MK-7246

{{Drugbox | Verifiedfields = changed | verifiedrevid = 477002123 | IUPAC_name = (2R)-2-[[4-(4-chlorophenyl)-2-thiazolyl]oxy]-3-methylbutanoic acid | image = | width = | image2 = | width2 = | tradename = | Drugs.com = | MedlinePlus = | pregnancy_AU = | pregnancy_US = | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = | routes_of_administration = | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | CAS_number = | ATC_prefix = | ATC_suffix = | PubChem = | DrugBank = | ChemSpiderID = | UNII = | KEGG = | ChEBI = | ChEMBL = | synonyms = }}

MK-7246 is an investigational drug developed by Merck & Co. that acts as a selective antagonist of the chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTH2), also known as the prostaglandin D2 receptor 2 (DP2). This receptor is involved in the inflammatory response and is implicated in various allergic and inflammatory conditions, including asthma and allergic rhinitis.

Mechanism of Action

MK-7246 functions by selectively blocking the CRTH2 receptor, which is a G-protein coupled receptor (GPCR) that binds to prostaglandin D2 (PGD2). PGD2 is a lipid mediator that plays a significant role in the pathophysiology of allergic diseases by promoting the recruitment and activation of Th2 cells, eosinophils, and basophils. By inhibiting this receptor, MK-7246 reduces the inflammatory response associated with these conditions.

Clinical Development

MK-7246 has been evaluated in several clinical trials to assess its efficacy and safety in treating conditions like asthma and allergic rhinitis. The drug has shown promise in reducing symptoms and improving lung function in patients with moderate to severe asthma. However, as of the latest updates, MK-7246 has not yet received regulatory approval for clinical use.

Potential Applications

The primary therapeutic applications of MK-7246 are in the treatment of allergic and inflammatory diseases. Its ability to modulate the immune response by targeting the CRTH2 receptor makes it a potential candidate for managing conditions such as:

• Asthma
• Allergic rhinitis
• Atopic dermatitis
• Chronic obstructive pulmonary disease (COPD)

Research and Development

Research on MK-7246 is ongoing, with studies focusing on its pharmacokinetics, pharmacodynamics, and long-term safety profile. The development of CRTH2 antagonists like MK-7246 represents a novel approach in the treatment of Th2-mediated diseases, offering an alternative to traditional therapies such as corticosteroids and beta-agonists.

Also see

• Prostaglandin D2 receptor
• Th2 cells
• G-protein coupled receptors
• Asthma treatment
• Allergic rhinitis treatment