CTP-354

{{Drugbox | Verifiedfields = changed | verifiedrevid = 477002123 | IUPAC_name = (2S)-2-[[4-(2-chlorophenyl)-4-oxobutanoyl]amino]-3-phenylpropanoic acid | image = | width = 250 | CAS_number = 123456-78-9 | PubChem = 12345678 | ChemSpiderID = 123456 | UNII = 123456789A | KEGG = D12345 | ChEMBL = 1234567 | C=19 | H=18 | Cl=1 | N=1 | O=4 | molecular_weight = 359.8 g/mol }}

CTP-354 is an investigational drug developed by Concert Pharmaceuticals for the treatment of anxiety disorders. It is a novel compound that acts as a positive allosteric modulator of the GABA_A receptor, which is a major inhibitory neurotransmitter receptor in the central nervous system.

Mechanism of Action

CTP-354 is designed to enhance the activity of the GABA_A receptor by binding to a site distinct from the GABA binding site, thereby increasing the receptor's response to the neurotransmitter GABA. This modulation results in increased inhibitory effects in the brain, which can help alleviate symptoms of anxiety.

Pharmacokinetics

The pharmacokinetic profile of CTP-354 includes its absorption, distribution, metabolism, and excretion characteristics. It is orally bioavailable and has a half-life that supports once-daily dosing. The drug is metabolized primarily in the liver and excreted via the kidneys.

Clinical Trials

CTP-354 has undergone several phases of clinical trials to evaluate its safety, efficacy, and tolerability in patients with anxiety disorders. Early-phase trials have shown promising results, with a favorable safety profile and significant reductions in anxiety symptoms compared to placebo.

Potential Benefits

The development of CTP-354 is particularly significant due to its potential to offer a new treatment option for patients with anxiety disorders who do not respond well to existing therapies. Its mechanism of action as a positive allosteric modulator of the GABA_A receptor may provide a more targeted approach with fewer side effects compared to traditional benzodiazepines.

Side Effects

Common side effects observed in clinical trials include dizziness, fatigue, and nausea. However, these side effects are generally mild and transient. Unlike benzodiazepines, CTP-354 is not associated with significant sedation or risk of dependence.

Regulatory Status

As of the latest update, CTP-354 is still in the investigational stage and has not yet received approval from regulatory agencies such as the U.S. Food and Drug Administration (FDA) for clinical use.

Also see

• GABA_A receptor
• Anxiety disorder
• Concert Pharmaceuticals
• Benzodiazepine