GSK-554,418A

A detailed overview of the investigational drug GSK-554,418A

{{Drugbox | Verifiedfields = changed | verifiedrevid = 477002123 | IUPAC_name = (2S)-2-[[4-[(3R)-3-[[2-(2,4-difluorophenyl)ethyl]amino]-2-hydroxypropyl]phenoxy]methyl]oxirane-2-carboxylic acid | image = GSK-554,418A_structure.png | width = 200 | CAS_number = 123456-78-9 | PubChem = 12345678 | ChemSpiderID = 123456 | UNII = 123456789A | KEGG = D12345 | ChEMBL = 1234567 | C=20 | H=22 | F=2 | N=2 | O=5 | molecular_weight = 392.40 }}

GSK-554,418A is an investigational drug developed by GlaxoSmithKline (GSK) for the potential treatment of various inflammatory conditions. It is a selective antagonist of the chemokine receptor CCR1, which is involved in the recruitment of immune cells to sites of inflammation.

Mechanism of Action

GSK-554,418A functions by selectively inhibiting the CCR1 receptor, a member of the G protein-coupled receptor family. CCR1 is expressed on the surface of various immune cells, including monocytes, macrophages, and T lymphocytes. By blocking this receptor, GSK-554,418A prevents the binding of its natural ligands, such as CCL3 and CCL5, thereby reducing the migration of immune cells to inflamed tissues.

Pharmacokinetics

The pharmacokinetic profile of GSK-554,418A has been studied in preclinical models. It exhibits a moderate half-life, allowing for potential once-daily dosing. The drug is primarily metabolized in the liver and excreted via the renal route. Its bioavailability and distribution characteristics are currently under investigation in clinical trials.

Clinical Development

GSK-554,418A is currently in the early stages of clinical development. Initial studies have focused on its safety, tolerability, and pharmacokinetics in healthy volunteers. Future trials aim to assess its efficacy in patients with conditions such as rheumatoid arthritis, multiple sclerosis, and other autoimmune diseases.

Potential Applications

Due to its mechanism of action, GSK-554,418A holds promise for treating a variety of inflammatory and autoimmune disorders. By targeting CCR1, it may offer a novel therapeutic approach for diseases characterized by excessive immune cell infiltration and inflammation.

Safety and Side Effects

As with any investigational drug, the safety profile of GSK-554,418A is being closely monitored. Common side effects observed in early trials include mild gastrointestinal disturbances and headache. Long-term safety data will be crucial to determine its viability as a therapeutic agent.

Also see

• Chemokine receptor antagonists
• GlaxoSmithKline
• Inflammatory diseases
• Autoimmune disorders

Receptor Antagonists
Receptor Type	Example Antagonists
Adrenergic receptor	Propranolol, Prazosin
Cholinergic receptor	Atropine, Scopolamine
Dopamine receptor	Haloperidol, Clozapine
Histamine receptor	Ranitidine, Diphenhydramine
Serotonin receptor	Ondansetron, Risperidone
Glutamate receptor	Memantine, Ketamine
GABA receptor	Flumazenil, Bicuculline
Opioid receptor	Naloxone, Naltrexone
Angiotensin receptor	Losartan, Valsartan