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Fluzoparib

drug
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Also known as FuzuloparibFuzuopaliHS-10160HS10160SHR-3162Shr3162US9273052, 19

Summary

Fluzoparib (CHEMBL3930624) is a phase-3 clinical-stage small molecule targeting PARP1; indicated across 21 conditions including exocrine pancreatic carcinoma and breast neoplasm.

At a glance

  • Status: Max clinical phase 3 (not approved)
  • Modality: Small molecule
  • Targets: 1 (PARP1)
  • Indications: 21 conditions
  • Clinical trials: 79
  • Chemistry: 472.4 Da · C22H16F4N6O2

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL3930624
NameFluzoparib
TypeSmall molecule
Max phase3
FDA approvedno
PubChem CID56649297
Molecular formulaC22H16F4N6O2
Molecular weight472.4
InChIKeyXJGXCBHXFWBOTN-UHFFFAOYSA-N

SMILES: C1CN2C(=NC(=N2)C(F)(F)F)CN1C(=O)C3=C(C=CC(=C3)CC4=NNC(=O)C5=CC=CC=C54)F

IUPAC name: 4-[[4-fluoro-3-[2-(trifluoromethyl)-6,8-dihydro-5H-[1,2,4]triazolo[1,5-a]pyrazine-7-carbonyl]phenyl]methyl]-2H-phthalazin-1-one

Also known as: Fluzoparib, Fuzuloparib, Fuzuopali, HS-10160, HS10160, SHR-3162, Shr3162, SHR3162, US9273052, 19, FLUZOPARIB

Patent coverage: 246 distinct patent families (594 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 565 (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
PARP1poly(ADP-ribose) polymerase 1Inhibition8.054.1%P09874

Broader ChEMBL bioactivity targets: 1 (assay-derived). Sample: Poly [ADP-ribose] polymerase 1.

Bioactivity

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

TargetpChemblTypeValueUnitActivity ID
PARP18.84IC501.46nMCHEMBL_ACT_24993459
PARP18.84IC501.46nMCHEMBL_ACT_25554601
PARP18.84IC501.46nMCHEMBL_ACT_25633796
PARP18.84IC501.46nMCHEMBL_ACT_25662123
PARP18.84IC501.46nMCHEMBL_ACT_25884149
PARP18.84IC501.46nMCHEMBL_ACT_25998851
PARP18.84IC501.46nMCHEMBL_ACT_29118512
PARP18.82IC501.5nMCHEMBL_ACT_25898557
PARP17.99IC5010.2nMCHEMBL_ACT_17745580
PARP17.99IC5010.2nMCHEMBL_ACT_26934772

Target pathways

Aggregated over 1 target gene(s): PARP1.

Top Reactome pathways

8 total, by targets touching each:

PathwayTargetsGenes
POLB-Dependent Long Patch Base Excision Repair1PARP1
vRNA Synthesis1PARP1
Downregulation of SMAD2/3:SMAD4 transcriptional activity1PARP1
SUMOylation of DNA damage response and repair proteins1PARP1
HDR through MMEJ (alt-NHEJ)1PARP1
DNA Damage Recognition in GG-NER1PARP1
Formation of Incision Complex in GG-NER1PARP1
Dual Incision in GG-NER1PARP1

Dominant GO biological processes

GO termTargets
negative regulation of transcription by RNA polymerase II1
telomere maintenance1
DNA repair1
double-strand break repair1
transcription by RNA polymerase II1
apoptotic process1
DNA damage response1
mitochondrion organization1
transforming growth factor beta receptor signaling pathway1
response to gamma radiation1
positive regulation of cardiac muscle hypertrophy1
carbohydrate biosynthetic process1
protein autoprocessing1
signal transduction involved in regulation of gene expression1
macrophage differentiation1

Indications & clinical

Indications

21 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
exocrine pancreatic carcinoma3MONDO:0005192EFO:0002618
breast neoplasm3MONDO:0021100MONDO:0007254
ovarian cancer3MONDO:0008170MONDO:0008170
ovarian neoplasm3MONDO:0021068EFO:0003893
malignant pancreatic neoplasm3MONDO:0009831EFO:1000359
neoplasm2MONDO:0005070EFO:0000616
renal cell carcinoma2MONDO:0005086EFO:0000681
non-small cell lung carcinoma2MONDO:0005233EFO:0003060
sarcoma2MONDO:0005089EFO:0000691
triple-negative breast carcinoma2MONDO:0005494EFO:0005537
esophageal squamous cell carcinoma2MONDO:0005580EFO:0005922
endometrial carcinoma2MONDO:0002447EFO:1001512
soft tissue sarcoma2MONDO:0018078EFO:1001968
nasopharyngeal carcinoma2MONDO:0015459MONDO:0015459
gastric neoplasm1MONDO:0021085MONDO:0001056
small cell lung carcinoma1MONDO:0008433EFO:0000702
liver disorder1MONDO:0005154EFO:0001421
kidney disorder1MONDO:0005240EFO:0003086
melanoma1MONDO:0005105EFO:0000756

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

Clinical trials

Total trials: 79.

Phase distribution

PhaseTrials
PHASE241
PHASE121
PHASE310
PHASE1/PHASE26
Not specified1

Top trials by phase / activity

NCTPhaseStatusTitle
NCT05891093PHASE3RECRUITINGEfficacy and Safety of Fluzoparib Combined With Adjuvant Endocrine Therapy for HR+/HER2- SNF3-subtype Early Breast Cancer (BCTOP-L-A01)
NCT06188455PHASE3NOT_YET_RECRUITINGMaintenance Therapy After Platinum-containing Chemotherapy in Patients With Recurrent Ovarian Cancer
NCT06255392PHASE3RECRUITINGRandomized, Open, Controlled, Multicenter Phase III Clinical Study of Fluzoparib in Combination With Apatinib Versus Investigator-Selected Chemotherapy for HRD-Positive/HER2-negative Advanced Breast Cancer
NCT06539091PHASE3NOT_YET_RECRUITINGFluzoparib in Combination With Apatinib Mesylate for Maintenance Therapy in Stage III-IV Ovarian Cancer
NCT06612814PHASE3ACTIVE_NOT_RECRUITINGPARP Inhibitor With CDK4/ 6 Inhibitor and Endocrine Therapy in HR+/ HER2-Advanced Breast Cancer
NCT06954584PHASE3RECRUITINGFluzoparib+Bevacizumab/Dietary Intervention vs Fluzoparib Monotherapy as First-line Maintenance in HRD+/- Advanced Ovarian Cancer
NCT03863860PHASE3COMPLETEDA Trial of Maintenance Treatment With Fluzoparib Versus Placebo in Relapsed Ovarian Cancer Patients
NCT04229615PHASE3UNKNOWNA Study of Fluzoparib±Apatinib Versus Placebo Maintenance Treatment in Patients With Advanced Ovarian Cancer Following Response on First-Line Platinum-Based Chemotherapy
NCT04296370PHASE3UNKNOWNA Study of Fluzoparib±Apatinib Versus Chemotherapy Treatment of Physician’s Choice in HER2-negative Metastatic Breast Cancer Patients With Germline BRCA Mutation
NCT04300114PHASE3TERMINATEDA Study of Maintenance Treatment With Fluzoparib in gBRCA/PALB2 Mutated Pancreatic Cancer Whose Disease Has Not Progressed on First Line Platinum-Based Chemotherapy
NCT04518501PHASE1/PHASE2RECRUITINGFuzuloparib Arsenic Trioxide Platinum Resistance Relapsed Ovarian Cancer
NCT05479487PHASE2NOT_YET_RECRUITINGFluzoparib and Apatinib Versus Fluzoparib in Relapsed Ovarian Carcinoma Maintenance Treatment
NCT05576389PHASE2ENROLLING_BY_INVITATIONNeoadjuvant Fluzoparib Combined With Camrelizumab in Germline BRCA-mutated HER2-negative Breast Cancer
NCT05582499PHASE2RECRUITINGFudan University Shanghai Cancer Center Breast Cancer Precision Platform Series Study- Neoadjuvant Therapy
NCT05594095PHASE2RECRUITINGSNF Platform Study of HR+/ HER2-advanced Breast Cancer
NCT05753826PHASE2RECRUITINGAdebrelimab Combined With Fuzuloparib in the Treatment of Patients With Recurrent Platinum-resistant Ovarian Cancer.
NCT05759546PHASE2RECRUITINGPARP Inhibitor With CDK4/6 Inhibitor and Endocrine Therapy in HR+/ HER2-Advanced Breast Cancer
NCT05761470PHASE2RECRUITINGNeoadjuvant Camrelizumab and Fluzoparib and Nab-paclitaxel in Early Breast Cancer With HRR Gene Mutation
NCT05834582PHASE2RECRUITINGNeoadjuvant Fluzoparib in Germline BRCA-mutated Three-negative Breast Cancer Breast Cancer
NCT05894018PHASE2RECRUITINGBrachytherapy (Iodine-125 Seeds) and Fluzoparib Combination Therapy for Advanced Unresectable Soft Tissue Sarcoma
NCT06063070PHASE2NOT_YET_RECRUITINGFirst-line Maintenance Treatment With Fluzoparib Plus Bevacizumab in Advanced BRCA Wild Type Ovarian Cancer
NCT06081595PHASE2NOT_YET_RECRUITINGFluzoparib Combined With Apatinib in Relapsed Ovarian Carcinoma Maintenance Treatment
NCT06208410PHASE1/PHASE2RECRUITINGA Clinical Study of JS105 in Combination With Other Anti-tumor Therapies in Patients With Solid Tumors
NCT06413992PHASE2RECRUITINGCamrelizumab Plus Fluzoparib for TP-53 Mutated Endometrial Cancer
NCT06446206PHASE2NOT_YET_RECRUITINGAdebrelimab Plus Chemotherapy, Bevacizumab and Fluzoparib in Platinum-Sensitive Relapsed Ovarian Cancer
NCT06516445PHASE2RECRUITINGSCRT Followed by Camrelizumab Combined With Fluzoparib and Chemotherapy as Neoadjuvant Therapy for LARC
NCT06541314PHASE2RECRUITINGFluzoparib Neoadjuvant Therapy for Ovarian Cancer
NCT06552858PHASE2NOT_YET_RECRUITINGFluzoparib Combined With Dalpiciclib for Platinum Resistant Recurrent Ovarian Cancer
NCT06561022PHASE2NOT_YET_RECRUITINGPrecision Treatment of HR+ HER2- Advanced Breast Cancer Based on SNF Molecular Subtyping
NCT06735326PHASE2RECRUITINGFluzoparib With or Without Bevacizumab for Neoadjuvant Therapy in Advanced Ovarian Cancer
NCT06827717PHASE2RECRUITINGPhase II Study of Irinotecan Liposome (II) Combined With Temozolomide and Fluzoparib in Recurrent or Metastatic Ewing Sarcoma
NCT07141771PHASE1/PHASE2NOT_YET_RECRUITINGAn Umbrella Study of Recurrent, Extensive Stage Small Cell Lung Cancer Based on Molecular Typing
NCT07321015PHASE2NOT_YET_RECRUITINGA Single-Arm Phase Ⅱ Study of Fluzoparib Maintenance in Platinum-sensitive Advanced Triple-Negative Breast Cance
NCT07353437PHASE2NOT_YET_RECRUITINGFluzoparib as Adjuvant Treatment in Patients With Germline Homologous Recombination Repair (HRR) Mutated Primary Breast Cancer (Flamenco)
NCT07355010PHASE2NOT_YET_RECRUITINGA Randomized, Open-label, Double-cohort Study of Fluzoparib Combined With Famitinib Malate or SHR-1701 for Neoadjuvant Therapy in Patients With Advanced Ovarian Cancer
NCT07382713PHASE2NOT_YET_RECRUITINGFluzoparib Plus Famitinib Maintenance After First-Line Platinum Response in Advanced Ovarian Cancer
NCT04102124PHASE2TERMINATEDA Study of SHR3680 in Combination With SHR3162 in the Treatment of mCRPC
NCT04228601PHASE1/PHASE2COMPLETEDA Study of Fluzoparib in Combination With mFOLFIRINOX in Patients With Advanced Pancreatic Cancer
NCT04355858PHASE2UNKNOWNMolecularly Targeted Umbrella Study in Luminal Advanced Breast Cancer
NCT04400188PHASE1/PHASE2COMPLETEDA Study of Fluzoparib (SHR-3162) and Temozolomide With or Without SHR-1316 in Treating Patients With Replapsed Small Cell Lung Cancer

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
AMITRIPTYLINEChEMBLPhase 4 (approved)PARP1
NIRAPARIBChEMBLPhase 4 (approved)PARP1
OLAPARIBChEMBLPhase 4 (approved)PARP1
PALBOCICLIBChEMBLPhase 4 (approved)PARP1
RUCAPARIBChEMBLPhase 4 (approved)PARP1
RUCAPARIB CAMSYLATEChEMBLPhase 4 (approved)PARP1
TALAZOPARIBChEMBLPhase 4 (approved)PARP1
INIPARIBChEMBLPhase 3PARP1
PAMIPARIBChEMBLPhase 3PARP1
SARUPARIBChEMBLPhase 3PARP1
VELIPARIBChEMBLPhase 3PARP1
2X-121ChEMBLPhase 2PARP1
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