Trazpiroben Explained

Class:

Dopamine antagonist

Cas Number:

1352993-39-5

Pubchem:

54768846

Chemspiderid:

81367274

Unii:

FH87H57Q4Y

Chembl:

4650340

Synonyms:

TAK-906; ATC-1906

Iupac Name:

3-1-cyclohexyl-4-oxo-8-(4-oxo-4-phenylbutyl)-1,3,8-triazaspiro[4.5]decan-3-ylmethyl]benzoic acid| C=31 | H=39 | N=3 | O=4| SMILES = C1CCC(CC1)N2CN(C(=O)C23CCN(CC3)CCCC(=O)C4=CC=CC=C4)CC5=CC(=CC=C5)C(=O)O| StdInChI = 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)| StdInChIKey = BDXJYAAYLZTLEK-UHFFFAOYSA-N}}

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. The drug has been found to strongly increase prolactin levels in humans, similarly to other peripherally selective D₂ receptor antagonists like domperidone. Clinical development of trazpiroben was discontinued before April 2022. Trazpiroben was originated by Altos Therapeutics and was under development by Takeda Oncology.

External links

• Trazpiroben - AdisInsight

Notes and References

1. Web site: Trazpiroben - Takeda Oncology - AdisInsight .
2. Whiting RL, Choppin A, Luehr G, Jasper JR . 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 . October 2021 . 34253646 . 10.1124/jpet.121.000698 . 235809216 . free .
3. Whiting RL, Darpo B, Chen C, Fletcher M, Combs D, Xue H, Stoltz RR . 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 . August 2021 . 33462988 . 8451790 . 10.1002/cpdd.906 .
4. Kuo B, Scimia C, Dukes G, Zhang W, Gupta S, Chen C, Chuang E, Camilleri M . 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 . August 2021 . 34148244 . 10.1111/apt.16451 . 235492049 .
5. Yamaguchi T, Kudou K, Okamoto H, Chen C, Whiting R, Sekino H . 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. December 2021 . 34967147 . 10.1002/cpdd.1057 . 9303893 . 245567576 .