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Search results for vitamin root_references_citation in Reference Text / Citation (approximate match)
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
PHA-543613 was discovered by Pfizer and has been under development primarily as a potential treatment of schizophrenia. PHA-543613 acts as an agonist to the Neuronal acetylcholine receptor protein alpha-7 subunit. A single human trial was conducted in healthy human volunteers, but the compound has been studied extensively in rat models for schizophrenia as well as Parkinson's disease and Alzheimer's disease.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Mephenytoin, (+)- is an (S)-enantiomer of anticonvulsant drug mephenytoin. Mephenytoin is usually administrated as a 1:1 racemic mixture of the (R)- and (S)-enantiomers. The marked stereoselectivity of 4’-hydroxylation of the phenyl ring of S-mephenytoin together with the relatively slow N-demethylation to R-PEH (R-5-phenyl-5-ethylhydantom) and even slower renal clearance results in a dramatic difference in the pharmacokinetic disposition of the S- and R-enantiomers of mephenytoin in man. As a consequence, S-mephenytoin provides a negligible contribution to circulating hydantoins, whereas R-mephenytoin is converted to the pharmacologically active demethylated product R-PEH which is the major circulating hydantoin during chronic administration of the racemic drug. Only the 4’-hydroxylation of the (S)-mephenytoin is absent in patents who are poor metabolizers of mephenytoin. It is not clear as to the clinical consequences of the accumulation of (S)-mephenytoin for the poor metabolizer phenotype. Indeed, it may be the extensive metabolizer who is at great risk of adverse effects by the formation of potentially toxic oxidative metabolites of (S)-mephenytoin.
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
GSK1070916 is a novel, azaindole derived, reversible and ATP-competitive inhibitor of the Aurora B/C kinases. GSK1070916 inhibits the proliferation of tumor cells and has antitumor effects in 10 human tumor xenograft models including breast, colon, lung, and two leukemia models. Nemucore Medical Innovations and Cancer Research UK are developing NMI 900 (previously GSK 1070916) for the intravenous treatment of cancer. The product was originally developed by GlaxoSmithKline. A phase I/II trial in patients with solid tumours has been completed in the UK. Phase II development in ovarian cancer is underway in the US.