Drug intelligence / Profile preview

uprosertib

Development stage
Phase 2
Lead developer
Laekna
Modality
Small Molecules
Administration
Oral
01

Overview

Uprosertib is an orally bioavailable, investigational small molecule inhibitor of the serine/threonine protein kinase Akt (also known as protein kinase B or PKB). It acts as a potent pan-Akt inhibitor, targeting all three isoforms (Akt1, Akt2, and Akt3) with nanomolar potency. By inhibiting Akt activity, uprosertib disrupts the PI3K/Akt signaling pathway—a pathway frequently dysregulated in cancer—leading to reduced tumor cell proliferation and increased apoptosis. Uprosertib has been studied primarily for its antineoplastic potential in various solid tumors and hematologic malignancies. Clinical development has included monotherapy and combination regimens (notably with trametinib), but poor tolerability and limited efficacy have led to discontinuation in several indications[1][2][3][4][5].

Brand names
uprosertib
Other names
uprosertib
02

Targets

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

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