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Description:

EC50: 38 nM for anti-proliferative growth effect in 19 of 25 AML cell lines

Lysine specific demethylase 1 (LSD1) is a histone H3K4me1/2 demethylase found in various transcriptional co-repressor complexes. LSD1 can interact with pluripotency factors in human embryonic stem cells and is important for decommissioning enhancers in stem cell differentiation. LSD1 is overexpressed in multiple cancer types and recent studies suggest inhibition of LSD1 reactivates the all-trans retinoic acid receptor pathway in acute myeloid leukemia (AML). GSK2879552 is a novel and irreversible LSD1 inhibitor.

In vitro: Six days of GSK2879552 treatment resulted in potent anti-proliferative growth effects in 19 of 25 AML cell lines representing a range of AML subtypes. Treating for longer time periods revealed sensitivity in all AML cell lines. AML blast colony forming ability was also inhibited in 4 of 5 bone marrow samples derived from primary AML patient samples [1].

In vivo: After 17 days of GSK2879552 treatment, control mice had 80% GFP+ cells in the bone marrow whereas treated mice had only 2.8% GFP positive cells, and the treated animals survived weeks beyond control mice [1].

Clinical trial: A phase I, open-label, multi-center, non-randomized, 2-part first time in human (FTIH) study for GSK2879552 has been condcuted to investigate the effect of GSK2879552 in subjects with relapsed/refractory small cell lung carcinoma.

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