R406 (free base) Clinical Trials

Size	Price	Qty
10mg	USD 270
50mg	USD 870

Clinical Trials

Numerous clinical trials have evaluated R406, the active moiety of fostamatinib, through Phase I and Phase II studies targeting rheumatoid arthritis as well as pharmacokinetic profiles in healthy volunteers and subjects with renal or hepatic impairment. Sponsored primarily by major pharmaceutical companies, multiple clinical trials assessed drug bioavailability, metabolic clearance, drug-drug interactions, and systemic exposure. Although recruitment across these trials is predominantly completed, select protocols were terminated during clinical evaluation.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04238832	COMPLETED	Smoking; Tobacco Use	Medical University of South Carolina	2020-06-16
NCT02571855	COMPLETED	Healthy Subjects	Idorsia Pharmaceuticals Ltd.	2015-10-01	PHASE1
NCT02453022	COMPLETED	Pulmonary Disease, Chronic Obstructive	GlaxoSmithKline	2015-05-18	PHASE1
NCT01645085	COMPLETED	Healthy Volunteers	AstraZeneca	2012-07	PHASE1
NCT01682408	COMPLETED	Pharmacokinetics	AstraZeneca	2012-09	PHASE1
NCT01725230	Completed	Rheumatoid Arthritis	AstraZeneca	2012-11	Phase 1
NCT01598571	COMPLETED	Healthy	AstraZeneca	2012-05	PHASE1
NCT01648179	COMPLETED	Infections, Bacterial	GlaxoSmithKline	2012-03	PHASE1
NCT01598571	Completed	Healthy	AstraZeneca	2012-05	Phase 1
NCT01398475	COMPLETED	Chronic Inflammatory Disorder; Arthritis, Rheumatoid	Eli Lilly and Company	2011-07	PHASE1
NCT01387308	Completed	Healthy	AstraZeneca	2011-08	Phase 1
NCT01336218	COMPLETED	Rheumatoid Arthritis; Healthy Volunteers	AstraZeneca	2011-04	PHASE1
NCT01245790	COMPLETED	Rheumatoid Arthritis; Renal Impairment	AstraZeneca	2010-11	PHASE1
NCT01222455	COMPLETED	Hepatic Impairment; Healthy Volunteers; Pharmacokinetics; Amount of R406 in Blood	AstraZeneca	2010-10	PHASE1
NCT01355354	Completed	Healthy Volunteers\|Rheumatoid Arthritis	AstraZeneca	2011-06	Phase 1
NCT01234142	COMPLETED	Smoking Cessation	Pfizer	2010-11	PHASE1
NCT01358344	COMPLETED	Acute Coronary Syndrome	Merck Sharp & Dohme LLC	2010-08	PHASE1
NCT01322451	COMPLETED	Healthy	Lakefront Biotherapeutics NV	2010-11	PHASE1
NCT01197781	COMPLETED	Drug Drug Interactions; Healthy Volunteers	AstraZeneca	2010-09	PHASE1
NCT01013454	COMPLETED	Smoking Cessation	Pfizer	2009-12	PHASE1
NCT00774605	COMPLETED	Smoking Cessation	Pfizer	2008-12	PHASE1
NCT02172131	TERMINATED	Healthy	Boehringer Ingelheim	2006-10	PHASE1
NCT02249403	COMPLETED	Alzheimer Disease	Boehringer Ingelheim	1999-01	PHASE2

(data from https://clinicaltrials.gov, updated on 2021-08-09)

Check the R406 (free base) product page for in-depth specifications, including solubility, stock solutions, MOA, and working concentrations.

Compliance for Clinical Use

Mechanism and Biochemical Profile

R406 selectively binds to spleen tyrosine kinase (Syk) with nanomolar affinity, blocking downstream enzymatic autophosphorylation and signaling pathways mediated by Fc and B-cell receptors. Consequently, this blockade impairs B-lymphocyte and monocyte activation, suppressing immune complex-driven cellular responses and inflammatory mediator release to attenuate tissue damage in clinical trial indications such as rheumatoid arthritis.

Appendix RUO and cGMP Quality Standards

Quality Dimension	RUO (Research Use Only)	cGMP (Current Good Manufacturing Practice)
Clinical Applicability	Prohibited in human clinical trials or medical diagnostics.	Mandatory for human clinical trials (Phase I–III) and therapies.
Regulatory Status	Non-regulated grade; exempt from drug manufacturing laws.	Legally enforced by health authorities (e.g., FDA, EMA, NMPA).
Facility Environment	Unclassified analytical or research laboratories.	Validated Cleanrooms (ISO Class 5–8) with continuous monitoring.
Quality Control	Basic purity and activity testing.	Rigorous safety release testing (Sterility, Endotoxin, Mycoplasma).
Process Validation	Basic equipment calibration; no process validation required.	Full qualification (IQ/OQ/PQ) and complete batch records.
Quality Assurance	Vendor self-declared without required formal QMS.	Mandatory QA/QC unit, Change Control, CAPA, and vendor audits.
Regulatory Impact	High risk of IND rejection if used as a critical raw material.	Required for IND/NDA filings, supported by Drug Master Files (DMF).

Footnotes

Regulatory Note: Governed by FDA (21 CFR Parts 210/211/312), EMA (EudraLex Vol 4), ICH Guidelines (E6/Q7/Q9/Q10), and compendial standards (USP <71>/<85>/<1043>).