Preclinical pharmacokinetics and in vitro ADME properties of PAT-1102: a novel HDAC inhibitor for cancer therapy.

ABSTRACT:

Background

Histone deacetylases (HDAC) are involved in chromatin remodelling, and histone deacetylases inhibitors have become the interest of research and shown promising antitumor effects against various cancer.

Methods

In the current study, an attempt was made to characterize the preclinical ADME properties of a novel hydroxamic based HDAC inhibitor, PAT-1102, with the help of in vitro assays and in vivo pharmacokinetic experiments in rats.

Results

PAT-1102 showed high aqueous solubility and high Caco-2 permeability in the in vitro assays. It was found to be not a substrate of efflux protein P-gp, found stable in metabolism experiments with incubations of rat and human liver microsomes. Inhibition experiments of human recombinant CYP enzymes revealed that PAT-1102 w

SUBMITTER: Doreswamy CM 

PROVIDER: S-EPMC12103360 | biostudies-literature | 2025 May

REPOSITORIES: biostudies-literature