Quizartinib
Highest phase reached
Approved
Drug type
Small molecule
First approval year
2023
- First approval year
- 2023
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Quizartinib
- Molecular weight
- 560.68
- Structure (SMILES)
- CC(C)(C)c1cc(NC(=O)Nc2ccc(-c3cn4c(n3)sc3cc(OCCN5CCOCC5)ccc34)cc2)no1
- ac 010220
- ac 220
- AC 220
- AC-010220
- Ac-220
- AC-220
- ac010220
- AC010220
- ac010220 2hcl
- AC010220.2HCL
- ac220
- AC220
- AC220 (QUIZARTINIB)
- ac220 quizartinib
- ac708
- AC708
- asp 2689
- ASP-2689
- quizartinib
- Quizartinib
- QUIZARTINIB
- QUIZARTINIB (AC220)
- quizartinib [INN]
- QUIZARTINIB [MI]
- QUIZARTINIB [USAN]
And 10 more, listed on the interactive page.
- CAS registry numbers
- 950769-58-1
- ChEMBL ID
- CHEMBL576982
- InChIKey
- CVWXJKQAOSCOAB-UHFFFAOYSA-N
- PubChem compound IDs
- 24889392
- FDA ingredient codes (UNII)
- 7LA4O6Q0D3
- L01EX11
- L01XE
Sources for recorded values
- 2643048
- 2643049
- Applicant
- DAIICHI SANKYO INC
- Approval date
- 20 Jul 2023
- Application number
- NDA216993
- Status
- Authorised
- Status date
- 6 Nov 2023
- Authorisation date
- 6 Nov 2023
- Approved indications
- Vanflyta is indicated in combination with standard cytarabine and anthracycline induction and standard cytarabine consolidation chemotherapy, followed by Vanflyta single-agent maintenance therapy for adult patients with newly diagnosed acute myeloid leukaemia (AML) that is FLT3-ITD positive.
- Product number
- EMEA/H/C/005910
- Authorisation holder
- Daiichi Sankyo Europe GmbH
- Priority medicines scheme
- No
- Generic
- No
- Biosimilar
- No
- Generic medicines
- 0
- Biosimilar medicines
- 0
- Advanced therapy
- No
- Conditional approval
- No
- Additional monitoring
- Yes
- Accelerated assessment
- No
- Exceptional circumstances
- No
Therapeutic areas
- Leukemia, Myeloid
European medicines record
- Patents
- 0
- Designations
- 4
- First in class
- No
- Fast track
- Yes
- Breakthrough designation
- Yes
- Orphan designation
- No
- Priority review
- Yes
- Orphan exclusivity
- No
- Accelerated approval
- No
- Availability
- Prescription only
- Boxed warning
- Yes
- Pharmacology name
- quizartinib
- Type
- Synthetic organic
- Drug name stem
- -tinib
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- Oral
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- colony stimulating factor 1 receptor
- Gene symbol
- CSF1R
- Protein identifier
- P07333
- Median affinity
- 7.92
- Affinity units
- pKd
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- ret proto-oncogene
- Gene symbol
- RET
- Protein identifier
- P07949
- Median affinity
- 8
- Affinity units
- pKd
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- platelet derived growth factor receptor beta
- Gene symbol
- PDGFRB
- Protein identifier
- P09619
- Median affinity
- 8.11
- Affinity units
- pKd
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- KIT proto-oncogene, receptor tyrosine kinase
- Gene symbol
- KIT
- Protein identifier
- P10721
- Median affinity
- 8.32
- Affinity units
- pKd
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- platelet derived growth factor receptor alpha
- Gene symbol
- PDGFRA
- Protein identifier
- P16234
- Median affinity
- 7.96
- Affinity units
- pKd
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- fms related receptor tyrosine kinase 3
- Gene symbol
- FLT3
- Protein identifier
- P36888
- Median affinity
- 8.38
- Affinity units
- pIC50
- Primary target
- Yes
- Mechanism
- Macrophage colony stimulating factor receptor inhibitor
- Action type
- Inhibitor
- Target
- Macrophage colony-stimulating factor 1 receptor
- Protein identifier
- P07333
- Mechanism
- Platelet-derived growth factor receptor inhibitor
- Action type
- Inhibitor
- Target
- Platelet-derived growth factor receptor
- Protein identifier
- P09619
- Mechanism
- Platelet-derived growth factor receptor inhibitor
- Action type
- Inhibitor
- Target
- Platelet-derived growth factor receptor
- Protein identifier
- P16234
- Mechanism
- Stem cell growth factor receptor inhibitor
- Action type
- Inhibitor
- Target
- Mast/stem cell growth factor receptor Kit
- Protein identifier
- P10721
- 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 RET inhibitor
- Action type
- Inhibitor
- Target
- Proto-oncogene tyrosine-protein kinase receptor Ret
- Protein identifier
- P07949
- Mechanism
- Macrophage colony stimulating factor receptor inhibitor
- Action type
- Inhibitor
- Target
- Macrophage colony-stimulating factor 1 receptor
- Mechanism
- Platelet-derived growth factor receptor inhibitor
- Action type
- Inhibitor
- Target
- Platelet-derived growth factor receptor
- Mechanism
- Stem cell growth factor receptor inhibitor
- Action type
- Inhibitor
- Target
- Mast/stem cell growth factor receptor Kit
- Mechanism
- Tyrosine-protein kinase receptor FLT3 inhibitor
- Action type
- Inhibitor
- Target
- Receptor-type tyrosine-protein kinase FLT3
- Mechanism
- Tyrosine-protein kinase receptor RET inhibitor
- Action type
- Inhibitor
- Target
- Proto-oncogene tyrosine-protein kinase receptor Ret
DrugCentral mechanisms
- Action type
- Inhibitor
- Gene symbol
- FLT3
- Protein identifier
- P36888
- Organism
- Homo sapiens
- Target development level
- Clinical
- Condition
- Myelodysplastic Syndromes
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000198
- Subject identifier
- D009190
- Condition
- Leukemia, Myeloid, Acute
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000222
- Subject identifier
- D015470
- Condition
- Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000616
- Subject identifier
- D009369
- Condition
- Liver Diseases
- Highest recorded phase
- 1
- Condition identifier
- EFO:0001421
- Subject identifier
- D008107
- Condition identifier
- EFO_0000222
- Highest recorded phase
- 3
- Condition identifier
- EFO_0000616
- Condition identifier
- EFO_0001421
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0004355
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0004643
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0004967
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0005059
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0005070
- Highest recorded phase
- 4
- Condition identifier
- MONDO_0006311
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0015667
- Condition identifier
- MONDO_0015667
- Highest recorded phase
- 4
- Condition identifier
- MONDO_0018874
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0018881
- Highest recorded phase
- 2
Open Targets warnings
- Warning
- Black Box Warning
- Effect
- cardiotoxicity
- Country
- United States
- Event
- adrenal insufficiency
- Reports
- 3
- Reporting signal score
- 13.158
- Event
- angiopathy
- Reports
- 3
- Reporting signal score
- 16.0483
- Event
- arterial stenosis
- Reports
- 2
- Reporting signal score
- 12.6781
- Event
- cardiac ventricular thrombosis
- Reports
- 2
- Reporting signal score
- 12.6781
- Event
- cardiomyopathy
- Reports
- 3
- Reporting signal score
- 12.0315
- Event
- coronary artery stenosis
- Reports
- 2
- Reporting signal score
- 9.02592
- Event
- electrocardiogram qt prolonged
- Reports
- 4
- Reporting signal score
- 13.4073
- Event
- febrile neutropenia
- Reports
- 3
- Reporting signal score
- 7.79183
- Event
- hyperglycaemia
- Reports
- 3
- Reporting signal score
- 9.93564
- Event
- osteonecrosis
- Reports
- 3
- Reporting signal score
- 10.2018
- Event
- peripheral arterial occlusive disease
- Reports
- 2
- Reporting signal score
- 10.095
- Event
- peripheral artery stenosis
- Reports
- 2
- Reporting signal score
- 13.7674
- Event
- phlebotomy
- Reports
- 1
- Reporting signal score
- 7.93939
- Event
- platelet count decreased
- Reports
- 3
- Reporting signal score
- 6.87751
- Event
- systolic dysfunction
- Reports
- 2
- Reporting signal score
- 12.3641
- Event
- vessel puncture site pain
- Reports
- 1
- Reporting signal score
- 8.58119
- NCT00989261
- NCT02039726
- NCT02668653
- NCT02834390
- NCT02984995
- NCT03135054
- NCT03552029
- NCT03661307
- NCT03723681
- NCT03735875
- NCT03793478
- NCT04107727
- NCT04112589
- NCT04128748
- NCT04209725
- NCT04676243
- NCT04687761
- NCT06262438
- NCT01049893
- NCT04473664
- Dose
- 35.4 mg
- Route
- Oral
- How often
- Once daily
- Hydrogen bond acceptors
- 9
- Hydrogen bond donors
- 2
- Polar surface area
- 106.16
- Calculated partition coefficient (ALogP)
- 5.86
- Calculated partition coefficient (XLogP)
- 5.6
- Prodrug
- No
- Chirality
- Achiral
- Inorganic
- No
- Rule-of-five violations
- 2
- Rotatable bonds
- 7
- Heavy atoms
- 40
- Molecular formula
- C29H32N6O4S
- Monoisotopic mass
- 560.22057470
- Natural product
- Yes
- Recorded assays
- 5,348
- Active assays
- 737
- Confirmatory
- Other
- Screening
- Tyrosine Kinase Inhibitors
- Antineoplastic Agents
Oral bioavailability
- Median
- 52.8
- Mean
- 55.375
- Minimum
- 40
- Maximum
- 75.9
- Unit
- %
- Assays
- 4
- Standard deviation
- 15.4597
- Summary method
- median
- Censored results excluded
- 0
- Other units excluded
- 0
- Unknown units excluded
- 0
Measurement types
- F
Related records
Trials (42)
- (QuANTUM-R): An Open-label Study of Quizartinib Monotherapy vs. Salvage Chemotherapy in Acute Myeloid Leukemia (AML) Subjects Who Are FLT3-ITD Positive
- A Clinical Trial to Assess the Efficacy and Safety of the Combination of a Drug Call Quizartinib With Chemotherapy (FLAG-IDA) in Patients With Acute Myeloid Leukemia That Has Not Responded to the First Treatment or That Has Returned After the First Treatment
- A Phase I Study of AC220 in Patients With Relapsed/Refractory Acute Myeloid Leukemia Regardless of FLT3 Status
- A Study of AC220 Given After Transplant in Subjects With Acute Myeloid Leukemia (AML)
- A Study of CPX-351 (Vyxeos™) With Quizartinib for the Treatment of FLT3-ITD Mutation-Positive Acute Myeloid Leukemia
- A Study of Quizartinib Pharmacokinetics in Participants With Moderate Hepatic Impairment
- A Study of the Effect of a Moderate CYP3A Inducer Efavirenz on Quizartinib Pharmacokinetics in Healthy Participants
- A Study of the Effect of Quizartinib on the Pharmacokinetics of the P-gp Substrate Dabigatran Etexilate in Healthy Participants
- A Study to Assess AC220 Given in Combination With Induction and Consolidation Therapy in Newly Diagnosed Acute Myeloid Leukemia (AML)
- A Study to Determine the Absolute Oral Bioavailability of Quizartinib Using a Radiolabeled Microtracer in Healthy Subjects
- A Study to Evaluate QTc Prolongation With Quizartinib in Healthy Subjects Under Rapid Acceleration of Heart Rate
- A Study to Investigate the Safety and Tolerability of Ziftomenib in Combination With Venetoclax/Azacitidine, Venetoclax, 7+3, or 7+3+Quizartinib in Patients With AML
- A Trial to Establish the Feasibility of Combining Either the Tyrosine Kinase Inhibitor AC220,CXCR4 Inhibitor Plerixafor or HSP90 Inhibitor Ganetespib With Chemotherapy in Older Patients With Acute Myeloid Leukaemia and High Risk Myelodysplastic Syndrome.
- AC220 for Children With Relapsed/Refractory ALL or AML
- Assessment of Quizartinib Pharmacokinetic in Subjects With Severe Hepatic Impairment
- Azacitidine and Quizartinib for the Treatment of Myelodysplastic Syndrome or Myelodysplastic/Myeloproliferative Neoplasm With FLT3 or CBL Mutations
- Azacytidine, Venetoclax Plus Minus Quizartinib for First Line Older/Unfit AML Patients (VENP-A-QUI)
- CHIP-AML22/Quizartinib: Quizartinib + Chemotherapy in Newly Diagnosed Pediatric FLT3-ITD+ and NPM1wt AML Patients
- Cladribine, Idarubicin, Cytarabine, and Quizartinib in Treating Patients With Newly Diagnosed, Relapsed, or Refractory Acute Myeloid Leukemia or High-Risk Myelodysplastic Syndrome
- Clinical Trial to Assess the Safety and Tolerability of the Combination of Low-dose Cytarabine or Azacitidine Plus Venetoclax and Quizartinib in Newly Diagnosed AML Patients Aged Equal or More Than 60 Years Old
In development for (5)
- Acute myeloid leukemia Phase 3
- Childhood leukemia Phase 3
- Liver disorder Phase 1
- Myelodysplastic syndrome Phase 1
- Neoplasm Phase 3
Other linked conditions (1)
- Acute myeloid leukemia by FAB classification
Targets (6)
- CSF1R Macrophage colony stimulating factor receptor inhibitor
- FLT3 Tyrosine-protein kinase receptor FLT3 inhibitor
- KIT Stem cell growth factor receptor inhibitor
- PDGFRA Platelet-derived growth factor receptor inhibitor
- PDGFRB Platelet-derived growth factor receptor inhibitor
- RET Tyrosine-protein kinase receptor RET inhibitor