Fostamatinib
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Also known as R-788R-788 FREE ACIDR-935788R-935788 FREE ACIDR788 FREE ACIDR935788 FREE ACIDSID174006453
Summary
Fostamatinib (CHEMBL2103830) is an approved small molecule (ATC B02BX09); indicated across 14 conditions including rheumatoid arthritis and autoimmune thrombocytopenic purpura.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: B02BX09
- Indications: 14 conditions
- Clinical trials: 44
- Chemistry: 580.5 Da · C23H26FN6O9P
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL2103830 |
| Name | Fostamatinib |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 11671467 |
| ATC | B02BX09 |
| Molecular formula | C23H26FN6O9P |
| Molecular weight | 580.5 |
| InChIKey | GKDRMWXFWHEQQT-UHFFFAOYSA-N |
SMILES: CC1(C(=O)N(C2=C(O1)C=CC(=N2)NC3=NC(=NC=C3F)NC4=CC(=C(C(=C4)OC)OC)OC)COP(=O)(O)O)C
IUPAC name: [6-[[5-fluoro-2-(3,4,5-trimethoxyanilino)pyrimidin-4-yl]amino]-2,2-dimethyl-3-oxopyrido[3,2-b][1,4]oxazin-4-yl]methyl dihydrogen phosphate
Also known as: Fostamatinib, R-788, R-788 FREE ACID, R-935788, R-935788 FREE ACID, R788 FREE ACID, R935788 FREE ACID, FOSTAMATINIB, SID174006453, fostamatinib
Parent form; salt/anhydrous children: CHEMBL3989516
Patent coverage: 1,424 distinct patent families (3,841 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 3,384 (88%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.
Targets
Targets
Broader ChEMBL bioactivity targets: 21 (assay-derived). Sample: Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma, Bromodomain testis-specific protein, Receptor-type tyrosine-protein kinase FLT3, Proto-oncogene tyrosine-protein kinase receptor Ret, Aurora kinase B, Mitogen-activated protein kinase 8, Tyrosine-protein kinase SYK, Macrophage-stimulating protein receptor, Focal adhesion kinase 1, Mitogen-activated protein kinase kinase kinase 11, Inhibitor of nuclear factor kappa-B kinase subunit epsilon, Serine/threonine-protein kinase PLK4, Serine/threonine-protein kinase 16, AarF domain-containing protein kinase 1, Mitogen-activated protein kinase 9, Aurora kinase A, Interleukin-1 receptor-associated kinase 3, Serine/threonine-protein kinase Nek9, Non-receptor tyrosine-protein kinase TNK1, Broad substrate specificity ATP-binding cassette transporter ABCG2.
Bioactivity
ChEMBL activities: 24 potent at pChembl ≥ 5 of 26 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| SYK | 7.77 | IC50 | 17 | nM | CHEMBL_ACT_12718372 |
| SYK | 7.77 | IC50 | 17 | nM | CHEMBL_ACT_25073434 |
| SYK | 7.52 | Ki | 30 | nM | CHEMBL_ACT_25500492 |
| NEK9 | 7.39 | Kd | 41 | nM | CHEMBL_ACT_17921758 |
| SYK | 7.39 | IC50 | 41 | nM | CHEMBL_ACT_25500491 |
| ABCG2 | 7.3 | IC50 | 50 | nM | CHEMBL_ACT_24777468 |
| TNK1 | 6.8 | Kd | 160 | nM | CHEMBL_ACT_17945585 |
| SYK | 6.57 | IC50 | 267 | nM | CHEMBL_ACT_12717445 |
| AURKA | 6.52 | Kd | 300 | nM | CHEMBL_ACT_17884098 |
| PLK4 | 6.24 | Kd | 570 | nM | CHEMBL_ACT_17927880 |
| FLT3 | 6.07 | Kd | 843 | nM | CHEMBL_ACT_17903603 |
| ADCK1 | 5.97 | Kd | 1071 | nM | CHEMBL_ACT_17881423 |
| RET | 5.94 | Kd | 1147 | nM | CHEMBL_ACT_17935135 |
| IRAK3 | 5.89 | Kd | 1290 | nM | CHEMBL_ACT_17908339 |
| IKBKE | 5.88 | Kd | 1320 | nM | CHEMBL_ACT_17907300 |
| MAPK9 | 5.81 | Kd | 1533 | nM | CHEMBL_ACT_17916580 |
| MAPK8 | 5.7 | Kd | 2011 | nM | CHEMBL_ACT_17916352 |
| LATS1 | 5.67 | Kd | 2157 | nM | CHEMBL_ACT_17909067 |
| MST1R | 5.67 | Kd | 2132 | nM | CHEMBL_ACT_17919510 |
| STK16 | 5.61 | Kd | 2484 | nM | CHEMBL_ACT_17941161 |
| MAP3K11 | 5.6 | Kd | 2506 | nM | CHEMBL_ACT_17911840 |
| AURKB | 5.59 | Kd | 2550 | nM | CHEMBL_ACT_17884342 |
| PIP4K2C | 5.58 | Kd | 2635 | nM | CHEMBL_ACT_17926748 |
| PTK2 | 5.27 | Kd | 5400 | nM | CHEMBL_ACT_17932607 |
Target pathways
No target-pathway data for this drug (no mapped target genes).
Indications & clinical
Indications
12 diseases in clinical trials (phase 1–3, investigational — not approved indications). Highest ChEMBL trial phase per disease; a non-cancer approved use is occasionally logged at phase 3 here.
| Disease (in trials) | Phase | MONDO | EFO |
|---|---|---|---|
| rheumatoid arthritis | 3 | MONDO:0008383 | EFO:0000685 |
| autoimmune thrombocytopenic purpura | 3 | MONDO:0008558 | EFO:0007160 |
| diffuse large B-cell lymphoma | 2 | MONDO:0018905 | EFO:0000403 |
| IgA glomerulonephritis | 2 | MONDO:0005342 | EFO:0004194 |
| autoimmune hemolytic anemia | 2 | MONDO:0020108 | EFO:1001264 |
| primary myelofibrosis | 2 | MONDO:0009692 | MONDO:0044903 |
| severe acute respiratory syndrome | 2 | MONDO:0005091 | MONDO:0100096 |
| hidradenitis suppurativa | 2 | MONDO:0006559 | EFO:1000710 |
| lymphoma | 1 | MONDO:0005062 | EFO:0000574 |
| lymphoid neoplasm | 1 | MONDO:0005157 | EFO:0001642 |
| ovarian cancer | 1 | MONDO:0008170 | MONDO:0008170 |
| pneumonia | 1 | MONDO:0005249 | EFO:0003106 |
2 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 44.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE1 | 17 |
| PHASE2 | 13 |
| PHASE3 | 5 |
| Not specified | 4 |
| PHASE1/PHASE2 | 3 |
| PHASE2/PHASE3 | 2 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT01197521 | PHASE3 | COMPLETED | Evaluation of Effectiveness of Two Dosing Regimens of Fostamatinib Compared to Placebo in Patients With Rheumatoid Arthritis (RA) Who Are Taking Methotrexate But Not Responding. |
| NCT01197534 | PHASE3 | COMPLETED | Evaluation of Effectiveness of Two Dosing Regimens of Fostamatinib Compared to Placebo in Patients With Rheumatoid Arthritis (RA) Who Are Taking Disease Modifying Anti-rheumatic Drug (DMARD) But Not Responding. |
| NCT01197755 | PHASE3 | COMPLETED | Evaluation of Effectiveness of Two Dosing Regimens of Fostamatinib Compared to Placebo in Patients With Rheumatoid Arthritis (RA) Who Are Taking Methotrexate and Have Had Inadequate Response to Single TNF-alpha Antagonist |
| NCT01242514 | PHASE3 | TERMINATED | Evaluation of Long-term Safety and Effectiveness of Fostamatinib in the Treatment of Rheumatoid Arthritis (RA) |
| NCT04629703 | PHASE3 | COMPLETED | Double-Blind, Randomized, Placebo-Controlled, Multi-Center Phase 3 Study to Evaluate the Efficacy and Safety of Fostamatinib in COVID-19 Subjects |
| NCT04924660 | PHASE2/PHASE3 | COMPLETED | Novel Experimental COVID-19 Therapies Affecting Host Response |
| NCT05593770 | PHASE2/PHASE3 | TERMINATED | International Sites: Novel Experimental COVID-19 Therapies Affecting Host Response |
| NCT03991780 | PHASE1/PHASE2 | ACTIVE_NOT_RECRUITING | Fostamatinib in the Treatment of Chronic Active Antibody Mediated Rejection |
| NCT06564207 | PHASE2 | NOT_YET_RECRUITING | Fostamatinib for Treating Acute Respiratory Distress Syndrome (ARDS) in Hospitalized Adults |
| NCT00446095 | PHASE1/PHASE2 | COMPLETED | Efficacy and Safety Study of Fostamatinib Tablets to Treat B-cell Lymphoma |
| NCT01264770 | PHASE2 | TERMINATED | Evaluation of Efficacy and Safety of Fostamatinib Monotherapy Compared With Adalimumab Monotherapy in Patients With Rheumatoid Arthritis (RA) |
| NCT01499303 | PHASE2 | COMPLETED | Study to Learn if 200mg Test Drug (Fostamatinib) Helps People With Large B-Cell Lymphoma,a Type of Blood Cancer |
| NCT01563978 | PHASE2 | COMPLETED | Study of the Effect of Fostamatinib Twice Daily on Blood Pressure in Patients With Rheumatoid Arthritis |
| NCT01569074 | PHASE2 | TERMINATED | Evaluation of Safety and Effectiveness of Fostamatinib Compared to Placebo in Patients in Asia With Rheumatoid Arthritis |
| NCT01640054 | PHASE2 | TERMINATED | A Long Term Study to Assess the Safety of Fostamatinib in Patients in Asia With Rheumatoid Arthritis |
| NCT02092961 | PHASE2 | TERMINATED | Randomised Double-Blind, Placebo-Controlled, Parallel Group Study in Patients With Active Rheumatoid Arthritis:Magnetic Resonance Imaging Sub-Study |
| NCT02112838 | PHASE2 | COMPLETED | Safety and Efficacy Study of Fostamatinib to Treat Immunoglobin A (IgA) Nephropathy |
| NCT04543279 | PHASE2 | TERMINATED | Fostamatinib as a Single Agent or in Combination With Ruxolitinib for Treatment of Patients With Myelofibrosis With Severe Thrombocytopenia |
| NCT04579393 | PHASE2 | COMPLETED | Fostamatinib for Hospitalized Adults With COVID-19 |
| NCT04581954 | PHASE1/PHASE2 | COMPLETED | Inflammatory Signal Inhibitors for COVID-19 (MATIS) |
| NCT05040698 | PHASE2 | COMPLETED | Study of the Effect of Fostamatinib Upon Cutaneous Inflammation in the Setting of Hidradenitis Suppurativa |
| NCT05502783 | PHASE2 | TERMINATED | Using Fostamatinib to Treat Post-Hematopoietic Stem Cell Transplant Immune-mediated Cytopenias |
| NCT05509582 | PHASE2 | WITHDRAWN | Extension Study (Extended Access) of Syk-inhibition Using Fostamatinib to Treat Posttransplant Immune-mediated Cytopenias |
| NCT05904093 | PHASE1 | RECRUITING | Study to Evaluate the Safety and Tolerability of Escalating Doses of Fostamatinib in Subjects With Stable Sickle Cell Disease |
| NCT06233110 | PHASE1 | RECRUITING | Ruxolitinib Plus Fostamatinib for Steroid Refractory cGvHD |
| NCT06948097 | PHASE1 | NOT_YET_RECRUITING | Syk Inhibition in MItigating Lung Allograft Rejection (SIMILAR): A Trial to Evaluate the Safety and Tolerability of Fostamatinib in Lung Transplant Patients With Donor-Specific Antibodies |
| NCT01208155 | PHASE1 | COMPLETED | Study in Healthy Males to Assess Bioavailability of 4 Different Fostamatinib Tablets |
| NCT01222455 | PHASE1 | COMPLETED | A Study of Fostamatinib in Subjects With Impaired Hepatic (Liver) Function |
| NCT01245790 | PHASE1 | COMPLETED | A Study of Fostamatinib in Subjects With Impaired Kidney Function |
| NCT01276262 | PHASE1 | COMPLETED | Effects of Administration of Fostamatinib on Blood Concentrations of an Oral Contraceptive in Healthy Female Subjects |
| NCT01309854 | PHASE1 | COMPLETED | Effects of Administration of Fostamatinib on Blood Concentrations of Pioglitazone in Healthy Subjects |
| NCT01311622 | PHASE1 | COMPLETED | Effects of Administration of Fostamatinib on Blood Concentrations of Warfarin in Healthy Subjects |
| NCT01336218 | PHASE1 | COMPLETED | Effects of Administration of Fostamatinib on Blood Concentrations of Rifampicin in Healthy Subjects. |
| NCT01355354 | PHASE1 | COMPLETED | Effects of Administration of Fostamatinib on Blood Concentrations of Digoxin in Healthy Subjects |
| NCT01387308 | PHASE1 | COMPLETED | Study in Healthy Males to Assess the Bioavailability of 4 Different Fostamatinib Tablets |
| NCT01598571 | PHASE1 | COMPLETED | Study in Healthy Males to Assess Bioavailability of Single Fostamatinib With iv Micro Tracer Dose |
| NCT01608542 | PHASE1 | COMPLETED | A Single and Multiple Dose Study to Assess Blood and Urine Drug Levels of Fostamatinib in Healthy Japanese Subjects |
| NCT01725230 | PHASE1 | COMPLETED | Assess the Pharmacokinetics of Rosuvastatin and Simvastatin When Administered Alone or in Combination With Fostamatinib |
| NCT02611063 | PHASE1 | COMPLETED | Evaluation of Fostamatinib in Patients With cGVHD After Allogeneic Stem Cell Transplant |
| NCT05030675 | PHASE1 | COMPLETED | Fostamatinib for the Treatment of Lower-risk Myelodysplastic Syndromes or Chronic Myelomonocytic Leukemia Who Have Failed Therapy With Hypomethylating Agents |
| NCT06757257 | Not specified | RECRUITING | Special Drug Use-results Survey for Long-term Use (Fostamatinib) |
| NCT04904276 | Not specified | TERMINATED | Observational Study of Fostamatinib as Second Line Therapy in Adult Patients With Immune Thrombocytopenia (ITP) and Insufficient Response to a Prior Therapy |
| NCT05613296 | Not specified | COMPLETED | Real World Evaluation of the Activity and Safety of Fostamatinib in Consecutive Adult Patients With ITP |
| NCT06071520 | Not specified | COMPLETED | Andalusian Experience in the Use of Fostamatinib in Patients With ITP. FOSTASUR Study |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No PharmGKB pharmacogenomic data curated for this drug.
Related molecules
Related molecules
No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).