Nilotinib
Highest phase reached
Approved
Drug type
Small molecule
First approval year
2007
- First approval year
- 2007
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Nilotinib
- Molecular weight
- 529.53
- Structure (SMILES)
- Cc1cn(-c2cc(NC(=O)c3ccc(C)c(Nc4nccc(-c5cccnc5)n4)c3)cc(C(F)(F)F)c2)cn1
- amn 107
- AMN 107
- AMN-107
- amn107
- AMN107
- nilotinib
- Nilotinib
- NILOTINIB [EMA EPAR]
- NILOTINIB [HSDB]
- nilotinib [INN]
- NILOTINIB [MART.]
- NILOTINIB [MI]
- NILOTINIB [USAN]
- NILOTINIB [USP-RS]
- NILOTINIB [VANDF]
- Nilotinib [WHO-DD]
- nilotinib ema epar
- nilotinib hsdb
- nilotinib inn
- nilotinib mart
- nilotinib mi
- nilotinib usan
- nilotinib usp rs
- nilotinib vandf
- nilotinib who dd
And 2 more, listed on the interactive page.
- ATC classification codes
- L01EA03
Sources for recorded values
- CAS registry numbers
- 641571-10-0
- ChEMBL ID
- CHEMBL255863
- InChIKey
- HHZIURLSWUIHRB-UHFFFAOYSA-N
- PubChem compound IDs
- 644241
- FDA ingredient codes (UNII)
- F41401512X
- 662281
- 1804015
- Applicant
- AZURITY
- Approval date
- 7 Nov 2024
- Application number
- NDA219293
- Status
- Authorised
- Status date
- 19 Nov 2007
- Authorisation date
- 19 Nov 2007
- Approved indications
- Tasigna is indicated for the treatment of: adult and paediatric patients with newly diagnosed Philadelphia chromosome positive chronic myelogenous leukaemia (CML) in the chronic phase, paediatric patients with Philadelphia chromosome positive CML in chronic phase with resistance or intolerance to prior therapy including imatinib. Tasigna is indicated for the treatment of: adult and paediatric patients with newly diagnosed Philadelphia chromosome positive chronic myelogenous leukaemia (CML) in the chronic phase, adult patients with chronic phase and accelerated phase Philadelphia chromosome positive CML with resistance or intolerance to prior therapy including imatinib. Efficacy data in patients with CML in blast crisis are not available, paediatric patients with chronic phase Philadelphia chromosome positive CML with resistance or intolerance to prior therapy including imatinib.
- Product number
- EMEA/H/C/000798
- Authorisation holder
- Novartis Europharm Limited
- Priority medicines scheme
- No
- Generic
- No
- Biosimilar
- No
- Generic medicines
- 1
- Biosimilar medicines
- 0
- Advanced therapy
- No
- Conditional approval
- No
- Additional monitoring
- No
- Accelerated assessment
- No
- Exceptional circumstances
- No
Therapeutic areas
- Leukemia, Myelogenous, Chronic, BCR-ABL Positive
European medicines record
- Patents
- 3
- Designations
- 5
- Earliest recorded loss of exclusivity
- 18 Feb 2040
- First in class
- Yes
- Fast track
- Yes
- Breakthrough designation
- No
- Orphan designation
- No
- Priority review
- No
- Orphan exclusivity
- No
- Accelerated approval
- Yes
- Availability
- Prescription only
- Boxed warning
- Yes
- Pharmacology name
- nilotinib
- Type
- Synthetic organic
- Drug name stem
- -tinib
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- Oral
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- ABL proto-oncogene 1, non-receptor tyrosine kinase
- Gene symbol
- ABL1
- Protein identifier
- P00519
- Median affinity
- 7.8
- Affinity units
- pIC50
- Primary target
- Yes
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- discoidin domain receptor tyrosine kinase 1
- Gene symbol
- DDR1
- Protein identifier
- Q08345
- Median affinity
- 7.37
- Affinity units
- pIC50
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- discoidin domain receptor tyrosine kinase 2
- Gene symbol
- DDR2
- Protein identifier
- Q16832
- Median affinity
- 9.3
- Affinity units
- pIC50
- Mechanism
- Bcr/Abl fusion protein inhibitor
- Action type
- Inhibitor
- Target
- Bcr/Abl fusion protein
- Mechanism
- Tyrosine-protein kinase ABL inhibitor
- Action type
- Inhibitor
- Target
- Tyrosine-protein kinase ABL1
DrugCentral mechanisms
- Action type
- Inhibitor
- Gene symbol
- ABL1
- Protein identifier
- P00519
- Organism
- Homo sapiens
- Target development level
- Clinical
- Condition
- Precursor Cell Lymphoblastic Leukemia-Lymphoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000220
- Subject identifier
- D054198
- Condition
- Leukemia, Myeloid, Acute
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000222
- Subject identifier
- D015470
- Condition
- Leukemia, Myelogenous, Chronic, BCR-ABL Positive
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000339
- Subject identifier
- D015464
- Condition
- Melanoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000389
- Subject identifier
- D008545
- Condition
- Leukemia
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000565
- Subject identifier
- D007938
- Condition
- Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000616
- Subject identifier
- D009369
- Condition
- Melanoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000756
- Subject identifier
- D008545
- Condition
- Hypertension, Pulmonary
- Highest recorded phase
- 2
- Condition identifier
- EFO:0001361
- Subject identifier
- D006976
- Condition
- Melanoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0002617
- Subject identifier
- D008545
- Condition
- Paraganglioma
- Highest recorded phase
- 2
- Condition identifier
- EFO:1000453
- Subject identifier
- D010235
- Condition
- Sarcoma
- Highest recorded phase
- 3
- Condition identifier
- EFO:1001968
- Subject identifier
- D012509
- Condition
- Neuroma, Acoustic
- Highest recorded phase
- 2
- Condition identifier
- HP:0009588
- Subject identifier
- D009464
- Condition
- Cerebellar Ataxia
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0000437
- Subject identifier
- D002524
- Condition
- Precursor Cell Lymphoblastic Leukemia-Lymphoma
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0000870
- Subject identifier
- D054198
- Condition
- Leukemia, Myeloid
- Highest recorded phase
- 3
- Condition identifier
- MONDO:0004643
- Subject identifier
- D007951
- Condition
- Alzheimer Disease
- Highest recorded phase
- 3
- Condition identifier
- MONDO:0004975
- Subject identifier
- D000544
- Condition
- Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- MONDO:0004992
- Subject identifier
- D009369
- Condition
- Parkinson Disease
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0005180
- Subject identifier
- D010300
- Condition
- Breast Neoplasms
- Highest recorded phase
- 1
- Condition identifier
- MONDO:0007254
- Subject identifier
- D001943
- Condition
- Huntington Disease
- Highest recorded phase
- 1
- Condition identifier
- MONDO:0007739
- Subject identifier
- D006816
- Condition
- Chordoma
- Highest recorded phase
- 1
- Condition identifier
- MONDO:0008978
- Subject identifier
- D002817
- Condition
- Gastrointestinal Stromal Tumors
- Highest recorded phase
- 3
- Condition identifier
- MONDO:0011719
- Subject identifier
- D046152
- Condition
- Graft vs Host Disease
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0013730
- Subject identifier
- D006086
- Condition
- Bronchiolitis Obliterans Syndrome
- Highest recorded phase
- 1
- Condition identifier
- MONDO:0020547
- Subject identifier
- D000092122
- Condition
- Colonic Neoplasms
- Highest recorded phase
- 0.5
- Condition identifier
- MONDO:0021063
- Subject identifier
- D003110
And 2 more, listed on the interactive page.
- Condition identifier
- EFO_0000220
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000222
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000339
- Condition identifier
- EFO_0000389
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000565
- Highest recorded phase
- 3
- Condition identifier
- EFO_0000616
- Condition identifier
- EFO_0000658
- Highest recorded phase
- 1
- Condition identifier
- EFO_0000756
- Highest recorded phase
- 2
- Condition identifier
- EFO_0001361
- Highest recorded phase
- 2
- Condition identifier
- EFO_0002617
- Highest recorded phase
- 2
- Condition identifier
- EFO_0004952
- Highest recorded phase
- 2
- Condition identifier
- EFO_0006792
- Highest recorded phase
- 2
- Condition identifier
- EFO_1000178
- Highest recorded phase
- 1
- Condition identifier
- EFO_1000453
- Highest recorded phase
- 2
- Condition identifier
- HP_0009588
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0000437
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0000544
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0000548
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0003199
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0003219
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0003865
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0004643
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0004967
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0004975
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0005028
- Highest recorded phase
- 2
And 38 more, listed on the interactive page.
- Warning
- Black Box Warning
- Effect
- cardiotoxicity
- Country
- United States
- Warning
- Black Box Warning
- Effect
- musculoskeletal toxicity
- Country
- United States
- Event
- acute myocardial infarction
- Reports
- 198
- Reporting signal score
- 224.32
- Event
- angina pectoris
- Reports
- 252
- Reporting signal score
- 352.397
- Event
- blast crisis in myelogenous leukaemia
- Reports
- 67
- Reporting signal score
- 262.428
- Event
- blood bilirubin increased
- Reports
- 254
- Reporting signal score
- 336.708
- Event
- chronic myeloid leukaemia
- Reports
- 185
- Reporting signal score
- 562.703
- Event
- chronic myeloid leukaemia recurrent
- Reports
- 45
- Reporting signal score
- 173.907
- Event
- chronic myeloid leukaemia transformation
- Reports
- 38
- Reporting signal score
- 163.391
- Event
- coronary artery disease
- Reports
- 186
- Reporting signal score
- 149.609
- Event
- coronary artery stenosis
- Reports
- 113
- Reporting signal score
- 228.038
- Event
- cytogenetic analysis abnormal
- Reports
- 186
- Reporting signal score
- 830.224
- Event
- drug intolerance
- Reports
- 288
- Reporting signal score
- 150.628
- Event
- drug resistance
- Reports
- 236
- Reporting signal score
- 321.474
- Event
- electrocardiogram qt prolonged
- Reports
- 544
- Reporting signal score
- 925.953
- Event
- intermittent claudication
- Reports
- 101
- Reporting signal score
- 308.177
- Event
- lipase increased
- Reports
- 187
- Reporting signal score
- 383.791
- Event
- myocardial infarction
- Reports
- 414
- Reporting signal score
- 320.308
- Event
- myocardial ischaemia
- Reports
- 111
- Reporting signal score
- 151.133
- Event
- pancreatitis
- Reports
- 255
- Reporting signal score
- 222.536
- Event
- peripheral arterial occlusive disease
- Reports
- 237
- Reporting signal score
- 773.289
- Event
- peripheral artery stenosis
- Reports
- 48
- Reporting signal score
- 167.684
- Event
- philadelphia chromosome positive
- Reports
- 57
- Reporting signal score
- 211.67
- Event
- pleural effusion
- Reports
- 405
- Reporting signal score
- 480.862
- Event
- rash
- Reports
- 873
- Reporting signal score
- 352.904
- Event
- second primary malignancy
- Reports
- 214
- Reporting signal score
- 515.84
- NCT00129740
- NCT00264160
- NCT00471497
- NCT00481052
- NCT00644878
- NCT00702403
- NCT00718263
- NCT00760877
- NCT00802841
- NCT01126892
- NCT01220648
- NCT01223898
- NCT01254188
- NCT01274351
- NCT01275196
- NCT01294618
- NCT01400074
- NCT01456676
- NCT01535391
- NCT01690065
- NCT01698905
- NCT01702064
- NCT01743989
- NCT01744665
- NCT01774630
And 84 more, listed on the interactive page.
- Dose
- 300 mg
- Route
- Oral
- How often
- Twice daily
- Do not consume food for at least 2 hours before and 1 hour after dose
- Swallow capsules whole or disperse in applesauce if unable to swallow
- Take on an empty stomach, with water, at approximately 12-hour intervals
- Hydrogen bond acceptors
- 7
- Hydrogen bond donors
- 2
- Polar surface area
- 97.62
- Calculated partition coefficient (ALogP)
- 6.36
- Calculated partition coefficient (XLogP)
- 4.9
- Prodrug
- No
- Chirality
- Achiral
- Inorganic
- No
- Rule-of-five violations
- 2
- Rotatable bonds
- 6
- Heavy atoms
- 39
- Molecular formula
- C28H22F3N7O
- Monoisotopic mass
- 529.18379284
- Natural product
- No
- 24338-154
- 24338-155
- 31722-779
- 31722-780
- 69097-030
- 69097-031
- 69097-032
- 70709-191
- 70709-192
- 72205-237
- 72205-238
- 72205-239
- 73190-033
- 73190-034
- 76282-788
- 76282-789
- 76282-790
- 60505-3801
- 60505-3802
- 60505-3803
- Recorded assays
- 3,863
- Active assays
- 627
- Confirmatory
- Other
- Screening
- Tyrosine Kinase Inhibitors
These details could not be displayed.
Related records
Trials (167)
- 2nd or 3rd TKI-stop After 2 Years Nilotinib Pre-treatment in CML-patients
- A Bioavailability Study of Nilotinib in Healthy, Adult, Human Subjects Under Fasted Conditions.
- A Clinical Trial to Evaluate the Effect of Nilotinib on the PK/PD of Meformin
- A Pharmacokinetic (PK) Study of Nilotinib in Pediatric Patients With Philadelphia Chromosome-positive (Ph+) Chronic Myelogenous Leukemia (CML) or Acute Lymphoblastic Leukemia (ALL)
- A Phase I Study of Nilontinib and Cetuximab in Patients With Solid Tumors
- A Phase I Study of Oral Asciminib (ABL001) in Patients With CML or Ph+ ALL
- A Phase III Randomized Trial of the Reduction of Chemotherapy in Philadelphia Chromosome-positive ALL of Young Adults
- A Phase l/ll Study of AMN107 in Adult Patients With Glivec-intolerant CML or Relapsed-refractory Ph+ALL
- A Randomized Phase III Study to Assess the Effect of a Longer Duration of Consolidation Treatment With Nilotinib on TFR in CP CML.
- A Study Comparing Ponatinib and Nilotinib in Participants With Chronic Myeloid Leukemia
- A Study of AMNN107 in the Treatment of Metastatic and/or Inoperable Melanoma Harboring a c-Kit Mutation
- A Study of Full Treatment-free Remission in Patients With Chronic Myeloid Leukemia
- A Study of Imatinib and Nilotinib in Patients With Chronic Myelogenous Leukemia in Chronic Phase
- A Study of Imatinib Versus Nilotinib in Adult Patients With Newly Diagnosed Philadelphia Chromosome Positive (Ph+) Chronic Myelogenous Leukemia in Chronic Phase (CML-CP)
- A Study of Nilotinib in Adult Patients With Imatinib Resistant or - Intolerant Chronic Myeloid Leukemia in Blast Crisis, Accelerated Phase or Chronic Phase
- A Study of Nilotinib in Growing Vestibular Schwannomas
- A Study of Nilotinib Versus Imatinib in GIST Patients
- A Study of Oral AMN107 in Adults With Chronic Myelogenous Leukemia (CML) or Other Hematologic Malignancies
- A Study of Oral Asciminib Versus Other TKIs in Adult Patients With Newly Diagnosed Ph+ CML-CP
- A Study of REduction And DIscontinuation Treatment of TKI (Imatinib, Nilotinib, Dasatinib and Bosutinib)
In development for (28)
- Acoustic neuroma Phase 2
- Acute lymphoblastic leukemia Phase 2
- Acute myeloid leukemia Phase 2
- Alzheimer disease Phase 3
- Breast cancer Phase 1
- Cancer Phase 3
- Cerebellar ataxia Phase 2
- Childhood acute lymphoblastic leukemia Phase 2
- Chordoma Phase 1
- Chronic graft versus host disease Phase 1
- Chronic myeloid leukemia Phase 3
- Cutaneous melanoma Phase 2
- Gastrointestinal stromal tumor Phase 3
- Graft versus host disease Phase 2
- Huntington disease Phase 1
- Leukemia Phase 3
- Lewy body dementia Phase 2
- Low grade glioma Phase 2
- Malignant colon neoplasm Early phase 1
- Melanoma Phase 2
Other linked conditions (1)
- Systemic mastocytosis