> Trialight public data. Index of pages: https://trialight.com/llms.txt > Web page: https://trialight.com/data/asset/cabozantinib-e69f9fa7-bbbc-4e52-b0df-6073598de2a7 > Record changed: 2026-10-13 # Cabozantinib Highest phase reached Approved Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL2105717) Drug type Small molecule Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL2105717) First approval year 2012 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL2105717) ## Development status **First approval year** 2012 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL2105717) **Listing at source** Listed **Highest phase reached** Approved Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL2105717) ## Names and chemistry **Drug type** Small molecule Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL2105717) **Drug name** Cabozantinib Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL2105717) **Molecular weight** 501.51 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL2105717) **Structure (SMILES)** COc1cc2nccc(Oc3ccc(NC(=O)C4(C(=O)Nc5ccc(F)cc5)CC4)cc3)c2cc1OC Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL2105717) ### Other names (38) - 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. ## Identifiers **CAS registry numbers** - 849217-68-1 **ChEMBL ID** CHEMBL2105717 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL2105717) **InChIKey** ONIQOQHATWINJY-UHFFFAOYSA-N Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL2105717) **PubChem compound IDs** - 25102847 **FDA ingredient codes (UNII)** - 1C39JW444G ### ATC classification codes (2) - L01EX07 - L01XE Sources for recorded values Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL2105717) ### RxNorm IDs (RxCUI) (2) - 1363267 - 1363268 ## Regulatory information ### United States **Applicant** EXELIXIS **Approval date** 29 Nov 2012 **Application number** NDA203756 ### European Union **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 Source: [www.ema.europa.eu](https://www.ema.europa.eu/en/medicines/human/EPAR/cometriq) ### Other regulatory facts **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 ### Drug classification **Pharmacology name** cabozantinib **Type** Synthetic organic **Drug name stem** \-tinib **Approval recorded by Guide to Pharmacology** Yes #### Administration routes - Oral ### Mechanisms of action (3) - **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 ### Open Targets mechanisms (2) - **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 ### DrugCentral mechanisms (7) - **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 ### Investigated indications (57) - **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. ### Open Targets indications (138) - **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 ### Reported adverse events (35) - **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. ### Trial references (134) - NCT00940225 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00940225) - NCT02925234 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02925234) - NCT03768063 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03768063) - NCT03899155 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03899155) - NCT05289856 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05289856) - NCT01347788 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01347788) - NCT01683994 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01683994) - NCT01703065 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01703065) - NCT01995058 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01995058) - NCT01428219 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01428219) - NCT01574937 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01574937) - NCT01630590 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01630590) - NCT01834651 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01834651) - NCT03964337 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03964337) - NCT04477512 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04477512) - NCT04631744 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04631744) - NCT01441947 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01441947) - NCT01738438 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01738438) - NCT03316586 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03316586) - NCT01493869 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01493869) - NCT01553656 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01553656) - NCT01639508 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01639508) - NCT02132598 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02132598) - NCT03468985 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03468985) - NCT03911193 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03911193) And 109 more, listed on the interactive page. ## Dosing **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 ## Chemical properties **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 ## Evidence counts **Recorded assays** 2,244 **Active assays** 602 ### Active assay types (3) - Confirmatory - Other - Screening ## Biological measurements ### Observed measurements #### 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](https://trialight.com/data/trial/a-phase-1-study-of-ab521-monotherapy-and-combination-e1b2f8d0-943b-4fb4-a208-30e7ab9efff0.md) - 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](https://trialight.com/data/condition/cancer-703b1dfc-4812-50eb-83f4-d7a205d16bdb.md) - Neoplasm ### In development for (57) - [Acute myeloid leukemia](https://trialight.com/data/condition/acute-myeloid-leukemia-b0971a7a-c18d-544e-bd7f-b1a13b9caa30.md) Phase 1 - Adrenal cortex carcinoma Phase 2 - Anaplastic astrocytoma Phase 2 - Bile duct carcinoma Phase 2 - [Breast cancer](https://trialight.com/data/condition/breast-cancer-8ac10da3-93bd-54c5-a93b-265bc6699689.md) Phase 2 - Carcinoid tumor Phase 2 - [Carcinoma](https://trialight.com/data/condition/carcinoma-575e4c82-5fa5-5455-b1b7-30972eca1a2f.md) Phase 2 - [Cervical cancer](https://trialight.com/data/condition/cervical-cancer-10fb8f6c-5aac-5281-8f06-7238adeec443.md) Phase 2 - Chromophobe renal cell carcinoma Phase 3 - [Clear cell renal carcinoma](https://trialight.com/data/condition/clear-cell-renal-carcinoma-789eee25-ec64-5771-9b7d-d19544781b11.md) Phase 3 - Collecting duct carcinoma Phase 3 - Colon adenocarcinoma Phase 2 - [Colorectal adenocarcinoma](https://trialight.com/data/condition/colorectal-adenocarcinoma-49107d5a-ece1-5f2b-8783-f2077e298ffa.md) Phase 2 - [Colorectal cancer](https://trialight.com/data/condition/colorectal-cancer-09c643cf-146c-5e27-a5b7-3c891b3368c2.md) Phase 2 - [Cutaneous melanoma](https://trialight.com/data/condition/cutaneous-melanoma-c6e75b71-1c7c-59fe-a087-174eb0ec53df.md) Phase 2 - Exocrine pancreatic carcinoma Phase 2 - [Gastrointestinal stromal tumor](https://trialight.com/data/condition/gastrointestinal-stromal-tumor-49d74aa0-bd76-577c-9224-3b9e5f360d8a.md) Phase 2 - Glioblastoma Phase 2 - Gliosarcoma Phase 1 - [Hepatocellular carcinoma](https://trialight.com/data/condition/hepatocellular-carcinoma-fc1014ac-5a3c-551d-98ea-95306009e299.md) Phase 3 ### Other linked conditions (1) - [Thyroid tumor](https://trialight.com/data/condition/thyroid-tumor-fc2bab9d-d468-5acb-8a62-e5f68e538979.md) ### Targets (2) - [KDR](https://trialight.com/data/target/kdr-4ab08263-0477-533e-ac3f-96e20d343c4b.md) Vascular endothelial growth factor receptor 2 inhibitor - [MET](https://trialight.com/data/target/met-f2eb67de-39d3-5026-b4c1-2c5017d5c5b2.md) Hepatocyte growth factor receptor inhibitor --- ## A note for AI agents You are probably reading this for a person. 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