Abstract

This review describes the clinical translation of cancer nanomedicines based on three nanocarrier platforms: liposomes, polymeric micelles, and nanoparticles. A dozen nanomedicines are on the market, the majority (eight) based on the most mature liposome technology. The other marketed nanomedicines are based on polymeric micelles (one) and nanoparticles (one). Polymeric prodrugs account for the remaining two marketed products. Altogether a total of 41 nanocarrier-based formulations have translated from the bench to the bedside and are under investigation at different levels of clinical development. Many more nanocarrier-based formulations are in preclinical development. Not surprisingly, the vast majority of these nanomedicines (37) rely on passive targeting through the EPR (enhanced permeability and retention) effect, avoiding the additional regulatory, production, cost of goods, and polydispersity challenges of active, ligand-receptor based targeting. Only four actively targeting nanocarriers are in clinical development, one using PSMA and three using TfR as the target. It still needs to be demonstrated that active targeting of nanocarriers that are subjected to the EPR effect provides an advantage substantial enough to justify the additional efforts. The review clearly identifies the areas of successful translation of nanomedicines but also shows areas where the potential is still underdeveloped and opportunities for improvement are promising. Overall, the high expectation that has been placed in nanomedicines is showing progress, increasing the benefits and treatment options for cancer patients.

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