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Pamiparib

drug
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Also known as Bgb-290US9260440, 69

Summary

Pamiparib (CHEMBL4112930) is a phase-3 clinical-stage small molecule (ATC L01XK06) targeting PARP1 and PARP2; indicated across 13 conditions including neoplasm and gastric neoplasm.

At a glance

  • Status: Max clinical phase 3 (not approved)
  • Modality: Small molecule
  • ATC class: L01XK06
  • Targets: 2 (PARP1, PARP2)
  • Indications: 13 conditions
  • Clinical trials: 29
  • Chemistry: 298.31 Da · C16H15FN4O

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL4112930
NamePamiparib
TypeSmall molecule
Max phase3
FDA approvedno
PubChem CID135565554
ATCL01XK06
Molecular formulaC16H15FN4O
Molecular weight298.31
InChIKeyDENYZIUJOTUUNY-MRXNPFEDSA-N

SMILES: C[C@]12CCCN1CC3=NNC(=O)C4=C5C3=C2NC5=CC(=C4)F

IUPAC name: (2R)-14-fluoro-2-methyl-6,9,10,19-tetrazapentacyclo[14.2.1.02,6.08,18.012,17]nonadeca-1(18),8,12(17),13,15-pentaen-11-one

Also known as: Bgb-290, BGB-290, Pamiparib, US9260440, 69, PAMIPARIB

Patent coverage: 865 distinct patent families (2,114 SureChEMBL compound mentions), from 1 matched compound structure(s). 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
PARP1poly(ADP-ribose) polymerase 1Inhibition8.894.1%P09874
PARP2poly(ADP-ribose) polymerase 2Inhibition9.050.2%Q9UGN5

Broader ChEMBL bioactivity targets: 14 (assay-derived). Sample: Solute carrier family 22 member 6, Organic anion transporter 3, Solute carrier organic anion transporter family member 1B1, Solute carrier organic anion transporter family member 1B3, Protein mono-ADP-ribosyltransferase TIPARP, Protein mono-ADP-ribosyltransferase PARP11, Protein mono-ADP-ribosyltransferase PARP10, Protein mono-ADP-ribosyltransferase PARP12, Protein mono-ADP-ribosyltransferase PARP8, Poly [ADP-ribose] polymerase 1.

Bioactivity

ChEMBL activities: 25 potent at pChembl ≥ 5 of 31 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
PARP29.96IC500.11nMCHEMBL_ACT_25073013
PARP19.7EC500.2nMCHEMBL_ACT_22440940
PARP29.52IC500.3nMCHEMBL_ACT_25662129
PARP29.3IC500.5nMCHEMBL_ACT_17741781
PARP19.08IC500.83nMCHEMBL_ACT_25073008
PARP19.05IC500.9nMCHEMBL_ACT_17741759
PARP29.05IC500.9nMCHEMBL_ACT_22440997
PARP19.05IC500.9nMCHEMBL_ACT_25898556
PARP29.05IC500.9nMCHEMBL_ACT_29118523
PARP29.04IC500.92nMCHEMBL_ACT_25998878
PARP18.89IC501.3nMCHEMBL_ACT_22441054
PARP18.89IC501.3nMCHEMBL_ACT_25998865
PARP18.89IC501.3nMCHEMBL_ACT_29118513
PARP18.3IC505nMCHEMBL_ACT_29087905
PARP28.22IC506nMCHEMBL_ACT_29087930
PARP18.19IC506.5nMCHEMBL_ACT_25662122
PARP17.89EC5013nMCHEMBL_ACT_22440895
PARP37.17IC5068nMCHEMBL_ACT_22440910
TNKS26.85IC50140nMCHEMBL_ACT_22440908
PARP36.73IC50185nMCHEMBL_ACT_17741791
TNKS6.64IC50230nMCHEMBL_ACT_22440909
TNKS26.12IC50766nMCHEMBL_ACT_17741812
PARP125.62IC502400nMCHEMBL_ACT_22440902
PARP115.57IC502700nMCHEMBL_ACT_22440903
PARP85.08IC508400nMCHEMBL_ACT_22440905

Target pathways

Aggregated over 2 target gene(s): PARP1, PARP2.

Top Reactome pathways

8 total, by targets touching each:

PathwayTargetsGenes
POLB-Dependent Long Patch Base Excision Repair2PARP1, PARP2
HDR through MMEJ (alt-NHEJ)2PARP1, PARP2
DNA Damage Recognition in GG-NER2PARP1, PARP2
Formation of Incision Complex in GG-NER2PARP1, PARP2
Dual Incision in GG-NER2PARP1, PARP2
vRNA Synthesis1PARP1
Downregulation of SMAD2/3:SMAD4 transcriptional activity1PARP1
SUMOylation of DNA damage response and repair proteins1PARP1

Dominant GO biological processes

GO termTargets
DNA repair2
double-strand break repair2
DNA damage response2
DNA ADP-ribosylation2
decidualization2
protein poly-ADP-ribosylation2
protein auto-ADP-ribosylation2
protein localization to chromatin2
DNA repair-dependent chromatin remodeling2
negative regulation of transcription by RNA polymerase II1
telomere maintenance1
transcription by RNA polymerase II1
apoptotic process1
mitochondrion organization1
transforming growth factor beta receptor signaling pathway1

Indications & clinical

Indications

13 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
gastric neoplasm2MONDO:0021085MONDO:0001056
breast neoplasm2MONDO:0021100MONDO:0007254
ovarian cancer2MONDO:0008170MONDO:0008170
small cell lung carcinoma2MONDO:0008433EFO:0000702
metastatic prostate carcinoma2MONDO:0004956EFO:0000196
glioblastoma1MONDO:0018177EFO:0000519
central nervous system neoplasm1MONDO:0006130EFO:1000158
head and neck squamous cell carcinoma1MONDO:0010150EFO:0000181
non-small cell lung carcinoma1MONDO:0005233EFO:0003060

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

Clinical trials

Total trials: 29.

Phase distribution

PhaseTrials
PHASE216
PHASE16
PHASE1/PHASE23
PHASE32
EARLY_PHASE11
Not specified1

Top trials by phase / activity

NCTPhaseStatusTitle
NCT03519230PHASE3ACTIVE_NOT_RECRUITINGMaintenance Treatment With BGB-290 Versus Placebo in Participants With Platinum-sensitive Recurrent Ovarian Cancer
NCT04164199PHASE3ACTIVE_NOT_RECRUITINGStudy of Tislelizumab, Pamiparib, and Other Investigational Agents in Participants With Advanced Malignancies
NCT05652283PHASE2ACTIVE_NOT_RECRUITINGPamiparib Combined With Surufatinib for the Neoadjuvant Treatment of Unresectable Ovarian Cancer
NCT06387056PHASE2RECRUITINGGenomic Biomarker-guided Neoadjuvant Therapy for Prostate Cancer (SEGNO)
NCT06692491PHASE2NOT_YET_RECRUITINGStudy of Precision Treatment for Rare Tumours in China Guided by PDO and NGS
NCT03150862PHASE1/PHASE2COMPLETEDA Study Assessing Pamiparib With Radiation and/or Temozolomide (TMZ) in Participants With Newly Diagnosed or Recurrent Glioblastoma
NCT03333915PHASE1/PHASE2COMPLETEDStudy of the Efficacy, Safety and Pharmacokinetics of Pamiparib (BGB-290) in Participants With Advanced Solid Tumors
NCT03427814PHASE2COMPLETEDStudy of BGB-290 or Placebo in Participants With Advanced or Inoperable Gastric Cancer
NCT03575065PHASE2COMPLETEDEfficacy and Safety of BGB-290 in the Treatment of Metastatic HER2-Negative Breast Cancer Patients With BRCA Mutation in China
NCT03712930PHASE2TERMINATEDTreatment of Metastatic Castration-Resistant Prostate Cancer With Homologous Recombination Deficiency
NCT03933761PHASE2WITHDRAWNPamiparib in Fusion Positive, Reversion Negative High Grade Serous Ovarian Cancer or Carcinosarcoma With BRCA1/2 Gene Mutations If Progression on Substrate Poly ADP Ribose Polymerase Inhibitbor (PARPI) or Chemotherapy
NCT04603365PHASE2WITHDRAWNPamiparib and Temozolomide for the Treatment of Hereditary Leiomyomatosis and Renal Cell Cancer
NCT04796454PHASE2WITHDRAWNPamiparib and Low Dose Temozolomide In Patients With Platinum Sensitive Biliary Tract Cancer
NCT04985721PHASE2UNKNOWNA Trial of Pamiparib With Tislelizumab in Patients With Advanced Tumours With Homologous Recombination Repair Defects
NCT05044871PHASE2COMPLETEDBiomarker-driven Targeted Therapy in Patients With Recurrent Platinum-resistant Epithelial Ovarian Cancer
NCT05327621PHASE2UNKNOWNPamiparib in mCRPC With HRD or BRCA1/2 Mutation
NCT05376722PHASE2UNKNOWNA Study of Pamiparib Combined With Abiraterone Acetate in Neoadjuvant Treatment of Prostate Cancer
NCT05483543PHASE2UNKNOWNPamiparib for Consolidation Treatment of Unprogressed LS-SCLC After Concurrent Chemoradiotherapy
NCT05489926PHASE2UNKNOWNA Study to Explore Pamiparib Treatment in Epithelial Ovarian Cancer After Prior PARP Inhibitor Exposure
NCT05494580PHASE1/PHASE2COMPLETEDPamiparib Plus Surufatinib in Patients With Platinum-resistant Ovarian Cancer
NCT05669768PHASE2UNKNOWNStudy on the Efficacy and Toxicity of Pamiparib Combined With Tamoxifen in the Treatment of Epithelial Ovarian Cancer Patients With Biochemical Recurrence During First-line PARPi Maintenance Therapy
NCT05526924PHASE1RECRUITINGDosing Study of Radiation Combined With Tislelizumab and Pamiparib in Patients With Previously Treated Head and Neck Cancer
NCT02361723PHASE1COMPLETEDPhase 1a/1b BGB-290 for Advanced Solid Tumors.
NCT02660034PHASE1COMPLETEDThe Safety, Pharmacokinetics and Antitumor Activity of BGB-A317 in Combination With BGB-290 in Participants With Advanced Solid Tumors
NCT03150810PHASE1COMPLETEDStudy to Assess Safety, Tolerability and Clinical Activity of BGB-290 in Combination With Temozolomide (TMZ) in Participants With Locally Advanced or Metastatic Solid Tumors
NCT03994211PHASE1COMPLETEDStudy to Investigate the Effect of Rifampin and Itraconazole on the Action of Pamiparib in Participants With Cancer
NCT05038839PHASE1COMPLETEDCabozantinib and Pamiparib for the Treatment of Advanced of Refractory Solid Tumors
NCT04614909EARLY_PHASE1COMPLETEDStudy of Pamiparib in Newly Diagnosed and rGBM
NCT04774406Not specifiedCOMPLETEDArterial Hypertension Related to PARP Inhibitors (ArteRIB)

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.

54 molecules share ≥1 primary target. Top 54 by shared-target count:

MoleculeSourceStatusShared targets
TALAZOPARIBChEMBL + PubChemPhase 4 (approved)PARP1, PARP2
NIRAPARIBChEMBLPhase 4 (approved)PARP1, PARP2
OLAPARIBChEMBLPhase 4 (approved)PARP1, PARP2
RUCAPARIBChEMBLPhase 4 (approved)PARP1, PARP2
SARUPARIBChEMBLPhase 3PARP1, PARP2
VELIPARIBChEMBLPhase 3PARP1, PARP2
2X-121ChEMBLPhase 2PARP1, PARP2
AMITRIPTYLINEChEMBLPhase 4 (approved)PARP1
PALBOCICLIBChEMBLPhase 4 (approved)PARP1
RUCAPARIB CAMSYLATEChEMBLPhase 4 (approved)PARP1
FLUZOPARIBChEMBLPhase 3PARP1
INIPARIBChEMBLPhase 3PARP1
AMELPARIBChEMBLPhase 2PARP1
CHLORTHENOXAZINEChEMBLPhase 2PARP1
E-7016ChEMBLPhase 2PARP1
FLAVONEChEMBLPhase 2PARP1
LUTEOLINChEMBLPhase 2PARP1
NESUPARIBChEMBLPhase 2PARP1
AfatinibPubChemApprovedPARP1
ApixabanPubChemApprovedPARP1
belumosudilPubChemApprovedPARP1
BinimetinibPubChemApprovedPARP1
CarfilzomibPubChemApprovedPARP1
chenodiolPubChemApprovedPARP1
ClascoteronePubChemApprovedPARP1
ClofarabinePubChemApprovedPARP1
CrizotinibPubChemApprovedPARP1
cytisiniclinePubChemApprovedPARP1
dacomitinibPubChemApprovedPARP1
ElagolixPubChemApprovedPARP1
EribulinPubChemApprovedPARP1
FingolimodPubChemApprovedPARP1
IdelalisibPubChemApprovedPARP1
LactulosePubChemApprovedPARP1
LinagliptinPubChemApprovedPARP1
MavacamtenPubChemApprovedPARP1
MegestrolPubChemApprovedPARP1
NitisinonePubChemApprovedPARP1
PazopanibPubChemApprovedPARP1
podofiloxPubChemApprovedPARP1
PramipexolePubChemApprovedPARP1
PyrazinamidePubChemApprovedPARP1
regorafenibPubChemApprovedPARP1
RelugolixPubChemApprovedPARP1
RiociguatPubChemApprovedPARP1
RitlecitinibPubChemApprovedPARP1
RolapitantPubChemApprovedPARP1
saxagliptinPubChemApprovedPARP1
SelumetinibPubChemApprovedPARP1
TadalafilPubChemApprovedPARP1
TaurinePubChemApprovedPARP1
TrabectedinPubChemApprovedPARP1
TrametinibPubChemApprovedPARP1
VorapaxarPubChemApprovedPARP1

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