Inupadenant

CaptionSynonyms

Inupadenant

Drug Information
Image	250
Identifiers ChEBI		Chemical Data C H N O Molecular Weight

Inupadenant is an investigational small molecule drug that acts as an antagonist of the adenosine A2A receptor. It is being studied for its potential use in the treatment of various types of cancer, particularly in the context of immunotherapy.

Mechanism of Action

Inupadenant functions by selectively inhibiting the adenosine A2A receptor, which is a G protein-coupled receptor involved in the regulation of immune responses. The adenosine A2A receptor is known to play a role in the suppression of immune cell activity in the tumor microenvironment. By blocking this receptor, inupadenant aims to enhance the activity of T cells and other immune cells, thereby promoting an anti-tumor immune response.

Clinical Development

Inupadenant is currently undergoing clinical trials to evaluate its safety and efficacy in patients with advanced solid tumors. Early-phase studies have shown promising results, with some patients experiencing tumor shrinkage and prolonged disease stabilization. The drug is often studied in combination with other immunotherapies, such as checkpoint inhibitors, to assess potential synergistic effects.

Pharmacokinetics

The pharmacokinetic profile of inupadenant includes its absorption, distribution, metabolism, and excretion characteristics. 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 via the urine and feces.

Safety and Side Effects

In clinical trials, inupadenant has been generally well-tolerated. Common side effects include fatigue, nausea, and headache. Serious adverse events are rare but may include immune-related reactions due to enhanced immune activity.

Research and Future Directions

Ongoing research is focused on identifying biomarkers that predict response to inupadenant, optimizing dosing regimens, and exploring its use in combination with other therapeutic agents. Future studies may expand its application to other types of cancer and investigate its role in overcoming resistance to existing therapies.

Also see

• Adenosine receptor
• Immunotherapy
• Checkpoint inhibitor
• Cancer treatment

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