Pharmacokinetics of LSD1 Inhibitor Derivatives

LSD1 inhibitors used in this study include RN-1 (Calbiochem, San Diego, CA), ORY-1001 (Cayman Chemical, Ann Arbor, MI), OG-L002 (Selleck Chemicals, Houston, TX), S2101 (Millipore, Temecula, CA) and two N-alkylated derivatives of S2101, S2116 and S2157 (synthesized by Tokyo Chemical Industry, Tokyo, Japan) (15 (link)). A pharmacokinetic study was conducted with a single intraperitoneal injection of either S2116 or S2157 at 50 mg/kg to nonobese diabetic/severe combined immunodeficiency (NOD/SCID) mice (Charles River Laboratories, Wilmington, MA), followed by serial sampling of blood at 1, 2, 4, 8 and 24 hours after administration. Brain tissues were harvested at 0.5 hour and homogenized in deionized water. Plasma and brain samples were subjected to LC-MS/MS analysis to determine the concentrations of each drug.

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Saito S., Kikuchi J., Koyama D., Sato S., Koyama H., Osada N., Kuroda Y., Akahane K., Inukai T., Umehara T, & Furukawa Y. (2018). Eradication of central nervous system leukemia of T-cell origin with a brain-permeable LSD1 inhibitor. Clinical cancer research : an official journal of the American Association for Cancer Research, 25(5), 1601-1611.

Publication 2018

ORY-1001 OG-L002 S2101 NOD/SCID) mice

Brain Cayman Derivatives Drug Inhibitors Intraperitoneal injection Lsd1 Ms ms Nonobese diabetic mice Plasma River Severe combined immunodeficiency Tissues

Corresponding Organization : Jichi Medical University

Other organizations : RIKEN Center for Sustainable Resource Science, University of Yamanashi

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Variable analysis

independent variables

Type of LSD1 inhibitor (RN-1, ORY-1001, OG-L002, S2101, S2116, S2157)

dependent variables

Concentration of LSD1 inhibitors in plasma and brain samples

control variables

Mouse strain (nonobese diabetic/severe combined immunodeficiency (NOD/SCID))
Route of administration (single intraperitoneal injection)
Dose of LSD1 inhibitors (50 mg/kg)

controls

Positive control: Not explicitly mentioned
Negative control: Not explicitly mentioned

Annotations

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