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Taselisib

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Also known as GDC-0032RG-7604

Summary

Taselisib (CHEMBL2387080) is a phase-3 clinical-stage small molecule targeting PIK3CA, PIK3CB, and PIK3CD; indicated across 6 conditions including breast neoplasm and squamous cell lung carcinoma; with CIViC clinical evidence for 7 variant-indication associations (e.g. PIK3CA Mutation in lung non-small cell carcinoma).

At a glance

  • Status: Max clinical phase 3 (not approved)
  • Modality: Small molecule
  • Targets: 4 (PIK3CA, PIK3CB, PIK3CD…)
  • Indications: 6 conditions
  • Clinical trials: 15
  • Precision-oncology evidence (CIViC): 7 variant–indication associations
  • Chemistry: 460.5 Da · C24H28N8O2

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL2387080
NameTaselisib
TypeSmall molecule
Max phase3
FDA approvedno
PubChem CID51001932
Molecular formulaC24H28N8O2
Molecular weight460.5
InChIKeyBEUQXVWXFDOSAQ-UHFFFAOYSA-N

SMILES: CC1=NN(C(=N1)C2=CN3CCOC4=C(C3=N2)C=CC(=C4)C5=CN(N=C5)C(C)(C)C(=O)N)C(C)C

IUPAC name: 2-methyl-2-[4-[2-(5-methyl-2-propan-2-yl-1,2,4-triazol-3-yl)-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepin-9-yl]pyrazol-1-yl]propanamide

Also known as: GDC-0032, RG-7604, Taselisib, TASELISIB

Patent coverage: 1,249 distinct patent families (3,473 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 2,855 (82%) 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 alphaInhibition10.0542.7%P42336
PIK3CBphosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit betaInhibition7.285%P42338
PIK3CDphosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit deltaInhibition10.16%O00329
PIK3CGphosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gammaInhibition8.840.7%P48736

Broader ChEMBL bioactivity targets: 8 (assay-derived). Sample: Phosphatidylinositol 3-kinase catalytic subunit type 3, Serine/threonine-protein kinase mTOR, 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, Phosphatidylinositol 3-kinase regulatory subunit beta, Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta.

Bioactivity

ChEMBL activities: 35 potent at pChembl ≥ 5 of 35 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
PIK3CD10.1Ki0.08nMCHEMBL_ACT_26989741
PIK3CG10.1Ki0.08nMCHEMBL_ACT_28202294
PIK3CG10.1Ki0.08nMCHEMBL_ACT_28202399
PIK3CA10.05Ki0.09nMCHEMBL_ACT_24873749
PIK3CA10.05Ki0.09nMCHEMBL_ACT_28202288
PIK3CA10.05Ki0.09nMCHEMBL_ACT_28202396
PIK3CD9.92Ki0.12nMCHEMBL_ACT_13313861
PIK3CD9.92Ki0.12nMCHEMBL_ACT_24954268
PIK3CA9.54Ki0.29nMCHEMBL_ACT_13313974
PIK3CA9.54Ki0.29nMCHEMBL_ACT_24954266
PIK3CA9.54IC500.29nMCHEMBL_ACT_29205883
PIK3CA9.52Ki0.3nMCHEMBL_ACT_16485089
PIK3CG9.04IC500.91nMCHEMBL_ACT_29205889
PIK3CG9.01Ki0.97nMCHEMBL_ACT_13313860
PIK3CG9.01Ki0.97nMCHEMBL_ACT_24954269
PIK3CD9.01IC500.97nMCHEMBL_ACT_29205892
PIK3CG8.85Ki1.43nMCHEMBL_ACT_26989744
PIK3CD8.85Ki1.43nMCHEMBL_ACT_28202297
PIK3CA8.4IC504nMCHEMBL_ACT_13313948
PIK3CA8.4IC504nMCHEMBL_ACT_24953800
PIK3CB8.4IC504nMCHEMBL_ACT_24953801
PIK3CD8.4IC504nMCHEMBL_ACT_24953802
PIK3CG8.4IC504nMCHEMBL_ACT_24953803
PIK3CB8.04Ki9.1nMCHEMBL_ACT_13313862
PIK3CB8.04Ki9.1nMCHEMBL_ACT_24954267
PIK3CA7.62EC5024nMCHEMBL_ACT_24873822
PIK3CD7.62Ki23.7nMCHEMBL_ACT_26989846
PIK3CA7.51IC5031nMCHEMBL_ACT_13313859
PIK3R27.28Ki53nMCHEMBL_ACT_26989738
PIK3CB7.28Ki53nMCHEMBL_ACT_28202291

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

6 indications (0 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 neoplasm3MONDO:0021100MONDO:0007254
squamous cell lung carcinoma2MONDO:0005097EFO:0000708
plasma cell myeloma2MONDO:0009693EFO:0001378
non-Hodgkin lymphoma1MONDO:0018908EFO:0005952
lung neoplasm1MONDO:0021117MONDO:0008903
triple-negative breast carcinoma1MONDO:0005494EFO:0005537

Clinical trials

Total trials: 15.

Phase distribution

PhaseTrials
PHASE16
PHASE24
PHASE1/PHASE23
PHASE31
Not specified1

Top trials by phase / activity

NCTPhaseStatusTitle
NCT02340221PHASE3TERMINATEDA Study of Taselisib + Fulvestrant Versus Placebo + Fulvestrant in Participants With Advanced or Metastatic Breast Cancer Who Have Disease Recurrence or Progression During or After Aromatase Inhibitor Therapy
NCT02465060PHASE2ACTIVE_NOT_RECRUITINGTargeted Therapy Directed by Genetic Testing in Treating Patients With Advanced Refractory Solid Tumors, Lymphomas, or Multiple Myeloma (The MATCH Screening Trial)
NCT04439175PHASE2ACTIVE_NOT_RECRUITINGTesting GDC-0032 (Taselisib) as a Potential Targeted Treatment in Cancers With PIK3CA Genetic Changes (MATCH-Subprotocol I)
NCT02273973PHASE2COMPLETEDA Study of Neoadjuvant Letrozole + Taselisib Versus Letrozole + Placebo in Post-Menopausal Women With Breast Cancer (LORELEI)
NCT02285179PHASE1/PHASE2COMPLETEDClinical Trial to Evaluate the Safety and Effectiveness of GDC-0032 When Given Alongside Tamoxifen
NCT02457910PHASE1/PHASE2TERMINATEDTaselisib and Enzalutamide in Treating Patients With Androgen Receptor Positive Triple-Negative Metastatic Breast Cancer
NCT02785913PHASE2COMPLETEDLung-MAP: Taselisib as Therapy in Treating Patients With Stage IV Squamous Cell Lung Cancer and Positive Biomarker Matches
NCT03290092PHASE1/PHASE2TERMINATEDTrial of Taselisib in Overgrowth
NCT01296555PHASE1TERMINATEDA Dose Escalation Study Evaluating the Safety and Tolerability of GDC-0032 in Participants With Locally Advanced or Metastatic Solid Tumors or Non-Hodgkin’s Lymphoma (NHL) and in Combination With Endocrine Therapy in Locally Advanced or Metastatic Hormone Receptor-Positive Breast Cancer
NCT01814709PHASE1COMPLETEDA Drug Interaction Study of GDC-0032 Co-administered With Rifampin or Itraconazole in Healthy Volunteers
NCT01862081PHASE1COMPLETEDA Dose-escalation Study to Assess the Safety, Tolerability, and Pharmacokinetics of GDC-0032 in Combination With Docetaxel or With Paclitaxel in Patients With HER2-negative Locally Recurrent or Metastatic Breast Cancer or Non-small Cell Lung Cancer
NCT01967966PHASE1COMPLETEDA Bioavailability and Pharmacokinetic Study of GDC-0032 in Healthy Volunteers
NCT01980953PHASE1COMPLETEDA Study to Evaluate the Effect of Particle Size, Formulation and Food on the Pharmacokinetics of GDC-0032 in Healthy Volunteers
NCT02390427PHASE1COMPLETEDPhase Ib Dose-escalation Trial of Taselisib (GDC-0032) in Combination With Anti-HER2 Therapies in Participants With Advanced HER2+ Breast Cancer
NCT02154490Not specifiedCOMPLETEDLung-MAP: Biomarker-Targeted Second-Line Therapy in Treating Patients With Recurrent Stage IV Squamous Cell Lung Cancer

Clinical evidence (CIViC)

Variant × indication × effect (7 predictive associations from 7 curated evidence items):

VariantIndicationEffectTherapyLevelCIViC
PIK3CA MutationLung Non-small Cell CarcinomaSensitivity/ResponseTaselisibCIViC BEID7400
PIK3CA MutationCancerSensitivity/ResponseTaselisibCIViC CEID11679
CCNE1 AmplificationEndometrial Serous AdenocarcinomaSensitivity/ResponseTaselisib + FadraciclibCIViC DEID10181
PIK3CA AmplificationHead And Neck Squamous Cell CarcinomaSensitivity/ResponseTaselisibCIViC DEID1464
PIK3CA H1047RHead And Neck Squamous Cell CarcinomaSensitivity/ResponseTaselisibCIViC DEID1465
PIK3CA MutationHead And Neck Squamous Cell CarcinomaSensitivity/ResponseTaselisib + Radiation TherapyCIViC DEID1490
PTEN MutationHead And Neck Squamous Cell CarcinomaResistanceTaselisibCIViC DEID1467

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
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
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

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

Generated
Atlas version
v1.1.2
BioBTree
v2.0.2

Sources 30

This page pulls from 30 datasets indexed by BioBTree:

chebichembl_activitychembl_moleculechembl_targetcivic_evidenceclingen_dosageclinical_trialsdepmapefoensemblentrezgogoparentgtopdbgtopdb_interactiongtopdb_ligandhgncmeshmondomsigdbpatent_compoundpharmgkbpharmgkb_guidelinepubchempubchem_activityreactomereactomeparentrefseqtranscriptuniprot