Trazpiroben

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]

Trazpiroben
Clinical data
Other namesTAK-906; ATC-1906
Drug classDopamine antagonist
Identifiers
IUPAC name
  • 3-[[1-cyclohexyl-4-oxo-8-(4-oxo-4-phenylbutyl)-1,3,8-triazaspiro[4.5]decan-3-yl]methyl]benzoic acid
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC31H39N3O4
Molar mass517.670 g·mol−1
3D model (JSmol)
SMILES
  • C1CCC(CC1)N2CN(C(=O)C23CCN(CC3)CCCC(=O)C4=CC=CC=C4)CC5=CC(=CC=C5)C(=O)O
InChI
  • 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

References
  1. "Trazpiroben - Takeda Oncology - AdisInsight".
  2. 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.
  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. 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.



This article is issued from Wikipedia. The text is licensed under Creative Commons - Attribution - Sharealike. Additional terms may apply for the media files.