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Sipagladenant
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| Clinical data | |
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| Other names | KW-6356 |
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| Formula | C20H19N3O4S |
| Molar mass | 397.45 g·mol−1 |
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Sipagladenant (KW-6356) is a non-xanthine selective antagonist/inverse agonist of the adenosine A2A receptor that was previously under development by Kyowa Kirin as a monotherapy and adjunctive to levodopa therapy in Parkinsonism.[1]
Pharmacology
[edit]Pharmacodynamics
[edit]KW-6356 is a selective A2A adenosine antagonist/inverse agonist displaying insurmountable antagonism of this adenosine subtype. Compared to the first generation A2A adenosine inverse agonist Istradefylline, KW-6356 possesses a 100-fold greater affinity for the A2A adenosine receptor and dissociates more slowly from the receptor.[2]
The metabolism of KW-6356 generates M6, an active metabolite with similar potency as a A2A antagonist/inverse agonist.[2]
Pharmacokinetics
[edit]The half-life of KW-6356 is 22.9 hours. The half-life of M6 is 4.34 hours.[2]
Development
[edit]Kyowa Kirin halted development of KW-6356 in 2022 based on regulatory and developmental challenges surrounding the drug.[3]
References
[edit]- ^ Maeda T, Kimura T, Sugiyama K, Yamada K, Hiraiwa R, Nishi M, et al. (December 2023). "Randomized controlled trial of KW-6356 monotherapy in patients with early untreated Parkinson's disease". Parkinsonism & Related Disorders. 117 105907. doi:10.1016/j.parkreldis.2023.105907. PMID 37948832.
- ^ a b c Ohno Y, Suzuki M, Asada H, Kanda T, Saki M, Miyagi H, et al. (June 2023). "In Vitro Pharmacological Profile of KW-6356, a Novel Adenosine A2A Receptor Antagonist/Inverse Agonist". Molecular Pharmacology. 103 (6): 311–324. doi:10.1124/molpharm.122.000633. PMID 36894319.
- ^ "Kyowa Kirin Announced Discontinuation of KW-6356" (PDF).