Afuresertib (GSK-2110183)

Mechanism of action

From the NCI Drug Dictionary: An orally bioavailable inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity. Afuresertib binds to and inhibits the activity of Akt, which may result in inhibition of the PI3K/Akt signaling pathway and tumor cell proliferation and the induction of tumor cell apoptosis.

Preliminary data

Note: This is not meant to be an exhaustive list of preliminary results. References included in this section include non-randomized studies published in high-profile journals (e.g., NEJM) and experimental arms of phase 3 RCTs. Inclusion here is not an indication of impending regulatory approval, although many of these drugs do end up receiving approval by a regulatory authority.

Multiple myeloma

1. PKB112835: Spencer A, Yoon SS, Harrison SJ, Morris SR, Smith DA, Brigandi RA, Gauvin J, Kumar R, Opalinska JB, Chen C. The novel AKT inhibitor afuresertib shows favorable safety, pharmacokinetics, and clinical activity in multiple myeloma. Blood. 2014 Oct 2;124(14):2190-5. Epub 2014 Jul 29. link to original article link to PMC article PubMed NCT00881946

Also known as

• Code names: GSK-2110183, LAE-002