Drug intelligence / Profile preview

LY326020

Development stage
Unknown
Lead developer
Eli Lilly
Modality
Small Molecules
Administration
Oral
01

Overview

LY326020 is the major active metabolite of **enzastaurin**, an orally administered small molecule and serine/threonine kinase inhibitor targeting protein kinase C (PKC) and AKT pathways. LY326020 is formed in vivo during the metabolism of enzastaurin and is pharmacologically active, displaying similar exposure (AUC and steady-state plasma concentrations) as the parent drug. The mechanism of action includes inhibition of PKC and AKT signaling, leading to anti-tumor and anti-angiogenic effects. Enzastaurin (and thus LY326020) has been investigated primarily in oncology, including for malignant glioma and other solid tumors, primarily as part of clinical trials[1][3][7][9].

02

Targets

PRKCB (Protein kinase C beta)

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