Dalvastatin is a synthetic HMG-CoA reductase inhibitor developed by Rhône-Poulenc Rorer. Dalvastatin is a prodrug and is itself an inactive lactone. After oral ingestion, the drug is hydrolyzed in vivo to the corresponding beta-hydroxy acid, which is the pharmacologically active form. HMG-CoA reductase is the rate-limiting enzyme in the cholesterol biosynthetic pathway. An active form of dalvastatin inhibits HMG-CoA reductase with IC50 of 3.4 nM. In ex vivo assay, orally administered dalvastatin inhibited cholesterol biosynthesis in rat liver slices with an ED50 value of 0.9. The efficacy of dalvastatin to lower cholesterol was investigated in the clinical trials in the 1990s, but no results were reported.

A-443654 is a potent and selective AKT inhibitor. A-443654 induces rapid Akt Ser-473 phosphorylation independent of mTORC1 inhibition. A-443654 interferes with mitotic progression by regulating aurora a kinase expression. A-443654 inhibits all three Akt isoforms in FL5.12 cells stably transfected with constitutively active myristoylated Akt1/2/3, and showed moderate selectivity when screened against related kinases in the AGC family, such as PKA and PKC20. A-443654 has being shown to extend survival in an intracranial glioma animal model. A-443654, either alone or in combination with existing drugs, may be a useful therapy for primary and drug-resistant T-ALL.