From Wikipedia, the free encyclopedia
Chemical compound
Trazpiroben
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Other names | TAK-906; ATC-1906 |
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Drug class |
Dopamine antagonist |
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3-[[1-cyclohexyl-4-oxo-8-(4-oxo-4-phenylbutyl)-1,3,8-triazaspiro[4.5]decan-3-yl]methyl]benzoic acid
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CAS Number | |
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PubChem
CID | |
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ChemSpider | |
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UNII | |
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ChEMBL | |
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Formula | C31H39N3O4 |
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Molar mass | 517.670 g·mol−1 |
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3D model (
JSmol) | |
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C1CCC(CC1)N2CN(C(=O)C23CCN(CC3)CCCC(=O)C4=CC=CC=C4)CC5=CC(=CC=C5)C(=O)O
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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
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Trazpiroben (developmental code name TAK-906) is a
dopamine antagonist drug which was under development for the treatment of
gastroparesis.
[1]
[2]
[3]
[4]
[5] It acts as a
peripherally selective
dopamine
D2 and
D3 receptor
antagonist.
[1]
[2] The drug has been found to strongly increase
prolactin levels in humans, similarly to other peripherally selective D2 receptor antagonists like
domperidone.
[5] Clinical development of trazpiroben was discontinued before April 2022.
[1] Trazpiroben was originated by Altos Therapeutics and was under development by
Takeda Oncology.
[1]
References
- ^
a
b
c
d
"Trazpiroben - Takeda Oncology - AdisInsight".
- ^
a
b Whiting 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.
-
^ 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.
-
^ 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.
- ^
a
b Yamaguchi 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