Drug intelligence / Profile preview

AKI-001

Development stage
Preclinical
Lead developer
Genentech
Modality
Small Molecules
Administration
Oral (preclinical)
01

Overview

AKI-001 is a small molecule experimental drug that functions as a potent inhibitor of both Aurora A and Aurora B kinases (serine/threonine-protein kinase Aurora-A and Aurora-B). These kinases are critical regulators of mitosis and cell division. By inhibiting their activity at low nanomolar concentrations (IC50 < 100 nM), AKI-001 disrupts cell proliferation and exhibits strong antimitotic effects. Preclinical studies have demonstrated that the compound has good oral bioavailability and can significantly inhibit tumor growth in vivo. The drug was initially developed by Genentech for oncology indications but has not advanced beyond preclinical or early development stages[1][2][3][7].

Other names
8-ethyl-2,5,6,12-tetrahydro-3,10,10-trimethyl-9-oxopyrazolo(4',3'-6,7)cyclohepta(1,2-b)pyrrolo(2,3-f)indole
02

Targets

AURKA (Aurora kinase A)AURKB (Aurora kinase B)

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