cabozantinib
Trade name: cometriq
Small moleculeapprovedOrphan Drug FDAFast Track FDA
Approved
Nov 29, 2012
Cabozantinib (development code name XL184; marketed under the trade name Cometriq) is an orally bioavailable, small molecule receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic activity. Cabozantinib strongly binds to and inhibits several RTKs, which are often overexpressed in a variety of cancer cell types, including hepatocyte growth factor receptor (MET), RET (rearranged during transfection), vascular endothelial growth factor receptor types 1 (VEGFR-1), 2 (VEGFR-2), and 3 (VEGFR-3), mast/stem cell growth factor (KIT), FMS-like tyrosine kinase 3 (FLT-3), TIE-2 (TEK tyrosine kinase, endothelial), tropomyosin-related kinase B (TRKB) and AXL. This may result in an inhibition of both tumor growth and angiogenesis, and eventually lead to tumor regression. Cabozantinib was granted orphan drug status by the U.S. Food and Drug Administration (FDA) in January 2011. It is currently undergoing clinical trials for the treatment of prostate, bladder, ovarian, brain, melanoma, breast, non-small cell lung, pancreatic, hepatocellular and kidney cancers. — NCATS
Clinical trial activity
247 trials · 166 clinical orgs · 5 marketing orgs
Phase 1
63
Phase 2
190
Phase 3
25
Phase 4
6
Earliest trial started Sep 1, 2005 (NCT00215605)
Timeline
2000s
2010s
2020s
- Oct 27, 2022
Teva — Marketing Organization
- Jul 21, 2025
MSN Laboratories — Marketing Organization
- Oct 24, 2025
Azurity — Marketing Organization
- Mar 17, 2026
Biocon Limited — Marketing Organization
Indications
Studied for
- Adenocarcinoma · Phase 2
- Adrenal Cortex Neoplasms · Phase 2
- Adrenal Gland Neoplasms · Phase 2
- Adrenocortical Carcinoma · Phase 2
- Anemia · Phase 1
- Astrocytoma · Phase 2
- Bile Duct Neoplasms · Phase 2
- Brain Neoplasms · Phase 2
- Breast Neoplasms · Phase 2
- Carcinoid Tumor · Phase 3
- Carcinoma · Phase 3
- Carcinoma, Hepatocellular · Phase 4
- Carcinoma, Merkel Cell · Phase 2
- Carcinoma, Neuroendocrine · Phase 2
- Carcinoma, Non-Small-Cell Lung · Phase 3
- Carcinoma, Renal Cell · Phase 3
- Carcinoma, Squamous Cell · Phase 2
- Carcinoma, Transitional Cell · Phase 3
- Carcinosarcoma · Phase 2
- Central Nervous System Neoplasms · Phase 2
- Cholangiocarcinoma · Phase 2
- Chondrosarcoma · Phase 2
- Cognitive Aging · Phase 2
- Colonic Neoplasms · Phase 2
- Colorectal Neoplasms · Phase 2
- Endometrial Neoplasms · Phase 2
- Esophageal Neoplasms · Phase 2
- Fallopian Tube Neoplasms · Phase 2
- Gallbladder Neoplasms · Phase 2
- Genes, ras · Phase 1
- Genital Neoplasms, Female · Phase 1/Phase 2
- Glioblastoma · Phase 2
- Glioma · Phase 2
- Gliosarcoma · Phase 1/Phase 2
- Hamartoma · Phase 2
- Head and Neck Neoplasms · Phase 2
- Healthy Volunteers · Phase 1
- Hepatoblastoma · Phase 2
- HIV Infections · Phase 1
- Hodgkin Disease · Phase 1
- Hypopharyngeal Neoplasms · Phase 2
- Intestinal Neoplasms · Phase 2
- Kidney · Phase 2
- Kidney Diseases · Phase 3
- Kidney Failure, Chronic · Phase 1
- Kidney Neoplasms · Phase 4
- Laryngeal Neoplasms · Phase 2
- Leiomyosarcoma · Phase 2
- Leukemia, Lymphocytic, Chronic, B-Cell · Phase 1
- Leukemia, Myelogenous, Chronic, BCR-ABL Positive · Phase 1
- Leukemia, Myeloid, Acute · Phase 1
- Leukemia, Myeloid, Chronic, Atypical, BCR-ABL Negative · Phase 1
- Leukemia, Myeloid, Chronic-Phase · Phase 1
- Leukemia, Myelomonocytic, Chronic · Phase 1
- Liposarcoma · Phase 2
- Liver Cirrhosis · Phase 2
- Liver Diseases · Phase 1
- Liver Neoplasms · Phase 2
- Liver Transplantation · Phase 2
- Lung Neoplasms · Phase 3
- Lymphoma · Phase 1
- Lymphoma, Large-Cell, Immunoblastic · Phase 2
- Lymphoma, Non-Hodgkin · Phase 1
- Lymphoma, Primary Cutaneous Anaplastic Large Cell · Phase 1
- Melanoma · Phase 2
- Meningioma · Phase 2
- Mesothelioma · Phase 1
- Mesothelioma, Malignant · Phase 1
- Mouth Neoplasms · Phase 2
- Multiple Myeloma · Phase 1/Phase 2
- Myelodysplastic Syndromes · Phase 1
- Myeloproliferative Disorders · Phase 1
- Nasopharyngeal Carcinoma · Phase 2
- Neoplasm Metastasis · Phase 3
- Neoplasms, Germ Cell and Embryonal · Phase 2
- Neuroblastoma · Phase 2
- Neuroendocrine Tumors · Phase 3
- Neurofibroma · Phase 2
- Neurofibroma, Plexiform · Phase 2
- Neurofibromatoses · Phase 2
- Neurofibromatosis 1 · Phase 1
- Oropharyngeal Neoplasms · Phase 2
- Osteosarcoma · Phase 2/Phase 3
- Ovarian Neoplasms · Phase 2
- Pain · Phase 3
- Pancreatic Neoplasms · Phase 3
- Paraganglioma · Phase 2
- Penile Neoplasms · Phase 2
- Pheochromocytoma · Phase 2
- Precursor B-Cell Lymphoblastic Leukemia-Lymphoma · Phase 1
- Primary Myelofibrosis · Phase 1
- Prostatic Neoplasms · Phase 3
- Prostatic Neoplasms, Castration-Resistant · Phase 3
- Rectal Neoplasms · Phase 2
- Rhabdomyosarcoma · Phase 2
- Salivary Gland Neoplasms · Phase 2
- Sarcoma · Phase 2
- Sarcoma, Alveolar Soft Part · Phase 2
- Sarcoma, Clear Cell · Phase 2
- Sarcoma, Ewing · Phase 2
- Sarcoma, Kaposi · Phase 1
- Seminoma · Phase 2
- Skin Neoplasms · Phase 2
- Small Cell Lung Carcinoma · Phase 1
- Soft Tissue Neoplasms · Phase 2
- Squamous Cell Carcinoma of Head and Neck · Phase 2
- Stomach Neoplasms · Phase 2
- Testicular Neoplasms · Phase 2
- Thymoma · Phase 3
- Thymus Neoplasms · Phase 3
- Thyroid Cancer, Papillary · Phase 2
- Thyroid Carcinoma, Anaplastic · Phase 2
- Triple Negative Breast Neoplasms · Phase 1/Phase 2
- Ureteral Neoplasms · Phase 3
- Urethral Neoplasms · Phase 3
- Urinary Bladder Neoplasms · Phase 3
- Uterine Cervical Neoplasms · Phase 2
- Uterine Neoplasms · Phase 2
- Vulvar Neoplasms · Phase 2
- Wilms Tumor · Phase 2
Mechanism of action
KDR inhibitor
Multi-kinase inhibitor; Cabozantinib (XL184) is a potent inhibitor of MET and VEGFR2 that also inhibits RET, KIT, AXL, and FLT3, all of which have been implicated in tumor pathogenesis (PMID: 21926191)
- Hepatocyte growth factor receptorINHIBITOR
MET inhibitor
Multi-kinase inhibitor; Cabozantinib (XL184) is a potent inhibitor of MET and VEGFR2 that also inhibits RET, KIT, AXL, and FLT3, all of which have been implicated in tumor pathogenesis (PMID: 21926191)
Approval history
- approvedPriority reviewFast trackNov 29, 2012
Chemistry & pharmacology
Loading structure…
SMILES
COc1cc2nccc(Oc3ccc(NC(=O)C4(C(=O)Nc5ccc(F)cc5)CC4)cc3)c2cc1OC- Mol. weight
- 501.51 g/mol
- Lipinski Ro5
- 2 violation(s)
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
- Availability
- Prescription Only
Oral
Yes
Parenteral
No
Topical
No
Black box warningFirst in class
Sources
- ChEMBLCHEMBL2105717 ↗
- WikipediaCabozantinib ↗
- NCATSDR7ST46X58 ↗
- ChEMBLCHEMBL2103868 ↗
Also known as
- bms907351
- bms 907351
- bms-907351
- bms-907351
- bms-907351
- bms-907351
- cabometyx
- cabometyx
- cabometyx
- cabozantinib
- cabozantinib
- cabozantinib
- cabozantinib
- cabozantinib
- cabozantinib
- cabozantinib
- cabozantinib
- cabozantinib
- cabozantinib
- cabozantinib (s)-malate
- cabozantinib (s)-malate
- cabozantinib (s)-malate
- cabozantinib (s)-malate
- cabozantinib (s)-malate
- cabozantinib s-malate
- cabozantinib s-malate
- cabozantinib s-malate
- cabozantinib s-malate
- cabozantinib s-malate
- cabozantinib s-malate
- cometriq
- cometriq
- cometriq
- cometriq
- cometriq
- cometriq
- lu 177
- xl184
- xl184
- xl184
- xl 184
- xl-184
- xl-184
- xl-184
- xl-184
- xl184 cpd
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT06900595 | Phase 2 | Jul 19, 2026 | National Cancer Institute (NCI) |
| NCT07187869 | Phase 1 | Mar 31, 2026 | Exelixis, University of Texas at Houston |
| NCT07293351 | Phase 1/Phase 2 (Phase 2) | Mar 26, 2026 | Biontech, Bristol-Myers Squibb |
| NCT07169825 | N/A | Feb 13, 2026 | General Electric, University of Texas at Houston |
| NCT07227402 | Phase 3 | Dec 29, 2025 | Exelixis, Merck |
| NCT07194044 | Phase 1 | Oct 31, 2025 | National Pediatric Cancer Foundation, University of South Florida |
| NCT07028125 | Phase 4 | Oct 1, 2025 | University of Caen-Normandie |
| NCT07151326 | Phase 2 | Sep 30, 2025 | Chang Gung University, China Medical University, Government of Taiwan, Mackay Medical College, National Cheng Kung University, National Taiwan University, Taichung Veterans General Hospital, Taipei Veteran General hospital, Taiwan Cooperative Oncology Group |
| NCT07011719 | Phase 3 | Sep 8, 2025 | Arcus Biosciences, Inc. |
| NCT07077161 | Phase 2 | Sep 1, 2025 | Leiden University |
| NCT07010393 | Phase 4 | Jul 1, 2025 | Fujian Medical University |
| NCT06811116 | Phase 1/Phase 2 (Phase 2) | May 16, 2025 | National Cancer Institute (NCI), University of Pittsburgh |
| NCT06934057 | Phase 4 | May 16, 2025 | Institut Gustave Roussy, Ipsen |
| NCT06835972 | Phase 1/Phase 2 (Phase 2) | Feb 14, 2025 | Eli Lilly, Exelixis, Memorial Sloan-Kettering Cancer Center |
| NCT06502171 | Phase 1 | Jan 1, 2025 | Department of Defense, Indiana University, University of Alabama, Birmingham, University of Pennsylvania |
| NCT06341712 | Phase 2 | Oct 31, 2024 | Ipsen |
| NCT06716853 | Phase 1/Phase 2 (Phase 2) | Oct 22, 2024 | Alira Health, Arithmos srl, Genenta Science S.R.L., Vita-Salute University of Milano. Italy |
| NCT06726421 | Phase 3 | Sep 18, 2024 | Sun Yat-Sen University |
| NCT06475989 | Phase 3 | Sep 13, 2024 | ECOG-ACRIN Cancer Research Group, National Cancer Institute (NCI) |
| NCT06535737 | Phase 2 | Aug 31, 2024 | Chulalongkorn University, Mahidol University |
Showing 20 of 247 trials
Page 1 / 13
Organizations
Research & Development (166)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Exelixis | For profit | 86 | 23 | 5 | 2005 |
| National Cancer Institute (NCI) | Government | 50 | 39 | 4 | 2012 |
| Bristol-Myers Squibb | For profit | 16 | 4 | 3 | 2010 |
| Harvard University | Academic/Hospital | 16 | 15 | 2 | 2011 |
| University of Texas at Houston | Academic/Hospital | 16 | 15 | 3 | 2014 |
| Ipsen | For profit | 14 | 2 | 2 | 2018 |
| Merck | For profit | 6 | 2 | 2 | 2017 |
| Roche | For profit | 6 | 3 | 2 | 2020 |
| University of Milan | Academic/Hospital | 6 | 5 | 2 | 2018 |
| Emory University | Academic/Hospital | 4 | 4 | 2 | 2018 |
| Genentech | For profit | 4 | 0 | 1 | 2014 |
| Indiana University | Academic/Hospital | 4 | 3 | 2 | 2017 |
| Memorial Sloan-Kettering Cancer Center | Academic/Hospital | 4 | 4 | 2 | 2018 |
| University of Alabama, Birmingham | Academic/Hospital | 4 | 4 | 2 | 2014 |
| University of Utah | Academic/Hospital | 4 | 4 | 2 | 2018 |
| Apices Soluciones S.L. | For profit | 3 | 0 | 1 | 2018 |
| Chao Family Comprehensive Cancer Center | Academic/Hospital | 3 | 0 | 2 | 2019 |
| City of Hope National Medical Center | Academic/Hospital | 3 | 2 | 2 | 2013 |
| Cornell University | Academic/Hospital | 3 | 3 | 1 | 2012 |
| ECOG-ACRIN Cancer Research Group | Academic/Hospital | 3 | 1 | 2 | 2018 |
166 organizations
Page 1 / 9
Marketing (7)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Azurity | For profit | MKTG | Oct 24, 2025 |
| Biocon Limited | For profit | MKTG | Mar 17, 2026 |
| Exelixis | For profit | SYN | Nov 29, 2012 |
| Exelixis | For profit | SYN | Apr 25, 2016 |
| Exelixis | For profit | NDA | Nov 29, 2012 |
| MSN Laboratories | For profit | MKTG | Jul 21, 2025 |
| Teva | For profit | MKTG | Oct 27, 2022 |