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Saruparib

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Also known as Azd 5305Azd-5305AZD5305US11325906Example 4

Summary

Saruparib (CHEMBL5095220) is a phase-3 clinical-stage small molecule targeting PARP1 and PARP2; indicated across 6 conditions including breast neoplasm and neoplasm.

At a glance

  • Status: Max clinical phase 3 (not approved)
  • Modality: Small molecule
  • Targets: 2 (PARP1, PARP2)
  • Indications: 6 conditions
  • Clinical trials: 16
  • Chemistry: 406.5 Da · C22H26N6O2

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL5095220
NameSaruparib
TypeSmall molecule
Max phase3
FDA approvedno
PubChem CID155586901
Molecular formulaC22H26N6O2
Molecular weight406.5
InChIKeyWQAVGRAETZEADU-UHFFFAOYSA-N

SMILES: CCC1=CC2=C(C=C(C=N2)CN3CCN(CC3)C4=CN=C(C=C4)C(=O)NC)NC1=O

IUPAC name: 5-[4-[(7-ethyl-6-oxo-5H-1,5-naphthyridin-3-yl)methyl]piperazin-1-yl]-N-methylpyridine-2-carboxamide

Also known as: Azd 5305, Azd-5305, AZD5305, Saruparib, SARUPARIB, AZD-5305, AZD 5305, US11325906, Example 4

Patent coverage: 186 distinct patent families (357 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 320 (90%) 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 1Inhibition8.44.1%P09874
PARP2poly(ADP-ribose) polymerase 2Inhibition5.820.2%Q9UGN5

Broader ChEMBL bioactivity targets: 5 (assay-derived). Sample: Protein mono-ADP-ribosyltransferase PARP6, Protein mono-ADP-ribosyltransferase TIPARP, Poly [ADP-ribose] polymerase 1, Protein mono-ADP-ribosyltransferase PARP3, Poly [ADP-ribose] polymerase 2.

Bioactivity

ChEMBL activities: 19 potent at pChembl ≥ 5 of 20 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
PARP19.51IC500.31nMCHEMBL_ACT_24870078
PARP19.26Kd0.55nMCHEMBL_ACT_29104508
PARP19.19IC500.65nMCHEMBL_ACT_24870134
PARP18.52IC503nMCHEMBL_ACT_24867292
PARP18.52IC503nMCHEMBL_ACT_29087906
PARP28.4IC504nMCHEMBL_ACT_24870106
PARP18.4IC504nMCHEMBL_ACT_28695233
PARP17.95EC5011.3nMCHEMBL_ACT_29104511
PARP17.61EC5024.7nMCHEMBL_ACT_29104514
PARP17.44EC5036nMCHEMBL_ACT_29104517
TIPARP7.38IC5041.7nMCHEMBL_ACT_29104547
PARP26.62IC50239.6nMCHEMBL_ACT_24870162
PARP26.38EC50415nMCHEMBL_ACT_29104520
PARP16.34IC50460nMCHEMBL_ACT_29104225
PARP25.85IC501400nMCHEMBL_ACT_24867317
PARP25.85IC501400nMCHEMBL_ACT_29087931
PARP35.47IC503400nMCHEMBL_ACT_29104535
PARP35.33IC504700nMCHEMBL_ACT_28695239
PARP25IC5010000nMCHEMBL_ACT_29104267

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

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
neoplasm2MONDO:0005070EFO:0000616
metastatic prostate carcinoma1MONDO:0004956EFO:0000196
non-small cell lung carcinoma1MONDO:0005233EFO:0003060

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

Clinical trials

Total trials: 16.

Phase distribution

PhaseTrials
PHASE1/PHASE26
PHASE15
PHASE33
PHASE21
EARLY_PHASE11

Top trials by phase / activity

NCTPhaseStatusTitle
NCT06120491PHASE3ACTIVE_NOT_RECRUITINGSaruparib (AZD5305) vs Placebo in Men With Metastatic Castration-Sensitive Prostate Cancer Receiving Physician’s Choice New Hormonal Agents
NCT06380751PHASE3RECRUITINGSaruparib (AZD5305) Plus Camizestrant Compared With CDK4/6 Inhibitor Plus Endocrine Therapy or Plus Camizestrant in HR-Positive, HER2-Negative (IHC 0, 1+, 2+/ ISH Non-amplified), BRCA1, BRCA2, or PALB2m Advanced Breast Cancer
NCT06952803PHASE3RECRUITINGA Study of Metastases Free Survival With Saruparib vs Placebo Added to a Standard RT/ADT in Men With High-risk Prostate Cancer With a BRCA Mutation
NCT04644068PHASE1/PHASE2ACTIVE_NOT_RECRUITINGStudy of AZD5305 as Monotherapy and in Combination With Anti-cancer Agents in Patients With Advanced Solid Malignancies
NCT05367440PHASE1/PHASE2ACTIVE_NOT_RECRUITINGStudy of AZD5305 When Given in Combination With New Hormonal Agents in Patients With Metastatic Prostate Cancer
NCT05797168PHASE1/PHASE2RECRUITINGPhase I/IIa Study of AZD5335 as Monotherapy and Combination Therapy in Participants With Solid Tumors
NCT06769126PHASE2RECRUITINGUsing Biomarker Tests to Select and Test New, Personalized Treatments for Extensive Stage Small Cell Lung Cancer, PRISM Study
NCT07336446PHASE1/PHASE2RECRUITINGA Trial to Learn How Safe AZD9750 is and How Well it Works in People With Metastatic Prostate Cancer When Given With or Without Other Anticancer Drugs
NCT07446855PHASE1/PHASE2RECRUITINGStudy of AZD4956 as Monotherapy and in Combination With Anti-Cancer Agents in Participants With Advanced/Metastatic Homologous Recombination Deficient Solid Tumours
NCT07060365PHASE1/PHASE2WITHDRAWNA Master Protocol Study to Investigate Biomarker-guided Novel Anticancer Agent(s) as Monotherapy or Combination Therapy in Participants With Advanced/Recurrent Ovarian Cancer
NCT04550104PHASE1RECRUITINGA Platform Study of Novel Agents in Combination With Radiotherapy in NSCLC
NCT05938270PHASE1RECRUITINGA Study to Investigate the Biological Effects of Saruparib (AZD5305), Darolutamide, and in Combination in Men With Newly Diagnosed Prostate Cancer.
NCT06713369PHASE1RECRUITINGAZD5305 hADME in Patients With Advanced Solid Malignancies
NCT06899061PHASE1ACTIVE_NOT_RECRUITINGModular Clinical Pharmacology Study to Evaluate the Drug-drug Interaction Potential and Relative Bioavailability of Saruparib
NCT05573724PHASE1COMPLETEDDrug-drug Interaction Study With AZD5305 and Itraconazole in Patients With Advanced Solid Malignancies
NCT04005690EARLY_PHASE1RECRUITINGTargeted Pathway Inhibition in Patients With Pancreatic 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
TALAZOPARIBChEMBL + PubChemPhase 4 (approved)PARP1, PARP2
NIRAPARIBChEMBLPhase 4 (approved)PARP1, PARP2
OLAPARIBChEMBLPhase 4 (approved)PARP1, PARP2
RUCAPARIBChEMBLPhase 4 (approved)PARP1, PARP2
PAMIPARIBChEMBLPhase 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