axitinib
Trade name: inlyta
Small moleculeapprovedFast Track FDA
Approved
Jan 27, 2012
Axitinib (trade name Inlyta) is a small molecule tyrosine kinase inhibitor developed by Pfizer. It has been shown to significantly inhibit growth of breast cancer in animal (xenograft) models and has shown partial responses in clinical trials with renal cell carcinoma (RCC) and several other tumour types. Axitinib has been shown to inhibit receptor tyrosine kinases including vascular endothelial growth factor receptors (VEGFR)-1, VEGFR-2, and VEGFR-3 at therapeutic plasma concentrations. These receptors are implicated in pathologic angiogenesis, tumor growth, and cancer progression. VEGF-mediated endothelial cell proliferation and survival were inhibited by axitinib in vitro and in mouse models. It was approved by the U.S. Food and Drug Administration. — NCATS
Clinical trial activity
180 trials · 156 clinical orgs · 4 marketing orgs
Phase 1
52
Phase 2
138
Phase 3
15
Phase 4
1
Earliest trial started Nov 1, 2002 (NCT01469052)
Timeline
Indications
Approved for
Studied for
- Adenocarcinoma · Phase 2
- Adrenal Cortex Neoplasms · Phase 2
- Antineoplastic Agents · Phase 2
- Biliary Tract Neoplasms · Phase 2
- Breast Neoplasms · Phase 1/Phase 2
- Carcinoid Tumor · Phase 2
- Carcinoma · Phase 2
- Carcinoma, Adenoid Cystic · Phase 2
- Carcinoma, Hepatocellular · Phase 2
- Carcinoma, Non-Small-Cell Lung · Phase 3
- Carcinoma, Pancreatic Ductal · Phase 3
- Carcinoma, Transitional Cell · Phase 3
- Colorectal Neoplasms · Phase 2
- Diabetic Retinopathy · Phase 3
- Drugs, Investigational · Phase 2
- Endometrial Neoplasms · Phase 2
- Endometriosis · Phase 1/Phase 2
- Ependymoma · Phase 1/Phase 2
- Female Urogenital Diseases · Phase 2
- Gastrointestinal Stromal Tumors · Phase 2
- Genes, erbB-2 · Phase 1
- Glioblastoma · Phase 2
- Glioma · Phase 2
- Gliosarcoma · Phase 1
- Healthy Volunteers · Phase 1
- Hepatic Insufficiency · Phase 1
- Immune Checkpoint Inhibitors · Phase 2
- Immunotherapy · Phase 2
- Kidney Diseases · Phase 2
- Kidney Neoplasms · Phase 3
- Leukemia, Myelogenous, Chronic, BCR-ABL Positive · Phase 1/Phase 2
- Leukemia, Myeloid, Acute · Phase 2
- Leukemia, Myeloid, Chronic-Phase · Phase 1/Phase 2
- Liver Neoplasms · Phase 2
- Lung Neoplasms · Phase 2
- Lymphoma · Phase 3
- Lymphoma, Non-Hodgkin · Phase 2
- Macular Degeneration · Phase 3
- Male Urogenital Diseases · Phase 2
- Medulloblastoma · Phase 1/Phase 2
- Melanoma · Phase 3
- Mesothelioma, Malignant · Phase 1/Phase 2
- Multiple Myeloma · Phase 2
- Mutation · Phase 1
- Myelodysplastic Syndromes · Phase 2
- Neoadjuvant Therapy · Phase 2
- Neoplasm Metastasis · Phase 2
- Nephrectomy · Phase 2
- Neuroendocrine Tumors · Phase 2
- Neurofibromatosis 2 · Phase 2
- Neuroma, Acoustic · Phase 2
- Ovarian Neoplasms · Phase 3
- Pancreatic Neoplasms · Phase 2
- Paraganglioma · Phase 2
- Pheochromocytoma · Phase 2
- Prostatic Neoplasms · Phase 2
- Prostatic Neoplasms, Castration-Resistant · Phase 1
- Radiotherapy · Phase 2
- Salivary Gland Neoplasms · Phase 2
- Sarcoma · Phase 2
- Sarcoma, Alveolar Soft Part · Phase 2
- Sarcoma, Clear Cell · Phase 2
- Skin Neoplasms · Phase 2
- Solitary Fibrous Tumors · Phase 2
- Squamous Cell Carcinoma of Head and Neck · Phase 2
- Stomach Neoplasms · Phase 1
- Thrombosis · Phase 2
- Thyroid Neoplasms · Phase 2
- Urogenital Diseases · Phase 2
- Urogenital Neoplasms · Phase 2
- Urologic Diseases · Phase 2
- Urologic Neoplasms · Phase 2
- Wet Macular Degeneration · Phase 1
Mechanism of action
Vascular endothelial growth factor receptor inhibitor
Approval history
- approvedFast trackJan 27, 2012
Chemistry & pharmacology
Loading structure…
SMILES
CNC(=O)C1=CC=CC=C1SC2=CC3=C(C=C2)C(\C=C\C4=CC=CC=N4)=NN3- Mol. weight
- 386.47 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
- Availability
- Prescription Only
Oral
Yes
Parenteral
No
Topical
No
Sources
- WikipediaAxitinib ↗
- NCATSC9LVQ0YUXG ↗
- ChEMBLCHEMBL1289926 ↗
Also known as
- ag013736
- ag013736
- ag013736
- ag 013736
- ag 013736
- ag-013736
- ag-013736
- ag-013736
- ag-013736
- ag-013736
- ag-103736
- ag-13736
- ag-13736
- ag 6013736
- axitinib
- axitinib
- axitinib
- axitinib
- axitinib
- axitinib
- axitinib
- axitinib
- axitinib
- axitinib
- axitinib
- axitinib
- axitinibum
- axitinibum
- inlyta
- inlyta
- inlyta
- inlyta
- inlyta
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT07123090 | Phase 2 | Feb 28, 2026 | Harvard University, Pfizer |
| NCT07277972 | Phase 2 | Feb 15, 2026 | Tianjin Medical University |
| NCT07235085 | Phase 3 | Nov 17, 2025 | Ocular Therapeutix, Inc. |
| NCT07159191 | Phase 2 | Sep 1, 2025 | Chinese Academy of Medical Sciences |
| NCT07172386 | Phase 2 | Jul 31, 2025 | Tianjin Medical University |
| NCT06962787 | Phase 2 | Jul 28, 2025 | Baili Pharmaceutical Group |
| NCT06969001 | Phase 1 | May 29, 2025 | SCAI Therapeutics |
| NCT06860386 | Phase 2 | Feb 25, 2025 | University of South Florida |
| NCT06485908 | Phase 1/Phase 2 (Phase 2) | Oct 31, 2024 | Aix-University of Marseille |
| NCT06726421 | Phase 3 | Sep 18, 2024 | Sun Yat-Sen University |
| NCT06690697 | Phase 2 | Jun 1, 2024 | Fudan University |
| NCT06364631 | Phase 3 | Apr 12, 2024 | European Commission, Institut Gustave Roussy, Medical University of Vienna, National Cancer Institute, France, Netherlands Cancer Institute, Spanish National Health System, Universidad Complutense de Madrid, University of Duisburg-Essen, University of London, University of Milan, University of Rennes |
| NCT06279403 | Phase 2 | Mar 1, 2024 | Jiao Tong University |
| NCT06211114 | Phase 2 | Feb 29, 2024 | Peking University |
| NCT06223958 | Phase 3 | Jan 29, 2024 | California Retina Consultants, Duke University, Fortrea, Ocular Therapeutix, Inc. |
| NCT06161558 | Phase 1 | Jan 3, 2024 | National Cancer Institute (NCI) |
| NCT05949632 | Phase 1/Phase 2 (Phase 2) | Dec 15, 2023 | Incyte |
| NCT05969496 | Phase 2 | Dec 14, 2023 | Cancer League of Colorado, Inc, University of Colorado, Denver |
| NCT05769153 | Phase 1/Phase 2 (Phase 2) | Dec 6, 2023 | Aerie Pharmaceuticals, Alcon |
| NCT05808608 | Phase 1/Phase 2 (Phase 2) | Sep 30, 2023 | Sichuan University |
Showing 20 of 180 trials
Page 1 / 9
Organizations
Research & Development (156)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Pfizer | For profit | 84 | 41 | 4 | 2002 |
| National Cancer Institute (NCI) | Government | 10 | 5 | 2 | 2010 |
| Merck | For profit | 7 | 2 | 3 | 2014 |
| Chinese Academy of Medical Sciences | Academic/Hospital | 6 | 5 | 4 | 2019 |
| University of Texas at Houston | Academic/Hospital | 6 | 6 | 2 | 2011 |
| Sun Yat-Sen University | Academic/Hospital | 5 | 3 | 3 | 2020 |
| Bristol-Myers Squibb | For profit | 4 | 1 | 1 | 2016 |
| Fudan University | Academic/Hospital | 4 | 1 | 3 | 2022 |
| National Comprehensive Cancer Network | Academic/Hospital | 4 | 0 | 1 | 2011 |
| Tianjin Medical University | Academic/Hospital | 4 | 4 | 1 | 2021 |
| AstraZeneca | For profit | 3 | 0 | 2 | 2016 |
| Chinese University of Hong Kong | Academic/Hospital | 3 | 3 | 1 | 2010 |
| Jiao Tong University | Academic/Hospital | 3 | 3 | 2 | 2020 |
| Nanjing University | Academic/Hospital | 3 | 2 | 2 | 2021 |
| Netherlands Cancer Institute | Academic/Hospital | 3 | 2 | 2 | 2009 |
| Ocular Therapeutix, Inc. | For profit | 3 | 3 | 2 | 2021 |
| Peking University | Academic/Hospital | 3 | 2 | 2 | 2019 |
| Roche | For profit | 3 | 1 | 1 | 2017 |
| Sichuan University | Academic/Hospital | 3 | 2 | 2 | 2020 |
| Universidad Complutense de Madrid | Academic/Hospital | 3 | 0 | 2 | 2011 |
156 organizations
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