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Saracatinib

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Also known as AZ-10353926Azd-0530AZD0530SID137275842SID164339484SARACATINIB (AZD0530)

Summary

Saracatinib (CHEMBL217092) is a phase-3 clinical-stage small-molecule antineoplastic agent targeting ABL1, LCK, and SRC; indicated across 21 conditions including osteosarcoma and non-small cell lung carcinoma.

At a glance

  • Status: Max clinical phase 3 (not approved)
  • Modality: Small molecule
  • Targets: 4 (ABL1, LCK, SRC…)
  • Indications: 21 conditions
  • Clinical trials: 32
  • Chemistry: 542 Da · C27H32ClN5O5

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL217092
NameSaracatinib
TypeSmall molecule
Max phase3
FDA approvedno
PubChem CID10302451
ChEBICHEBI:47458
Molecular formulaC27H32ClN5O5
Molecular weight542
InChIKeyOUKYUETWWIPKQR-UHFFFAOYSA-N

SMILES: CN1CCN(CC1)CCOC2=CC3=C(C(=C2)OC4CCOCC4)C(=NC=N3)NC5=C(C=CC6=C5OCO6)Cl

IUPAC name: N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5-(oxan-4-yloxy)quinazolin-4-amine

ChEBI definition: A member of the class of quinazolines that is quinazoline substituted by (5-chloro-2H-1,3-benzodioxol-4-yl)amino, (oxan-4-yl)oxy and 2-(4-methylpiperazin-1-yl)ethoxy groups at positions 4, 5 and 7, respectively. It is a dual inhibitor of the tyrosine kinases c-Src and Abl (IC50 = 2.7 and 30 nM, respectively). Saracatinib was originally developed by AstraZeneca for the treatment of cancer but in 2019 it was granted orphan drug designation by the US Food and Drug Administration for the treatment of idiopathic pulmonary fibrosis (IPF), a type of lung disease that results in scarring (fibrosis) of the lungs.

Pharmacological roles (ChEBI): antineoplastic agent, EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor, radiosensitizing agent, autophagy inducer, apoptosis inducer, anticoronaviral agent, antifibrotic agent.

Also known as: AZ-10353926, Azd-0530, AZD-0530, AZD0530, Saracatinib, SARACATINIB, SID137275842, SID164339484, SARACATINIB (AZD0530), Saracatinib (AZD0530)

Parent form; salt/anhydrous children: CHEMBL2105677

Patent coverage: 1,541 distinct patent families (3,982 SureChEMBL compound mentions), from 4 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
ABL1ABL proto-oncogene 1, non-receptor tyrosine kinaseInhibition7.521.2%P00519
LCKLCK proto-oncogene, Src family tyrosine kinaseInhibition8.40.1%P06239
SRCSRC proto-oncogene, non-receptor tyrosine kinaseInhibition8.573.7%P12931
YES1YES proto-oncogene 1, Src family tyrosine kinaseInhibition8.40.7%P07947

Broader ChEMBL bioactivity targets: 52 (assay-derived). Sample: Receptor-interacting serine/threonine-protein kinase 3, Tyrosine-protein kinase Fyn, Tyrosine-protein kinase ABL1, Platelet-derived growth factor receptor beta, Mast/stem cell growth factor receptor Kit, Receptor-type tyrosine-protein kinase FLT3, Platelet-derived growth factor receptor alpha, Epidermal growth factor receptor, Proto-oncogene tyrosine-protein kinase receptor Ret, Ephrin type-A receptor 2.

Bioactivity

ChEMBL activities: 76 potent at pChembl ≥ 5 of 85 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
YES19.15IC500.7nMCHEMBL_ACT_13395971
SRC9IC501nMCHEMBL_ACT_2200439
RIPK28.7Kd2nMCHEMBL_ACT_17935466
SRC8.57IC502.7nMCHEMBL_ACT_1779153
SRC8.57IC502.7nMCHEMBL_ACT_18997586
SRC8.57IC502.7nMCHEMBL_ACT_24788709
SRC8.57IC502.7nMCHEMBL_ACT_24789088
SRC8.57IC502.7nMCHEMBL_ACT_3302211
SRC8.57IC502.7nMCHEMBL_ACT_6175410
SRC8.52IC503nMCHEMBL_ACT_2206875
SRC8.52IC503nMCHEMBL_ACT_2419440
YES18.4IC504nMCHEMBL_ACT_1779377
ACVR18.4Kd4nMCHEMBL_ACT_17880697
YES18.4IC504nMCHEMBL_ACT_2206877
LCK8.4IC504nMCHEMBL_ACT_2206878
YES18.4IC504nMCHEMBL_ACT_3316532
YES18.21IC506.2nMCHEMBL_ACT_13395981
LCK8.05Kd9nMCHEMBL_ACT_17909332
EPHA18Kd10nMCHEMBL_ACT_17899275
SRC8IC5010nMCHEMBL_ACT_2419441
BCR7.8Kd16nMCHEMBL_ACT_17884608
BMPR1B7.54Kd29nMCHEMBL_ACT_17885319
ABL17.52IC5030nMCHEMBL_ACT_1779385
ABL17.52IC5030nMCHEMBL_ACT_2206879
ABL17.52IC5030nMCHEMBL_ACT_3316531
PKMYT17.4Ki39.8nMCHEMBL_ACT_18664787
ABL17.28Kd53nMCHEMBL_ACT_17878406
BMPR1A7.22Kd60nMCHEMBL_ACT_17885068
EGFR7.18IC5066nMCHEMBL_ACT_19218784
SRC7.12IC5076nMCHEMBL_ACT_1779226

Target pathways

Aggregated over 4 target gene(s): ABL1, LCK, SRC, YES1.

Top Reactome pathways

183 total, by targets touching each:

PathwayTargetsGenes
Hemostasis3ABL1, LCK, SRC
Signaling by SCF-KIT3LCK, SRC, YES1
Regulation of KIT signaling3LCK, SRC, YES1
Signal Transduction3ABL1, LCK, SRC
Disease3ABL1, LCK, SRC
Immune System3ABL1, LCK, SRC
Signaling by Rho GTPases3ABL1, LCK, SRC
PECAM1 interactions3LCK, SRC, YES1
Co-stimulation by CD283LCK, SRC, YES1
Co-inhibition by CTLA43LCK, SRC, YES1
Infectious disease3ABL1, LCK, SRC
RUNX2 regulates osteoblast differentiation3ABL1, SRC, YES1
FCGR3A-mediated phagocytosis3ABL1, SRC, YES1
Signaling by phosphorylated juxtamembrane, extracellular and kinase domain KIT mutants3LCK, SRC, YES1
Signaling by Rho GTPases, Miro GTPases and RHOBTB33ABL1, LCK, SRC
Signaling by ERBB22SRC, YES1
PIP3 activates AKT signaling2LCK, SRC
Developmental Biology2ABL1, SRC
Cytokine Signaling in Immune system2LCK, SRC
Innate Immune System2ABL1, LCK
Negative regulation of the PI3K/AKT network2LCK, SRC
FCGR activation2SRC, YES1
Generic Transcription Pathway2ABL1, SRC
PI3K/AKT Signaling in Cancer2LCK, SRC
Constitutive Signaling by Aberrant PI3K in Cancer2LCK, SRC
EPH-Ephrin signaling2SRC, YES1
Signaling by ROBO receptors2ABL1, SRC
EPHB-mediated forward signaling2SRC, YES1
EPHA-mediated growth cone collapse2SRC, YES1
EPH-ephrin mediated repulsion of cells2SRC, YES1

Dominant GO biological processes

GO termTargets
protein phosphorylation4
intracellular signal transduction3
Fc-gamma receptor signaling pathway involved in phagocytosis3
ephrin receptor signaling pathway3
cellular response to transforming growth factor beta stimulus3
T cell costimulation3
leukocyte migration3
epidermal growth factor receptor signaling pathway2
integrin-mediated signaling pathway2
response to xenobiotic stimulus2
substrate adhesion-dependent cell spreading2
protein modification process2
positive regulation of transcription by RNA polymerase II2
T cell receptor signaling pathway2
B cell receptor signaling pathway2

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
osteosarcoma2MONDO:0009807EFO:0000637
non-small cell lung carcinoma2MONDO:0005233EFO:0003060
male breast carcinoma2MONDO:0005628EFO:0006861
neoplasm2MONDO:0005070EFO:0000616
melanoma2MONDO:0005105EFO:0000756
thymoma2MONDO:0006456EFO:1000581
colorectal adenocarcinoma2MONDO:0005008EFO:0000365
rectal cancer2MONDO:0006519EFO:1000657
fallopian tube neoplasm2MONDO:0021092MONDO:0002158
ovarian cancer2MONDO:0008170MONDO:0008170
colonic neoplasm2MONDO:0005401MONDO:0021063
breast neoplasm2MONDO:0021100MONDO:0007254
Alzheimer disease2MONDO:0004975MONDO:0004975
myositis ossificans2MONDO:0003964MONDO:0007606
lymphangioleiomyomatosis2MONDO:0011705MONDO:0011705
thymus neoplasm2MONDO:0005197EFO:0002626
exocrine pancreatic carcinoma1MONDO:0005192EFO:0002618
alcohol abuse1MONDO:0002046MONDO:0007079

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

Clinical trials

Total trials: 32.

Phase distribution

PhaseTrials
PHASE218
PHASE110
PHASE1/PHASE22
PHASE2/PHASE31
EARLY_PHASE11

Top trials by phase / activity

NCTPhaseStatusTitle
NCT01196741PHASE2/PHASE3COMPLETEDSaracatinib and Paclitaxel in Platinum-resistant Ovarian Cancer
NCT00265876PHASE1/PHASE2COMPLETEDAZD0530 and Gemcitabine in Locally Advanced/Metastatic Pancreatic Cancer That Cannot Be Removed By Surgery
NCT00397878PHASE2TERMINATEDAZD0530 (NSC 735464) in Treating Patients With Previously Treated Metastatic Colon Cancer or Rectal Cancer
NCT00513071PHASE2COMPLETEDAZD0530 in Treating Patients With Prostate Cancer That Did Not Respond to Hormone Therapy
NCT00513435PHASE2COMPLETEDSaracatinib in Treating Patients With Recurrent or Metastatic Head and Neck Cancer
NCT00528645PHASE2COMPLETEDAZD0530 in Treating Patients With Extensive Stage Small Cell Lung Cancer
NCT00558272PHASE2COMPLETEDStudy to Evaluate the Safety and Effects AZD0530 on Prostate and Breast Cancer Subjects With Metastatic Bone Disease
NCT00559507PHASE2COMPLETEDSaracatinib in Treating Patients With Metastatic or Locally Advanced Breast Cancer That Cannot Be Removed By Surgery
NCT00607594PHASE2COMPLETEDSaracatinib in Treating Patients With Locally Advanced or Metastatic Stomach or Gastroesophageal Junction Cancer
NCT00610714PHASE2COMPLETEDAZD0530 Phase II Study in Patients With Advanced Ovarian Cancer
NCT00638937PHASE2COMPLETEDAZD0530 to Treat Recurrent Stage IIIB/IV NSCLC Previously Treated With Combination Chemotherapy
NCT00659360PHASE2COMPLETEDAZD0530 in Treating Patients With Recurrent Locally Advanced or Metastatic Soft Tissue Sarcoma
NCT00669019PHASE2COMPLETEDSaracatinib in Treating Patients With Stage III or Stage IV Melanoma That Cannot Be Removed By Surgery
NCT00718809PHASE2TERMINATEDSaracatinib in Treating Patients With Relapsed or Refractory Thymoma or Thymic Cancer
NCT00735917PHASE2COMPLETEDSaracatinib in Treating Patients With Previously Treated Metastatic Pancreatic Cancer
NCT00752206PHASE2TERMINATEDA Placebo-Controlled Study of Saracatinib (AZD0530) in Patients With Recurrent Osteosarcoma Localized to the Lung
NCT01216176PHASE1/PHASE2COMPLETEDA Pharmacokinetic and Randomized Trial of Neoadjuvant Treatment With Anastrozole Plus AZD0530 in Postmenopausal Patients With Hormone Receptor Positive Breast Cancer
NCT01267266PHASE2TERMINATEDSaracatinib in Treating Patients With Prostate Cancer
NCT02085603PHASE2COMPLETEDSarCaBon: A Randomised Phase II Trial of Saracatinib Versus Placebo for Cancer-induced Bone Pain
NCT02737202PHASE2TERMINATEDSafety and Efficacy of Saracatinib In Subjects With Lymphangioleiomyomatosis
NCT02955186PHASE2COMPLETEDSaracatinib and Alcohol Drinking
NCT00475956PHASE1COMPLETEDSafety and Tolerability Study of AZD2171 in Combination With AZD0530 in Patients With Advanced Solid Tumours
NCT00496028PHASE1COMPLETEDPhase I Study in Patients With Solid Tumours
NCT00704366PHASE1COMPLETEDAZD0530 Study 21 - Phase I Study in Patients With Solid Tumours
NCT00771979PHASE1COMPLETEDRelative Bioavailability of Phase II and Phase III Formulations of AZD0530
NCT00853983PHASE1COMPLETEDPhase I Study to Assess Absorption, Metabolism & Excretion of a Single Oral Dose [14C]AZD0530 in Healthy Male Volunteers
NCT01000896PHASE1WITHDRAWNStudy to Assess Safety and Tolerability of AZD0530 in Combination With Carboplatin and Paclitaxel
NCT01864655PHASE1COMPLETEDSafety and Tolerability of AZD0530 (Saracatinib) in Alzheimer’s Disease
NCT02116712PHASE1COMPLETEDThe Tolerability of Saracatinib in Subjects With Lymphangioleiomyomatosis (LAM) (SLAM-1)
NCT02262026PHASE1COMPLETEDThe Tolerability and Effects of AZD0530 in Individuals With or Without a Family History of Alcoholism
NCT02732587PHASE1COMPLETEDInvestigating the Interactions of AZD0530 With Alcohol in Social Drinkers
NCT03661125EARLY_PHASE1UNKNOWNSRC Inhibition as a Potential Target for Parkinson’s Disease Psychosis

Clinical evidence (CIViC)

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

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.

181 molecules share ≥1 primary target. Top 60 by shared-target count:

MoleculeSourceStatusShared targets
AFATINIBChEMBL + PubChemPhase 4 (approved)ABL1, LCK, SRC, YES1
CRIZOTINIBChEMBL + PubChemPhase 4 (approved)ABL1, LCK, SRC, YES1
dacomitinibChEMBL + PubChemPhase 4 (approved)ABL1, LCK, SRC, YES1
ERLOTINIBChEMBL + PubChemPhase 4 (approved)ABL1, LCK, SRC, YES1
FEDRATINIBChEMBL + PubChemPhase 4 (approved)ABL1, LCK, SRC, YES1
GEFITINIBChEMBL + PubChemPhase 4 (approved)ABL1, LCK, SRC, YES1
PAZOPANIBChEMBL + PubChemPhase 4 (approved)ABL1, LCK, SRC, YES1
REGORAFENIBChEMBL + PubChemPhase 4 (approved)ABL1, LCK, SRC, YES1
BOSUTINIBChEMBLPhase 4 (approved)ABL1, LCK, SRC, YES1
BRIGATINIBChEMBLPhase 4 (approved)ABL1, LCK, SRC, YES1
DASATINIBChEMBLPhase 4 (approved)ABL1, LCK, SRC, YES1
IBRUTINIBChEMBLPhase 4 (approved)ABL1, LCK, SRC, YES1
INFIGRATINIBChEMBLPhase 4 (approved)ABL1, LCK, SRC, YES1
MIDOSTAURINChEMBLPhase 4 (approved)ABL1, LCK, SRC, YES1
NERATINIBChEMBLPhase 4 (approved)ABL1, LCK, SRC, YES1
NILOTINIBChEMBLPhase 4 (approved)ABL1, LCK, SRC, YES1
NINTEDANIBChEMBLPhase 4 (approved)ABL1, LCK, SRC, YES1
PONATINIBChEMBLPhase 4 (approved)ABL1, LCK, SRC, YES1
SUNITINIBChEMBLPhase 4 (approved)ABL1, LCK, SRC, YES1
VANDETANIBChEMBLPhase 4 (approved)ABL1, LCK, SRC, YES1
CANERTINIBChEMBLPhase 3ABL1, LCK, SRC, YES1
CEDIRANIBChEMBLPhase 3ABL1, LCK, SRC, YES1
DOVITINIBChEMBLPhase 3ABL1, LCK, SRC, YES1
LESTAURTINIBChEMBLPhase 3ABL1, LCK, SRC, YES1
MASITINIBChEMBLPhase 3ABL1, LCK, SRC, YES1
TESEVATINIBChEMBLPhase 3ABL1, LCK, SRC, YES1
AT-9283ChEMBLPhase 2ABL1, LCK, SRC, YES1
BMS-690514ChEMBLPhase 2ABL1, LCK, SRC, YES1
DANUSERTIBChEMBLPhase 2ABL1, LCK, SRC, YES1
DORAMAPIMODChEMBLPhase 2ABL1, LCK, SRC, YES1
ENMD-2076ChEMBLPhase 2ABL1, LCK, SRC, YES1
FORETINIBChEMBLPhase 2ABL1, LCK, SRC, YES1
MILCICLIBChEMBLPhase 2ABL1, LCK, SRC, YES1
NEFLAMAPIMODChEMBLPhase 2ABL1, LCK, SRC, YES1
OSI-632ChEMBLPhase 2ABL1, LCK, SRC, YES1
PELITINIBChEMBLPhase 2ABL1, LCK, SRC, YES1
R-406ChEMBLPhase 2ABL1, LCK, SRC, YES1
RAF-265ChEMBLPhase 2ABL1, LCK, SRC, YES1
REBASTINIBChEMBLPhase 2ABL1, LCK, SRC, YES1
SU-014813ChEMBLPhase 2ABL1, LCK, SRC, YES1
TOZASERTIBChEMBLPhase 2ABL1, LCK, SRC, YES1
BinimetinibPubChemApprovedABL1, LCK, SRC, YES1
FostamatinibPubChemApprovedABL1, LCK, SRC, YES1
IdelalisibPubChemApprovedABL1, LCK, SRC, YES1
SelumetinibPubChemApprovedABL1, LCK, SRC, YES1
AXITINIBChEMBLPhase 4 (approved)ABL1, LCK, YES1
CABOZANTINIBChEMBLPhase 4 (approved)ABL1, LCK, SRC
CERITINIBChEMBLPhase 4 (approved)ABL1, LCK, SRC
DABRAFENIBChEMBLPhase 4 (approved)ABL1, LCK, YES1
ENTRECTINIBChEMBLPhase 4 (approved)ABL1, LCK, SRC
IMATINIBChEMBLPhase 4 (approved)ABL1, LCK, SRC
QUIZARTINIBChEMBLPhase 4 (approved)ABL1, LCK, YES1
SORAFENIBChEMBLPhase 4 (approved)ABL1, LCK, SRC
TIVOZANIBChEMBLPhase 4 (approved)ABL1, LCK, SRC
ALISERTIBChEMBLPhase 3ABL1, LCK, SRC
ALVOCIDIBChEMBLPhase 3ABL1, LCK, SRC
BRIVANIBChEMBLPhase 3ABL1, LCK, SRC
MOTESANIBChEMBLPhase 3ABL1, LCK, YES1
QUERCETINChEMBLPhase 3LCK, SRC, YES1
BMS-754807ChEMBLPhase 2ABL1, LCK, SRC

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