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CSF1R-IN-15 (compound 23) is an inhibitor targeting CSF1R. The colony-stimulating factor-1 receptor (CSF1R) is a tyrosine kinase embedded in the cell membrane of macrophages. The receptor is activated by colony-stimulating factor-1 (CSF-1) and interleukin-34, and signaling via CSF1R is crucial for the differentiation, proliferation, and survival of macrophages[1]. | [in vivo]
In vivo pharmacokinetic indices were derived from cassette dosing studies. The t1/2, C0, AUC0-∞, CLobs, and Vss,obs of CSF1R-IN-15 were 0.5 h, 37 ng/mL, 18 h*ng/mL, 54 L/h/kg, and 32 L/kg in C57BLKS mice[1].
Pharmacokinetic Analysis in CSF1R-IN-15 (compound 23) for a cassette dosing study in C57BLKS mice[1]
| t1/2 (h) | C0 (ng/mL) | AUC0-∞ (h*ng/mL) | CLobs (L/h/kg) | Vss,obs (L/kg) | | 0.5 | 37 | 18 | 54 | 32 |
| Animal Model: | In Vivo Pharmacokinetic Study | | Dosage: | 1mg/kg | | Administration: | Intravenous injection (i.v.) single dosing of drugs (1 mg/kg each) in a 20% DMSO, 80% PEG400 formulation. Blood sampling was done after 10, 30, 60, 120, 240, and 480 min. | | Result: | In vivo pharmacokinetic indexes were t1/2 (0.5 h), C0 (37 ng/mL), AUC0-∞ (18 h*ng/mL), CLobs (54 L/h/kg), and Vss,obs (32 L/kg), respectively.
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| [References]
[1] Aarhus TI, et al. Synthesis and Development of Highly Selective Pyrrolo[2,3-d]pyrimidine CSF1R Inhibitors Targeting the Autoinhibited Form. J Med Chem. 2023 May 25;66(10):6959-6980. DOI:10.1021/acs.jmedchem.3c00428 |
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