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Trazpiroben

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
Trazpiroben
Clinical data
Other namesTAK-906; ATC-1906
Drug classDopamine antagonist
Identifiers
  • 3-[[1-cyclohexyl-4-oxo-8-(4-oxo-4-phenylbutyl)-1,3,8-triazaspiro[4.5]decan-3-yl]methyl]benzoic acid
CAS Number
PubChemCID
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC31H39N3O4
Molar mass517.670 g·mol−1
3D model (JSmol)
  • C1CCC(CC1)N2CN(C(=O)C23CCN(CC3)CCCC(=O)C4=CC=CC=C4)CC5=CC(=CC=C5)C(=O)O
  • InChI=1S/C31H39N3O4/c35-28(25-10-3-1-4-11-25)15-8-18-32-19-16-31(17-20-32)30(38)33(23-34(31)27-13-5-2-6-14-27)22-24-9-7-12-26(21-24)29(36)37/h1,3-4,7,9-12,21,27H,2,5-6,8,13-20,22-23H2,(H,36,37)
  • Key:BDXJYAAYLZTLEK-UHFFFAOYSA-N

Trazpiroben (developmental code nameTAK-906) is adopamine antagonist drug which was under development for the treatment ofgastroparesis.[1][2][3][4][5] It acts as aperipherally selectivedopamineD2 andD3 receptorantagonist.[1][2] The drug has been found to strongly increaseprolactin levels in humans, similarly to other peripherally selective D2 receptor antagonists likedomperidone.[5] Clinical development of trazpiroben was discontinued before April 2022.[1] Trazpiroben was originated by Altos Therapeutics and was under development byTakeda Oncology.[1]

References

[edit]
  1. ^abcd"Trazpiroben - Takeda Oncology - AdisInsight".
  2. ^abWhiting RL, Choppin A, Luehr G, Jasper JR (October 2021)."Preclinical Evaluation of the Effects of Trazpiroben (TAK-906), a Novel, Potent Dopamine D2/D3 Receptor Antagonist for the Management of Gastroparesis".J Pharmacol Exp Ther.379 (1):85–95.doi:10.1124/jpet.121.000698.PMID 34253646.S2CID 235809216.
  3. ^Whiting RL, Darpo B, Chen C, Fletcher M, Combs D, Xue H, Stoltz RR (August 2021)."Safety, Pharmacokinetics, and Pharmacodynamics of Trazpiroben (TAK-906), a Novel Selective D2 /D3 Receptor Antagonist: A Phase 1 Randomized, Placebo-Controlled Single- and Multiple-Dose Escalation Study in Healthy Participants".Clin Pharmacol Drug Dev.10 (8):927–939.doi:10.1002/cpdd.906.PMC 8451790.PMID 33462988.
  4. ^Kuo B, Scimia C, Dukes G, Zhang W, Gupta S, Chen C, Chuang E, Camilleri M (August 2021)."Randomised clinical trial: safety, pharmacokinetics and pharmacodynamics of trazpiroben (TAK-906), a dopamine D2 /D3 receptor antagonist, in patients with gastroparesis".Aliment Pharmacol Ther.54 (3):267–280.doi:10.1111/apt.16451.PMID 34148244.S2CID 235492049.
  5. ^abYamaguchi T, Kudou K, Okamoto H, Chen C, Whiting R, Sekino H (December 2021)."Evaluating the Safety, Tolerability, and Disposition of Trazpiroben, a D2 /D3 Receptor Antagonist: Phase I Single- and Multiple-Ascending Dose Studies in Healthy Japanese Participants".Clin Pharmacol Drug Dev.11 (6):695–706.doi:10.1002/cpdd.1057.PMC 9303893.PMID 34967147.S2CID 245567576.

External links

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D1-like
Agonists
PAMs
Antagonists
D2-like
Agonists
Antagonists


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