Drug intelligence / Profile preview

miransertib + paclitaxel

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

Overview

Miransertib (ARQ 092) is an orally bioavailable, selective pan-AKT (protein kinase B) inhibitor that potently inhibits the AKT1, AKT2, and AKT3 isoforms. It acts as a non-ATP competitive allosteric inhibitor by binding to both inactive and active forms of AKT, preventing membrane localization and activation of the kinase. This results in inhibition of the PI3K/AKT signaling pathway—a pathway frequently deregulated in cancer—leading to reduced tumor cell proliferation and increased apoptosis[1][6][7][8]. Paclitaxel is a well-established microtubule-stabilizing chemotherapeutic agent used for various cancers. The combination of miransertib (ARQ 092) with paclitaxel has demonstrated enhanced antitumor activity compared to either agent alone in preclinical breast cancer models[4]. Miransertib has been investigated for use in solid tumors with activated PI3K/AKT pathways as well as rare overgrowth syndromes such as Proteus syndrome[7].

Other names
AKT inhibitor 2ARQ 092 Free BaseARQ092 Free BaseARQ-092 Free Base
02

Targets

AKT2 (Rac-beta serine/threonine-protein kinase)AKT1 (Proto-oncogene serine/threonine-protein kinase Akt1)TUBB (Tubulin (alpha and beta subunits))

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