Drug intelligence / Profile preview

vevorisertib

Development stage
Preclinical
Lead developer
Merck
Modality
Small Molecules
Administration
Oral
01

Overview

Vevorisertib (ARQ 751) is an orally bioavailable, potent, and selective small molecule inhibitor of the serine/threonine kinase AKT (also known as protein kinase B), targeting all three isoforms: AKT1, AKT2, and AKT3. It acts by blocking phosphorylation of AKT, thereby inhibiting the PI3K/AKT/mTOR signaling pathway that is frequently activated in various cancers. Vevorisertib has been investigated primarily for the treatment of advanced solid tumors and hepatocellular carcinoma (HCC), both as a monotherapy and in combination with other agents such as sorafenib or paclitaxel. The drug was originally developed by ArQule and later by Merck & Co. Clinical development reached phase 1 trials but was terminated due to business decisions[1][4][5][6][7].

Brand names
vevorisertib
Other names
1416775-46-6V6SX910Y31V-6SX910Y31V 6SX910Y31UNII-V6SX910Y31UNII-V-6SX910Y31UNII-V 6SX910Y31
02

Targets

AKT2 (Rac-beta serine/threonine-protein kinase)AKT1 (Proto-oncogene serine/threonine-protein kinase Akt1)

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