Perifosine, an oral, anti-cancer agent and inhibitor of the Akt pathway: mechanistic actions, pharmacodynamics, pharmacokinetics, and clinical activity

PG Richardson, C Eng, J Kolesar… - Expert opinion on …, 2012 - Taylor & Francis
Introduction: Perifosine is a novel targeted oral Akt inhibitor currently in Phase III clinical
development for treatment of colorectal cancer (CRC, in combination with capecitabine) and …

Perifosine: update on a novel Akt inhibitor

JJ Gills, PA Dennis - Current oncology reports, 2009 - Springer
Abstract The PI3K/Akt/mTOR pathway is aberrantly active in most human cancers and
contributes to cell growth, proliferation, and survival. Akt is a nodal regulator of cellular …

Current view on the mechanism of action of perifosine in cancer.

J Fensterle, B Aicher, I Seipelt, M Teifel… - Anti-cancer agents in …, 2014 - europepmc.org
Perifosine treatment exhibits a complex molecular response including the inhibition of Akt or
the induction of apoptosis via clustering of death receptors in lipid rafts. However, the …

Pharmacodynamic markers of perifosine efficacy

BT Hennessy, Y Lu, E Poradosu, Q Yu, S Yu, H Hall… - Clinical cancer …, 2007 - AACR
Purpose: It is critical to develop methods to quantify the early pharmacodynamic effects of
targeted therapeutics in vivo to make drug development more efficient and ensure …

Enhancing perifosine's anticancer efficacy by preventing autophagy

SY Sun - Autophagy, 2010 - Taylor & Francis
Our long-term research goal is to develop efficacious regimens for cancer therapy through
our understanding of cancer biology and drug mechanisms. Perifosine is an …

Perifosine, an oral bioactive novel alkylphospholipid, inhibits Akt and induces in vitro and in vivo cytotoxicity in human multiple myeloma cells

T Hideshima, L Catley, H Yasui, K Ishitsuka, N Raje… - Blood, 2006 - ashpublications.org
Perifosine is a synthetic novel alkylphospholipid, a new class of antitumor agents which
targets cell membranes and inhibits Akt activation. Here we show that baseline …

Proapoptotic activity and chemosensitizing effect of the novel Akt inhibitor perifosine in acute myelogenous leukemia cells

V Papa, PL Tazzari, F Chiarini, A Cappellini, F Ricci… - Leukemia, 2008 - nature.com
The serine/threonine kinase Akt, a downstream effector of phosphatidylinositol 3-kinase
(PI3K), is known to play an important role in antiapoptotic signaling and has been implicated …

Synergistic induction of apoptosis in human leukemia T cells by the Akt inhibitor perifosine and etoposide through activation of intrinsic and Fas-mediated extrinsic cell …

M Nyakern, A Cappellini, I Mantovani… - Molecular cancer …, 2006 - AACR
Perifosine is an Akt inhibitor displaying strong antineoplastic effects in human tumor cell
lines and is currently being tested in phase II clinical trials for treatment of major human …

Perifosine Inhibits Multiple Signaling Pathways in Glial Progenitors and Cooperates With Temozolomide to Arrest Cell Proliferation in Gliomas In vivo

H Momota, E Nerio, EC Holland - Cancer research, 2005 - AACR
Perifosine is an oral Akt inhibitor which exerts a marked cytotoxic effect on human tumor cell
lines, and is currently being tested in several phase II trials for treatment of major human …

The alkylphospholipid perifosine induces apoptosis of human lung cancer cells requiring inhibition of Akt and activation of the extrinsic apoptotic pathway

HA Elrod, YD Lin, P Yue, X Wang, S Lonial… - Molecular Cancer …, 2007 - AACR
The Akt inhibitor, perifosine, is an alkylphospholipid exhibiting antitumor properties and is
currently in phase II clinical trials for various types of cancer. The mechanisms by which …