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Discovery of DS-3801b, a non-macrolide GPR38 agonist with N-methylanilide structure.
Toda N, Shida T, Takano R, Katagiri T, Hirouchi M, Abe M, Soma K, Nakagami Y, Yamazaki M. Toda N, et al. Bioorg Med Chem Lett. 2022 Mar 1;59:128554. doi: 10.1016/j.bmcl.2022.128554. Epub 2022 Jan 18. Bioorg Med Chem Lett. 2022. PMID: 35051575
We identified a series of N-methylanilide derivatives as novel non-macrolide GPR38 agonists. Among them, 12 di-l-tartrate (DS-3801b) was selected as a clinical candidate for further evaluation....
We identified a series of N-methylanilide derivatives as novel non-macrolide GPR38 agonists. Among them, 12 di-l-tartrate (DS-3801 …
Predictive Gene Signatures Determine Tumor Sensitivity to MDM2 Inhibition.
Ishizawa J, Nakamaru K, Seki T, Tazaki K, Kojima K, Chachad D, Zhao R, Heese L, Ma W, Ma MCJ, DiNardo C, Pierce S, Patel KP, Tse A, Davis RE, Rao A, Andreeff M. Ishizawa J, et al. Cancer Res. 2018 May 15;78(10):2721-2731. doi: 10.1158/0008-5472.CAN-17-0949. Epub 2018 Feb 28. Cancer Res. 2018. PMID: 29490944 Free PMC article.
A Phase 1 Study to Assess the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of Single Oral Doses of DS-3801b, a Motilin Receptor Agonist, in Healthy Subjects.
Dennie J, Atiee G, Warren V, Tao B, Morimoto K, Senaldi G. Dennie J, et al. J Clin Pharmacol. 2017 Sep;57(9):1221-1230. doi: 10.1002/jcph.919. Epub 2017 May 2. J Clin Pharmacol. 2017. PMID: 28464321 Clinical Trial.
DS-3801b is an orally active, nonmacrolide, selective motilin receptor agonist. ...In part B, 12 subjects received 50 mg of DS-3801b or placebo to assess GE. DS-3801b is safe and generally well tolerated after doses up to 50 mg, resulting …
DS-3801b is an orally active, nonmacrolide, selective motilin receptor agonist. ...In part B, 12 subjects received 50 mg of …