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Talazoparib

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Also known as BMN 673BMN-673LT-673PF-06944076BICALUTAMIDETALAZOPARIB TOSYLATETALAZOPARIB (BMN 673)

Summary

Talazoparib (CHEMBL3137320) is an approved small molecule (ATC L01XK04) targeting PARP1 and PARP2; indicated across 26 conditions including breast neoplasm and neoplasm; with CIViC clinical evidence for 28 variant-indication associations (e.g. ATR Loss-of-function in castration-resistant prostate carcinoma).

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: L01XK04
  • Targets: 2 (PARP1, PARP2)
  • Indications: 26 conditions
  • Clinical trials: 242
  • Precision-oncology evidence (CIViC): 28 variant–indication associations
  • Chemistry: 380.4 Da · C19H14F2N6O

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL3137320
NameTalazoparib
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID135565082
ATCL01XK04
Molecular formulaC19H14F2N6O
Molecular weight380.4
InChIKeyHWGQMRYQVZSGDQ-HZPDHXFCSA-N

SMILES: CN1C(=NC=N1)[C@@H]2[C@H](NC3=CC(=CC4=C3C2=NNC4=O)F)C5=CC=C(C=C5)F

IUPAC name: (11S,12R)-7-fluoro-11-(4-fluorophenyl)-12-(2-methyl-1,2,4-triazol-3-yl)-2,3,10-triazatricyclo[7.3.1.05,13]trideca-1,5(13),6,8-tetraen-4-one

Also known as: BMN 673, BMN-673, LT-673, PF-06944076, Talazoparib, TALAZOPARIB, BICALUTAMIDE, TALAZOPARIB TOSYLATE, TALAZOPARIB (BMN 673), Talazoparib (BMN 673)

Parent form; salt/anhydrous children: CHEMBL3137318

Patent coverage: 2,341 distinct patent families (5,534 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 5,283 (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 1Inhibition4.1%P09874
PARP2poly(ADP-ribose) polymerase 2Inhibition0.2%Q9UGN5

Broader ChEMBL bioactivity targets: 10 (assay-derived). Sample: Protein mono-ADP-ribosyltransferase PARP11, Protein mono-ADP-ribosyltransferase PARP10, Protein mono-ADP-ribosyltransferase PARP8, Poly [ADP-ribose] polymerase 1, PARP 1, 2 and 3, Protein mono-ADP-ribosyltransferase PARP16, Protein mono-ADP-ribosyltransferase PARP3, Poly [ADP-ribose] polymerase 2, Protein mono-ADP-ribosyltransferase PARP4, Poly [ADP-ribose] polymerase tankyrase-1.

Bioactivity

ChEMBL activities: 48 potent at pChembl ≥ 5 of 48 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
PARP29.7IC500.2nMCHEMBL_ACT_24919332
PARP29.52IC500.3nMCHEMBL_ACT_25662128
PARP29.52IC500.3nMCHEMBL_ACT_25884153
PARP19.24IC500.57nMCHEMBL_ACT_16474335
PARP19.24IC500.58nMCHEMBL_ACT_19441985
PARP19.24IC500.57nMCHEMBL_ACT_19483631
PARP19.24Ki0.58nMCHEMBL_ACT_24775557
PARP19.24IC500.57nMCHEMBL_ACT_24775559
PARP19.24IC500.57nMCHEMBL_ACT_25073016
PARP19.24IC500.57nMCHEMBL_ACT_25950812
PARP19.24IC500.57nMCHEMBL_ACT_29118510
PARP29.24IC500.58nMCHEMBL_ACT_29118522
PARP19.22IC500.6nMCHEMBL_ACT_15251056
PARP29.22IC500.6nMCHEMBL_ACT_22432627
PARP19.22IC500.6nMCHEMBL_ACT_24919331
PARP19.22IC500.6nMCHEMBL_ACT_25554603
PARP19.22Kd0.6nMCHEMBL_ACT_25616306
PARP49.15Kd0.7nMCHEMBL_ACT_24867484
PARP19.15IC500.7nMCHEMBL_ACT_25662121
PARP19.15IC500.7nMCHEMBL_ACT_25884148
PARP29.07Ki0.85nMCHEMBL_ACT_16475228
PARP29.05Ki0.9nMCHEMBL_ACT_19483629
PARP19IC501nMCHEMBL_ACT_22432609
PARP29IC501nMCHEMBL_ACT_24775564
PARP18.96Kd1.1nMCHEMBL_ACT_24867466
PARP18.96IC501.1nMCHEMBL_ACT_25616293
PARP18.92Ki1.2nMCHEMBL_ACT_16474336
PARP18.92Ki1.2nMCHEMBL_ACT_19483630
PARP18.6EC502.5nMCHEMBL_ACT_15251106
PARP18.6EC502.51nMCHEMBL_ACT_16475266

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

26 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:0021100EFO:0003869
neoplasm3MONDO:0005070EFO:0000616
ovarian cancer3MONDO:0008170MONDO:0008170
breast carcinoma3MONDO:0004989EFO:0000305
squamous cell lung carcinoma2MONDO:0005097EFO:0000708
non-small cell lung carcinoma2MONDO:0005233EFO:0003060
hereditary breast ovarian cancer syndrome2MONDO:0003582Orphanet:145
prostate adenocarcinoma2MONDO:0005082EFO:0000673
renal cell carcinoma2MONDO:0005086EFO:0000681
small cell lung carcinoma2MONDO:0008433EFO:0000702
triple-negative breast carcinoma2MONDO:0005494EFO:0005537
metastatic prostate carcinoma2MONDO:0004956EFO:0000196
angiosarcoma2MONDO:0016982EFO:0003968
endometrium neoplasm2MONDO:0021251MONDO:0011962
glioblastoma2MONDO:0018177EFO:0000519
urothelial carcinoma2MONDO:0040679EFO:0008528
adrenal gland pheochromocytoma2MONDO:0004974EFO:0000239
melanoma2MONDO:0005105EFO:0000756
acute myeloid leukemia1MONDO:0018874EFO:0000222
leukemia1MONDO:0005059EFO:0000565
exocrine pancreatic carcinoma1MONDO:0005192EFO:0002618
neuroendocrine neoplasm1MONDO:0019496EFO:1001901
colorectal neoplasm1MONDO:0005335MONDO:0005575

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

Clinical trials

Total trials: 242.

Phase distribution

PhaseTrials
PHASE2108
PHASE148
PHASE341
PHASE1/PHASE221
Not specified15
PHASE43
PHASE2/PHASE33
EARLY_PHASE13

Top trials by phase / activity

NCTPhaseStatusTitle
NCT00255268PHASE4WITHDRAWNCMAB vs IMAB in Metastatic Prostate Cancer
NCT00470834PHASE4COMPLETEDProstate Cancer Study In Men Who Have Failed First-Line Androgen Deprivation Therapy
NCT04248621PHASE4UNKNOWNAndrogen Deprivation Therapy on Bone Mineral Density Change in Prostate Cancer Patients
NCT02531516PHASE3ACTIVE_NOT_RECRUITINGAn Efficacy and Safety Study of JNJ-56021927 (Apalutamide) in High-risk Prostate Cancer Subjects Receiving Primary Radiation Therapy: ATLAS
NCT03458221PHASE2/PHASE3RECRUITINGSignal TrAnsduction Pathway Activity Analysis in OVarian cancER
NCT03678025PHASE3RECRUITINGStandard Systemic Therapy With or Without Definitive Treatment in Treating Participants With Metastatic Prostate Cancer
NCT04513717PHASE3ACTIVE_NOT_RECRUITINGTwo Studies for Patients With High Risk Prostate Cancer Testing Less Intense Treatment for Patients With a Low Gene Risk Score and Testing a More Intense Treatment for Patients With a High Gene Risk Score, The PREDICT-RT Trial
NCT05019846PHASE3RECRUITINGSRT Versus SRT+ADT in Prostate Cancer
NCT05050084PHASE3ACTIVE_NOT_RECRUITINGTwo Studies for Patients With Unfavorable Intermediate Risk Prostate Cancer Testing Less Intense Treatment for Patients With a Low Gene Risk Score and Testing a More Intense Treatment for Patients With a Higher Gene Risk Score, The Guidance Trial
NCT05059522PHASE3ACTIVE_NOT_RECRUITINGContinued Access Study for Participants Deriving Benefit in Pfizer-Sponsored Avelumab Parent Studies That Are Closing
NCT06650579PHASE3RECRUITINGREVELUTION-2: Relugolix+Abiraterone Acetate (AA) Versus Leuprolide+AA Cardiac Trial
NCT00002633PHASE3COMPLETEDHormone Therapy With or Without Surgery or Radiation Therapy in Treating Patients With Prostate Cancer
NCT00002651PHASE3COMPLETEDSWOG-9346, Hormone Therapy in Treating Men With Stage IV Prostate Cancer
NCT00002855PHASE3COMPLETEDChemotherapy Plus Hormone Therapy Versus Androgen Suppression in Treating Patients With Metastatic or Unresectable Prostate Cancer
NCT00002874PHASE3COMPLETEDRadiation Therapy With or Without Bicalutamide for Recurrent pT3N0 Prostate Cancer After Radical Prostatectomy
NCT00003026PHASE3COMPLETEDHormone Therapy in Treating Patients With Advanced Prostate Cancer
NCT00003653PHASE3COMPLETEDHormone Therapy in Treating Patients With Rising PSA Levels Following Radiation Therapy for Prostate Cancer
NCT00004054PHASE3COMPLETEDHormone Therapy Plus Radiation Therapy With or Without Combination Chemotherapy in Treating Patients With Prostate Cancer
NCT00004124PHASE3COMPLETEDS9921, Hormone Therapy With or Without Mitoxantrone and Prednisone in Patients Who Have Undergone Radical Prostatectomy for Prostate Cancer
NCT00014586PHASE3TERMINATEDBicalutamide Compared With Observation Followed by Bicalutamide Plus Either Goserelin or Orchiectomy in Treating Patients With Prostate Cancer
NCT00021450PHASE3COMPLETEDRadiation Therapy With or Without Bicalutamide and Goserelin in Treating Patients With Prostate Cancer
NCT00023829PHASE3COMPLETEDAdjuvant Radiation Therapy Plus Hormone Therapy Compared With Radiation Therapy Alone in Treating Patients With Stage II or Stage III Prostate Cancer
NCT00030654PHASE3COMPLETEDHormone Therapy Plus Chemotherapy in Treating Patients With Prostate Cancer
NCT00055731PHASE3COMPLETEDHormone Therapy With or Without Docetaxel And Estramustine in Treating Patients With Prostate Cancer That is Locally Advanced or At High Risk of Relapse
NCT00067015PHASE3COMPLETEDRadiation Therapy With or Without Bicalutamide and Goserelin in Treating Patients With Prostate Cancer
NCT00233610PHASE3COMPLETEDTwo Different Regimens of Nolvadex in Preventing Gynecomastia Induced by Casodex 150 mg in Patients With Prostate Cancer
NCT00388804PHASE3TERMINATEDExternal Beam Radiation Therapy (EBRT) With or Without Hormonal Therapy in Prostate Cancer
NCT00421694PHASE2/PHASE3COMPLETEDPositive Surgical Margins Rate and EGFR Family Members Expression in Prostate Cancer Treated With Bicalutamide
NCT00514917PHASE3TERMINATEDA Study of Androgen Deprivation With Leuprolide, +/- Docetaxel for Clinically Asymptomatic Prostate Cancer Participants With a Rising Prostate Specific Antigen (PSA)
NCT00541047PHASE3COMPLETEDRADICALS - Radiotherapy and Androgen Deprivation In Combination After Local Surgery
NCT00651326PHASE3TERMINATEDAndrogen Suppression and Radiation With/Out Docetaxel in High-Risk Localized Prostate Cancer
NCT00657904PHASE3COMPLETEDBicalutamide (Casodex™) Versus Placebo in Patients With Early Prostate Cancer
NCT00672282PHASE3COMPLETEDCasodex vs Placebo in Non-Metastatic Early Prostate Cancer
NCT00673205PHASE3COMPLETED(Bicalutamide) Casodex vs Placebo in Non-metastatic Early Prostate Cancer
NCT00831233PHASE3TERMINATEDSymptomatic Study Investigating Degarelix in Patients Suffering From Prostate Cancer
NCT00833248PHASE3COMPLETEDNeoadjuvant Study Investigating Degarelix in Patients Suffering From Prostate Cancer
NCT00846976PHASE3COMPLETEDTreatment Protocol to Monitor the Safety of a 200 mg Dose of Bicalutamide in Patients With Advanced Prostate Cancer
NCT00884273PHASE3COMPLETEDInvestigation of the Effect of Degarelix in Terms of Prostate Volume Reduction in Prostate Cancer Patients
NCT00936390PHASE3COMPLETEDRadiation Therapy With or Without Androgen-Deprivation Therapy in Treating Patients With Prostate Cancer
NCT01809691PHASE3COMPLETEDS1216, Phase III ADT+TAK-700 vs. ADT+Bicalutamide for Metastatic Prostate Cancer

Clinical evidence (CIViC)

Variant × indication × effect (28 predictive associations from 28 curated evidence items):

VariantIndicationEffectTherapyLevelCIViC
ATR Loss-of-functionCastration-resistant Prostate CarcinomaSensitivity/ResponseTalazoparib + EnzalutamideCIViC AEID12217
BRCA1 MutationCastration-resistant Prostate CarcinomaSensitivity/ResponseTalazoparib + EnzalutamideCIViC AEID11734
BRCA2 MutationCastration-resistant Prostate CarcinomaSensitivity/ResponseTalazoparib + EnzalutamideCIViC AEID11733
CDK12 MutationCastration-resistant Prostate CarcinomaSensitivity/ResponseTalazoparib + EnzalutamideCIViC AEID11735
AR OVEREXPRESSIONSalivary Gland CancerSensitivity/ResponseBicalutamide + LeuprolideCIViC BEID6953
ATM MutationCastration-resistant Prostate CarcinomaSensitivity/ResponseEnzalutamide + TalazoparibCIViC BEID11736
BRCA1 Loss-of-functionBreast CancerSensitivity/ResponseTalazoparibCIViC BEID4838
BRCA1 Loss-of-functionOvarian CancerSensitivity/ResponseTalazoparibCIViC BEID4876
BRCA2 Loss-of-functionBreast CancerSensitivity/ResponseTalazoparibCIViC BEID4839
BRCA2 Loss-of-functionOvarian CancerSensitivity/ResponseTalazoparibCIViC BEID4875
CHEK2 mutationCastration-resistant Prostate CarcinomaSensitivity/ResponseEnzalutamide + TalazoparibCIViC BEID11737
PALB2 Oncogenic Mutations (loss of function alterations)Her2-receptor Negative Breast CancerSensitivity/ResponseTalazoparibCIViC BEID10856
AR MutationProstate CancerResistanceFlutamide + Cyproterone Acetate + Nilutamide + BicalutamideCIViC BEID1521
EMSY AmplificationAcral Lentiginous MelanomaSensitivity/ResponseTalazoparibCIViC CEID12148
PALB2 MutationPancreatic Ductal AdenocarcinomaSensitivity/ResponseTalazoparibCIViC CEID10835
ATRX Loss-of-functionGlioblastomaSensitivity/ResponseOlaparib + TalazoparibCIViC DEID10940
BRCA2 Loss-of-functionProstate CancerSensitivity/ResponseDasatinib + TalazoparibCIViC DEID8980
BRCA2 Loss-of-functionProstate CancerSensitivity/ResponseTalazoparib + BosutinibCIViC DEID8982
CDK12 Loss-of-functionBreast CarcinomaSensitivity/ResponseTalazoparib + OlaparibCIViC DEID12571
CDK12 Loss-of-functionProstate CancerSensitivity/ResponseTalazoparib + Olaparib + Rucaparib + VeliparibCIViC DEID12572
EGFR AmplificationGlioblastomaSensitivity/ResponseTalazoparibCIViC DEID7785
MRE11 LossEndometrial CancerSensitivity/ResponseTalazoparibCIViC DEID876
MYCN OverexpressionNeuroblastomaSensitivity/ResponseNiraparib + Veliparib + Olaparib + TalazoparibCIViC DEID9006
PSMD4 AmplificationBreast CancerSensitivity/ResponseTalazoparibCIViC DEID4834
RB1 Loss-of-functionOsteosarcomaSensitivity/ResponseOlaparib + Niraparib + TalazoparibCIViC DEID12032
SLFN11 EXPRESSIONLung Small Cell CarcinomaSensitivity/ResponseTemozolomide + TalazoparibCIViC DEID5883
AR W742Prostate CarcinomaResistanceBicalutamideCIViC DEID448
CFLAR EXPRESSIONProstate CancerResistanceBicalutamideCIViC DEID925

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.

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

MoleculeSourceStatusShared targets
NIRAPARIBChEMBLPhase 4 (approved)PARP1, PARP2
OLAPARIBChEMBLPhase 4 (approved)PARP1, PARP2
RUCAPARIBChEMBLPhase 4 (approved)PARP1, PARP2
PAMIPARIBChEMBLPhase 3PARP1, 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