Drug intelligence / Profile preview

miransertib

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

Overview

Miransertib is an orally bioavailable, selective, pan-AKT (protein kinase B) inhibitor that potently inhibits the AKT1, AKT2, and AKT3 isoforms. It acts in a non-ATP competitive manner by binding both inactive and active forms of AKT to prevent membrane localization and activation or directly inhibit activity. This results in inhibition of the PI3K/AKT signaling pathway, which is often deregulated in cancer and overgrowth disorders. Miransertib has been primarily developed for rare overgrowth conditions such as PIK3CA-related Overgrowth Spectrum (PROS) and Proteus syndrome, as well as being investigated for certain cancers including lymphoma and endometrial cancer. It has also shown potential activity against visceral and cutaneous leishmaniasis by enhancing mTOR-dependent autophagy in infected macrophages[1][3][4][5][6][7][8].

Other names
miransertibARQ 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)

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