Ciforadenant

{{Drugbox | Verifiedfields = changed | verifiedrevid = 477002123 | IUPAC_name = 5-[[3-[[6-amino-3,5-dicyano-4-[[3-(trifluoromethyl)phenyl]amino]pyridin-2-yl]amino]phenyl]methyl]-1,3,4-thiadiazole-2-carboxamide | image = Ciforadenant_structure.png | width = 250 | tradename = | synonyms = CPI-444 | CAS_number = 1448168-86-9 | ATC_prefix = | ATC_suffix = | PubChem = 71587780 | ChemSpiderID = 32700000 | UNII = | KEGG = | ChEMBL = 3301614 | C=20 | H=14 | F=3 | N=9 | O=1 | S=1 | molecular_weight = 481.44 }}

Ciforadenant (also known as CPI-444) is a small molecule drug that acts as an antagonist of the adenosine A2A receptor. It is being investigated for its potential use in cancer immunotherapy.

Mechanism of Action

Ciforadenant works by inhibiting the adenosine A2A receptor, which is a G protein-coupled receptor involved in the regulation of immune responses. Adenosine is a purine nucleoside that can accumulate in the tumor microenvironment and suppress the activity of immune cells such as T cells and natural killer cells. By blocking the A2A receptor, ciforadenant aims to enhance the anti-tumor immune response by preventing adenosine-mediated immunosuppression.

Clinical Development

Ciforadenant is currently undergoing clinical trials to evaluate its safety and efficacy in treating various types of cancer. It is often studied in combination with other immunotherapies, such as checkpoint inhibitors, to assess potential synergistic effects. Early-phase clinical trials have shown promising results, with some patients experiencing tumor shrinkage and prolonged disease stabilization.

Pharmacokinetics

The pharmacokinetic profile of ciforadenant includes its absorption, distribution, metabolism, and excretion. It is administered orally, and studies have shown that it has a favorable bioavailability. The drug is metabolized primarily in the liver, and its metabolites are excreted through the urine.

Side Effects

Common side effects of ciforadenant include fatigue, nausea, and diarrhea. As with many cancer therapies, there is also a risk of immune-related adverse events due to the modulation of the immune system.

Research and Future Directions

Research is ongoing to better understand the full potential of ciforadenant in cancer treatment. Studies are exploring its use in combination with other therapies and in different cancer types. The role of adenosine in the tumor microenvironment continues to be a significant area of interest, and ciforadenant represents a promising approach to targeting this pathway.

Also see

• Adenosine receptor
• Cancer immunotherapy
• Checkpoint inhibitor
• T cell
• Natural killer cell

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