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Epigenetic modification plays a major role in the expression of genetic information. The DNA methyltransferase is an attractive target for tumor chemotherapy

2023-07-17
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Epigenetic modification, like DNA methylation, plays a major role in the expression of genetic information. The DNA methyltransferases (DNMTs), maintain DNA methylation, is an attractive target for tumor chemotherapy. WK-23 displays a good inhibitory effect on human DNMT1 with an IC50 value of 5.0 µM. The PK profile of WK-23 was obtained with quite satisfying oral bioavailability and elimination half-life. In vivo pharmacokinetic properties of WK-22, WK-23, WK-27, and DC_517 were performed by Medicilon.

35.jpgReference:

Ennian Li, et al. Design, synthesis, and biological evaluation of novel carbazole derivatives as potent DNMT1 inhibitors with reasonable PK properties. J Enzyme Inhib Med Chem. 2022 Dec;37(1):1537-1555. doi: 10.1080/14756366.2022.2079640.



Epigenetic-modificationDNA-methylationtumor-chemotherapyPK-profileoral-bioavailabilityhalf-life
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Amorphous solid dispersion of Sorafenib was used to develop an immediate release tablet with improved oral bioavailability. The PK study was performed by Medicilon
2023-07-11
An amorphous solid dispersion (ASD) of Sorafenib (SOR) was used to develop an immediate release tablet with improved oral bioavailability. The SOR ASD tablets exhibited approximately 50% higher relative bioavailability in dogs than the marketed SOR tablet product, Nexavar®. The pharmacokinetic (PK) study of SOR ASD tablets and Nexavar® tablets was performed by Medicilon.
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