Late-Stage Microsomal Oxidation Reduces Drug–Drug Interaction and Identifies Phosphodiesterase 2A Inhibitor PF-06815189

[Image: see text] Late-stage oxidation using liver microsomes was applied to phosphodiesterase 2 inhibitor 1 to reduce its clearance by cytochrome P450 enzymes, introduce renal clearance, and minimize the risk for victim drug–drug interactions. This approach yielded PF-06815189 (2) with improved phy...

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Detalles Bibliográficos
Autores principales: Stepan, Antonia F., Tran, Tuan P., Helal, Christopher J., Brown, Maria S., Chang, Cheng, O’Connor, Rebecca E., De Vivo, Michael, Doran, Shawn D., Fisher, Ethan L., Jenkinson, Stephen, Karanian, David, Kormos, Bethany L., Sharma, Raman, Walker, Gregory S., Wright, Ann S., Yang, Edward X., Brodney, Michael A., Wager, Travis T., Verhoest, Patrick R., Obach, R. Scott
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2018
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5807869/
https://www.ncbi.nlm.nih.gov/pubmed/29456790
http://dx.doi.org/10.1021/acsmedchemlett.7b00343

Internet

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5807869/
https://www.ncbi.nlm.nih.gov/pubmed/29456790
http://dx.doi.org/10.1021/acsmedchemlett.7b00343

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