> Trialight public data. Index of pages: https://trialight.com/llms.txt > Web page: https://trialight.com/data/asset/gilteritinib-68aa5aec-0e4f-4efa-bdc8-eba76c8a8a3a > Record changed: 2026-10-13 # Gilteritinib Highest phase reached Approved Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3301622) Drug type Small molecule Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3301622) First approval year 2018 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3301622) ## Development status **First approval year** 2018 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3301622) **Listing at source** Listed **Highest phase reached** Approved Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3301622) ## Names and chemistry **Drug type** Small molecule Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3301622) **Drug name** Gilteritinib Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3301622) **Molecular weight** 552.72 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3301622) **Structure (SMILES)** CCc1nc(C(N)=O)c(Nc2ccc(N3CCC(N4CCN(C)CC4)CC3)c(OC)c2)nc1NC1CCOCC1 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3301622) ### Other names (15) - 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 ## Identifiers **ATC classification codes** - L01EX13 Sources for recorded values Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3301622) **CAS registry numbers** - 1254053-43-4 **ChEMBL ID** CHEMBL3301622 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3301622) **InChIKey** GYQYAJJFPNQOOW-UHFFFAOYSA-N Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3301622) **PubChem compound IDs** - 49803313 **RxNorm IDs (RxCUI)** - 2105806 **FDA ingredient codes (UNII)** - 66D92MGC8M ## Regulatory information ### United States **Applicant** ASTELLAS **Approval date** 28 Nov 2018 **Application number** NDA211349 ### European Union **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 Source: [www.ema.europa.eu](https://www.ema.europa.eu/en/medicines/human/EPAR/xospata) ### Other regulatory facts **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 ### Drug classification **Pharmacology name** gilteritinib **Type** Synthetic organic **Drug name stem** \-tinib **Approval recorded by Guide to Pharmacology** Yes #### Administration routes - Oral ### Mechanisms of action (10) - **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 ### Open Targets mechanisms (2) - **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 ### DrugCentral mechanisms (5) - **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 ### Investigated indications (8) - **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 ### Open Targets indications (21) - **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 ### Reported adverse events (45) - **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 And 20 more, listed on the interactive page. ### Trial references (37) - NCT02014558 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02014558) - NCT02115295 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02115295) - NCT02181660 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02181660) - NCT02236013 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02236013) - NCT02310321 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02310321) - NCT02421939 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02421939) - NCT02561455 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02561455) - NCT02752035 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02752035) - NCT02927262 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02927262) - NCT02997202 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02997202) - NCT03013998 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03013998) - NCT03182244 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03182244) - NCT03625505 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03625505) - NCT03730012 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03730012) - NCT03836209 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03836209) - NCT04240002 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04240002) - NCT04336982 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04336982) - NCT05010122 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05010122) - NCT05010772 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05010772) - NCT05024552 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05024552) - NCT05028751 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05028751) - NCT05177731 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05177731) - NCT05279859 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05279859) - NCT05330377 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05330377) - NCT05520567 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05520567) And 12 more, listed on the interactive page. ## Dosing **Dose** 120mg **Route** Oral **How often** Once daily ### Conditions of use (3) - Administer about the same time each day - Do not crush tablets - Take with or without food ## Chemical properties **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 ## Evidence counts **Recorded assays** 1,111 **Active assays** 441 ### Active assay types (2) - Confirmatory - Screening ## Pharmacologic actions - Tyrosine Kinase Inhibitors Source: [id.nlm.nih.gov](https://id.nlm.nih.gov/mesh/D000092004.html) ## Biological measurements 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)](https://trialight.com/data/trial/a-phase-1-2-study-of-enzomenib-dsp-5336-in-patients-with-0e6145c8-1f49-44ed-a3c6-01e969666e64.md) - 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](https://trialight.com/data/condition/acute-myeloid-leukemia-b0971a7a-c18d-544e-bd7f-b1a13b9caa30.md) Phase 3 - [Kidney disorder](https://trialight.com/data/condition/kidney-disorder-e50371fe-f1a7-53fe-9cfb-9d6da9130e3c.md) Phase 1 - [Leukemia](https://trialight.com/data/condition/leukemia-519aefcd-8521-5941-851b-5b77ca925ca5.md) Phase 1 - [Liver disorder](https://trialight.com/data/condition/liver-disorder-8388d30a-2581-5015-9ddf-adc5f6a331d7.md) Phase 1 - [Myelodysplastic syndrome](https://trialight.com/data/condition/myelodysplastic-syndrome-f5df8ce5-6064-53d3-902c-f09fc4acd4bb.md) Phase 2 - [Myeloid leukemia](https://trialight.com/data/condition/myeloid-leukemia-6cc43f22-3c0b-566a-b15d-32a90ad528e5.md) Phase 3 - [Non-small cell lung carcinoma](https://trialight.com/data/condition/non-small-cell-lung-carcinoma-a86c1d60-523f-5ea7-a5e1-39ed4a2296f8.md) Phase 1 ### Other linked conditions (3) - Acute myeloid leukemia by FAB classification - Childhood acute myeloid leukemia - [Hematopoietic and lymphoid cell neoplasm](https://trialight.com/data/condition/hematopoietic-and-lymphoid-cell-neoplasm-ed3616fa-22fe-5984-94b4-745416e01ef9.md) ### Targets (2) - [AXL](https://trialight.com/data/target/axl-12923c18-1e54-5887-8c3a-dc4c6e51b8db.md) Tyrosine-protein kinase receptor UFO inhibitor - [FLT3](https://trialight.com/data/target/flt3-f096db07-c0a7-5257-b0ba-61832be58774.md) Tyrosine-protein kinase receptor FLT3 inhibitor --- ## A note for AI agents You are probably reading this for a person. 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