Drug intelligence / Profile preview

Nanolipolee-007

Development stage
Preclinical
Lead developer
Cipher Pharmaceuticals
Modality
Lipid-based Nanoparticles → Nanoparticles → Drug Delivery Systems, Small Molecules
Administration
Intravenous
01

Overview

Nanolipolee-007 is an intravenously administered PEGylated nanoliposomal formulation of the plant‑derived diterpene leelamine, developed as a first‑in‑class cholesterol‑transport inhibitor for the treatment of melanoma.[10][4] By encapsulating leelamine in a neutral liposome composed of egg phosphatidylcholine and PEGylated phosphoethanolamine, Nanolipolee-007 improves the solubility, stability, and safety profile of leelamine, enabling systemic delivery that is not feasible with the free drug due to poor bioavailability and hemolytic toxicity.[10] Mechanistically, the released leelamine disrupts intracellular cholesterol transport, leading to simultaneous inhibition of PI3K/Akt, STAT3, and MAPK signaling pathways that are key drivers of melanoma cell survival, proliferation, and angiogenesis, resulting in preferential killing of melanoma cells and marked tumor growth inhibition in xenograft models with negligible major organ toxicity.[10][1][9] The agent originated from research at The Pennsylvania State University and was further developed by Melanovus Oncology and Cipher Pharmaceuticals as a preclinical candidate for advanced melanoma and potentially other skin cancer indications.[1][3][4][12]

Other names
Nanolipolee-007Nanolipolee007Nanolipolee 007
02

Targets

AKT (RAC-alpha serine/threonine-protein kinase)STAT3 (Signal Transducer and Activator of Transcription 3)MAPK3 (Mitogen-activated protein kinase 1)PI3K (Phosphoinositide-3-kinase regulatory subunit 6)

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