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Gilteritinib

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Also known as Asp-2215ASP2215Gilterinib

Summary

Gilteritinib (CHEMBL3301622) is an approved small-molecule EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor (ATC L01EX13) targeting FLT3, NTRK1, and AXL; indicated across 8 conditions including neoplasm and acute myeloid leukemia; with CIViC clinical evidence for 17 variant-indication associations (e.g. FLT3 ITD in acute myeloid leukemia).

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: L01EX13
  • Targets: 8 (FLT3, NTRK1, AXL…)
  • Indications: 8 conditions
  • Clinical trials: 61
  • Precision-oncology evidence (CIViC): 17 variant–indication associations
  • Chemistry: 552.7 Da · C29H44N8O3

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL3301622
NameGilteritinib
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID49803313
ChEBICHEBI:145372
ATCL01EX13
Molecular formulaC29H44N8O3
Molecular weight552.7
InChIKeyGYQYAJJFPNQOOW-UHFFFAOYSA-N

SMILES: CCC1=C(N=C(C(=N1)C(=O)N)NC2=CC(=C(C=C2)N3CCC(CC3)N4CCN(CC4)C)OC)NC5CCOCC5

IUPAC name: 6-ethyl-3-[3-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]anilino]-5-(oxan-4-ylamino)pyrazine-2-carboxamide

ChEBI definition: A member of the class of pyrazines that is pyrazine-2-carboxamide which is substituted by {3-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl}nitrilo, (oxan-4-yl)nitrilo and ethyl groups at positions 3,5 and 6, respectively. It is a potent inhibitor of FLT3 and AXL tyrosine kinase receptors (IC50 = 0.29 nM and 0.73 nM, respectively). Approved by the FDA for the treatment of acute myeloid leukemia in patients who have a FLT3 gene mutation.

Pharmacological roles (ChEBI): apoptosis inducer, EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor, antineoplastic agent.

Also known as: Asp-2215, ASP-2215, ASP2215, Gilteritinib, GILTERITINIB, gilteritinib, Gilterinib

Parent form; salt/anhydrous children: CHEMBL3301603, CHEMBL4524472

Patent coverage: 1,044 distinct patent families (2,395 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 2,253 (94%) 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
FLT3fms related receptor tyrosine kinase 3Inhibition9.520.9%P36888
NTRK1neurotrophic receptor tyrosine kinase 1Inhibition8.960.1%P04629
AXLAXL receptor tyrosine kinaseInhibition9.11.1%P30530
MERTKMER proto-oncogene, tyrosine kinaseInhibition8.520.6%Q12866
LTKleukocyte receptor tyrosine kinaseInhibition9.70.2%P29376
ALKALK receptor tyrosine kinaseInhibition9.30.8%Q9UM73
ROS1c-ros oncogene 1, receptor tyrosine kinaseInhibition8.820.1%P08922
RETret proto-oncogeneInhibition8.770.4%P07949

Broader ChEMBL bioactivity targets: 91 (assay-derived). Sample: Serine/threonine-protein kinase TAO2, GTP-binding nuclear protein Ran, Mitotic checkpoint serine/threonine-protein kinase BUB1, Receptor-interacting serine/threonine-protein kinase 3, Cyclin-dependent kinase 2/cyclin E1, Platelet-derived growth factor receptor beta, EKC/KEOPS complex subunit TP53RK, Receptor-type tyrosine-protein kinase FLT3, Epidermal growth factor receptor, Proto-oncogene tyrosine-protein kinase receptor Ret, Tyrosine-protein kinase Yes, Muscarinic acetylcholine receptor M2, Dual specificity mitogen-activated protein kinase kinase 6, Mitogen-activated protein kinase 8, Delta(24)-sterol reductase, D(3) dopamine receptor, Ribosomal protein S6 kinase alpha-3, Phosphorylase b kinase gamma catalytic chain, liver/testis isoform, Myosin light chain kinase, smooth muscle, Calcium/calmodulin-dependent protein kinase type IV.

Bioactivity

ChEMBL activities: 143 potent at pChembl ≥ 5 of 147 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
FLT39.8IC500.16nMCHEMBL_ACT_24992748
FLT39.73IC500.19nMCHEMBL_ACT_25596923
FLT39.7IC500.2nMCHEMBL_ACT_24992757
FLT39.7IC500.2nMCHEMBL_ACT_25596921
FLT39.54IC500.29nMCHEMBL_ACT_19067270
FLT39.54IC500.29nMCHEMBL_ACT_22960943
FLT39.54IC500.29nMCHEMBL_ACT_24788710
FLT39.54IC500.29nMCHEMBL_ACT_24862941
FLT39.54IC500.29nMCHEMBL_ACT_24862967
FLT39.54IC500.29nMCHEMBL_ACT_24975314
FLT39.54IC500.29nMCHEMBL_ACT_29064074
LTK9.46IC500.35nMCHEMBL_ACT_24862971
FLT39.39IC500.41nMCHEMBL_ACT_17663015
FLT39.39IC500.41nMCHEMBL_ACT_26590172
FLT39.37IC500.43nMCHEMBL_ACT_29215421
AXL9.14IC500.73nMCHEMBL_ACT_19067271
AXL9.14IC500.73nMCHEMBL_ACT_24788488
AXL9.14IC500.73nMCHEMBL_ACT_24862944
AXL9.14IC500.73nMCHEMBL_ACT_24862968
AXL9.14IC500.73nMCHEMBL_ACT_24975320
AXL9.14IC500.73nMCHEMBL_ACT_25838237
AXL9.14IC500.73nMCHEMBL_ACT_29064075
AXL9.14IC500.73nMCHEMBL_ACT_29212338
FLT39IC501nMCHEMBL_ACT_29189891
ALK8.92IC501.2nMCHEMBL_ACT_24862946
ALK8.92IC501.2nMCHEMBL_ACT_24862972
ALK8.82IC501.5nMCHEMBL_ACT_17662961
EML48.82IC501.5nMCHEMBL_ACT_19328854
FLT38.82IC501.5nMCHEMBL_ACT_29232110
FLT38.82Kd1.5nMCHEMBL_ACT_29275477
FLT38.74IC501.8nMCHEMBL_ACT_26045850
FLT38.74IC501.8nMCHEMBL_ACT_29212339
FLT38.73IC501.86nMCHEMBL_ACT_26195111
ROS18.72IC501.9nMCHEMBL_ACT_17662997
FLT38.7Ki2nMCHEMBL_ACT_23174524
FLT38.7IC502nMCHEMBL_ACT_25467763
FLT38.7IC502.02nMCHEMBL_ACT_26195211
RET8.47IC503.4nMCHEMBL_ACT_17662979
AXL8.34IC504.6nMCHEMBL_ACT_23216023
FLT38.3IC505nMCHEMBL_ACT_24992772
AXL8.29IC505.15nMCHEMBL_ACT_28858043
AXL8.27IC505.33nMCHEMBL_ACT_28858040
EML48.24IC505.7nMCHEMBL_ACT_19328895
AXL8.23IC505.87nMCHEMBL_ACT_28858037
ULK38.22Kd6nMCHEMBL_ACT_17947453
AXL8.21IC506.24nMCHEMBL_ACT_28858046
AXL8.19IC506.5nMCHEMBL_ACT_28858052
AXL8.18IC506.62nMCHEMBL_ACT_28858034
FLT38.15Kd7nMCHEMBL_ACT_17903580
IRAK38.15Kd7nMCHEMBL_ACT_17908329
AXL8.15IC507.01nMCHEMBL_ACT_28858031
AXL8.15IC507.1nMCHEMBL_ACT_28858049
AXL8.13IC507.46nMCHEMBL_ACT_28858025
AXL8.13IC507.35nMCHEMBL_ACT_28858028
FLT38.11IC507.7nMCHEMBL_ACT_25723136
AXL8.07IC508.5nMCHEMBL_ACT_19367705
GAK8.05Kd9nMCHEMBL_ACT_17904333
FLT38Ki10nMCHEMBL_ACT_23174504
FLT38IC5010nMCHEMBL_ACT_25468085
FLT37.97IC5010.59nMCHEMBL_ACT_25921607
Q6ZSR97.96Kd11nMCHEMBL_ACT_17933730
FLT37.96IC5011nMCHEMBL_ACT_25723118
AXL7.95IC5011.3nMCHEMBL_ACT_19367694
FLT37.92IC5012nMCHEMBL_ACT_25467722
PLK47.75Kd18nMCHEMBL_ACT_17927890
AAK17.6Kd25nMCHEMBL_ACT_17878211
FLT37.5IC5031.5nMCHEMBL_ACT_26045854
ACVR17.41Kd39nMCHEMBL_ACT_17880724
TNK17.41Kd39nMCHEMBL_ACT_17945456
BMP2K7.34Kd46nMCHEMBL_ACT_17884776
PHKG27.32Kd48nMCHEMBL_ACT_17925781
RET7.3Kd50nMCHEMBL_ACT_17935023
SLK7.17Kd68nMCHEMBL_ACT_17939348
MAP4K16.97Kd108nMCHEMBL_ACT_17913347
FLT36.93IC50117nMCHEMBL_ACT_26045852
BMPR1A6.92Kd121nMCHEMBL_ACT_17885082
STK106.83Kd149nMCHEMBL_ACT_17940754
ADCK16.82Kd152nMCHEMBL_ACT_17881414
CAMK2G6.77Kd169nMCHEMBL_ACT_17886728
AURKA6.74Kd184nMCHEMBL_ACT_17884107
FER6.73Kd188nMCHEMBL_ACT_17902691
MYLK6.73Kd188nMCHEMBL_ACT_17920140
BUB16.72Kd191nMCHEMBL_ACT_17886208
CYC16.7Kd202nMCHEMBL_ACT_17895263
MAP4K46.7Kd202nMCHEMBL_ACT_17914023
ACSL56.68Kd208nMCHEMBL_ACT_17880102
CAMK2D6.68Kd207nMCHEMBL_ACT_17886472
LATS16.66Kd221nMCHEMBL_ACT_17909100
STK246.64Kd230nMCHEMBL_ACT_17941362
EPHB66.62Kd241nMCHEMBL_ACT_17901078
MAP4K26.61Kd244nMCHEMBL_ACT_17913540
NEK26.61Kd247nMCHEMBL_ACT_17921237
MAPK156.58Kd263nMCHEMBL_ACT_17915444
STK166.53Kd295nMCHEMBL_ACT_17941226
CAMK46.38Kd421nMCHEMBL_ACT_17886964
DHCR246.37Kd432nMCHEMBL_ACT_17897365
MAPK96.37Kd430nMCHEMBL_ACT_17916552
SLC25A56.35Kd451nMCHEMBL_ACT_17938869
YES16.35Kd445nMCHEMBL_ACT_17948395
TUFM6.33Kd464nMCHEMBL_ACT_17946731

Target pathways

Aggregated over 8 target gene(s): FLT3, NTRK1, AXL, MERTK, LTK, ALK, ROS1, RET.

Top Reactome pathways

63 total, by targets touching each:

PathwayTargetsGenes
Signal Transduction2ALK, LTK
RAF/MAP kinase cascade2FLT3, RET
Signaling by Receptor Tyrosine Kinases2ALK, LTK
Dengue Virus Attachment and Entry2AXL, MERTK
Hemostasis1MERTK
PI3K Cascade1FLT3
PIP3 activates AKT signaling1FLT3
Disease1ALK
PLC-gamma1 signalling1NTRK1
Signalling to RAS1NTRK1
Frs2-mediated activation1NTRK1
ARMS-mediated activation1NTRK1
Retrograde neurotrophin signalling1NTRK1
NGF-independant TRKA activation1NTRK1
TRKA activation by NGF1NTRK1
Signalling to p38 via RIT and RIN1NTRK1
PI3K/AKT activation1NTRK1
Signalling to STAT31NTRK1
Signaling by ALK1ALK
Cell surface interactions at the vascular wall1MERTK
Constitutive Signaling by Aberrant PI3K in Cancer1FLT3
VEGFA-VEGFR2 Pathway1AXL
Diseases of signal transduction by growth factor receptors and second messengers1ALK
PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling1FLT3
RET signaling1RET
FLT3 Signaling1FLT3
STAT5 Activation1FLT3
Signaling by ALK in cancer1ALK
ALK mutants bind TKIs1ALK
Drug resistance of ALK mutants1ALK
FLT3 mutants bind TKIs1FLT3
STAT5 activation downstream of FLT3 ITD mutants1FLT3
KW2449-resistant FLT3 mutants1FLT3
semaxanib-resistant FLT3 mutants1FLT3
crenolanib-resistant FLT3 mutants1FLT3
gilteritinib-resistant FLT3 mutants1FLT3
lestaurtinib-resistant FLT3 mutants1FLT3
midostaurin-resistant FLT3 mutants1FLT3
pexidartinib-resistant FLT3 mutants1FLT3
ponatinib-resistant FLT3 mutants1FLT3
quizartinib-resistant FLT3 mutants1FLT3
sorafenib-resistant FLT3 mutants1FLT3
sunitinib-resistant FLT3 mutants1FLT3
tandutinib-resistant FLT3 mutants1FLT3
linifanib-resistant FLT3 mutants1FLT3
tamatinib-resistant FLT3 mutants1FLT3
Signaling by FLT3 ITD and TKD mutants1FLT3
Negative regulation of FLT31FLT3
FLT3 signaling through SRC family kinases1FLT3
FLT3 signaling by CBL mutants1FLT3

Dominant GO biological processes

GO termTargets
cell surface receptor protein tyrosine kinase signaling pathway8
protein phosphorylation8
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction6
nervous system development5
signal transduction5
spermatogenesis4
cell migration3
protein autophosphorylation3
positive regulation of neuron projection development3
peptidyl-tyrosine autophosphorylation3
negative regulation of apoptotic process3
cell differentiation3
peptidyl-tyrosine phosphorylation2
B cell differentiation2
regulation of apoptotic process2

Indications & clinical

Indications

3 approved indications. FDA phase 4, plus an anticancer drug’s labelled cancer uses (which ChEMBL often logs at phase 3).

IndicationPhaseMONDOEFO
neoplasm4MONDO:0005070EFO:0000616
acute myeloid leukemia3MONDO:0018874EFO:0000222
myeloid leukemia3MONDO:0004643MONDO:0004643

5 diseases in clinical trials (phase 1–3, investigational — not approved indications). Highest ChEMBL trial phase per disease; a non-cancer approved use is occasionally logged at phase 3 here.

Disease (in trials)PhaseMONDOEFO
myelodysplastic syndrome2MONDO:0018881EFO:0000198
liver disorder1MONDO:0005154EFO:0001421
non-small cell lung carcinoma1MONDO:0005233EFO:0003060
kidney disorder1MONDO:0005240EFO:0003086
leukemia1MONDO:0005059EFO:0000565

Clinical trials

Total trials: 61.

Phase distribution

PhaseTrials
PHASE116
PHASE1/PHASE215
PHASE211
Not specified10
PHASE38
PHASE2/PHASE31

Top trials by phase / activity

NCTPhaseStatusTitle
NCT03182244PHASE3ACTIVE_NOT_RECRUITINGA Study of ASP2215 Versus Salvage Chemotherapy In Patients With Relapsed or Refractory Acute Myeloid Leukemia (AML) With FMS-like Tyrosine Kinase 3 (FLT3) Mutation
NCT04027309PHASE3ACTIVE_NOT_RECRUITINGA Study of Gilteritinib Versus Midostaurin in Combination With Induction and Consolidation Therapy Followed by One-year Maintenance in Patients With Newly Diagnosed Acute Myeloid Leukemia or Myelodysplastic Syndromes With Excess Blasts-2 With FLT3 Mutations Eligible for Intensive Chemotherapy
NCT05177731PHASE3ACTIVE_NOT_RECRUITINGVenetoclax + Decitabine vs. 7+3 Induction Chemotherapy in Young AML
NCT07407140PHASE3NOT_YET_RECRUITINGVAG Versus Standard Chemotherapy With FLT3 Inhibitor in Adult Patients With FLT3-Mutated AML
NCT07425808PHASE2/PHASE3NOT_YET_RECRUITINGFLT3-ITD Targeted Therapy in Fit AML Patients
NCT07463651PHASE3RECRUITINGMRD-guided Maintenance Post-HCT: Gilteritini vs Sorafenib
NCT02421939PHASE3COMPLETEDA Study of ASP2215 Versus Salvage Chemotherapy in Patients With Relapsed or Refractory Acute Myeloid Leukemia (AML) With FMS-like Tyrosine Kinase (FLT3) Mutation
NCT02752035PHASE3COMPLETEDA Study of ASP2215 (Gilteritinib) by Itself, ASP2215 Combined With Azacitidine or Azacitidine by Itself to Treat Adult Patients Who Have Recently Been Diagnosed With Acute Myeloid Leukemia With a FLT3 Gene Mutation and Who Cannot Receive Standard Chemotherapy
NCT02997202PHASE3COMPLETEDA Trial of the FMS-like Tyrosine Kinase 3 (FLT3) Inhibitor Gilteritinib Administered as Maintenance Therapy Following Allogeneic Transplant for Patients With FLT3/Internal Tandem Duplication (ITD) Acute Myeloid Leukemia (AML)
NCT02115295PHASE2RECRUITINGCladribine, Idarubicin, Cytarabine, and Venetoclax in Treating Patients With Acute Myeloid Leukemia, High-Risk Myelodysplastic Syndrome, or Blastic Phase Chronic Myeloid Leukemia
NCT03013998PHASE1/PHASE2RECRUITINGStudy of Biomarker-Based Treatment of Acute Myeloid Leukemia
NCT03836209PHASE2ACTIVE_NOT_RECRUITINGGilteritinib vs Midostaurin in FLT3 Mutated Acute Myeloid Leukemia
NCT04140487PHASE1/PHASE2RECRUITINGAzacitidine, Venetoclax, and Gilteritinib in Treating Patients With Recurrent/Refractory FLT3-Mutated Acute Myeloid Leukemia, Chronic Myelomonocytic Leukemia, or High-Risk Myelodysplastic Syndrome/Myeloproliferative Neoplasm
NCT04988555PHASE1/PHASE2RECRUITINGA Phase 1/2 Study of Enzomenib (DSP-5336) in Patients With Acute Leukemia (Horizen-1)
NCT05010122PHASE1/PHASE2RECRUITINGASTX727, Venetoclax, and Gilteritinib for the Treatment of Newly Diagnosed, Relapsed or Refractory FLT3-Mutated Acute Myeloid Leukemia or High-Risk Myelodysplastic Syndrome
NCT05520567PHASE1/PHASE2ACTIVE_NOT_RECRUITINGA Study of Gilteritinib, Venetoclax and Azacitidine as a Combined Treatment for People Newly Diagnosed With Acute Myeloid Leukemia
NCT05564390PHASE2RECRUITINGMYELOMATCH: A Screening Study to Assign People With Myeloid Cancer to a Treatment Study or Standard of Care Treatment Within myeloMATCH (MyeloMATCH Screening Trial)
NCT06221683PHASE2RECRUITINGClinical Study of Induction Therapy Options Based on Molecular Subtyping and MRD in Children and Adolescents With AML
NCT06235801PHASE1/PHASE2RECRUITINGA Phase I/II Study of Gilteritinib and Momelotinib for Patients With Relapsed or Refractory FLT3-Mutated Acute Myeloid Leukemia
NCT06317649PHASE2RECRUITINGVenetoclax and HMA Treatment of Older and Unfit Adults With FLT3 Mutated Acute Myeloid Leukemia (AML) (A MyeloMATCH Treatment Trial)
NCT06561880PHASE1/PHASE2RECRUITINGThe Efficacy of Triple Regimen in Newly Diagnosed AML Patients With FLT3 Mutation
NCT06667973PHASE2NOT_YET_RECRUITINGEfficacy of Gilteritinib in Combination With FLAI as Induction Therapy of FLT3-positive Acute Myeloid Leukemia
NCT06696183PHASE2RECRUITINGGilteritinib in Combination With Venetoclax and Azacitidine for AML Patients With FLT3 Mutations Ineligible for Intensive Treatment
NCT07032727PHASE2RECRUITINGOlutasidenib Combined With Co-targeted Therapy in Relapsed or Refractory IDH1-mutated Myeloid Malignancies Harboring Activated Signaling Pathway Mutations
NCT07548710PHASE2RECRUITINGStudy of SA+X in the Treatment of Newly Diagnosed AML
NCT02014558PHASE1/PHASE2COMPLETEDDose Escalation Study Investigating the Safety, Tolerability, Pharmacokinetics, Pharmacodynamics of ASP2215 in Patients With Relapsed or Refractory Acute Myeloid Leukemia
NCT02310321PHASE1/PHASE2COMPLETEDA Study of ASP2215 in Combination With Induction and Consolidation Chemotherapy in Patients With Newly Diagnosed Acute Myeloid Leukemia.
NCT02495233PHASE1/PHASE2TERMINATEDA Study of ASP2215 in Combination With Erlotinib in Subjects With Epidermal Growth Factor Receptor (EGFR) Activating Mutation-Positive (EGFRm+) Advanced Non-Small-Cell Lung Cancer (NSCLC) Who Have Acquired Resistance to an EGFR Tyrosine Kinase Inhibitor (TKI)
NCT02561455PHASE1/PHASE2COMPLETEDRollover Study for Subjects Who Have Participated in an Astellas Sponsored ASP2215 Trial
NCT02927262PHASE2COMPLETEDA Study of ASP2215 (Gilteritinib), Administered as Maintenance Therapy Following Induction/Consolidation Therapy for Subjects With FMS-like Tyrosine Kinase 3 (FLT3/ITD) Acute Myeloid Leukemia (AML) in First Complete Remission
NCT03730012PHASE1/PHASE2COMPLETEDA Study of ASP2215 (Gilteritinib) Combined With Atezolizumab in Patients With Relapsed or Treatment Refractory FMS-like Tyrosine Kinase (FLT3) Mutated Acute Myeloid Leukemia (AML)
NCT04240002PHASE1/PHASE2TERMINATEDA Study of Gilteritinib (ASP2215) Combined With Chemotherapy in Children, Adolescents and Young Adults With FMS-like Tyrosine Kinase 3 (FLT3)/Internal Tandem Duplication (ITD) Positive Relapsed or Refractory Acute Myeloid Leukemia (AML)
NCT05028751PHASE1/PHASE2TERMINATEDA Study to Evaluate Lanraplenib (LANRA) in Combination With Gilteritinib in Participants With FLT3-mutated Relapsed or Refractory Acute Myeloid Leukemia (AML)
NCT05279859PHASE1/PHASE2WITHDRAWNA Study of Anti-Cancer Therapies Targeting the MAPK Pathway in Patients With Hematologic Malignancies
NCT05955261PHASE2SUSPENDEDA Study of Venetoclax in Combination With Conventional Chemotherapy in Pediatric Patients With Acute Myeloid Leukemia
NCT05010772PHASE1RECRUITINGDecitabine Alone or in Combination With Venetoclax, Gilteritinib, Enasidenib, or Ivosidenib as Maintenance Therapy for the Treatment of Acute Myeloid Leukemia in Remission
NCT05024552PHASE1RECRUITINGVyxeos Plus Gilteritinib in Relapsed or Refractory, FLT3-Mutated AML
NCT05546580PHASE1RECRUITINGStudy of Iadademstat and Gilteritinib in Patients With R/R AML With FMS-like Tyrosine Kinase Mutation (FLT3 Mut+)
NCT05756777PHASE1RECRUITINGA Study of Gilteritinib in Combination With Ivosidenib or Enasidenib in People With Acute Myeloid Leukemia (AML)
NCT06001788PHASE1RECRUITINGSafety and Tolerability of Ziftomenib Combinations in Patients With Relapsed/Refractory Acute Myeloid Leukemia
NCT06222580PHASE1RECRUITINGSNDX-5613 and Gilteritinib for the Treatment of Relapsed or Refractory FLT3-Mutated Acute Myeloid Leukemia and Concurrent MLL-Rearrangement or NPM1 Mutation
NCT06225427PHASE1RECRUITINGGilteritinib for the Treatment of ALK NSCLC
NCT07140016PHASE1RECRUITINGA Study of Gilteritinib in Adults With Advanced ALK-positive Non-small Cell Lung Cancer (NSCLC)
NCT02181660PHASE1COMPLETEDDose Escalation Study to Investigate the Safety, Tolerability and Pharmacokinetics of ASP2215 in Japanese Patients With Relapsed or Refractory Acute Myeloid Leukemia
NCT02236013PHASE1COMPLETEDA Study of ASP2215 in Combination With Induction and Consolidation Chemotherapy in Patients With Newly Diagnosed Acute Myeloid Leukemia
NCT02456883PHASE1COMPLETEDStudy to Investigate the Absorption, Metabolism and Excretion of [14C] ASP2215 in Patients With Advanced Solid Tumors
NCT02571816PHASE1COMPLETEDA Study to Investigate the Effect of Hepatic Impairment on the Pharmacokinetics, Safety and Tolerability of ASP2215
NCT03625505PHASE1COMPLETEDA Study to Assess Safety and Efficacy of Venetoclax in Combination With Gilteritinib in Participants With Relapsed/Refractory Acute Myeloid Leukemia
NCT03964038PHASE1COMPLETEDA Study to Assess the Relative Bioavailability of Gilteritinib Following a Single Dose of Gilteritinib Mini-tablet Oral Suspension and Gilteritinib Mini-tablets Compared to a Single Dose of Gilteritinib Tablet in Healthy Subjects
NCT04336982PHASE1TERMINATEDA Safety and Efficacy Study of CC-90009 Combinations in Subjects With Acute Myeloid Leukemia
NCT04699877PHASE1COMPLETEDA Study to Investigate the Effect of Severe Renal Impairment on Gilteritinib Compared to Healthy Participants With Normal Renal Function
NCT06265545Not specifiedRECRUITINGMulticenter, Platform-type Clinical Study of Refractory/Recurrent Acute Myeloid Leukemia
NCT06992934Not specifiedNOT_YET_RECRUITINGImmunological Impact of a Post Cell Therapy Treatment With FLT3 Inhibitors
NCT07131059Not specifiedRECRUITINGMRD-positive AML Clinical Study
NCT03070093Not specifiedAPPROVED_FOR_MARKETINGExpanded Access Study of Gilteritinib (ASP2215) in Patients With FMS-like Tyrosine Kinase 3 (FLT3) Mutated Relapsed or Refractory Acute Myeloid Leukemia (AML) or FLT3-Mutated AML in Complete Remission (CR) With Minimal Residual Disease (MRD)
NCT03315299Not specifiedNO_LONGER_AVAILABLEIndividual Patient Expanded Access Gilteritinib (ASP2215)
NCT03409081Not specifiedNO_LONGER_AVAILABLEEarly Access Program (EAP) of Gilteritinib (ASP2215) in Patients With FMS-like Tyrosine Kinase 3 (FLT3) Mutated Relapsed or Refractory Acute Myeloid Leukemia (AML) or With FLT3-Mutated AML in Complete Remission (CR) With Minimal Residual Disease (MRD)
NCT04691648Not specifiedCOMPLETEDA Study to Assess the Safety of Xospata in Patients With Relapsed or Refractory Acute Myeloid Leukemia (AML) With FMS-Like Tyrosine Kinase 3 (FLT3) Mutation
NCT05312112Not specifiedUNKNOWNReal World Outcomes Using Novel Agents for AML in the UK
NCT05791890Not specifiedUNKNOWNGilteRInf 2022 Study (Gilteritinib Related Infections)
NCT06734585Not specifiedCOMPLETEDUsing Gilteritinib to Keep People With Acute Myeloid Leukemia Cancer-free After a Stem Cell Transplant

Clinical evidence (CIViC)

Variant × indication × effect (17 predictive associations from 20 curated evidence items):

VariantIndicationEffectTherapyLevelCIViC
FLT3 ITDAcute Myeloid LeukemiaSensitivity/ResponseGilteritinibCIViC AEID12621 +2
FLT3 D835 OR FLT3 I836Acute Myeloid LeukemiaSensitivity/ResponseGilteritinibCIViC AEID12622
FLT3 ITD AND FLT3 D835 AND FLT3 I836Acute Myeloid LeukemiaSensitivity/ResponseGilteritinibCIViC AEID11260
FLT3 ITD OR FLT3 D835 OR FLT3 I836Acute Myeloid LeukemiaSensitivity/ResponseGilteritinibCIViC AEID7728
FLT3 MutationAcute Myeloid LeukemiaSensitivity/ResponseGilteritinibCIViC BEID7283
FLT3 D835YAcute Myeloid LeukemiaSensitivity/ResponseGilteritinibCIViC CEID12620 +1
FLT3 Q575delAcute Myeloid LeukemiaSensitivity/ResponseGilteritinibCIViC CEID9303
FLT3 D835HAcute Myeloid LeukemiaSensitivity/ResponseGilteritinibCIViC DEID8517
FLT3 D835IAcute Myeloid LeukemiaSensitivity/ResponseGilteritinibCIViC DEID8351
FLT3 D835VAcute Myeloid LeukemiaSensitivity/ResponseGilteritinibCIViC DEID8518
FLT3 D835YCancerSensitivity/ResponseGilteritinibCIViC DEID8106
FLT3 N841IAcute Myeloid LeukemiaSensitivity/ResponseGilteritinibCIViC DEID12510
FLT3 Y572CAcute Myeloid LeukemiaSensitivity/ResponseGilteritinibCIViC DEID12786
FLT3 G697SAcute Myeloid LeukemiaReduced SensitivityGilteritinibCIViC DEID9022
FLT3 F691LAcute Myeloid LeukemiaResistanceGilteritinibCIViC DEID8562
FLT3 G697SAcute Myeloid LeukemiaResistanceGilteritinibCIViC DEID8898
FLT3 Y693Acute Myeloid LeukemiaResistanceGilteritinibCIViC DEID8285

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.

179 molecules share ≥1 primary target. Top 100 by shared-target count:

MoleculeSourceStatusShared targets
AFATINIBChEMBL + PubChemPhase 4 (approved)ALK, AXL, FLT3, LTK, MERTK, NTRK1, RET, ROS1
CRIZOTINIBChEMBL + PubChemPhase 4 (approved)ALK, AXL, FLT3, LTK, MERTK, NTRK1, RET, ROS1
FEDRATINIBChEMBL + PubChemPhase 4 (approved)ALK, AXL, FLT3, LTK, MERTK, NTRK1, RET, ROS1
GEFITINIBChEMBL + PubChemPhase 4 (approved)ALK, AXL, FLT3, LTK, MERTK, NTRK1, RET, ROS1
MIDOSTAURINChEMBL + PubChemPhase 4 (approved)ALK, AXL, FLT3, LTK, MERTK, NTRK1, RET, ROS1
PAZOPANIBChEMBL + PubChemPhase 4 (approved)ALK, AXL, FLT3, LTK, MERTK, NTRK1, RET, ROS1
NINTEDANIBChEMBLPhase 4 (approved)ALK, AXL, FLT3, LTK, MERTK, NTRK1, RET, ROS1
LESTAURTINIBChEMBLPhase 3ALK, AXL, FLT3, LTK, MERTK, NTRK1, RET, ROS1
BMS-754807ChEMBLPhase 2ALK, AXL, FLT3, LTK, MERTK, NTRK1, RET, ROS1
FORETINIBChEMBLPhase 2ALK, AXL, FLT3, LTK, MERTK, NTRK1, RET, ROS1
R-406ChEMBLPhase 2ALK, AXL, FLT3, LTK, MERTK, NTRK1, RET, ROS1
TOZASERTIBChEMBLPhase 2ALK, AXL, FLT3, LTK, MERTK, NTRK1, RET, ROS1
IdelalisibPubChemApprovedALK, AXL, FLT3, LTK, MERTK, NTRK1, RET, ROS1
SelumetinibPubChemApprovedALK, AXL, FLT3, LTK, MERTK, NTRK1, RET, ROS1
AXITINIBChEMBL + PubChemPhase 4 (approved)AXL, FLT3, LTK, MERTK, NTRK1, RET, ROS1
BOSUTINIBChEMBL + PubChemPhase 4 (approved)ALK, AXL, FLT3, LTK, MERTK, NTRK1, RET
ENTRECTINIBChEMBL + PubChemPhase 4 (approved)ALK, AXL, FLT3, LTK, NTRK1, RET, ROS1
ERLOTINIBChEMBL + PubChemPhase 4 (approved)ALK, AXL, FLT3, LTK, MERTK, RET, ROS1
QUIZARTINIBChEMBL + PubChemPhase 4 (approved)AXL, FLT3, LTK, MERTK, NTRK1, RET, ROS1
SORAFENIBChEMBL + PubChemPhase 4 (approved)AXL, FLT3, LTK, MERTK, NTRK1, RET, ROS1
SUNITINIBChEMBL + PubChemPhase 4 (approved)ALK, AXL, FLT3, LTK, MERTK, NTRK1, RET
LINIFANIBChEMBLPhase 3ALK, AXL, FLT3, LTK, MERTK, NTRK1, RET
ILORASERTIBChEMBLPhase 2ALK, AXL, FLT3, LTK, NTRK1, RET, ROS1
REBASTINIBChEMBLPhase 2AXL, FLT3, LTK, MERTK, NTRK1, RET, ROS1
SU-014813ChEMBLPhase 2ALK, AXL, FLT3, LTK, MERTK, NTRK1, RET
VANDETANIBChEMBL + PubChemPhase 4 (approved)ALK, AXL, FLT3, LTK, MERTK, RET
CEDIRANIBChEMBLPhase 3ALK, AXL, FLT3, LTK, MERTK, RET
DOVITINIBChEMBLPhase 3ALK, AXL, FLT3, MERTK, NTRK1, RET
CENISERTIBChEMBLPhase 2ALK, AXL, FLT3, LTK, RET, ROS1
OSI-632ChEMBLPhase 2ALK, AXL, FLT3, LTK, RET, ROS1
BRIGATINIBChEMBL + PubChemPhase 4 (approved)ALK, FLT3, LTK, RET, ROS1
RUXOLITINIBChEMBL + PubChemPhase 4 (approved)ALK, LTK, NTRK1, RET, ROS1
CABOZANTINIBChEMBLPhase 4 (approved)AXL, FLT3, MERTK, NTRK1, RET
CERITINIBChEMBLPhase 4 (approved)ALK, FLT3, NTRK1, RET, ROS1
ALVOCIDIBChEMBLPhase 3ALK, AXL, FLT3, LTK, MERTK
CANERTINIBChEMBLPhase 3ALK, AXL, FLT3, LTK, RET
BEMCENTINIBChEMBLPhase 2ALK, AXL, FLT3, MERTK, RET
BMS-777607ChEMBLPhase 2AXL, FLT3, MERTK, NTRK1, RET
DORAMAPIMODChEMBLPhase 2FLT3, LTK, MERTK, NTRK1, RET
MERESTINIBChEMBLPhase 2AXL, FLT3, MERTK, NTRK1, RET
AlectinibChEMBL + PubChemPhase 4 (approved)ALK, LTK, RET, ROS1
IBRUTINIBChEMBL + PubChemPhase 4 (approved)FLT3, LTK, MERTK, RET
LapatinibChEMBL + PubChemPhase 4 (approved)LTK, MERTK, RET, ROS1
LORLATINIBChEMBL + PubChemPhase 4 (approved)ALK, LTK, NTRK1, ROS1
NERATINIBChEMBL + PubChemPhase 4 (approved)AXL, FLT3, LTK, MERTK
PONATINIBChEMBL + PubChemPhase 4 (approved)FLT3, LTK, NTRK1, RET
INFIGRATINIBChEMBLPhase 4 (approved)ALK, FLT3, RET, ROS1
ALISERTIBChEMBLPhase 3LTK, NTRK1, RET, ROS1
QUERCETINChEMBLPhase 3ALK, AXL, FLT3, RET
BI-2536ChEMBLPhase 2ALK, FLT3, LTK, MERTK
CEP-11981ChEMBLPhase 2ALK, FLT3, NTRK1, RET
DEFOSBARASERTIBChEMBLPhase 2AXL, FLT3, LTK, RET
MK-2461ChEMBLPhase 2FLT3, MERTK, NTRK1, RET
PELITINIBChEMBLPhase 2ALK, AXL, FLT3, MERTK
TANDUTINIBChEMBLPhase 2AXL, FLT3, MERTK, NTRK1
BinimetinibPubChemApprovedFLT3, MERTK, NTRK1, RET
TrametinibPubChemApprovedAXL, FLT3, NTRK1, RET
ABEMACICLIBChEMBL + PubChemPhase 4 (approved)FLT3, LTK, NTRK1
FOSTAMATINIBChEMBL + PubChemPhase 4 (approved)FLT3, NTRK1, RET
NILOTINIBChEMBL + PubChemPhase 4 (approved)FLT3, LTK, RET
REGORAFENIBChEMBL + PubChemPhase 4 (approved)FLT3, NTRK1, RET
REPOTRECTINIBChEMBL + PubChemPhase 4 (approved)ALK, NTRK1, ROS1
UPADACITINIBChEMBL + PubChemPhase 4 (approved)ALK, LTK, RET
DASATINIBChEMBLPhase 4 (approved)AXL, FLT3, RET
PALBOCICLIBChEMBLPhase 4 (approved)ALK, FLT3, RET
CRENOLANIBChEMBLPhase 3FLT3, NTRK1, RET
DEFACTINIBChEMBLPhase 3FLT3, NTRK1, RET
ENTOSPLETINIBChEMBLPhase 3FLT3, NTRK1, ROS1
SEMAXANIBChEMBLPhase 3ALK, FLT3, RET
SITRAVATINIBChEMBLPhase 3AXL, FLT3, NTRK1
AT-9283ChEMBLPhase 2FLT3, MERTK, RET
AZD-1480ChEMBLPhase 2FLT3, NTRK1, RET
DANUSERTIBChEMBLPhase 2FLT3, NTRK1, RET
ENMD-2076ChEMBLPhase 2FLT3, NTRK1, RET
GLESATINIBChEMBLPhase 2AXL, FLT3, MERTK
GOLVATINIBChEMBLPhase 2FLT3, NTRK1, RET
MILCICLIBChEMBLPhase 2FLT3, NTRK1, RET
PEXMETINIBChEMBLPhase 2MERTK, NTRK1, RET
SELITRECTINIBChEMBLPhase 2ALK, NTRK1, ROS1
UCN-01ChEMBLPhase 2FLT3, NTRK1, RET
belumosudilPubChemApprovedALK, RET, ROS1
dacomitinibPubChemApprovedFLT3, NTRK1, RET
MomelotinibPubChemApprovedLTK, MERTK, ROS1
IMATINIBChEMBL + PubChemPhase 4 (approved)FLT3, LTK
TofacitinibChEMBL + PubChemPhase 4 (approved)LTK, RET
AMITRIPTYLINEChEMBLPhase 4 (approved)NTRK1, RET
FILGOTINIBChEMBLPhase 4 (approved)FLT3, MERTK
LAROTRECTINIBChEMBLPhase 4 (approved)NTRK1, ROS1
PRALSETINIBChEMBLPhase 4 (approved)FLT3, RET
TIVOZANIBChEMBLPhase 4 (approved)FLT3, RET
BARASERTIBChEMBLPhase 3FLT3, RET
DACTOLISIBChEMBLPhase 3ALK, LTK
ENZASTAURINChEMBLPhase 3AXL, FLT3
ITACITINIBChEMBLPhase 3AXL, MERTK
MOTESANIBChEMBLPhase 3FLT3, RET
ORANTINIBChEMBLPhase 3FLT3, RET
POVORCITINIBChEMBLPhase 3AXL, MERTK
RUBOXISTAURINChEMBLPhase 3FLT3, ROS1
SARACATINIBChEMBLPhase 3FLT3, RET
SURUFATINIBChEMBLPhase 3FLT3, MERTK

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
v1.1.4
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