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Parsaclisib

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Also known as INCB-050465Incb050465

Summary

Parsaclisib (CHEMBL4297615) is a phase-3 clinical-stage small molecule (ATC L01EM05) targeting PIK3CD; indicated across 17 conditions including neoplasm and autoimmune hemolytic anemia.

At a glance

  • Status: Max clinical phase 3 (not approved)
  • Modality: Small molecule
  • ATC class: L01EM05
  • Targets: 1 (PIK3CD)
  • Indications: 17 conditions
  • Clinical trials: 34
  • Chemistry: 432.9 Da · C20H22ClFN6O2

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL4297615
NameParsaclisib
TypeSmall molecule
Max phase3
FDA approvedno
PubChem CID86677874
ATCL01EM05
Molecular formulaC20H22ClFN6O2
Molecular weight432.9
InChIKeyZQPDJCIXJHUERQ-QWRGUYRKSA-N

SMILES: CCOC1=C(C(=C(C=C1[C@H](C)N2C3=NC=NC(=C3C(=N2)C)N)Cl)F)[C@H]4CC(=O)NC4

IUPAC name: (4R)-4-[3-[(1S)-1-(4-amino-3-methylpyrazolo[3,4-d]pyrimidin-1-yl)ethyl]-5-chloro-2-ethoxy-6-fluorophenyl]pyrrolidin-2-one

Also known as: INCB-050465, Incb050465, INCB050465, Parsaclisib, PARSACLISIB

Parent form; salt/anhydrous children: CHEMBL4298155

Patent coverage: 256 distinct patent families (666 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 664 (100%) 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
PIK3CDphosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit deltaInhibition86%O00329

Broader ChEMBL bioactivity targets: 2 (assay-derived). Sample: Voltage-gated inwardly rectifying potassium channel KCNH2, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform.

Bioactivity

ChEMBL activities: 6 potent at pChembl ≥ 5 of 7 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
PIK3CD9IC501nMCHEMBL_ACT_19036875
PIK3CD8.96IC501.1nMCHEMBL_ACT_19290451
PIK3CD8.96IC501.1nMCHEMBL_ACT_19290458
PIK3CD8.7IC502nMCHEMBL_ACT_19290452
PIK3CD7.5IC5032nMCHEMBL_ACT_26846923
PIK3CD6.9IC50125nMCHEMBL_ACT_27957233

Target pathways

Aggregated over 1 target gene(s): PIK3CD.

Top Reactome pathways

14 total, by targets touching each:

PathwayTargetsGenes
PIP3 activates AKT signaling1PIK3CD
Synthesis of PIPs at the plasma membrane1PIK3CD
Constitutive Signaling by Aberrant PI3K in Cancer1PIK3CD
CD28 dependent PI3K/Akt signaling1PIK3CD
Interleukin-3, Interleukin-5 and GM-CSF signaling1PIK3CD
PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling1PIK3CD
RET signaling1PIK3CD
Erythropoietin activates Phosphoinositide-3-kinase (PI3K)1PIK3CD
Interleukin receptor SHC signaling1PIK3CD
Regulation of signaling by CBL1PIK3CD
Signaling by CSF1 (M-CSF) in myeloid cells1PIK3CD
Antigen activates B Cell Receptor (BCR) leading to generation of second messengers1PIK3CD
High laminar flow shear stress activates signaling by PIEZO1 and PECAM1:CDH5:KDR in endothelial cells1PIK3CD
Co-stimulation by ICOS1PIK3CD

Dominant GO biological processes

GO termTargets
natural killer cell differentiation1
positive regulation of cytokine production1
positive regulation of endothelial cell proliferation1
adaptive immune response1
mast cell chemotaxis1
respiratory burst involved in defense response1
protein phosphorylation1
inflammatory response1
immune response1
signal transduction1
positive regulation of endothelial cell migration1
positive regulation of gene expression1
T cell chemotaxis1
cell migration1
natural killer cell activation1

Indications & clinical

Indications

17 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
neoplasm3MONDO:0005070EFO:0000616
neoplasm of mature B-cells3MONDO:0004949EFO:0000096
autoimmune hemolytic anemia3MONDO:0020108EFO:1001264
follicular lymphoma3MONDO:0018906MONDO:0018906
mantle cell lymphoma3MONDO:0018876EFO:1001469
lymphoma2MONDO:0005062EFO:0000574
Sjogren syndrome2MONDO:0010030EFO:0000699
pemphigus vulgaris2MONDO:0008219EFO:0004719
diffuse large B-cell lymphoma1MONDO:0018905EFO:0000403
melanoma1MONDO:0005105EFO:0000756
breast neoplasm1MONDO:0021100MONDO:0007254
endometrium neoplasm1MONDO:0021251MONDO:0011962
B-cell chronic lymphocytic leukemia1MONDO:0004948EFO:0000095
mature T-cell and NK-cell non-Hodgkin lymphoma1MONDO:0000430MONDO:0000430
non-Hodgkin lymphoma1MONDO:0018908EFO:0005952

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

Clinical trials

Total trials: 34.

Phase distribution

PhaseTrials
PHASE114
PHASE210
PHASE1/PHASE25
PHASE34
Not specified1

Top trials by phase / activity

NCTPhaseStatusTitle
NCT04551053PHASE3TERMINATEDTo Evaluate Efficacy and Safety of Parsaclisib and Ruxolitinib in Participants With Myelofibrosis Who Have Suboptimal Response to Ruxolitinib (LIMBER-304)
NCT04551066PHASE3TERMINATEDTo Evaluate the Efficacy and Safety of Parsaclisib and Ruxolitinib in Participants With Myelofibrosis (LIMBER-313)
NCT04796922PHASE3WITHDRAWNTo Evaluate Efficacy and Safety of Parsaclisib Plus Either Rituximab or Obinutuzumab in R/R Follicular Lymphoma (FL) and Marginal Zone Lymphoma (MZL) (CITADEL-302)
NCT04849715PHASE3WITHDRAWNA Study of Parsaclisib, a PI3Kδ Inhibitor, in Combination With Bendamustine and Rituximab in Patients With Newly Diagnosed Mantle Cell Lymphoma
NCT04509700PHASE2ACTIVE_NOT_RECRUITINGRollover Study to Provide Continued Treatment for Participants With B-Cell Malignancies Previously Enrolled in Studies of Parsaclisib (INCB050465)
NCT04661007PHASE1/PHASE2ACTIVE_NOT_RECRUITINGTo Assess the Safety and Tolerability of Tafasitamab Alone or in Combination With Other Drugs in Japanese Participants With Non-Hodgkins Lymphoma (NHL)
NCT02018861PHASE1/PHASE2COMPLETEDA Phase 1/2, Open-Label, Dose Escalation, Safety and Tolerability Study of INCB050465 and Itacitinib in Subjects With Previously Treated B-Cell Malignancies (CITADEL-101)
NCT02265510PHASE1/PHASE2TERMINATEDAn Open-Label Study of a Novel JAK-inhibitor, INCB052793, Given to Patients With Advanced Malignancies
NCT02718300PHASE2TERMINATEDA Study of INCB050465 in Combination With Ruxolitinib in Subjects With Myelofibrosis
NCT02998476PHASE2COMPLETEDA Phase 2 Safety and Efficacy Study of INCB050465 in Subjects With Relapsed or Refractory Diffuse Large B-Cell Lymphoma (CITADEL-202)
NCT03126019PHASE2COMPLETEDA Study of INCB050465 in Relapsed or Refractory Follicular Lymphoma
NCT03144674PHASE2COMPLETEDA Study of INCB050465 in Subjects With Relapsed or Refractory Marginal Zone Lymphoma (CITADEL-204)
NCT03235544PHASE2COMPLETEDA Study of INCB050465 in Relapsed or Refractory Mantle Cell Lymphoma Previously Treated With or Without a Bruton’s Tyrosine Kinase (BTK) Inhibitor
NCT03538041PHASE2COMPLETEDA Study of INCB050465 in Participants With Autoimmune Hemolytic Anemia
NCT03627065PHASE2COMPLETEDA Study of INCB050465 in Primary Sjögren’s Syndrome
NCT03780166PHASE2WITHDRAWNA Study of the Safety and Tolerability of INCB050465 in Pemphigus Vulgaris
NCT04434937PHASE2COMPLETEDOpen-Label Study of Parsaclisib, in Japanese Participants With Relapsed or Refractory Follicular Lymphoma (CITADEL-213)
NCT04809467PHASE1/PHASE2TERMINATEDA Study Evaluating Safety, PK, and Efficacy of Tafasitamab and Parsaclisib in Participants With Relapsed/Refractory Non Hodgkin Lymphoma (R/R NHL) or Chronic Lymphocytic Leukemia (CLL)
NCT05238064PHASE1/PHASE2UNKNOWNParsaclisib in Combination With CHOP in Participants With Previously Untreated PTCL
NCT04323956PHASE1ACTIVE_NOT_RECRUITINGParsaclisib Plus the Standard Drug Therapy in Patients With Newly Diagnosed, High Risk Diffuse Large B-cell Lymphoma
NCT02559492PHASE1TERMINATEDItacitinib Combined With INCB024360 and/or Itacitinib Combined With INCB050465 in Advanced Solid Tumors
NCT02646748PHASE1COMPLETEDPembrolizumab Combined With Itacitinib (INCB039110) and/or Pembrolizumab Combined With INCB050465 in Advanced Solid Tumors
NCT03039114PHASE1COMPLETEDStudy Evaluating Safety and Efficacy of INCB050465 Combined With Bendamustine and Obinutuzumab in Relapsed or Refractory Follicular Lymphoma (CITADEL-102)
NCT03314922PHASE1COMPLETEDA Study of INCB050465 in Japanese Subjects With Previously Treated B-Cell Lymphoma (CITADEL-111)
NCT03424122PHASE1COMPLETEDINCB050465 in Combination With Rituximab, Bendamustine and Rituximab, or Ibrutinib in Participants With Previously Treated B-Cell Lymphoma (CITADEL-112)
NCT03589651PHASE1COMPLETEDINCMGA00012 in Combination With Other Therapies in Patients With Advanced Solid Tumors
NCT03688152PHASE1COMPLETEDA Safety and Tolerability Study of INCB053914 in Combination With INCB050465 in Diffuse Large B-Cell Lymphoma
NCT04142554PHASE1WITHDRAWNParsaclisib in Newly Diagnosed Stage I-IIIC Triple Negative or HER2+ Breast Cancer
NCT04774068PHASE1COMPLETEDRomidepsin and Parsaclisib for the Treatment of Relapsed or Refractory T-Cell Lymphomas
NCT04831944PHASE1COMPLETEDTo Evaluate the Safety, and Pharmacokinetics of Parscaclisib in Participants With Normal Hepatic Function and Hepatic Impairment.
NCT04831996PHASE1COMPLETEDTo Evaluate the Safety, and Pharmacokinetics of Parscaclisib in Participants With Normal Renal Function and Renal Impairment.
NCT05083208PHASE1TERMINATEDPI3Kδ Inhibitor Parsaclisib Combined With Chidamide for the Treatment of Relapsed/Refractory Peripheral T-cell Lymphoma
NCT05867030PHASE1WITHDRAWNParsaclisib in Patients With Relapsed or Refractory Follicular Lymphoma
NCT07149818Not specifiedNOT_YET_RECRUITINGA Single-arm Phase 2 Prospective Clinical Study of Linprixel in the Treatment of Relapsed/Refractory Autoimmune Hemolytic Anemia

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

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.

59 molecules share ≥1 primary target. Top 59 by shared-target count:

MoleculeSourceStatusShared targets
IDELALISIBChEMBL + PubChemPhase 4 (approved)PIK3CD
INAVOLISIBChEMBL + PubChemPhase 4 (approved)PIK3CD
ALPELISIBChEMBLPhase 4 (approved)PIK3CD
CAFFEINEChEMBLPhase 4 (approved)PIK3CD
COPANLISIBChEMBLPhase 4 (approved)PIK3CD
DASATINIBChEMBLPhase 4 (approved)PIK3CD
DUVELISIBChEMBLPhase 4 (approved)PIK3CD
LENIOLISIBChEMBLPhase 4 (approved)PIK3CD
SUNITINIBChEMBLPhase 4 (approved)PIK3CD
THEOPHYLLINEChEMBLPhase 4 (approved)PIK3CD
UMBRALISIBChEMBLPhase 4 (approved)PIK3CD
BUPARLISIBChEMBLPhase 3PIK3CD
DACTOLISIBChEMBLPhase 3PIK3CD
GEDATOLISIBChEMBLPhase 3PIK3CD
LESTAURTINIBChEMBLPhase 3PIK3CD
POVORCITINIBChEMBLPhase 3PIK3CD
TASELISIBChEMBLPhase 3PIK3CD
ACALISIBChEMBLPhase 2PIK3CD
AMDIZALISIBChEMBLPhase 2PIK3CD
AMG-319ChEMBLPhase 2PIK3CD
APITOLISIBChEMBLPhase 2PIK3CD
AZD-6482ChEMBLPhase 2PIK3CD
AZD-8154ChEMBLPhase 2PIK3CD
BGT-226 FREE BASEChEMBLPhase 2PIK3CD
BI-2536ChEMBLPhase 2PIK3CD
BIMIRALISIBChEMBLPhase 2PIK3CD
DEZAPELISIBChEMBLPhase 2PIK3CD
EGANELISIBChEMBLPhase 2PIK3CD
FIMEPINOSTATChEMBLPhase 2PIK3CD
GSK-2636771ChEMBLPhase 2PIK3CD
IZORLISIBChEMBLPhase 2PIK3CD
LINPERLISIBChEMBLPhase 2PIK3CD
NARAZACICLIBChEMBLPhase 2PIK3CD
NEMIRALISIBChEMBLPhase 2PIK3CD
OMIPALISIBChEMBLPhase 2PIK3CD
ONATASERTIBChEMBLPhase 2PIK3CD
PAXALISIBChEMBLPhase 2PIK3CD
PF-04691502ChEMBLPhase 2PIK3CD
PICTILISIBChEMBLPhase 2PIK3CD
PILARALISIBChEMBLPhase 2PIK3CD
QUISINOSTATChEMBLPhase 2PIK3CD
R-406ChEMBLPhase 2PIK3CD
RISOVALISIBChEMBLPhase 2PIK3CD
ROGINOLISIBChEMBLPhase 2PIK3CD
SAMOTOLISIBChEMBLPhase 2PIK3CD
SAPANISERTIBChEMBLPhase 2PIK3CD
SELETALISIBChEMBLPhase 2PIK3CD
SERABELISIBChEMBLPhase 2PIK3CD
SONOLISIBChEMBLPhase 2PIK3CD
TENALISIBChEMBLPhase 2PIK3CD
TG100-115ChEMBLPhase 2PIK3CD
VISTUSERTIBChEMBLPhase 2PIK3CD
VOXTALISIBChEMBLPhase 2PIK3CD
ZSTK-474ChEMBLPhase 2PIK3CD
AfatinibPubChemApprovedPIK3CD
CrizotinibPubChemApprovedPIK3CD
GefitinibPubChemApprovedPIK3CD
PazopanibPubChemApprovedPIK3CD
SelumetinibPubChemApprovedPIK3CD

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