Gilteritinib
Highest phase reached
Approved
Drug type
Small molecule
First approval year
2018
- First approval year
- 2018
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Gilteritinib
- Molecular weight
- 552.72
- Structure (SMILES)
- CCc1nc(C(N)=O)c(Nc2ccc(N3CCC(N4CCN(C)CC4)CC3)c(OC)c2)nc1NC1CCOCC1
- asp 2215
- Asp-2215
- ASP-2215
- asp2215
- ASP2215
- gilteritinib
- Gilteritinib
- gilteritinib [INN]
- GILTERITINIB [MI]
- GILTERITINIB [USAN]
- Gilteritinib [WHO-DD]
- gilteritinib inn
- gilteritinib mi
- gilteritinib usan
- gilteritinib who dd
- ATC classification codes
- L01EX13
Sources for recorded values
- CAS registry numbers
- 1254053-43-4
- ChEMBL ID
- CHEMBL3301622
- InChIKey
- GYQYAJJFPNQOOW-UHFFFAOYSA-N
- PubChem compound IDs
- 49803313
- RxNorm IDs (RxCUI)
- 2105806
- FDA ingredient codes (UNII)
- 66D92MGC8M
- Applicant
- ASTELLAS
- Approval date
- 28 Nov 2018
- Application number
- NDA211349
- Status
- Authorised
- Status date
- 24 Oct 2019
- Authorisation date
- 24 Oct 2019
- Approved indications
- Xospata is indicated as monotherapy for the treatment of adult patients who have relapsed or refractory acute myeloid leukaemia (AML) with a FLT3 mutation.
- Product number
- EMEA/H/C/004752
- Authorisation holder
- Astellas Pharma Europe B.V.
- Priority medicines scheme
- No
- Generic
- No
- Biosimilar
- No
- Generic medicines
- 0
- Biosimilar medicines
- 0
- Advanced therapy
- No
- Conditional approval
- No
- Additional monitoring
- No
- Accelerated assessment
- No
- Exceptional circumstances
- No
Therapeutic areas
- Leukemia, Myeloid, Acute
European medicines record
- Patents
- 0
- Designations
- 3
- Earliest recorded loss of exclusivity
- 28 Oct 2029
- First in class
- No
- Fast track
- Yes
- Breakthrough designation
- No
- Orphan designation
- Yes
- Priority review
- Yes
- Orphan exclusivity
- No
- Accelerated approval
- No
- Availability
- Prescription only
- Boxed warning
- Yes
- Pharmacology name
- gilteritinib
- Type
- Synthetic organic
- Drug name stem
- -tinib
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- Oral
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- neurotrophic receptor tyrosine kinase 1
- Gene symbol
- NTRK1
- Protein identifier
- P04629
- Median affinity
- 8.96
- Affinity units
- pIC50
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- ret proto-oncogene
- Gene symbol
- RET
- Protein identifier
- P07949
- Median affinity
- 8.77
- Affinity units
- pIC50
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- c-ros oncogene 1, receptor tyrosine kinase
- Gene symbol
- ROS1
- Protein identifier
- P08922
- Median affinity
- 8.82
- Affinity units
- pIC50
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- leukocyte receptor tyrosine kinase
- Gene symbol
- LTK
- Protein identifier
- P29376
- Median affinity
- 9.7
- Affinity units
- pIC50
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- AXL receptor tyrosine kinase
- Gene symbol
- AXL
- Protein identifier
- P30530
- Median affinity
- 9.1
- Affinity units
- pIC50
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- fms related receptor tyrosine kinase 3
- Gene symbol
- FLT3
- Protein identifier
- P36888
- Median affinity
- 9.52
- Affinity units
- pIC50
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- MER proto-oncogene, tyrosine kinase
- Gene symbol
- MERTK
- Protein identifier
- Q12866
- Median affinity
- 8.52
- Affinity units
- pIC50
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- ALK receptor tyrosine kinase
- Gene symbol
- ALK
- Protein identifier
- Q9UM73
- Median affinity
- 9.3
- Affinity units
- pIC50
- Mechanism
- Tyrosine-protein kinase receptor FLT3 inhibitor
- Action type
- Inhibitor
- Target
- Receptor-type tyrosine-protein kinase FLT3
- Protein identifier
- P36888
- Mechanism
- Tyrosine-protein kinase receptor UFO inhibitor
- Action type
- Inhibitor
- Target
- Tyrosine-protein kinase receptor UFO
- Protein identifier
- P30530
- Mechanism
- Tyrosine-protein kinase receptor FLT3 inhibitor
- Action type
- Inhibitor
- Target
- Receptor-type tyrosine-protein kinase FLT3
- Mechanism
- Tyrosine-protein kinase receptor UFO inhibitor
- Action type
- Inhibitor
- Target
- Tyrosine-protein kinase receptor UFO
- Action type
- Inhibitor
- Gene symbol
- NTRK1
- Protein identifier
- P04629
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Inhibitor
- Gene symbol
- LTK
- Protein identifier
- P29376
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Inhibitor
- Gene symbol
- AXL
- Protein identifier
- P30530
- Organism
- Homo sapiens
- Target development level
- Chemical evidence
- Action type
- Inhibitor
- Gene symbol
- FLT3
- Protein identifier
- P36888
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Inhibitor
- Gene symbol
- MERTK
- Protein identifier
- Q12866
- Organism
- Homo sapiens
- Target development level
- Chemical evidence
- Condition
- Myelodysplastic Syndromes
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000198
- Subject identifier
- D009190
- Condition
- Leukemia, Myeloid, Acute
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000222
- Subject identifier
- D015470
- Condition
- Leukemia
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000565
- Subject identifier
- D007938
- Condition
- Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000616
- Subject identifier
- D009369
- Condition
- Liver Diseases
- Highest recorded phase
- 1
- Condition identifier
- EFO:0001421
- Subject identifier
- D008107
- Condition
- Carcinoma, Non-Small-Cell Lung
- Highest recorded phase
- 1
- Condition identifier
- EFO:0003060
- Subject identifier
- D002289
- Condition
- Kidney Diseases
- Highest recorded phase
- 1
- Condition identifier
- EFO:0003086
- Subject identifier
- D007674
- Condition
- Leukemia, Myeloid
- Highest recorded phase
- 3
- Condition identifier
- MONDO:0004643
- Subject identifier
- D007951
- Condition identifier
- EFO_0000222
- Condition identifier
- EFO_0000330
- Condition identifier
- EFO_0000616
- Condition identifier
- EFO_0001421
- Highest recorded phase
- 1
- Condition identifier
- EFO_0003060
- Condition identifier
- EFO_0003086
- Highest recorded phase
- 1
- Condition identifier
- EFO_0004952
- Condition identifier
- MONDO_0004643
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0004643
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0005059
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0005070
- Highest recorded phase
- 4
- Condition identifier
- MONDO_0005170
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0005233
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0011996
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0015667
- Condition identifier
- MONDO_0015667
- Highest recorded phase
- 4
- Condition identifier
- MONDO_0018874
- Highest recorded phase
- 4
- Condition identifier
- MONDO_0018881
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0020076
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0020311
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0044881
Open Targets warnings
- Warning
- Black Box Warning
- Effect
- carcinogenicity
- Country
- United States
- Event
- acute febrile neutrophilic dermatosis
- Reports
- 12
- Reporting signal score
- 35.6925
- Event
- acute graft versus host disease
- Reports
- 7
- Reporting signal score
- 13.7533
- Event
- acute graft versus host disease in skin
- Reports
- 7
- Reporting signal score
- 17.8327
- Event
- acute myeloid leukaemia
- Reports
- 50
- Reporting signal score
- 156.77
- Event
- acute myeloid leukaemia recurrent
- Reports
- 31
- Reporting signal score
- 156.683
- Event
- anaemia
- Reports
- 58
- Reporting signal score
- 31.6541
- Event
- bacteraemia
- Reports
- 13
- Reporting signal score
- 21.4677
- Event
- blast cell count increased
- Reports
- 14
- Reporting signal score
- 58.3571
- Event
- blood creatine phosphokinase increased
- Reports
- 17
- Reporting signal score
- 13.1477
- Event
- blood lactate dehydrogenase increased
- Reports
- 20
- Reporting signal score
- 33.363
- Event
- bone marrow failure
- Reports
- 26
- Reporting signal score
- 39.6623
- Event
- bronchopulmonary aspergillosis
- Reports
- 8
- Reporting signal score
- 14.929
- Event
- chronic graft versus host disease
- Reports
- 7
- Reporting signal score
- 14.3665
- Event
- chronic graft versus host disease in skin
- Reports
- 6
- Reporting signal score
- 19.6946
- Event
- chronic graft versus host disease oral
- Reports
- 3
- Reporting signal score
- 14.043
- Event
- cytopenia
- Reports
- 45
- Reporting signal score
- 133.648
- Event
- differentiation syndrome
- Reports
- 29
- Reporting signal score
- 155.029
- Event
- dizziness
- Reports
- 4
- Reporting signal score
- 17.6156
- Event
- electrocardiogram qt prolonged
- Reports
- 30
- Reporting signal score
- 36.7882
- Event
- febrile neutropenia
- Reports
- 155
- Reporting signal score
- 370.438
- Event
- graft versus host disease
- Reports
- 15
- Reporting signal score
- 36.9828
- Event
- graft versus host disease in gastrointestinal tract
- Reports
- 6
- Reporting signal score
- 15.9376
- Event
- graft versus host disease in liver
- Reports
- 6
- Reporting signal score
- 23.3995
- Event
- graft versus host disease in skin
- Reports
- 7
- Reporting signal score
- 17.9282
- Event
- hepatic cytolysis
- Reports
- 8
- Reporting signal score
- 17.8494
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And 12 more, listed on the interactive page.
- Dose
- 120mg
- Route
- Oral
- How often
- Once daily
- Administer about the same time each day
- Do not crush tablets
- Take with or without food
- Hydrogen bond acceptors
- 10
- Hydrogen bond donors
- 3
- Polar surface area
- 121.11
- Calculated partition coefficient (ALogP)
- 2.7
- Calculated partition coefficient (XLogP)
- 3.5
- Prodrug
- No
- Chirality
- Achiral
- Inorganic
- No
- Rule-of-five violations
- 1
- Rotatable bonds
- 9
- Heavy atoms
- 40
- Molecular formula
- C29H44N8O3
- Monoisotopic mass
- 552.35363730
- Natural product
- Yes
- Recorded assays
- 1,111
- Active assays
- 441
- Confirmatory
- Screening
- Tyrosine Kinase Inhibitors
These details could not be displayed.
Related records
Trials (64)
- A Phase 1/2 Study of Enzomenib (DSP-5336) in Patients With Acute Leukemia (Horizen-1)
- A Phase I/II Study of Gilteritinib and Momelotinib for Patients With Relapsed or Refractory FLT3-Mutated Acute Myeloid Leukemia
- A Safety and Efficacy Study of CC-90009 Combinations in Subjects With Acute Myeloid Leukemia
- A Study of Anti-Cancer Therapies Targeting the MAPK Pathway in Patients With Hematologic Malignancies
- A 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
- A Study of ASP2215 (Gilteritinib) Combined With Atezolizumab in Patients With Relapsed or Treatment Refractory FMS-like Tyrosine Kinase (FLT3) Mutated Acute Myeloid Leukemia (AML)
- A 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
- A 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)
- A Study of ASP2215 in Combination With Induction and Consolidation Chemotherapy in Patients With Newly Diagnosed Acute Myeloid Leukemia
- A Study of ASP2215 in Combination With Induction and Consolidation Chemotherapy in Patients With Newly Diagnosed Acute Myeloid Leukemia.
- A Study of ASP2215 Versus Salvage Chemotherapy in Patients With Relapsed or Refractory Acute Myeloid Leukemia (AML) With FMS-like Tyrosine Kinase (FLT3) Mutation
- A Study of ASP2215 Versus Salvage Chemotherapy In Patients With Relapsed or Refractory Acute Myeloid Leukemia (AML) With FMS-like Tyrosine Kinase 3 (FLT3) Mutation
- A 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)
- A Study of Gilteritinib in Adults With Advanced ALK-positive Non-small Cell Lung Cancer (NSCLC)
- A Study of Gilteritinib in Combination With Ivosidenib or Enasidenib in People With Acute Myeloid Leukemia (AML)
- A 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
- A Study of Gilteritinib, Venetoclax and Azacitidine as a Combined Treatment for People Newly Diagnosed With Acute Myeloid Leukemia
- A Study of Venetoclax in Combination With Conventional Chemotherapy in Pediatric Patients With Acute Myeloid Leukemia
- A Study to Assess Safety and Efficacy of Venetoclax in Combination With Gilteritinib in Participants With Relapsed/Refractory Acute Myeloid Leukemia
- A 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
Approved for (1)
- Neoplasm
In development for (7)
- Acute myeloid leukemia Phase 3
- Kidney disorder Phase 1
- Leukemia Phase 1
- Liver disorder Phase 1
- Myelodysplastic syndrome Phase 2
- Myeloid leukemia Phase 3
- Non-small cell lung carcinoma Phase 1
Other linked conditions (3)
- Acute myeloid leukemia by FAB classification
- Childhood acute myeloid leukemia
- Hematopoietic and lymphoid cell neoplasm