KW‑6356
Selective adenosine A2A antagonist / inverse agonist, investigational Parkinson's drug.
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Pharmacology
Contents
WHAT IS KW-6356?
Detailed overview
KW-6356 (sipagladenant) is a selective adenosine A2A receptor antagonist and inverse agonist being developed for Parkinson's disease. By blocking the A2A receptor it indirectly supports striatal dopaminergic signaling: it removes the adenosine-mediated brake that opposes dopamine in the basal ganglia, thereby improving motor function. Pharmacologically it shows insurmountable binding, slow dissociation, and an active metabolite that gives it a long elimination half-life. It has been tested in humans: a Phase 2 randomized controlled trial evaluated it as monotherapy in early Parkinson's disease, with constipation and nasopharyngitis among the most common adverse effects. It is an investigational compound, not an approved medicine in most regions.
Mechanism
Adenosine A2A antagonist / inverse agonist
Evidence
Human Phase 2 (Parkinson's, investigational)
Legal status
Investigational, unapproved drug
Receptor profile
- Adenosine A2A receptorsStrong
- Striatal dopaminergic signaling (indirect)Moderate
- Adenosine A1 receptors (high A2A selectivity)Weak
Safety
Side effects, stop signs, contraindications
Side effects · 5
- Constipation, one of the most common complaints in early human trials
- Nasopharyngitis, also frequently reported in early trials
- Theoretical dyskinesia (involuntary movement) risk when combined with L-DOPA, though this appeared low in animal models
- Headache and nausea, as is common with the adenosine antagonist class
- Long-term safety in humans is only partly known: the compound is still investigational
Contraindications · 4
- Pregnancy and breastfeeding: safety not established, avoid
- Unapproved investigational drug: appropriate only within a clinical trial protocol under medical supervision
- Additive effect possible with other adenosine antagonists (e.g. caffeine, istradefylline)
- Effects may be prolonged due to the active metabolite and long half-life: interaction profile in humans not fully characterized
Related Nootropics
Same therapeutic category
Studies
Related research and clinical findings
In Vitro Pharmacological Profile of KW-6356, a Novel Adenosine A2A Receptor Antagonist/Inverse Agonist
Ohno Y, et al.
Randomized controlled trial of KW-6356 monotherapy in patients with early untreated Parkinson's disease
Maeda T, et al.
Anti-parkinsonian activity of the adenosine A2A receptor antagonist/inverse agonist KW-6356 as monotherapy in MPTP-treated common marmosets
Ohno Y, et al.
The adenosine A2A receptor antagonist/inverse agonist, KW-6356 enhances the anti-parkinsonian activity of L-DOPA with a low risk of dyskinesia in MPTP-treated common marmosets
Ohno Y, et al.
Safety, Tolerability, and Pharmacokinetics of the Novel Adenosine A2A Antagonist/Inverse Agonist KW-6356 Following Single and Multiple Oral Administration in Healthy Volunteers
Tayama T, et al.
FAQ
FAQ
Selective adenosine A2A antagonist / inverse agonist, investigational Parkinson's drug.
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Structure & chemistry
The information here is strictly for educational and scientific purposes. It does not replace medical advice or clinical consultation, and it does not encourage illegal substance or pharmaceutical use. Data is sourced. When in doubt, consult your doctor.