fostamatinib
Small moleculeapprovedOrphan Drug FDA
Approved
Apr 17, 2018
Fostamatinib is a pro-drug of a Syk inhibitor R406 initially developed by Rigel Pharmaceuticals, but then in-licensed by AstraZeneca. It reached phase III of clinical trials for such diseases as Rheumatoid Arthritis and Immune Thrombocytopenic Purpura, however, AstraZeneca decided not to proceed with regulatory filings and return the rights to the compound to Rigel Pharmaceuticals. In 2018 the drug was approved by the FDA for treatment of chronic immune thrombocytopenia. Fostamatinib is being developed for Autoimmune Hemolytic Anemia (phase II), graft versus host disease (phase I) and ovarian cancer (phase I). — NCATS
Clinical trial activity
63 trials · 26 clinical orgs · 1 marketing orgs
Phase 1
26
Phase 2
37
Phase 3
13
Phase 4
0
Earliest trial started Aug 1, 2006 (NCT00326339)
Timeline
2000s
- Jan 1, 2006
Rigel Pharmaceuticals — Earliest Phase 2 Sponsor(trial)
- Jan 1, 2007
Rigel Pharmaceuticals — Earliest Phase 1 Sponsor(trial)
2010s
- Jan 1, 2010
Earliest Phase 3 Sponsor(trial)
- Aug 25, 2015
Orphan Drug Designation
- Apr 17, 2018
Rigel Pharmaceuticals — Earliest FDA Approval
- Apr 17, 2018
Rigel Pharmaceuticals — NDA Secondary Org
- Apr 17, 2018
Rigel Pharmaceuticals — NDA Organization
Indications
Studied for
- Anemia · Phase 2
- Anemia, Hemolytic, Autoimmune · Phase 2
- Anemia, Sickle Cell · Phase 1
- Arthritis, Rheumatoid · Phase 3
- beta-Thalassemia · Phase 1
- Biological Availability · Phase 1
- Carcinoma, Non-Small-Cell Lung · Phase 2
- Carcinoma, Renal Cell · Phase 2
- Colorectal Neoplasms · Phase 2
- Coronavirus · Phase 1/Phase 2
- Coronavirus Infections · Phase 3
- COVID-19 · Phase 3
- Drug Interactions · Phase 1
- Drugs, Investigational · Phase 1
- Glomerulonephritis, IGA · Phase 2
- Graft vs Host Disease · Phase 2
- Head and Neck Neoplasms · Phase 2
- Healthy Volunteers · Phase 1
- Hematologic Neoplasms · Phase 1
- Hemoglobin, Sickle · Phase 1
- Hidradenitis Suppurativa · Phase 2
- Kidney Failure, Chronic · Phase 1
- Kidney Transplantation · Phase 1/Phase 2
- Leukemia, Myelomonocytic, Chronic · Phase 1
- Liver Diseases · Phase 1
- Lung Transplantation · Phase 1
- Lupus Erythematosus, Systemic · Phase 2
- Lymphoma · Phase 1/Phase 2
- Lymphoma, Large B-Cell, Diffuse · Phase 2
- Lymphoma, T-Cell · Phase 2
- Myelodysplastic Syndromes · Phase 1
- Ovarian Neoplasms · Phase 1
- Pancreatic Neoplasms · Phase 1
- Pharmacokinetics · Phase 1
- Pheochromocytoma · Phase 2
- Pioglitazone · Phase 1
- Pneumonia · Phase 3
- Pneumonia, Viral · Phase 3
- Primary Myelofibrosis · Phase 2
- Purpura, Thrombocytopenic, Idiopathic · Phase 3
- Respiratory Distress Syndrome · Phase 2
- Severe Acute Respiratory Syndrome · Phase 3
- Thrombocytopenia · Phase 2
Mechanism of action
- Tyrosine-protein kinase SYKINHIBITOR
SYK inhibitor
Prodrug - active metabolite is R-406
Approval history
- approvedApr 17, 2018
Chemistry & pharmacology
Loading structure…
SMILES
COc1cc(Nc2ncc(F)c(Nc3ccc4c(n3)N(COP(=O)([O-])[O-])C(=O)C(C)(C)O4)n2)cc(OC)c1OC.O.O.O.O.O.O.[Na+].[Na+]- Mol. weight
- 732.52 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
First in classProdrug
Sources
- ChEMBLCHEMBL3989516 ↗
- WikipediaFostamatinib ↗
- NCATSSQ8A3S5101 ↗
- ChEMBLCHEMBL2105644 ↗
- ChEMBLCHEMBL2103830 ↗
Also known as
- fostamatinib
- fostamatinib
- fostamatinib
- fostamatinib
- fostamatinib
- fostamatinib disodium
- fostamatinib disodium
- fostamatinib disodium
- fostamatinib disodium
- r788
- r788
- r-788
- r-788
- r 788 compound
- r788 compound
- r-788 free acid
- r-788 free acid
- r-788 sodium
- r-788 sodium
- r935788
- r935788
- r-935788
- r-935788
- r-935788 free acid
- r-935788 free acid
- r-935788 sodium
- r-935788 sodium
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT06948097 | Phase 1 | Dec 2, 2025 | National Heart, Lung, and Blood Institute (NHLBI) |
| NCT06639724 | Phase 1 | Dec 31, 2024 | Rigel Pharmaceuticals, University of California, San Diego |
| NCT06233110 | Phase 1 | Nov 1, 2024 | Duke University, Incyte, National Institutes of Health (NIH), Rigel Pharmaceuticals |
| NCT06564207 | Phase 2 | Nov 1, 2024 | Department of Health and Human Services, Inova Health System, Rigel Pharmaceuticals |
| NCT05904093 | Phase 1 | Jan 3, 2024 | National Heart, Lung, and Blood Institute (NHLBI) |
| NCT05509582 | Phase 2 | Dec 29, 2022 | National Heart, Lung, and Blood Institute (NHLBI) |
| NCT05502783 | Phase 2 | Dec 29, 2022 | National Heart, Lung, and Blood Institute (NHLBI) |
| NCT05593770 | Phase 2/Phase 3 (Phase 3) | Oct 27, 2022 | NEAT ID Foundation |
| NCT05040698 | Phase 2 | Oct 31, 2021 | Holdsworth House Medical Practice, Rigel Pharmaceuticals |
| NCT05030675 | Phase 1 | Aug 13, 2021 | National Cancer Institute (NCI), University of Texas at Houston |
| NCT04924660 | Phase 2/Phase 3 (Phase 3) | Jul 15, 2021 | National Heart, Lung, and Blood Institute (NHLBI), National Institutes of Health (NIH), Vanderbilt University |
| NCT04543279 | Phase 2 | Jan 31, 2021 | Rigel Pharmaceuticals, Washington University in St. Louis |
| NCT04629703 | Phase 3 | Dec 31, 2020 | Rigel Pharmaceuticals |
| NCT04579393 | Phase 2 | Oct 8, 2020 | National Heart, Lung, and Blood Institute (NHLBI), National Institutes of Health (NIH) |
| NCT04581954 | Phase 1/Phase 2 (Phase 2) | Oct 2, 2020 | Imperial College London, Novartis, Rigel Pharmaceuticals, University of London |
| NCT04132050 | Phase 3 | Oct 31, 2019 | Kissei Pharmaceuticals |
| NCT04138927 | Phase 3 | Oct 31, 2019 | Rigel Pharmaceuticals |
| NCT03991780 | Phase 1/Phase 2 (Phase 2) | May 8, 2019 | Imperial College London |
| NCT03764618 | Phase 3 | Apr 1, 2019 | Rigel Pharmaceuticals |
| NCT03246074 | Phase 1 | Feb 1, 2018 | Johns Hopkins University, Rigel Pharmaceuticals |
Showing 20 of 63 trials
Page 1 / 4
Organizations
Research & Development (26)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| AstraZeneca | For profit | 30 | 27 | 3 | 2007 |
| Rigel Pharmaceuticals | For profit | 24 | 17 | 4 | 2006 |
| IQVIA | For profit | 7 | 0 | 1 | 2010 |
| National Heart, Lung, and Blood Institute (NHLBI) | Government | 6 | 5 | 3 | 2020 |
| National Institutes of Health (NIH) | Government | 3 | 0 | 3 | 2020 |
| Duke University | Academic/Hospital | 2 | 2 | 1 | 2016 |
| Imperial College London | Academic/Hospital | 2 | 2 | 1 | 2019 |
| National Cancer Institute (NCI) | Government | 2 | 1 | 2 | 2009 |
| Orlando Clinical Research Center | For profit | 2 | 0 | 1 | 2010 |
| Parexel | For profit | 2 | 0 | 1 | 2010 |
| University of California, San Diego | Academic/Hospital | 2 | 1 | 2 | 2006 |
| Department of Health and Human Services | Government | 1 | 0 | 1 | 2024 |
| Harvard University | Academic/Hospital | 1 | 0 | 1 | 2006 |
| Holdsworth House Medical Practice | Academic/Hospital | 1 | 1 | 1 | 2021 |
| Incyte | For profit | 1 | 0 | 1 | 2024 |
| Inova Health System | Academic/Hospital | 1 | 1 | 1 | 2024 |
| Johns Hopkins University | Academic/Hospital | 1 | 1 | 1 | 2018 |
| Kissei Pharmaceuticals | For profit | 1 | 1 | 1 | 2019 |
| NEAT ID Foundation | Academic/Hospital | 1 | 1 | 1 | 2022 |
| Novartis | For profit | 1 | 0 | 1 | 2020 |
26 organizations
Page 1 / 2
Marketing (2)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Rigel Pharmaceuticals | For profit | NDA2 | Apr 17, 2018 |
| Rigel Pharmaceuticals | For profit | NDA | Apr 17, 2018 |