Application of in vitro Drug Metabolism Studies in Chemical Structure Optimization for the Treatment of Fibrodysplasia Ossificans Progressiva (FOP)

@inproceedings{Padilha2019ApplicationOI,
  title={Application of in vitro Drug Metabolism Studies in Chemical Structure Optimization for the Treatment of Fibrodysplasia Ossificans Progressiva (FOP)},
  author={Elias Carvalho Padilha and Jianyao Wang and Ed Kerns and Arthur Lee and Wenwei Huang and Jian-kang Jiang and John C. McKew and Abdul Mutlib and Ros{\^a}ngela Gonçalves Peccinini and Paul B Yu and Philip James Sanderson and Xin Xu},
  booktitle={Front. Pharmacol.},
  year={2019}
}
Currently no approved treatment exists for fibrodysplasia ossificans progressiva (FOP) patients, and disease progression results in severe restriction of joint function and premature mortality. LDN-193189 has been demonstrated to be efficacious in a mouse FOP disease model after oral administration. To support species selection for drug safety evaluation and to guide structure optimization for back-up compounds, in vitro metabolism of LDN-193189 was investigated in liver microsome and cytosol… CONTINUE READING

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