Drug intelligence / Profile preview

LY2780301 + paclitaxel

Development stage
Discontinued
Lead developer
Eli Lilly
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Oral, Intravenous
01

Overview

LY2780301 is a dual inhibitor of p70 ribosomal protein S6 kinase (p70S6K) and protein kinase B (AKT), both key components of the PI3K/AKT/mTOR signaling pathway, which is frequently activated in HER2-negative breast cancer. Paclitaxel is a well-established microtubule-stabilizing chemotherapeutic agent. The combination of LY2780301 with weekly paclitaxel has been investigated for the treatment of hormone-resistant HER2-negative advanced breast cancer, with preliminary evidence suggesting feasibility and efficacy in both the overall population and patients with activation of the PI3K/AKT pathway[1][2][3]. The recommended phase II dose was determined as LY2780301 500 mg once daily plus weekly paclitaxel 80 mg/m²[2].

Other names
LY2780301 and paclitaxelLY-2780301 and paclitaxelLY 2780301 and paclitaxelpaclitaxel plus LY2780301
02

Targets

RPS6KB1 (Ribosomal protein S6 kinase beta-1)TUBB (Tubulin (alpha and beta subunits))AKT (RAC-alpha serine/threonine-protein kinase)

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