◎ Sugi Atlas

Atlas / Drug / Olverembatinib

Olverembatinib

drug
On this page

Also known as D-824D-824 DIMESYLATEGZD-824GZD-824 DIMESYLATEHQP-1351HQP-1351 DIMESYLATEHqp1351HQP1351 DIMESYLATEOlverembatinib dimesylateGZD824 DIMESYLATE

Summary

Olverembatinib (CHEMBL2316582) is a phase-3 clinical-stage small molecule targeting ABL1; indicated across 6 conditions including chronic myeloid leukemia and acute lymphoblastic leukemia.

At a glance

  • Status: Max clinical phase 3 (not approved)
  • Modality: Small molecule
  • Targets: 1 (ABL1)
  • Indications: 6 conditions
  • Clinical trials: 32
  • Chemistry: 532.6 Da · C29H27F3N6O

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL2316582
NameOlverembatinib
TypeSmall molecule
Max phase3
FDA approvedno
PubChem CID51038269
Molecular formulaC29H27F3N6O
Molecular weight532.6
InChIKeyTZKBVRDEOITLRB-UHFFFAOYSA-N

SMILES: CC1=C(C=C(C=C1)C(=O)NC2=CC(=C(C=C2)CN3CCN(CC3)C)C(F)(F)F)C#CC4=CC5=C(NN=C5)N=C4

IUPAC name: 4-methyl-N-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]-3-[2-(1H-pyrazolo[5,4-b]pyridin-5-yl)ethynyl]benzamide

Also known as: D-824, D-824 DIMESYLATE, GZD-824, GZD-824 DIMESYLATE, HQP-1351, HQP-1351 DIMESYLATE, Hqp1351, HQP1351, HQP1351 DIMESYLATE, Olverembatinib, Olverembatinib dimesylate, OLVEREMBATINIB

Parent form; salt/anhydrous children: CHEMBL5575988

Patent coverage: 138 distinct patent families (353 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 297 (84%) 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
ABL1ABL proto-oncogene 1, non-receptor tyrosine kinaseInhibition9.471.2%P00519

Broader ChEMBL bioactivity targets: 8 (assay-derived). Sample: Leucine-rich repeat serine/threonine-protein kinase 2, Tyrosine-protein kinase ABL1, Protein deacetylase HDAC6, Receptor-type tyrosine-protein kinase FLT3, Platelet-derived growth factor receptor alpha, Cytochrome P450 2C9, Cytochrome P450 2C19, Fibroblast growth factor receptor 1.

Bioactivity

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

TargetpChemblTypeValueUnitActivity ID
ABL19.82IC500.15nMCHEMBL_ACT_12623382
ABL19.74Kd0.18nMCHEMBL_ACT_12623312
ABL19.64Kd0.23nMCHEMBL_ACT_12623305
ABL19.57IC500.27nMCHEMBL_ACT_12623414
ABL19.55Kd0.28nMCHEMBL_ACT_12623308
ABL19.54IC500.29nMCHEMBL_ACT_12623350
ABL19.49Kd0.32nMCHEMBL_ACT_12623318
ABL19.47Kd0.34nMCHEMBL_ACT_12623317
ABL19.47IC500.34nMCHEMBL_ACT_12623446
ABL19.46IC500.35nMCHEMBL_ACT_12623334
ABL19.46IC500.35nMCHEMBL_ACT_12623366
ABL19.34Kd0.46nMCHEMBL_ACT_12623315
ABL19.17IC500.68nMCHEMBL_ACT_12623430
ABL19.15Kd0.71nMCHEMBL_ACT_12623316
ABL19.15IC500.71nMCHEMBL_ACT_12623398
FLT38.88IC501.33nMCHEMBL_ACT_25030086
ABL18.74Kd1.8nMCHEMBL_ACT_12623313
PDGFRA8.68IC502.08nMCHEMBL_ACT_25030087
ABL18.49Kd3.2nMCHEMBL_ACT_12623310
FGFR18.38IC504.14nMCHEMBL_ACT_25030088
LRRK27.77IC5017nMCHEMBL_ACT_25654354
LRRK27.1IC5080nMCHEMBL_ACT_25654301
CYP2C96.96IC50110nMCHEMBL_ACT_12621448
CYP2C196IC50990nMCHEMBL_ACT_12621447
HDAC65.68IC502078nMCHEMBL_ACT_23141087

Target pathways

Aggregated over 1 target gene(s): ABL1.

Top Reactome pathways

53 total, by targets touching each:

PathwayTargetsGenes
Hemostasis1ABL1
Developmental Biology1ABL1
Signal Transduction1ABL1
Cell Cycle1ABL1
Disease1ABL1
Innate Immune System1ABL1
Immune System1ABL1
Signaling by Rho GTPases1ABL1
RHO GTPase Effectors1ABL1
Fcgamma receptor (FCGR) dependent phagocytosis1ABL1
Regulation of actin dynamics for phagocytic cup formation1ABL1
Epigenetic regulation of gene expression1ABL1
Generic Transcription Pathway1ABL1
Signaling by ROBO receptors1ABL1
Axon guidance1ABL1
Role of ABL in ROBO-SLIT signaling1ABL1
Mitotic G1 phase and G1/S transition1ABL1
Myogenesis1ABL1
Infectious disease1ABL1
RHO GTPases Activate WASPs and WAVEs1ABL1
HDR through Single Strand Annealing (SSA)1ABL1
DNA Double-Strand Break Repair1ABL1
Homology Directed Repair1ABL1
Recruitment and ATM-mediated phosphorylation of repair and signaling proteins at DNA double strand breaks1ABL1
HDR through Homologous Recombination (HRR) or Single Strand Annealing (SSA)1ABL1
DNA Double Strand Break Response1ABL1
Cyclin D associated events in G11ABL1
G1 Phase1ABL1
Cell Cycle, Mitotic1ABL1
RNA Polymerase II Transcription1ABL1

Dominant GO biological processes

GO termTargets
mitotic cell cycle1
neural tube closure1
B-1 B cell homeostasis1
B cell proliferation involved in immune response1
transitional one stage B cell differentiation1
mismatch repair1
regulation of DNA-templated transcription1
autophagy1
DNA damage response1
response to oxidative stress1
epidermal growth factor receptor signaling pathway1
positive regulation of cytosolic calcium ion concentration1
integrin-mediated signaling pathway1
canonical NF-kappaB signal transduction1
associative learning1

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
chronic myeloid leukemia3MONDO:0011996EFO:0000339
acute lymphoblastic leukemia3MONDO:0004967EFO:0000220
neoplasm1MONDO:0005070EFO:0000616
acute myeloid leukemia1MONDO:0018874EFO:0000222
leukemia1MONDO:0005059EFO:0000565
myeloid leukemia1MONDO:0004643MONDO:0004643

Clinical trials

Total trials: 32.

Phase distribution

PhaseTrials
PHASE212
PHASE16
Not specified6
PHASE35
PHASE1/PHASE22
EARLY_PHASE11

Top trials by phase / activity

NCTPhaseStatusTitle
NCT06051409PHASE3RECRUITINGA Study of Olverembatinib in Patients With Newly Diagnosed Ph+ ALL (POLARIS-1)
NCT06423911PHASE3RECRUITINGStudy of Olverembatinib (HQP1351) in Patients With CP-CML
NCT06640361PHASE3RECRUITINGA Study of Olverembatinib in SDH-deficient GIST.
NCT07152041PHASE3RECRUITINGNewly-diagnosed Pediatric Ph-positive B-ALL Protocol
NCT05311943PHASE3UNKNOWNTreatment With Olverembatinib in CML-CP Patients Who Failed to at Least Two Previously Administered Second-generation TKIs.
NCT04501120PHASE1/PHASE2RECRUITINGStudy of Lisaftoclax (APG-2575) Single Agent and Combination With Therapy in Patients Relapsed/Refractory AML
NCT05521204PHASE2RECRUITINGOlverembatinib for FGFR1-rearranged Neoplasms
NCT05931757PHASE2NOT_YET_RECRUITINGA Study of Olverembatinib Combined With Blinatumomab in the Treatment of Ph+ ALL
NCT06220487PHASE2RECRUITINGA Single-arm, Open-label Study of Olverembatinib, CD3/CD19 Bispecific T-cell Engager, and Chidamide in Patients With Newly Diagnosed Ph+ALL
NCT06754267PHASE2RECRUITINGVenetoclax Combined With Olverembatinib and Predinisone in Treating Ph+ B-ALL
NCT06757855PHASE1/PHASE2RECRUITINGOlverembatinib Combined With Venetoclax and Azacitidine in Blast Phase Ph Chromosome-positive CML
NCT06817720PHASE2RECRUITINGPhase II Study Assessing the Efficacy and Toxicity of Olverembatinib Monotherapy in Patients With Newly Diagnosed Chronic Myeloid Leukemia in Chronic Phase
NCT07178912PHASE2NOT_YET_RECRUITINGPhase II Study of the Combination of Subcutaneous Blinatumomab and Olverembatinib in Patients With Philadelphia Chromosome (ph)-Positive and/or BCR::ABL1 Positive Acute Lymphoblastic Leukemia (ALL)
NCT07443488PHASE2NOT_YET_RECRUITINGEfficacy and Safety of Olverembatinib Plus Inotuzumab Ozogamicin as First-Line Consolidation Therapy Followed by HSCT in Ph+ ALL
NCT03883087PHASE2UNKNOWNA Pivotal Study of HQP1351 in Patients of Chronic Myeloid Leukemia in Chronic Phase With T315I Mutation
NCT03883100PHASE2UNKNOWNA Pivotal Study of HQP1351 in Patients of Chronic Myeloid Leukemia in Accelerated Phase With T315I Mutation
NCT04126681PHASE2COMPLETEDA Pivotal Study of HQP1351 in Patients With Chronic Myeloid Leukemia in Chronic Phase
NCT05466175PHASE2UNKNOWNA Study of Olverembatinib in the Treatment of Ph+ ALL
NCT05594784PHASE2COMPLETEDOlverembatinib Combined With Reduced-Intensity Chemotherapy and Venetoclax for de Novo Ph+ ALL
NCT03594422PHASE1RECRUITINGA Study of HQP1351 in Patients With GIST or Other Solid Tumors
NCT06401603PHASE1RECRUITINGA Phase I Study of Decitabine, Lisaftoclax, and Olverembatinib in Patients With Advanced Chronic Myeloid Leukemia and Philadelphia Chromosome-Positive Acute Myeloid Leukemia
NCT07282093PHASE1RECRUITINGPharmacokinetics of Olverembatinib in Participants With Hepatic Impairment
NCT03882281PHASE1COMPLETEDPharmacokinetics Profiles of HQP1351 Under Fasting and High-fat Meals in Patients With Chronic Myeloid Leukemia
NCT04126707PHASE1COMPLETEDThe Absorption, Metabolism and Excretion of [14C] HQP1351 in Humans
NCT05495035PHASE1UNKNOWNStudy for Safety and Efficacy of Olverembatinib Combined With APG-2575 in Children With Relapsed/Refractory Ph + ALL
NCT07074496EARLY_PHASE1ACTIVE_NOT_RECRUITINGEfficacy, Safety, and Pharmacokinetics of ThisCART19A Combined With Olverembatinib in Patients With Newly Diagnosed Philadelphia Chromosome-Positive Acute Lymphoblastic Leukemia.
NCT05594758Not specifiedAVAILABLENamed Patient Program for Olverembatinib (HQP1351)
NCT06390306Not specifiedRECRUITINGThe Efficacy and Safety of Third-generation TKIs Combined With Azacitidine and Bcl-2 Inhibitor in Patients With CML-MBP
NCT06481228Not specifiedRECRUITINGEfficacy and Safety of TKI Combined With Chemotherapy and Sequential CAR-T Cells in ND Adult Patients With Ph+ ALL
NCT07383298Not specifiedENROLLING_BY_INVITATIONObservational Study on Dose Optimization of Olverembatinib in Patients With Chronic Myeloid Leukemia in Chronic or Accelerated Phase
NCT07454226Not specifiedRECRUITINGABL/JAK Inhibitors With Chemotherapy and Venetoclax for Ph-like ALL
NCT07493161Not specifiedRECRUITINGChemotherapy With Targeted-Immunotherapy for Newly Diagnosed Ph+ ALL

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.

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

MoleculeSourceStatusShared targets
AFATINIBChEMBL + PubChemPhase 4 (approved)ABL1
CRIZOTINIBChEMBL + PubChemPhase 4 (approved)ABL1
PAZOPANIBChEMBL + PubChemPhase 4 (approved)ABL1
REGORAFENIBChEMBL + PubChemPhase 4 (approved)ABL1
AFATINIB DIMALEATEChEMBLPhase 4 (approved)ABL1
ASCIMINIBChEMBLPhase 4 (approved)ABL1
AXITINIBChEMBLPhase 4 (approved)ABL1
BIOTINChEMBLPhase 4 (approved)ABL1
BOSUTINIBChEMBLPhase 4 (approved)ABL1
BRIGATINIBChEMBLPhase 4 (approved)ABL1
CABOZANTINIBChEMBLPhase 4 (approved)ABL1
CERITINIBChEMBLPhase 4 (approved)ABL1
DABRAFENIBChEMBLPhase 4 (approved)ABL1
DASATINIBChEMBLPhase 4 (approved)ABL1
ENTRECTINIBChEMBLPhase 4 (approved)ABL1
ERLOTINIBChEMBLPhase 4 (approved)ABL1
FEDRATINIBChEMBLPhase 4 (approved)ABL1
FILGOTINIBChEMBLPhase 4 (approved)ABL1
GEFITINIBChEMBLPhase 4 (approved)ABL1
IBRUTINIBChEMBLPhase 4 (approved)ABL1
IMATINIBChEMBLPhase 4 (approved)ABL1
INFIGRATINIBChEMBLPhase 4 (approved)ABL1
LAPATINIBChEMBLPhase 4 (approved)ABL1
LENVATINIBChEMBLPhase 4 (approved)ABL1
MEBENDAZOLEChEMBLPhase 4 (approved)ABL1
MIDOSTAURINChEMBLPhase 4 (approved)ABL1
NERATINIBChEMBLPhase 4 (approved)ABL1
NILOTINIBChEMBLPhase 4 (approved)ABL1
NINTEDANIBChEMBLPhase 4 (approved)ABL1
PONATINIBChEMBLPhase 4 (approved)ABL1
QUIZARTINIBChEMBLPhase 4 (approved)ABL1
RUXOLITINIBChEMBLPhase 4 (approved)ABL1
SORAFENIBChEMBLPhase 4 (approved)ABL1
SUNITINIBChEMBLPhase 4 (approved)ABL1
TIRBANIBULINChEMBLPhase 4 (approved)ABL1
TIVOZANIBChEMBLPhase 4 (approved)ABL1
TOFACITINIBChEMBLPhase 4 (approved)ABL1
TOVORAFENIBChEMBLPhase 4 (approved)ABL1
VANDETANIBChEMBLPhase 4 (approved)ABL1
ALISERTIBChEMBLPhase 3ABL1
ALVOCIDIBChEMBLPhase 3ABL1
BRIVANIBChEMBLPhase 3ABL1
CANERTINIBChEMBLPhase 3ABL1
CEDIRANIBChEMBLPhase 3ABL1
DEFACTINIBChEMBLPhase 3ABL1
DOVITINIBChEMBLPhase 3ABL1
FLUMATINIBChEMBLPhase 3ABL1
LESTAURTINIBChEMBLPhase 3ABL1
LINIFANIBChEMBLPhase 3ABL1
MASITINIBChEMBLPhase 3ABL1
MOTESANIBChEMBLPhase 3ABL1
RADOTINIBChEMBLPhase 3ABL1
RESVERATROLChEMBLPhase 3ABL1
SARACATINIBChEMBLPhase 3ABL1
SEMAXANIBChEMBLPhase 3ABL1
TANESPIMYCINChEMBLPhase 3ABL1
TESEVATINIBChEMBLPhase 3ABL1
ADAVOSERTIBChEMBLPhase 2ABL1
AEE-788ChEMBLPhase 2ABL1
APITOLISIBChEMBLPhase 2ABL1

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