Matsupexole

Last updated

Matsupexole
Matsupexole.svg
Clinical data
Other namesMatsupexol; AM006; AM-006; KDT-3594; KDT3594
Routes of
administration 		Oral [1] [2]
Drug class Dopamine receptor agonist; Dopamine D2 and D3 receptor agonist
Identifiers
  • (4aR,6R,8aR)-2-amino-3-cyano-N-[2-(dimethylamino)ethylcarbamoyl]-8-methyl-N-propyl-4a,5,6,7,8a,9-hexahydro-4H-thieno[3,2-g]quinoline-6-carboxamide
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
ChEMBL
Chemical and physical data
Formula C22H34N6O2S
Molar mass 446.61 g·mol−1
3D model (JSmol)
  • CCCN(C(=O)[C@@H]1C[C@@H]2CC3=C(C[C@H]2N(C1)C)SC(=C3C#N)N)C(=O)NCCN(C)C
  • InChI=1S/C22H34N6O2S/c1-5-7-28(22(30)25-6-8-26(2)3)21(29)15-9-14-10-16-17(12-23)20(24)31-19(16)11-18(14)27(4)13-15/h14-15,18H,5-11,13,24H2,1-4H3,(H,25,30)/t14-,15-,18-/m1/s1
  • Key:PJYJWXOMQPHSKB-IIDMSEBBSA-N

Matsupexole (INN Tooltip International Nonproprietary Name; developmental code names AM006 and KDT-3594) is a dopamine receptor agonist which is under development for the treatment of Parkinson's disease. [1] [3] [2] [4] [5] It is taken orally. [1] [2]

The drug is a non-ergoline derivative related to pramipexole and acts as a dopamine D2 and D3 receptor agonist. [5] [4] [6] It has far lower selectivity for the dopamine D3 receptor over the dopamine D2 receptor than pramipexole and other non-ergoline dopamine receptor agonists. [5] Relatedly, whereas pramipexole and other non-ergoline dopamine receptor agonists like ropinirole and rotigotine produce somnolence in humans and pramipexole has been found to strongly promote non-REM sleep in rodents, these side effects being associated with dopamine D3 receptor agonism, matsupexole and cabergoline did not promote non-REM sleep at efficacious antiparkinsonian doses in rodents. [5] This may be due to a better balance of wakefulness-promoting dopamine D2 receptor activation versus sedating dopamine D3 receptor activation. [5] Similarly to pramipexole, but unlike cabergoline, matsupexole showed negligible activity as a serotonin 5-HT2B receptor agonist and hence is not thought to have a risk of cardiac valvulopathy. [5]

Matsupexole was first described in the scientific literature by 2017. [7] It originated by Kissei Pharmaceutical and is being developed by Kissei Pharmaceutical and AffaMed Therapeutics in Japan and China. [1] [3] [2] As of August 2025, the drug is in phase 2 clinical trials. [1] [3] [2] Matsupexole is described by its developers as a potential best-in-class dopamine receptor agonist for Parkinson's disease. [5]

See also

References

  1. 1 2 3 4 5 "Kissei Pharmceutical". AdisInsight. 28 August 2025. Retrieved 25 January 2026.
  2. 1 2 3 4 5 "Matsupexole Drug Profile". Ozmosi. 1 January 1900. Retrieved 25 January 2026.
  3. 1 2 3 "Delving into the Latest Updates on Matsupexole with Synapse". Synapse. 24 January 2026. Retrieved 25 January 2026.
  4. 1 2 Mao Q, Qin WZ, Zhang A, Ye N (April 2020). "Recent advances in dopaminergic strategies for the treatment of Parkinson's disease". Acta Pharmacologica Sinica. 41 (4): 471–482. doi:10.1038/s41401-020-0365-y. PMC   7471472 . PMID   32112042. KDT3594 (structure undisclosed) is a D2 agonist developed by Kissei Pharmaceuticals [16]. A phase 2 study was initiated in February 2019 to investigate the efficacy, safety, and PK of KDT3594 vs. pramipexole in patients with early PD without concomitant treatment with L-DOPA (NCT03845387).
  5. 1 2 3 4 5 6 7 Suzuki T, Oana F, Oota M, Handa Y, Kaminuma O (January 2026). "Matsupexole: A novel nonergot dopamine receptor agonist with sustained efficacy in a rat model of Parkinson's disease and limited off-target activity". British Journal of Pharmacology bph.70351. doi:10.1111/bph.70351. PMID   41578631.
  6. ↑ Gros P, Armengou Garcia L, Fox SH (June 2025). "Motor fluctuations in Parkinson disease - a mini-review of emerging drugs". Expert Opinion on Emerging Drugs: 1–12. doi:10.1080/14728214.2025.2517582. PMID   40500235. Two other dopamine agonists have been evaluated in PD with motor fluctuations, but results are pending. KDT-3594 (matsupexole) is another non-ergot DA targeting dopamine D2 receptors [40] also currently in a phase II trial in individuals with advanced PD (ClinicalTrials.gov Identifier: NCT06722729).
  7. ↑ Ellis JM, Fell MJ (September 2017). "Current approaches to the treatment of Parkinson's Disease". Bioorganic & Medicinal Chemistry Letters. 27 (18): 4247–4255. doi:10.1016/j.bmcl.2017.07.075. PMID   28869077. Kissei Pharmaceuticals features a D2 agonist, KDT3594, on their pipeline chart in Phase 1 for PD.33 The structure has not been published, and there are no current US clinical trials listed.
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