL
NCT04433182PHASE2TERMINATEDCopanlisib With Rituximab-Bendamustine in Patients With Relapsed-Refractory Diffuse Large B-cell Lymphoma
NCT04685915PHASE2WITHDRAWNCopanlisib Plus Ibrutinib or Acalabrutinib in R/R CLL
NCT04750941PHASE2TERMINATEDStudy of Copanlisib and Ketogenic Diet
NCT05082025PHASE2TERMINATEDPhase 2 Study of PI3K Inhibitor Copanlisib in Combination With Fulvestrant in Selected ER+ and/or PR+ Cancers With PI3K (PIK3CA, PIK3R1) and/or PTEN Alterations
NCT05387616PHASE2UNKNOWNA Prospective Multicenter Phase 2 Study of the Chemotherapy-Free Combination of the Intravenous Phosphatidylinositol-3-Kinase (PI3K) Inhibitor Copanlisib in Combination With Obinutuzumab in Patients With Previously Untreated Follicular Lymphoma (FL) and a High Tumor Burden
NCT05687721PHASE1/PHASE2WITHDRAWNCopanlisib and Avelumab as a Maintenance Therapy for Advanced Bladder Cancer
NCT06218667PHASE1/PHASE2WITHDRAWNA Study of Copanlisib in Combination with Degarelix in People with Prostate Cancer
NCT03502733PHASE1ACTIVE_NOT_RECRUITINGTesting the Combination of Copanlisib, Nivolumab and Ipilimumab in Patients With Advanced Cancer and Lymphoma
NCT03586661PHASE1ACTIVE_NOT_RECRUITINGNiraparib and Copanlisib in Treating Patients With Recurrent Endometrial, Ovarian, Primary Peritoneal, or Fallopian Tube Cancer
NCT03884998PHASE1ACTIVE_NOT_RECRUITINGCopanlisib and Nivolumab in Treating Patients With Richter’s Transformation or Transformed Indolent Non-Hodgkin Lymphoma
NCT01392521PHASE1COMPLETEDPhase Ib Study of PI3(Phosphoinositol 3)-Kinase Inhibitor Copanlisib With MEK (Mitogen-activated Protein Kinase) Inhibitor Refametinib (BAY86-9766) in Patients With Advanced Cancer
NCT01404390PHASE1COMPLETEDJapanese BAY80-6946 Monotherapy Phase I Study
NCT01411410PHASE1COMPLETEDPhase I Study of PI3(Phosphoinositol 3)-Kinase Inhibitor BAY80-6946 With Paclitaxel in Patients With Advanced Cancer
NCT01460537PHASE1COMPLETEDPhase 1 Study of PI3 (Phosphatidylinositol-3)-Kinase Inhibitor Copanlisib With Gemcitabine or Cisplatin Plus Gemcitabine in Patients With Advanced Cancer
NCT02119221PHASE1COMPLETEDCopanlisib Mass Balance Study
NCT02155582PHASE1COMPLETEDCopanlisib Pharmacodynamic Study

Clinical evidence (CIViC)

Variant × indication × effect (2 predictive associations from 2 curated evidence items):

VariantIndicationEffectTherapyLevelCIViC
PIK3CA MutationCancerSensitivity/ResponseCopanlisibCIViC BEID11678
AURKB OverexpressionHead And Neck Squamous Cell CarcinomaSensitivity/ResponseAlisertib + Barasertib + CopanlisibCIViC DEID10836

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.

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

MoleculeSourceStatusShared targets
CrizotinibChEMBL + PubChemPhase 4 (approved)MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG
IdelalisibChEMBL + PubChemPhase 4 (approved)MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG
ALPELISIBChEMBLPhase 4 (approved)MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG
BUPARLISIBChEMBLPhase 3MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG
DACTOLISIBChEMBLPhase 3MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG
GEDATOLISIBChEMBLPhase 3MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG
TASELISIBChEMBLPhase 3MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG
APITOLISIBChEMBLPhase 2MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG
AZD-6482ChEMBLPhase 2MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG
BGT-226 FREE BASEChEMBLPhase 2MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG
BIMIRALISIBChEMBLPhase 2MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG
FIMEPINOSTATChEMBLPhase 2MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG
IZORLISIBChEMBLPhase 2MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG
OMIPALISIBChEMBLPhase 2MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG
ONATASERTIBChEMBLPhase 2MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG
PAXALISIBChEMBLPhase 2MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG
PF-04691502ChEMBLPhase 2MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG
PICTILISIBChEMBLPhase 2MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG
SAMOTOLISIBChEMBLPhase 2MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG
SAPANISERTIBChEMBLPhase 2MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG
TG100-115ChEMBLPhase 2MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG
VISTUSERTIBChEMBLPhase 2MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG
VOXTALISIBChEMBLPhase 2MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG
ZSTK-474ChEMBLPhase 2MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG
AfatinibPubChemApprovedMTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG
PazopanibPubChemApprovedMTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG
SelumetinibPubChemApprovedMTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG
INAVOLISIBChEMBL + PubChemPhase 4 (approved)PIK3CA, PIK3CB, PIK3CD, PIK3CG
DUVELISIBChEMBLPhase 4 (approved)PIK3CA, PIK3CB, PIK3CD, PIK3CG
LENIOLISIBChEMBLPhase 4 (approved)PIK3CA, PIK3CB, PIK3CD, PIK3CG
LESTAURTINIBChEMBLPhase 3PIK3CA, PIK3CB, PIK3CD, PIK3CG
AMG-319ChEMBLPhase 2PIK3CA, PIK3CB, PIK3CD, PIK3CG
EGANELISIBChEMBLPhase 2PIK3CA, PIK3CB, PIK3CD, PIK3CG
NEMIRALISIBChEMBLPhase 2PIK3CA, PIK3CB, PIK3CD, PIK3CG
PILARALISIBChEMBLPhase 2PIK3CA, PIK3CB, PIK3CD, PIK3CG
ROGINOLISIBChEMBLPhase 2PIK3CA, PIK3CB, PIK3CD, PIK3CG
SERABELISIBChEMBLPhase 2PIK3CA, PIK3CB, PIK3CD, PIK3CG
SONOLISIBChEMBLPhase 2MTOR, PIK3CA, PIK3CD, PIK3CG
GefitinibPubChemApprovedMTOR, PIK3CB, PIK3CD, PIK3CG
DASATINIBChEMBLPhase 4 (approved)MTOR, PIK3CA, PIK3CD
SUNITINIBChEMBLPhase 4 (approved)PIK3CA, PIK3CD, PIK3CG
RESVERATROLChEMBLPhase 3MTOR, PIK3CA, PIK3CB
DEZAPELISIBChEMBLPhase 2PIK3CB, PIK3CD, PIK3CG
OSI-027ChEMBLPhase 2MTOR, PIK3CA, PIK3CG
QUISINOSTATChEMBLPhase 2PIK3CA, PIK3CB, PIK3CD
RISOVALISIBChEMBLPhase 2PIK3CA, PIK3CB, PIK3CD
FEDRATINIBChEMBLPhase 4 (approved)PIK3CA, PIK3CG
UMBRALISIBChEMBLPhase 4 (approved)PIK3CD, PIK3CG
EPIGALOCATECHIN GALLATEChEMBLPhase 3MTOR, PIK3CA
ACALISIBChEMBLPhase 2PIK3CD, PIK3CG
AMDIZALISIBChEMBLPhase 2PIK3CD, PIK3CG
AZD-8154ChEMBLPhase 2PIK3CA, PIK3CD
BERZOSERTIBChEMBLPhase 2MTOR, PIK3CA
BI-2536ChEMBLPhase 2PIK3CA, PIK3CD
CC-115ChEMBLPhase 2MTOR, PIK3CA
GSK-2636771ChEMBLPhase 2PIK3CB, PIK3CD
SELETALISIBChEMBLPhase 2PIK3CD, PIK3CG
TENALISIBChEMBLPhase 2PIK3CD, PIK3CG
AMIODARONEChEMBLPhase 4 (approved)MTOR
AMITRIPTYLINEChEMBLPhase 4 (approved)MTOR