Drug intelligence / Profile preview

everolimus + pegylated liposomal doxorubicin

Development stage
Unknown
Lead developer
Novartis
Modality
Nanoparticles → Drug Delivery Systems, Small Molecules
Administration
Oral, Intravenous
01

Overview

everolimus + pegylated liposomal doxorubicin is a combination therapy investigated for the treatment of advanced solid tumors. Everolimus (RAD001) is a small molecule inhibitor of the mammalian target of rapamycin (mTOR), specifically the mTORC1 complex, which plays a central role in regulating cell growth, proliferation, and survival. Pegylated liposomal doxorubicin (Caelyx) is a formulation of the anthracycline doxorubicin encapsulated in liposomes, which improves its pharmacokinetic profile and reduces cardiotoxicity. Doxorubicin acts by intercalating into DNA and inhibiting topoisomerase II, leading to DNA damage and apoptosis. This combination was evaluated in a Phase 1 dose-finding study conducted by the Southern Europe New Drug Organization (SENDO) to establish the safety, tolerability, and recommended dose in patients with advanced malignancies.

Brand names
CaelyxAfinitorZortress
Other names
RAD001 + CaelyxEverolimus + PLDpegylated liposomal doxorubicinPLD
02

Targets

mTOR (Mammalian target of rapamycin kinase)DNATOP2A (DNA topoisomerase II)

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