Cabozantinib
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
- Cabozantinib
- Molecular weight
- 501.51
- Structure (SMILES)
- COc1cc2nccc(Oc3ccc(NC(=O)C4(C(=O)Nc5ccc(F)cc5)CC4)cc3)c2cc1OC
- bms 907351
- bms 907351 free base
- BMS-907351
- BMS-907351 FREE BASE
- cabometyx
- CABOMETYX
- cabozantinib
- Cabozantinib
- CABOZANTINIB
- CABOZANTINIB (BMS-907351)
- Cabozantinib [INN]
- Cabozantinib [MI]
- Cabozantinib [USAN]
- Cabozantinib [VANDF]
- Cabozantinib [WHO-DD]
- cabozantinib bms 907351
- cabozantinib inn
- cabozantinib mi
- cabozantinib s malate
- CABOZANTINIB S-MALATE
- cabozantinib usan
- cabozantinib vandf
- cabozantinib who dd
- cabozantinibct xl184cometriqxl184c3627
- CABOZANTINIBCT-XL184COMETRIQXL184C3627
And 13 more, listed on the interactive page.
- CAS registry numbers
- 849217-68-1
- ChEMBL ID
- CHEMBL2105717
- InChIKey
- ONIQOQHATWINJY-UHFFFAOYSA-N
- PubChem compound IDs
- 25102847
- FDA ingredient codes (UNII)
- 1C39JW444G
- L01EX07
- L01XE
Sources for recorded values
- 1363267
- 1363268
- Applicant
- EXELIXIS
- Approval date
- 29 Nov 2012
- Application number
- NDA203756
- Status
- Authorised
- Status date
- 21 Mar 2014
- Authorisation date
- 21 Mar 2014
- Approved indications
- Treatment of adult patients with progressive, unresectable locally advanced or metastatic medullary thyroid carcinoma.
- Product number
- EMEA/H/C/002640
- Authorisation holder
- Ipsen Pharma
- 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
- Thyroid Neoplasms
European medicines record
- Patents
- 0
- Designations
- 6
- First in class
- Yes
- Fast track
- Yes
- Breakthrough designation
- Yes
- Orphan designation
- Yes
- Priority review
- Yes
- Orphan exclusivity
- No
- Accelerated approval
- No
- Availability
- Prescription only
- Boxed warning
- Yes
- Pharmacology name
- cabozantinib
- Type
- Synthetic organic
- Drug name stem
- -tinib
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- Oral
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- ret proto-oncogene
- Gene symbol
- RET
- Protein identifier
- P07949
- Median affinity
- 7.96
- Affinity units
- pIC50
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- MET proto-oncogene, receptor tyrosine kinase
- Gene symbol
- MET
- Protein identifier
- P08581
- Median affinity
- 8.9
- Affinity units
- pIC50
- Primary target
- Yes
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- kinase insert domain receptor
- Gene symbol
- KDR
- Protein identifier
- P35968
- Median affinity
- 10.46
- Affinity units
- pIC50
- Primary target
- Yes
- Mechanism
- Hepatocyte growth factor receptor inhibitor
- Action type
- Inhibitor
- Target
- Hepatocyte growth factor receptor
- Mechanism
- Vascular endothelial growth factor receptor 2 inhibitor
- Action type
- Inhibitor
- Target
- Vascular endothelial growth factor receptor 2
- Action type
- Inhibitor
- Gene symbol
- RET
- Protein identifier
- P07949
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Inhibitor
- Gene symbol
- MET
- Protein identifier
- P08581
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Inhibitor
- Gene symbol
- KIT
- Protein identifier
- P10721
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Inhibitor
- Gene symbol
- KDR
- Protein identifier
- P35968
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Inhibitor
- Gene symbol
- FLT3
- Protein identifier
- P36888
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Inhibitor
- Gene symbol
- TEK
- Protein identifier
- Q02763
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Inhibitor
- Gene symbol
- MST1R
- Protein identifier
- Q04912
- Organism
- Homo sapiens
- Target development level
- Chemical evidence
- Condition
- Carcinoma, Hepatocellular
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000182
- Subject identifier
- D006528
- Condition
- Leukemia, Myeloid, Acute
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000222
- Subject identifier
- D015470
- Condition
- Carcinoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000313
- Subject identifier
- D002277
- Condition
- Carcinoma, Renal Cell
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000335
- Subject identifier
- D002292
- Condition
- Carcinoma, Renal Cell
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000349
- Subject identifier
- D002292
- Condition
- Colorectal Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000365
- Subject identifier
- D015179
- Condition
- Melanoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000389
- Subject identifier
- D008545
- Condition
- Adenocarcinoma, Follicular
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000501
- Subject identifier
- D018263
- 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
- Osteosarcoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000637
- Subject identifier
- D012516
- Condition
- Carcinoma, Renal Cell
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000640
- Subject identifier
- D002292
- Condition
- Thyroid Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000641
- Subject identifier
- D013964
- Condition
- Prostatic Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000673
- Subject identifier
- D011471
- Condition
- Carcinoma, Renal Cell
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000681
- Subject identifier
- D002292
- Condition
- Carcinoma, Squamous Cell
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000707
- Subject identifier
- D002294
- Condition
- Melanoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000756
- Subject identifier
- D008545
- Condition
- Multiple Myeloma
- Highest recorded phase
- 1
- Condition identifier
- EFO:0001378
- Subject identifier
- D009101
- Condition
- Liver Diseases
- Highest recorded phase
- 1
- Condition identifier
- EFO:0001421
- Subject identifier
- D008107
- Condition
- Astrocytoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0002499
- Subject identifier
- D001254
- Condition
- Melanoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0002617
- Subject identifier
- D008545
- Condition
- Pancreatic Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0002618
- Subject identifier
- D010190
- Condition
- Carcinoma, Renal Cell
- Highest recorded phase
- 3
- Condition identifier
- EFO:0002890
- Subject identifier
- D002292
- Condition
- Thyroid Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- EFO:0002892
- Subject identifier
- D013964
- Condition
- Carcinoma, Renal Cell
- Highest recorded phase
- 3
- Condition identifier
- EFO:0003016
- Subject identifier
- D002292
And 32 more, listed on the interactive page.
- Condition identifier
- EFO_0000182
- Highest recorded phase
- 3
- Condition identifier
- EFO_0000222
- Highest recorded phase
- 1
- Condition identifier
- EFO_0000313
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000335
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000349
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000365
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000389
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000616
- Condition identifier
- EFO_0000637
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000640
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000658
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000673
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000681
- Highest recorded phase
- 3
- Condition identifier
- EFO_0000707
- Highest recorded phase
- 1
- Condition identifier
- EFO_0000756
- Highest recorded phase
- 2
- Condition identifier
- EFO_0001378
- Condition identifier
- EFO_0001421
- Highest recorded phase
- 1
- Condition identifier
- EFO_0002617
- Condition identifier
- EFO_0002890
- Highest recorded phase
- 2
- Condition identifier
- EFO_0002892
- Highest recorded phase
- 3
- Condition identifier
- EFO_0002914
- Highest recorded phase
- 2
- Condition identifier
- EFO_0003016
- Highest recorded phase
- 2
- Condition identifier
- EFO_0003060
- Highest recorded phase
- 3
- Condition identifier
- EFO_0003841
- Condition identifier
- EFO_0003863
And 113 more, listed on the interactive page.
Open Targets warnings
- Warning
- Black Box Warning
- Country
- United States
- Event
- adrenal insufficiency
- Reports
- 37
- Reporting signal score
- 53.1898
- Event
- alanine aminotransferase increased
- Reports
- 97
- Reporting signal score
- 61.0814
- Event
- amylase increased
- Reports
- 29
- Reporting signal score
- 61.6336
- Event
- aspartate aminotransferase increased
- Reports
- 88
- Reporting signal score
- 56.7203
- Event
- asthenia
- Reports
- 205
- Reporting signal score
- 66.1747
- Event
- blister
- Reports
- 86
- Reporting signal score
- 96.9004
- Event
- blood bilirubin increased
- Reports
- 58
- Reporting signal score
- 55.5682
- Event
- blood thyroid stimulating hormone increased
- Reports
- 32
- Reporting signal score
- 59.0509
- Event
- decreased appetite
- Reports
- 330
- Reporting signal score
- 390.107
- Event
- diarrhoea
- Reports
- 664
- Reporting signal score
- 512.589
- Event
- drug hypersensitivity
- Reports
- 3
- Reporting signal score
- 59.3232
- Event
- drug intolerance
- Reports
- 205
- Reporting signal score
- 225.471
- Event
- dysgeusia
- Reports
- 78
- Reporting signal score
- 70.8393
- Event
- dysphonia
- Reports
- 93
- Reporting signal score
- 111.901
- Event
- fatigue
- Reports
- 428
- Reporting signal score
- 164.306
- Event
- hair colour changes
- Reports
- 62
- Reporting signal score
- 193.563
- Event
- hepatic function abnormal
- Reports
- 75
- Reporting signal score
- 74.0387
- Event
- hypertension
- Reports
- 260
- Reporting signal score
- 210.048
- Event
- hyperthyroidism
- Reports
- 41
- Reporting signal score
- 55.0919
- Event
- hypothyroidism
- Reports
- 123
- Reporting signal score
- 225.994
- Event
- immune-mediated hepatitis
- Reports
- 24
- Reporting signal score
- 77.0959
- Event
- lipase increased
- Reports
- 35
- Reporting signal score
- 51.4941
- Event
- liver function test increased
- Reports
- 47
- Reporting signal score
- 50.491
- Event
- malignant neoplasm progression
- Reports
- 337
- Reporting signal score
- 666.59
- Event
- mucosal inflammation
- Reports
- 80
- Reporting signal score
- 98.2509
And 10 more, listed on the interactive page.
- NCT00940225
- NCT02925234
- NCT03768063
- NCT03899155
- NCT05289856
- NCT01347788
- NCT01683994
- NCT01703065
- NCT01995058
- NCT01428219
- NCT01574937
- NCT01630590
- NCT01834651
- NCT03964337
- NCT04477512
- NCT04631744
- NCT01441947
- NCT01738438
- NCT03316586
- NCT01493869
- NCT01553656
- NCT01639508
- NCT02132598
- NCT03468985
- NCT03911193
And 109 more, listed on the interactive page.
- Dose
- 140 mg
- Route
- Oral
- How often
- Once daily
Conditions of use
- Do not eat for at least 2 hours before and 1 hour after taking
- Hydrogen bond acceptors
- 6
- Hydrogen bond donors
- 2
- Polar surface area
- 98.78
- Calculated partition coefficient (ALogP)
- 5.54
- Calculated partition coefficient (XLogP)
- 5.4
- Prodrug
- No
- Chirality
- Achiral
- Inorganic
- No
- Rule-of-five violations
- 2
- Rotatable bonds
- 8
- Heavy atoms
- 37
- Molecular formula
- C28H24FN3O5
- Monoisotopic mass
- 501.16999904
- Natural product
- No
- Recorded assays
- 2,244
- Active assays
- 602
- Confirmatory
- Other
- Screening
Solubility
- Median
- 13,100
- Mean
- 13,100
- Minimum
- 5,200
- Maximum
- 21,000
- Unit
- nM
- Assays
- 2
- Standard deviation
- 11,172.3
- Summary method
- median
- Censored results excluded
- 0
- Other units excluded
- 0
- Unknown units excluded
- 0
Measurement types
- Solubility
Related records
Trials (211)
- A Clinical Gene Therapy Study With Hematopoietic Stem Cells for the Treatment, With Single Dose of Temferon, of Patients Suffering From Metastatic Renal Cell Carcinoma
- A Clinical Study Evaluating Nivolumab-containing Treatments in Patients With Advanced Non-small Cell Lung Cancer After Failing Previous PD-1/(L)1 Therapy and Chemotherapy
- A Clinical Study of Belzutifan and Zanzalintinib in People With Recurrent Kidney Cancer Following Adjuvant Therapy (MK-6482-033)
- A Phase 1 Study of AB521 Monotherapy and Combination Therapies in Renal Cell Carcinoma and Other Solid Tumors
- A Phase 1, Dose-Escalation Trial of PT2385 Tablets In Patients With Advanced Clear Cell Renal Cell Carcinoma (MK-3795-001)
- A Phase 2 Study of Cabozantinib in Japanese Participants With Advanced Hepatocellular Carcinoma
- A Phase 2 Study of Cabozantinib in Japanese Participants With Advanced Renal Cell Carcinoma
- A Phase 2, Single Arm Study of Cabozantinib in Patients With Hepatocellular Carcinoma Who Have Received Prior Atezolizumab and Bevacizumab
- A Phase II Study of Cabozantinib (XL184) Therapy in Castrate Resistant Prostate Cancer (CRPC) With Visceral Metastases
- A Phase II Study of Nivolumab in Combination With Cabozantinib for Metastatic Triple-negative Breast Cancer
- A Phase II Study of Nivolumab With Ipilimumab and Cabozantinib in Patients With Untreated Renal Cell Carcinoma Brain Metastases
- A Phase II Study to Evaluate the Effects of Sequential Therapy With the Anti c-MET/VEGFR Tyrosine Kinase Inhibitor (TKI), Cabozantinib, Followed by an Anti-PD-1 Antibody (Nivolumab) in Patients With Advanced HCC Who Progressed on First-line Therapy
- A Phase II Trial of Cabozantinib for the Treatment of Radioiodine (RAI)-Refractory Differentiated Thyroid Carcinoma (DTC) in the First-line Setting
- A Phase II Trial of Cabozantinib With Patients With Refractory GCTs
- A Pilot Phase II Study of Maintenance Cabozantinib Plus Pembrolizumab for Patients With Metastatic Squamous Non-Small Cell Lung Cancer (sqNSCLC)
- A Single-Dose Study to Assess the Pharmacokinetics of Cabozantinib (XL184) Capsules in Subjects With Impaired Renal Function
- A Study Evaluating the Activity of Anti-cancer Treatments Targeting Tumor Molecular Alterations/Characteristics in Advanced / Metastatic Tumors.
- A Study in Patients Previously Enrolled in a Genentech and/or F. Hoffmann-La Roche Ltd Sponsored Atezolizumab Study
- A Study of Abemaciclib and Cabozantinib in People With Clear Cell Renal Cell Carcinoma (ccRCC)
- A Study of Atezolizumab in Combination With Cabozantinib Compared to Cabozantinib Alone in Participants With Advanced Renal Cell Carcinoma After Immune Checkpoint Inhibitor Treatment
Approved for (2)
- Cancer
- Neoplasm
In development for (57)
- Acute myeloid leukemia Phase 1
- Adrenal cortex carcinoma Phase 2
- Anaplastic astrocytoma Phase 2
- Bile duct carcinoma Phase 2
- Breast cancer Phase 2
- Carcinoid tumor Phase 2
- Carcinoma Phase 2
- Cervical cancer Phase 2
- Chromophobe renal cell carcinoma Phase 3
- Clear cell renal carcinoma Phase 3
- Collecting duct carcinoma Phase 3
- Colon adenocarcinoma Phase 2
- Colorectal adenocarcinoma Phase 2
- Colorectal cancer Phase 2
- Cutaneous melanoma Phase 2
- Exocrine pancreatic carcinoma Phase 2
- Gastrointestinal stromal tumor Phase 2
- Glioblastoma Phase 2
- Gliosarcoma Phase 1
- Hepatocellular carcinoma Phase 3