Alpelisib

drug
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Also known as Byl-719BYL719NVP-BYL719PiqrayVijoiceALPELISIB (BYL719)AlpesilibAlpelisib

Summary

Alpelisib (CHEMBL2396661) is an approved small molecule (ATC L01EM03) targeting PIK3CA, PIK3CB, and PIK3CD; indicated across 25 conditions including breast carcinoma and neoplasm; with CIViC clinical evidence for 20 variant-indication associations (e.g. PIK3CA C420R in breast cancer).

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: L01EM03
  • Targets: 4 (PIK3CA, PIK3CB, PIK3CD…)
  • Indications: 25 conditions
  • Clinical trials: 97
  • Precision-oncology evidence (CIViC): 20 variant–indication associations
  • Chemistry: 441.5 Da · C19H22F3N5O2S

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL2396661
NameAlpelisib
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID56649450
ATCL01EM03
Molecular formulaC19H22F3N5O2S
Molecular weight441.5
InChIKeySTUWGJZDJHPWGZ-LBPRGKRZSA-N

SMILES: CC1=C(SC(=N1)NC(=O)N2CCC[C@H]2C(=O)N)C3=CC(=NC=C3)C(C)(C)C(F)(F)F

IUPAC name: (2S)-1-N-[4-methyl-5-[2-(1,1,1-trifluoro-2-methylpropan-2-yl)-4-pyridinyl]-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide

Also known as: Alpelisib, Byl-719, BYL719, NVP-BYL719, Piqray, Vijoice, BYL-719, ALPELISIB, VIJOICE, PIQRAY, ALPELISIB (BYL719), alpelisib

Patent coverage: 2,467 distinct patent families (6,070 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 5,778 (95%) 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 alphaInhibition8.342.7%P42336
PIK3CBphosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit betaInhibition5.925%P42338
PIK3CDphosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit deltaInhibition6.546%O00329
PIK3CGphosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gammaInhibition6.60.7%P48736

Broader ChEMBL bioactivity targets: 12 (assay-derived). Sample: PI3-kinase p110-alpha/p85-alpha, PI3-kinase p110-delta/p85-alpha, cAMP-dependent protein kinase catalytic subunit gamma, 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-kinase beta, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform.

Bioactivity

ChEMBL activities: 64 potent at pChembl ≥ 5 of 64 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
PIK3CA8.77IC501.7nMCHEMBL_ACT_26030793
PIK3CA8.52IC503nMCHEMBL_ACT_25715642
PIK3R18.41IC503.9nMCHEMBL_ACT_22965936
PIK3CA8.4IC504nMCHEMBL_ACT_29055512
PIK3CA8.34IC504.6nMCHEMBL_ACT_16756869
PIK3CA8.34IC504.6nMCHEMBL_ACT_25645332
PIK3CA8.34IC504.6nMCHEMBL_ACT_25715517
PIK3CA8.32IC504.8nMCHEMBL_ACT_25715518
PIK3CA8.3IC505nMCHEMBL_ACT_13350818
PIK3CA8.3IC505nMCHEMBL_ACT_15687183
PIK3CA8.3IC505nMCHEMBL_ACT_15694977
PIK3CA8.3IC505nMCHEMBL_ACT_18135347
PIK3CA8.3IC505nMCHEMBL_ACT_22899846
PIK3CA8.3IC505nMCHEMBL_ACT_24954273
PIK3CA8.3IC505nMCHEMBL_ACT_25636466
PIK3CA8.3IC505nMCHEMBL_ACT_29055476
PIK3CA8.3IC505nMCHEMBL_ACT_29057539
PIK3CA8.21IC506.1nMCHEMBL_ACT_25956318
PIK3CA8.02IC509.5nMCHEMBL_ACT_22851172
PIK3CA7.75IC5017.8nMCHEMBL_ACT_22909027
PI4KB7.41IC5039nMCHEMBL_ACT_29165504
PIK3CD7.16IC5069nMCHEMBL_ACT_25636516
PIK3CD7.14IC5072nMCHEMBL_ACT_22966019
PIK3CA7.13IC5074nMCHEMBL_ACT_13350733
PIK3CA7.13IC5074nMCHEMBL_ACT_15686586
PIK3CA7.13IC5074nMCHEMBL_ACT_24953807
PIK3CA7.06IC5087nMCHEMBL_ACT_29294706
PIK3CG7.03IC5094nMCHEMBL_ACT_22965954
PIK3CG6.99IC50102nMCHEMBL_ACT_25636513
PIK3CG6.86IC50139nMCHEMBL_ACT_22851158

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

25 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
breast carcinoma4MONDO:0004989EFO:0000305
neoplasm4MONDO:0005070EFO:0000616
breast neoplasm4MONDO:0021100EFO:0003869
head and neck squamous cell carcinoma2MONDO:0010150EFO:0000181
squamous cell carcinoma2MONDO:0005096EFO:0000707
upper aerodigestive tract neoplasm2MONDO:0005398EFO:0004284
endometrium neoplasm2MONDO:0021251MONDO:0011962
triple-negative breast carcinoma2MONDO:0005494EFO:0005537
ovarian carcinoma2MONDO:0005140EFO:0001075
colorectal neoplasm2MONDO:0005335MONDO:0005575
lymphedema2MONDO:0019297MONDO:0019313
liver disorder1MONDO:0005154EFO:0001421
plasma cell myeloma1MONDO:0009693EFO:0001378
exocrine pancreatic carcinoma1MONDO:0005192EFO:0002618
esophageal squamous cell carcinoma1MONDO:0005580EFO:0005922
rectal cancer1MONDO:0006519EFO:1000657
oropharynx cancer1MONDO:0004608EFO:1001931
gastric neoplasm1MONDO:0021085MONDO:0001056
gastrointestinal stromal tumor1MONDO:0011719MONDO:0011719
meningioma1MONDO:0016642MONDO:0016642
uveal melanoma1MONDO:0006486EFO:1000616

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

Clinical trials

Total trials: 97.

Phase distribution

PhaseTrials
PHASE233
PHASE132
Not specified11
PHASE39
PHASE1/PHASE29
PHASE41
PHASE2/PHASE31
EARLY_PHASE11

Top trials by phase / activity

NCTPhaseStatusTitle
NCT05631795PHASE4COMPLETEDStudy to Assess the Safety of Alpelisib Plus Fulvestrant, in Men and Post-menopausal Women With HR-positive, HER2-negative, Advanced Breast Cancer (aBC) With PIK3CA Mutation, Whose Disease Progressed on or After Endocrine Treatment
NCT04208178PHASE3ACTIVE_NOT_RECRUITINGStudy of Alpelisib (BYL719) in Combination With Trastuzumab and Pertuzumab as Maintenance Therapy in Patients With HER2-positive Advanced Breast Cancer With a PIK3CA Mutation
NCT05038735PHASE3ACTIVE_NOT_RECRUITINGStudy to Assess the Efficacy and Safety of Alpelisib Plus Fulvestrant in Participants With HR-positive (HR+), HER2-negative, Advanced Breast Cancer After Treatment With a CDK4/6 Inhibitor and an Aromatase Inhibitor.
NCT05063786PHASE3ACTIVE_NOT_RECRUITINGTrastuzumab + Alpelisib +/- Fulvestrant vs Trastuzumab + CT in Patients With PIK3CA Mutated Previously Treated HER2+ Advanced BrEasT Cancer (ALPHABET)
NCT05501886PHASE3ACTIVE_NOT_RECRUITINGGedatolisib Plus Fulvestrant With or Without Palbociclib vs Standard-of-Care for the Treatment of Patients With Advanced or Metastatic HR+/HER2- Breast Cancer (VIKTORIA-1)
NCT05646862PHASE3ACTIVE_NOT_RECRUITINGA Study Evaluating the Efficacy and Safety of Inavolisib Plus Fulvestrant Compared With Alpelisib Plus Fulvestrant in Participants With HR-Positive, HER2-Negative, PIK3CA Mutated, Locally Advanced or Metastatic Breast Cancer Post CDK4/6i and Endocrine Combination Therapy
NCT05948943PHASE2/PHASE3RECRUITINGAlpelisib in Pediatric and Adult Patients With Lymphatic Malformations Associated With a PIK3CA Mutation.
NCT02437318PHASE3COMPLETEDStudy Assessing the Efficacy and Safety of Alpelisib Plus Fulvestrant in Men and Postmenopausal Women With Advanced Breast Cancer Which Progressed on or After Aromatase Inhibitor Treatment.
NCT03439046PHASE3COMPLETEDStudy of the Molecular Features of Postmenopausal Women With HR+ HER2-negative aBC on First-line Treatment With Ribociclib and Letrozole and, in Patients With a PIK3CA Mutation, on Second-line Treatment With Alpelisib Plus Fulvestrant
NCT04251533PHASE3TERMINATEDStudy Assessing the Efficacy and Safety of Alpelisib + Nab-paclitaxel in Subjects With Advanced TNBC Who Carry Either a PIK3CA Mutation or Have PTEN Loss
NCT04729387PHASE3TERMINATEDAlpelisib Plus Olaparib in Platinum-resistant/Refractory, High-grade Serous Ovarian Cancer, With no Germline BRCA Mutation Detected
NCT01872260PHASE1/PHASE2ACTIVE_NOT_RECRUITINGStudy of LEE011, BYL719 and Letrozole in Advanced ER+ Breast Cancer
NCT02925234PHASE2RECRUITINGThe Drug Rediscovery Protocol (DRUP Trial)
NCT04524000PHASE2ACTIVE_NOT_RECRUITINGStudy Assessing the Efficacy and Safety of Treatment With Alpelisib Plus Fulvestrant in Japanese Men and Postmenopausal Women With Advanced Breast Cancer
NCT04544189PHASE2ACTIVE_NOT_RECRUITINGStudy Assessing the Efficacy and Safety of Treatment With Alpelisib Plus Fulvestrant Versus Placebo Plus Fulvestrant in Chinese Men and Postmenopausal Women With Advanced Breast Cancer
NCT04589650PHASE2ACTIVE_NOT_RECRUITINGStudy Assessing the Efficacy, Safety and PK of Alpelisib (BYL719) in Pediatric and Adult Patients With PIK3CA-related Overgrowth Spectrum
NCT04762979PHASE2ACTIVE_NOT_RECRUITINGAlpelisib (BYL719) in Combination With Continued Endocrine Therapy Following Progression on Endocrine Therapy in Hormone Receptor Positive, HER2 Negative, PIK3CA Mutant Metastatic Breast Cancer
NCT04980833PHASE2ACTIVE_NOT_RECRUITINGStudy Assessing Long-term Safety and Efficacy of Alpelisib in Patients With PIK3CA-Related Overgrowth Spectrum (PROS) Who Previously Participated in Study CBYL719F12002 (EPIK-P1)
NCT05090358PHASE2ACTIVE_NOT_RECRUITINGPreventing High Blood Sugar in People Being Treated for Metastatic Breast Cancer
NCT05154487PHASE2ACTIVE_NOT_RECRUITINGA Study of Alpelisib and Fulvestrant to Treat Endometrial Cancer
NCT05230810PHASE1/PHASE2ACTIVE_NOT_RECRUITINGClinical Trial of Alpelisb and Tucatinib in Patients With PIK3CA-Mutant HER2+ Metastatic Breast Cancer.
NCT05563220PHASE1/PHASE2RECRUITINGOpen-Label Umbrella Study To Evaluate Safety And Efficacy Of Elacestrant In Various Combination In Participants With Metastatic Breast Cancer
NCT05564377PHASE2RECRUITINGTargeted Therapy Directed by Genetic Testing in Treating Patients With Locally Advanced or Advanced Solid Tumors, The ComboMATCH Screening Trial
NCT05577754PHASE2RECRUITINGAssessment of the Efficacy and Safety of Alpelisib (BYL719) in Pediatric and Adult Patients With Megalencephaly-CApillary Malformation Polymicrogyria Syndrome (MCAP)
NCT05625087PHASE2ACTIVE_NOT_RECRUITINGDetection of Tumor DNA in the Blood of Patients Receiving Standard Therapy for Hormone Receptor-positive (HR+) Non-HER2 Expressing (HER2-) Metastatic Breast Cancer as a Tool to Select Those Who May Benefit From the Next Course of Fulvestrant in Combination With Alpelisib or Ribociclib
NCT05933395PHASE2RECRUITINGGenetically-informed Therapy for ER+ Breast Cancer Post-CDK4/6 Inhibitor
NCT05983159PHASE2RECRUITINGA Trial of Targeted Therapies for Patients With Slow-Flow or Fast-Flow Vascular Malformations
NCT06145308PHASE2RECRUITINGPrecision Treatment of Recurrent/Metastatic Salivary Gland Carcinoma Guided by Molecular Typing
NCT06739395PHASE2RECRUITINGPrecision Medicine Trial Based on Molecular Matching Therapy for Patients With Standard Treatment Exhaustion
NCT06997588PHASE2RECRUITINGEPIK-P4: A Phase II Single-arm Study to Assess the Efficacy, Safety and Pharmacokinetics of Alpelisib (BYL719) in Pediatric and Adult Patients With PIK3CA-related Overgrowth Spectrum (PROS)
NCT07543822PHASE2ACTIVE_NOT_RECRUITING24VA022; VATCH Alpelisib for TIE2/PIK3CA Pathway VAs
NCT01708161PHASE1/PHASE2TERMINATEDA Phase Ib/II Study of the Combination of BYL719 Plus AMG 479 in Adult Patients With Selected Solid Tumors
NCT01719380PHASE2COMPLETEDStudy of LGX818 and Cetuximab or LGX818, BYL719, and Cetuximab in BRAF Mutant Metastatic Colorectal Cancer
NCT01923168PHASE2COMPLETEDStudy of Letrozole With or Without BYL719 or Buparlisib, for the Neoadjuvant Treatment of Postmenopausal Women
NCT02145312PHASE2UNKNOWNAn Open Label, Single Arm, Multicenter Phase II Study of BYL719 in Patients With Recurrent or Metastatic Squamous Cell Carcinoma of Head and Neck Who Failed to Respond to Platinum-based Therapy.
NCT02276027PHASE2COMPLETEDA Phase II, Open Label, Multiple Arm Study of AUY922, BYL719, INC280, LDK378 and MEK162 in Chinese Patients With Advanced Non-small Cell Lung Cancer
NCT02298595PHASE1/PHASE2WITHDRAWNCetuximab, Cisplatin and BYL719 for HPV-Associated Oropharyngeal Squamous Cell Carcinoma
NCT02379247PHASE1/PHASE2COMPLETEDBYL719 and Nab-Paclitaxel in Locally Recurrent or Metastatic HER-2 Negative Breast Cancer
NCT02506556PHASE2COMPLETEDPhosphatidylinositol 3-kinase (PI3K) Alpha iNhibition In Advanced Breast Cancer
NCT03056755PHASE2COMPLETEDStudy Assessing the Efficacy and Safety of Alpelisib Plus Fulvestrant or Letrozole, Based on Prior Endocrine Therapy, in Patients With PIK3CA Mutant, HR+, HER2- Advanced Breast Cancer Who Have Progressed on or After Prior Treatments

Clinical evidence (CIViC)

Variant × indication × effect (20 predictive associations from 21 curated evidence items):

VariantIndicationEffectTherapyLevelCIViC
PIK3CA C420RBreast CancerSensitivity/ResponseAlpelisib + FulvestrantCIViC AEID11275
PIK3CA E542KBreast CancerSensitivity/ResponseFulvestrant + AlpelisibCIViC AEID7315
PIK3CA E545K OR PIK3CA E545A OR PIK3CA E545G OR PIK3CA E545DBreast CancerSensitivity/ResponseFulvestrant + AlpelisibCIViC AEID7468
PIK3CA H1047R OR PIK3CA H1047Y OR PIK3CA H1047LBreast CancerSensitivity/ResponseFulvestrant + AlpelisibCIViC AEID7318
PIK3CA MutationBreast CancerSensitivity/ResponseAlpelisib + FulvestrantCIViC AEID7313
PIK3CA Q546E OR PIK3CA Q546RBreast CancerSensitivity/ResponseFulvestrant + AlpelisibCIViC AEID7316
BRAF V600Colorectal CancerSensitivity/ResponseCetuximab + Encorafenib + AlpelisibCIViC BEID6047
SGK1 OverexpressionBreast CancerResistanceAlpelisibCIViC BEID1730 +1
RB1 PHOSPHORYLATIONBreast CancerResistanceAlpelisibCIViC BEID1609
PIK3CA P447_L455delEstrogen-receptor Positive Breast CancerSensitivity/ResponseLetrozole + AlpelisibCIViC CEID9575
PIK3CA Q75ESquamous Cell CarcinomaSensitivity/ResponseAlpelisibCIViC CEID12159
CDK4 EXPRESSIONEstrogen-receptor Positive Breast CancerSensitivity/ResponseAlpelisibCIViC DEID264
PIK3CA AmplificationStomach CarcinomaSensitivity/ResponseAlpelisibCIViC DEID1403
PIK3CA H1047RHead And Neck CancerSensitivity/ResponseAlpelisibCIViC DEID1401
PIK3CA MutationCancerSensitivity/ResponseAlpelisibCIViC DEID1402
PIK3CA N345K OR PIK3CA M1043V OR PIK3CA Q75ESquamous Cell CarcinomaSensitivity/ResponseAlpelisibCIViC DEID12160
PTEN MutationProstate AdenocarcinomaSensitivity/ResponsePI3Kbeta Inhibitor AZD8186 + Enzalutamide + AlpelisibCIViC DEID1522
SGK1 OverexpressionBreast CancerSensitivity/ResponseSGK1-Inh + AlpelisibCIViC DEID1731
HRAS G12VHead And Neck Squamous Cell CarcinomaResistanceAlpelisibCIViC DEID9087
PTEN LossBreast CancerResistanceAlpelisibCIViC DEID716

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

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
IDELALISIBChEMBL + PubChemPhase 4 (approved)PIK3CA, PIK3CB, PIK3CD, PIK3CG
INAVOLISIBChEMBL + PubChemPhase 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