Axitinib
Highest phase reached
Approved
Drug type
Small molecule
First approval year
2012
- First approval year
- 2012
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Axitinib
- Molecular weight
- 386.48
- Structure (SMILES)
- CNC(=O)c1ccccc1Sc1ccc2c(/C=C/c3ccccn3)n[nH]c2c1
- inlyta
- Inlyta
- adebrelimab axitinib
- ag 013736
- ag 013736 axitinib
- ag 013736 docetaxel
- ag 13736
- AG-013736
- AG-013736 (axitinib)
- AG-013736 (Axitinib)
- AG-013736 (AXITINIB)
- AG-13736
- ag013736
- ak104 axitinib
- ak112 axitinib
- axitinib
- Axitinib
- AXITINIB
- Axitinib (AG-013736)
- Axitinib (VEGF-TKI)
- Axitinib [AG-013736]
- Axitinib [INN]
- Axitinib [JAN]
- Axitinib [MART.]
- Axitinib [MI]
- Axitinib [ORANGE BOOK]
- Axitinib [USAN]
And 47 more, listed on the interactive page.
- ATC classification codes
- L01EK01
Sources for recorded values
- CAS registry numbers
- 319460-85-0
- ChEMBL ID
- CHEMBL1289926
- InChIKey
- RITAVMQDGBJQJZ-FMIVXFBMSA-N
- PubChem compound IDs
- 6450551
- RxNorm IDs (RxCUI)
- 1242999
- FDA ingredient codes (UNII)
- C9LVQ0YUXG
- Applicant
- PF PRISM CV
- Approval date
- 27 Jan 2012
- Application number
- NDA202324
- Status
- Authorised
- Status date
- 3 Sept 2012
- Authorisation date
- 3 Sept 2012
- Approved indications
- Inlyta is indicated for the treatment of adult patients with advanced renal cell carcinoma (RCC) after failure of prior treatment with sunitinib or a cytokine.
- Product number
- EMEA/H/C/002406
- Authorisation holder
- Pfizer Europe MA EEIG
- 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
- Carcinoma, Renal Cell
European medicines record
- Patents
- 8
- Designations
- 3
- Earliest recorded loss of exclusivity
- 12 Jul 2037
- First in class
- No
- Fast track
- Yes
- Breakthrough designation
- Yes
- Orphan designation
- No
- Priority review
- No
- Orphan exclusivity
- No
- Accelerated approval
- No
- Availability
- Prescription only
- United States (FDA)
- Approved
- European Union (EMA)
- Authorised
- Pharmacology name
- axitinib
- Type
- Synthetic organic
- Drug name stem
- -tinib
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- Oral
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- polo like kinase 4
- Gene symbol
- PLK4
- Protein identifier
- O00444
- Median affinity
- 7.34
- Affinity units
- pIC50
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- kinase insert domain receptor
- Gene symbol
- KDR
- Protein identifier
- P35968
- Median affinity
- 9.6
- Affinity units
- pIC50
- Primary target
- Yes
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- kinase insert domain receptor
- Gene symbol
- KDR
- Protein identifier
- P35968
- Median affinity
- 8.23
- Affinity units
- pKd
- Primary target
- Yes
- Mechanism
- Vascular endothelial growth factor receptor inhibitor
- Action type
- Inhibitor
- Target
- Vascular endothelial growth factor receptor
- Protein identifier
- P17948
- Mechanism
- Vascular endothelial growth factor receptor inhibitor
- Action type
- Inhibitor
- Target
- Vascular endothelial growth factor receptor
- Protein identifier
- P35916
- Mechanism
- Vascular endothelial growth factor receptor inhibitor
- Action type
- Inhibitor
- Target
- Vascular endothelial growth factor receptor
- Protein identifier
- P35968
Open Targets mechanisms
- Mechanism
- Vascular endothelial growth factor receptor inhibitor
- Action type
- Inhibitor
- Target
- Vascular endothelial growth factor receptor
- Action type
- Inhibitor
- Gene symbol
- FLT1
- Protein identifier
- P17948
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Inhibitor
- Gene symbol
- FLT4
- Protein identifier
- P35916
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Inhibitor
- Gene symbol
- KDR
- Protein identifier
- P35968
- Organism
- Homo sapiens
- Target development level
- Clinical
- Condition
- Carcinoma, Squamous Cell
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000181
- Subject identifier
- D002294
- Condition
- Carcinoma, Hepatocellular
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000182
- Subject identifier
- D006528
- Condition
- Myelodysplastic Syndromes
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000198
- Subject identifier
- D009190
- Condition
- Leukemia, Myeloid, Acute
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000222
- Subject identifier
- D015470
- Condition
- Carcinoma, Adenoid Cystic
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000231
- Subject identifier
- D003528
- Condition
- Pheochromocytoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000239
- Subject identifier
- D010673
- Condition
- Carcinoma
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000313
- Subject identifier
- D002277
- Condition
- Carcinoma, Renal Cell
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000349
- Subject identifier
- D002292
- Condition
- Glioblastoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000519
- Subject identifier
- D005909
- Condition
- Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000616
- Subject identifier
- D009369
- Condition
- Carcinoma, Renal Cell
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000640
- Subject identifier
- D002292
- Condition
- Prostatic Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000673
- Subject identifier
- D011471
- Condition
- Carcinoma, Renal Cell
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000681
- Subject identifier
- D002292
- Condition
- Melanoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000756
- Subject identifier
- D008545
- Condition
- Mesothelioma
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000770
- Subject identifier
- D008654
- Condition
- Endometriosis
- Highest recorded phase
- 1
- Condition identifier
- EFO:0001065
- Subject identifier
- D004715
- Condition
- Carcinoma, Renal Cell
- Highest recorded phase
- 4
- Condition identifier
- EFO:0002890
- Subject identifier
- D002292
- Condition
- Carcinoma, Renal Cell
- Highest recorded phase
- 4
- Condition identifier
- EFO:0003016
- Subject identifier
- D002292
- Condition
- Carcinoma, Non-Small-Cell Lung
- Highest recorded phase
- 2
- Condition identifier
- EFO:0003060
- Subject identifier
- D002289
- Condition
- Thyroid Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0003841
- Subject identifier
- D013964
- Condition
- Pancreatic Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0003860
- Subject identifier
- D010190
- Condition
- Kidney Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- EFO:0003865
- Subject identifier
- D007680
- Condition
- Breast Neoplasms
- Highest recorded phase
- 1
- Condition identifier
- EFO:0003869
- Subject identifier
- D001943
- Condition
- Biliary Tract Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0003891
- Subject identifier
- D001661
- Condition
- Stomach Neoplasms
- Highest recorded phase
- 1
- Condition identifier
- EFO:0003897
- Subject identifier
- D013274
And 26 more, listed on the interactive page.
- Condition identifier
- EFO_0000181
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000182
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000231
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000313
- Highest recorded phase
- 1
- Condition identifier
- EFO_0000349
- Highest recorded phase
- 3
- Condition identifier
- EFO_0000519
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000616
- Condition identifier
- EFO_0000640
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000673
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000681
- Condition identifier
- EFO_0000756
- Highest recorded phase
- 2
- Condition identifier
- EFO_0001065
- Condition identifier
- EFO_0003016
- Highest recorded phase
- 2
- Condition identifier
- EFO_0003060
- Condition identifier
- EFO_0003841
- Highest recorded phase
- 2
- Condition identifier
- EFO_0003863
- Highest recorded phase
- 2
- Condition identifier
- EFO_0003865
- Highest recorded phase
- 3
- Condition identifier
- EFO_0003869
- Condition identifier
- EFO_0004142
- Highest recorded phase
- 2
- Condition identifier
- EFO_0004243
- Highest recorded phase
- 2
- Condition identifier
- EFO_0004252
- Highest recorded phase
- 2
- Condition identifier
- EFO_0007143
- Highest recorded phase
- 2
- Condition identifier
- EFO_0009260
- Highest recorded phase
- 1
- Condition identifier
- EFO_0009708
- Highest recorded phase
- 1
- Condition identifier
- EFO_1000796
- Highest recorded phase
- 2
And 78 more, listed on the interactive page.
- Event
- blood pressure increased
- Reports
- 210
- Reporting signal score
- 184.139
- Event
- decreased appetite
- Reports
- 307
- Reporting signal score
- 255.685
- Event
- dehydration
- Reports
- 166
- Reporting signal score
- 85.1407
- Event
- diarrhoea
- Reports
- 797
- Reporting signal score
- 522.785
- Event
- disease progression
- Reports
- 510
- Reporting signal score
- 870.343
- Event
- dysphonia
- Reports
- 282
- Reporting signal score
- 545.038
- Event
- fatigue
- Reports
- 527
- Reporting signal score
- 160.387
- Event
- hypertension
- Reports
- 426
- Reporting signal score
- 404.317
- Event
- hypothyroidism
- Reports
- 115
- Reporting signal score
- 169.563
- Event
- metastatic renal cell carcinoma
- Reports
- 70
- Reporting signal score
- 268.097
- Event
- neoplasm malignant
- Reports
- 93
- Reporting signal score
- 116.984
- Event
- neoplasm progression
- Reports
- 305
- Reporting signal score
- 740.701
- Event
- oral pain
- Reports
- 64
- Reporting signal score
- 82.4534
- Event
- palmar-plantar erythrodysaesthesia syndrome
- Reports
- 157
- Reporting signal score
- 269.672
- Event
- proteinuria
- Reports
- 81
- Reporting signal score
- 103.05
- Event
- renal cancer
- Reports
- 172
- Reporting signal score
- 575.791
- Event
- renal cell carcinoma
- Reports
- 79
- Reporting signal score
- 220.377
- Event
- second primary malignancy
- Reports
- 43
- Reporting signal score
- 67.8342
- Event
- stomatitis
- Reports
- 154
- Reporting signal score
- 173.546
- Event
- weight decreased
- Reports
- 220
- Reporting signal score
- 104.55
- NCT00071006
- NCT02638428
- NCT00076024
- NCT00094094
- NCT00735904
- NCT00768755
- NCT03386929
- NCT04585815
- NCT00094107
- NCT01174238
- NCT01321437
- NCT01533948
- NCT04493203
- NCT04640545
- NCT04996823
- NCT05070221
- NCT00219557
- NCT00282048
- NCT00569946
- NCT00835978
- NCT01334073
- NCT01441414
- NCT01649180
- NCT01693822
- NCT01727336
And 107 more, listed on the interactive page.
- Dose
- 5 mg
- Route
- Oral
- How often
- Twice daily
- Swallow whole with water
- Take approximately 12 hours apart
- With or without food
- Hydrogen bond acceptors
- 4
- Hydrogen bond donors
- 2
- Polar surface area
- 70.67
- Calculated partition coefficient (ALogP)
- 4.64
- Calculated partition coefficient (XLogP)
- 4.2
- Prodrug
- No
- Chirality
- Achiral
- Inorganic
- No
- Rule-of-five violations
- 0
- Rotatable bonds
- 5
- Heavy atoms
- 28
- Molecular formula
- C22H18N4OS
- Monoisotopic mass
- 386.12013238
- Natural product
- Yes
- 0069-0145
- 0069-0151
- 63539-026
- 63539-044
- Recorded assays
- 2,867
- Active assays
- 750
- Confirmatory
- Other
- Screening
- Summary
- Antineoplastic Agents
- Protein Kinase Inhibitors
Related records
Trials (195)
- A Bioequivalence Study Of AG-013736 Tablets In Healthy Volunteers
- A Bioequivalence Study Of AG-013736 Tablets Under Fed Conditions In Healthy Volunteers
- A Dose Finding Study To Evaluate Safety, Drug Interaction, Tumor Markers Of Axitinib In Combination With MK-3475 In Adult Patients With Previously Untreated Advanced Renal Cell Cancer
- A Phase 1b Study Of Axitinib In Combination With Crizotinib In Patients With Advanced Solid Tumors
- A Phase 2 Study in Patients With Advanced Non-Small Cell Lung Cancer Using New Agents With and Without Docetaxel.
- A Phase II Study of Axitinib in Metastatic Non-clear Cell Renal Cell Carcinoma Patients Previously Treated With Temsirolimus
- A Phase II Study of Axitinib in Patients With Metastatic Renal Cell Cancer Unsuitable for Nephrectomy
- A Randomized Phase II Clinical Trial on the Efficacy of Axitinib as a Monotherapy or in Combination With Lomustine for the Treatment of Patients With Recurrent Glioblastoma
- A Study Combining FOLFOX or FOLFIRI With AG-013736 or Bevacizumab (Avastin) in Patients With Metastatic Colorectal Cancer After Failure Of One First Line Regimen
- A Study In Patients With Advanced Solid Tumor
- A Study Of AG-013736 (Axitinib) Or Bevacizumab (Avastin) In Combination With Paclitaxel And Carboplatin In Patients With Advanced Lung Cancer.
- A Study of AGS-16C3F vs. Axitinib in Metastatic Renal Cell Carcinoma
- A Study of AK104 Monotherapy or AK104 Plus Axitinib in Advanced/Metastatic Renal Cell Carcinoma
- A Study of AK104 Plus Axitinib in Advanced/Metastatic Special Pathological Subtypes of Renal Cell Carcinoma
- A Study Of Avelumab In Combination With Axitinib In Advanced HCC (VEGF Liver 100)
- A Study Of Avelumab In Combination With Axitinib In Advanced Renal Cell Cancer (JAVELIN Renal 100)
- A Study of Avelumab in Combination With Axitinib In Non-Small Cell Lung Cancer (NSCLC) or Urothelial Cancer (Javelin Medley VEGF)
- A Study of Avelumab In Combination With Axitinib in Patients With Unresectable/Metastatic Gastrointestinal Stromal Tumor After Failure of Standard Therapy
- A Study of Avelumab With Axitinib Versus Sunitinib In Advanced Renal Cell Cancer (JAVELIN Renal 101)
- A Study of Axitinib in Advanced Carcinoid Tumors
Approved for (8)
- Cancer
- Clear cell renal carcinoma
- Collecting duct carcinoma
- Neoplasm
- Papillary renal cell carcinoma
- Renal carcinoma
- Renal cell adenocarcinoma
- Renal cell carcinoma
In development for (74)
- Acoustic neuroma Phase 2
- Acute myeloid leukemia Phase 2
- Adenocarcinoma Phase 2
- Adenoid cystic carcinoma Phase 2
- Adrenal cortex carcinoma Phase 2
- Adrenal gland pheochromocytoma Phase 2
- Age-related macular degeneration Phase 3
- Alveolar soft part sarcoma Phase 2
- Angiosarcoma Phase 2
- Basal cell carcinoma Phase 1
- Biliary tract neoplasm Phase 2
- Blast phase chronic myelogenous leukemia, BCR-ABL1 positive Phase 1
- Breast cancer Phase 1
- Breast neoplasm Phase 1
- Carcinoid tumor Phase 2
- Carcinoma Phase 1
- Chronic myeloid leukemia Phase 1
- Clear cell adenocarcinoma Phase 2
- Colorectal cancer Phase 2
- Colorectal carcinoma Phase 2