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m sildenafil
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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.
UNBS5162 is a naphthalimide that binds to DNA by intercalation and suppresses CXCL chemokine elaboration. In vivo and in vitro studies demonstrated potent antineoplastic properties of the compound. The phase 1 dose-escalation trial demonstrated that despite pre-clinical data suggesting low risk of QTc prolongation with UNBS5162 administration, there was a statistically significant relationship noted in
study patients. The magnitude of QTc prolongation at the highest doses warranted the study drug to be terminated.
