Drug intelligence / Profile preview

miransertib + anastrozole

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

Overview

ARQ 092, also known as miransertib, is an orally available, potent, and selective pan-AKT inhibitor that targets AKT1 (IC50 = 5.0 nM), AKT2 (IC50 = 4.5 nM), and AKT3 (IC50 = 16 nM). It acts as an allosteric inhibitor of the AKT pathway by blocking membrane translocation of inactive AKT and dephosphorylating the active form at the membrane. This disrupts downstream signaling involved in cell proliferation and survival[4][6]. Anastrozole is a nonsteroidal aromatase inhibitor that decreases estrogen production by inhibiting the aromatase enzyme, thereby slowing or stopping growth of estrogen-dependent cancer cells[1]. The combination has been studied in clinical trials for advanced solid tumors including endometrial cancer[2].

Other names
miransertib + anastrozole
02

Targets

CYP19A1 (Aromatase)AKT2 (Rac-beta serine/threonine-protein kinase)AKT1 (Proto-oncogene serine/threonine-protein kinase Akt1)ESR1 (ERα)

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