[CAS NO. 914295-16-2] Fostamatinibdisodiumhexahydrate
PRODUCTS SPECIFICATIONS [914295-16-2]
DESCRIPTION [914295-16-2]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 732.51 |
| Molecular Formula | C23H36FN6Na2O15P |
| SMILES | COC1=CC(NC2=NC=C(C(NC3=NC(N4COP(O[Na])(O[Na])=O)=C(C=C3)OC(C)(C)C4=O)=N2)F)=CC(OC)=C1OC.O.O.O.O.O.O |
7 Publications Citing Use of MCE
Summary
IC50 & Target
Syk, FLT3 [2]
In Vivo
Fostamatinib (R788) is highly bioavailable, and rapidly absorbed in Louvain rats. R406 following a single oral dose of R788 10 mg/kg or 20 mg/kg: AUC 0-16 hrs = 10618 ng*h/mL and 30650 ng*h/mL respectively; C max =2600 ng/mL and 6500 ng/mL respectively (observed at 1 hour); t 1/2 =4.2 hours. The prodrug was not detected in plasma suggesting R788 is completely converted to R406 [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT01245790 | AstraZeneca |
Rheumatoid Arthritis|Renal Impairment
|
November 2010 | Phase 1 |
| NCT03991780 | Imperial College London |
Renal Transplant Rejection
|
May 8, 2019 | Phase 1|Phase 2 |
| NCT01598571 | AstraZeneca |
Healthy
|
May 2012 | Phase 1 |
| NCT00752999 | Rigel Pharmaceuticals |
Systemic Lupus Erythematosus
|
November 2008 | Phase 2 |
| NCT02611063 | Stefanie Sarantopoulos, MD, PhD.|Duke University |
Hematological Malignancies
|
January 2016 | Phase 1 |
| NCT01311622 | AstraZeneca |
Rheumatoid Arthritis|Healthy Subjects
|
March 2011 | Phase 1 |
| NCT02092961 | AstraZeneca |
Rheumatoid Arthritis
|
February 2011 | Phase 2 |
| NCT01682408 | AstraZeneca |
Pharmacokinetics
|
September 2012 | Phase 1 |
| NCT00446095 | Rigel Pharmaceuticals |
Lymphoma
|
April 2007 | Phase 1|Phase 2 |
| NCT01355354 | AstraZeneca |
Healthy Volunteers|Rheumatoid Arthritis
|
June 2011 | Phase 1 |
| NCT04579393 | National Heart, Lung, and Blood Institute (NHLBI)|National Institutes of Health Clinical Center (CC) |
Coronavirus Disease 2019
|
October 8, 2020 | Phase 2 |
| NCT01242514 | AstraZeneca |
Rheumatoid Arthritis
|
January 2011 | Phase 3 |
| NCT00665626 | Rigel Pharmaceuticals |
Rheumatoid Arthritis
|
May 2008 | Phase 2 |
| NCT01197521 | AstraZeneca |
Rheumatoid Arthritis
|
September 2010 | Phase 3 |
| NCT01309854 | AstraZeneca |
Rheumatoid Arthritis|Healthy Volunteers|Pharmacokinetics|Pioglitazone|Drug-drug Interaction|Amount of Pioglitazone in Blood
|
March 2011 | Phase 1 |
| NCT04904276 | Rigel Pharmaceuticals |
ITP|Immune Thrombocytopenia
|
May 18, 2021 | |
| NCT05509582 | National Heart, Lung, and Blood Institute (NHLBI)|National Institutes of Health Clinical Center (CC) |
Immune Mediated Anemia|Immune Mediated Thrombocytopenia|Chronic GVHD
|
November 28, 2022 | Phase 2 |
| NCT01208155 | AstraZeneca |
Bioavailability|Pharmacokinetics
|
September 2010 | Phase 1 |
| NCT02112838 | Rigel Pharmaceuticals |
IGA Nephropathy
|
October 2014 | Phase 2 |
| NCT04581954 | Imperial College London|Imperial College Healthcare NHS Trust|Rigel Pharmaceuticals|Novartis |
Coronavirus|Covid19|Pneumonia
|
October 2, 2020 | Phase 1|Phase 2 |
| NCT01197534 | AstraZeneca |
Rheumatoid Arthritis
|
September 2010 | Phase 3 |
| NCT01499303 | AstraZeneca |
Diffuse Large B-Cell Lymphoma
|
December 2011 | Phase 2 |
| NCT01197755 | AstraZeneca |
Rheumatoid Arthritis
|
September 2010 | Phase 3 |
| NCT00706342 | Rigel Pharmaceuticals |
Purpura, Thrombocytopenic, Idiopathic
|
January 2007 | Phase 2 |
| NCT00326339 | Rigel Pharmaceuticals |
Rheumatoid Arthritis
|
August 2006 | Phase 2 |
| NCT01387308 | AstraZeneca |
Healthy
|
August 2011 | Phase 1 |
| NCT01640054 | AstraZeneca |
Rheumatoid Arthritis
|
July 2012 | Phase 2 |
| NCT04629703 | Rigel Pharmaceuticals |
Covid19|SARS (Severe Acute Respiratory Syndrome)|SARS Pneumonia|SARS-Associated Coronavirus as Cause of Disease Classified Elsewhere|Pneumonia|Pneumonia, Viral
|
February 22, 2021 | Phase 3 |
| NCT01608542 | AstraZeneca |
Healthy Japanese Volunteers
|
June 2012 | Phase 1 |
| NCT04924660 | Sean Collins|National Institutes of Health (NIH)|National Heart, Lung, and Blood Institute (NHLBI)|Vanderbilt University Medical Center |
COVID-19|SARS-CoV-2 Infection|Coronavirus Infection
|
July 15, 2021 | Phase 2|Phase 3 |
| NCT04543279 | Washington University School of Medicine|Rigel Pharmaceuticals |
Myelofibrosis
|
May 3, 2021 | Phase 2 |
| NCT01222455 | AstraZeneca |
Hepatic Impairment|Healthy Volunteers|Pharmacokinetics|Amount of R406 in Blood
|
October 2010 | Phase 1 |
| NCT01569074 | AstraZeneca |
Rheumatoid Arthritis
|
April 2012 | Phase 2 |
| NCT04132050 | Kissei Pharmaceutical Co., Ltd. |
Idiopathic Thrombocytopenic Purpura
|
December 24, 2019 | Phase 3 |
| NCT03764618 | Rigel Pharmaceuticals |
Warm Antibody Autoimmune Hemolytic Anemia
|
April 24, 2019 | Phase 3 |
| NCT05502783 | National Heart, Lung, and Blood Institute (NHLBI)|National Institutes of Health Clinical Center (CC) |
Immune Mediated Anemia|Immune Mediated Thrombocytopenia|Chronic GVHD
|
November 28, 2022 | Phase 2 |
| NCT01276262 | AstraZeneca |
Scientific Terminology Rheumatoid Arthritis, Healthy Female Volunteers, Pharmacokinetics, Oral Contraceptive, Drug-drug Interaction|Laymen Terminology Level of Oral Contraceptive in Blood, Oral Contraceptive, Rheumatoid Arthritis, Drug -Drug Interaction
|
March 2011 | Phase 1 |
| NCT05030675 | M.D. Anderson Cancer Center|National Cancer Institute (NCI) |
Refractory Chronic Myelomonocytic Leukemia|Refractory Myelodysplastic Syndrome
|
August 13, 2021 | Phase 1 |
| NCT03363334 | Rigel Pharmaceuticals |
Immune Thrombocytopenic Purpura
|
||
| NCT02433236 | Rigel Pharmaceuticals |
IGA Nephropathy
|
September 2015 | Phase 2 |
| NCT01264770 | AstraZeneca |
Rheumatoid Arthritis
|
January 2011 | Phase 2 |
| NCT01725230 | AstraZeneca |
Rheumatoid Arthritis
|
November 2012 | Phase 1 |
| NCT02076412 | Rigel Pharmaceuticals |
Immune Thrombocytopenic Purpura
|
January 2015 | Phase 3 |
| NCT05040698 | Holdsworth House Medical Practice|Rigel Pharmaceuticals |
Hidradenitis Suppurativa
|
October 1, 2021 | Phase 2 |
| NCT00923481 | National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) |
Head and Neck Neoplasms|Pheochromocytoma|Colorectal Neoplasms|Carcinoma, Non-Small-Cell Lung|Carcinoma, Renal Cell
|
April 2009 | Phase 2 |
| NCT05593770 | NEAT ID Foundation |
COVID-19|SARS-CoV2 Infection|Coronavirus Infection
|
October 27, 2022 | Phase 2|Phase 3 |
| NCT01563978 | AstraZeneca |
Rheumatoid Arthritis
|
April 2012 | Phase 2 |
| NCT04138927 | Rigel Pharmaceuticals |
Warm Antibody Autoimmune Hemolytic Anemia
|
October 30, 2019 | Phase 3 |
| NCT00805467 | AstraZeneca |
Rheumatoid Arthritis
|
August 2008 | Phase 2 |
| NCT00798096 | Rigel Pharmaceuticals |
T Cell Lymphoma
|
March 2009 | Phase 2 |
| NCT03246074 | Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins|Rigel Pharmaceuticals|Allegheny Singer Research Institute (also known as Allegheny Health Network Research Institute) |
Ovarian Cancer
|
April 3, 2018 | Phase 1 |
| NCT02076399 | Rigel Pharmaceuticals |
Immune Thrombocytopenic Purpura
|
July 14, 2014 | Phase 3 |
| NCT02612558 | Rigel Pharmaceuticals |
Warm Antibody Autoimmune Hemolytic Anemia
|
July 2016 | Phase 2 |
| NCT00665925 | Rigel Pharmaceuticals |
Rheumatoid Arthritis
|
May 2008 | Phase 2 |
| NCT05613296 | Gruppo Italiano Malattie EMatologiche dell´Adulto |
ITP - Immune Thrombocytopenia|Chronic ITP|Refractory ITP
|
December 2022 | |
| NCT02077192 | Rigel Pharmaceuticals |
Immune Thrombocytopenic Purpura
|
July 2014 | Phase 3 |
| NCT01336218 | AstraZeneca |
Rheumatoid Arthritis|Healthy Volunteers
|
April 2011 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 25 mg/mL ( 34.13 mM ; Need ultrasonic)
H 2 O : 2 mg/mL ( 2.73 mM ; ultrasonic and warming and heat to 60°C)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.3652 mL | 6.8258 mL | 13.6517 mL |
| 5 mM | 0.2730 mL | 1.3652 mL | 2.7303 mL |
| 10 mM | 0.1365 mL | 0.6826 mL | 1.3652 mL |
-
1.
Add each solvent one by one: Cremophor EL
Solubility: 10 mg/mL (13.65 mM); Suspended solution; Need ultrasonic
-
2.
Add each solvent one by one: 0.5% CMC-Na /saline water
Solubility: 8.33 mg/mL (11.37 mM); Suspended solution; Need ultrasonic
References
- [1] Stephen P McAdoo, et al. Fostamatinib Disodium. Drugs Future. 2011;36(4):273.
- [2] Sylvia Braselmann, et al. R406, an orally available spleen tyrosine kinase inhibitor blocks fc receptor signaling and reduces immune complex-mediated inflammation. J Pharmacol Exp Ther. 2006 Dec;319(3):998-1008.
- [3] Hoon-Suk Cha , et al. A novel spleen tyrosine kinase inhibitor blocks c-Jun N-terminal kinase-mediated gene expression in synoviocytes. J Pharmacol Exp Ther. 2006 May;317(2):571-8.