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. 2016 Jul;68(3):701–787. doi: 10.1124/pr.115.012070

TABLE 2.

Liposomal formulations of anticancer drugs in phase I clinical trials

Product Name Encapsulated Drugs Type of Liposomes Indications Lipid Composition Particle Size Status Reference
nm
Alocrest Vinorelbine Optisomes NSCLC and breast cancers, non-Hodgkin’s lymphoma, Hodgkin’s disease Sphingomyelin and cholesterol Phase I NCT00364676a (accessed on 14/4/15); Semple et al. (2005); Cattaneo et al. (2010);
Aroplatin Analog of cisplatin MLVs Advanced pancreatic and colorectal cancer, malignant pleural mesothelioma, advanced solid malignancies DMPC and DMPG Phase I/II NCT00043199a (accessed on 14/4/15); Lu et al. (2005); Dragovich et al. (2006)
ATI-1123 Docetaxel Protein stabilized liposomes NSCLC, gastric, pancreatic cancer, and soft tissue sarcoma Phospholipids, cholesterol, human serum albumin, and sucrose 60-80 Phase I Mahalingam et al. (2014)
Brakiva (TLI) Topotecan Optisomes Small cell lung, ovarian cancers and advanced solid tumors Sphingomyelin and cholesterol 100 Phase I NCT00765973a (accessed on 14/4/15); Tardi et al. (2000)
NanoVNB Vinorelbine PEGylated liposomes Advanced solid tumors DSPC, DSPE-PEG2000Da, cholesterol 98 Phase I Yang et al. (2012b); Lin et al. (2013)
MCC-465 Doxorubicin Antibody conjugated PEGylated liposomes Stomach cancer DPPC, maleimidated DPPE, PEG, GAH 143 Phase I Hamaguchi et al. (2004); Matsumura et al. (2004)
SGT-53 p53 DNA plasmid Anti-TfR conjugated cationic liposomes Solid tumors DOTAP and DOPE 114 Phase I NCT0047061a (accessed on 15/4/15); Xu et al. (2001); Camp et al. (2013); Kim et al. (2015)
TKM-080301 (TKM-PLK1) PLK1 siRNA Cationic PEGylated liposomes Gastrointestinal neuroendocrine tumors, adrenocortical carcinoma, hepatocellular carcinoma DSPC, DLin-MC3-DMA, DMG-PEG, and cholesterol 80-140 Phase I/II NCT01262235a (accessed on 15/4/15); Tam et al. (2013); Leung et al. (2014)
a

ClinicalTrials.gov identifier

DMPC, 1,2-dimyristoyl phosphatidylcholine; DMPG, 1,2-dimyristoyl phosphatidylglycerol; DPPE, 1,2-dipalmitoyl phosphatidylethanolamine; GAH, human monoclonal antibody; NSCLC, non-small cell lung cancer; DLin-MC3-DMA, heptatriaconta-6,9,28,31-tetraen-19-yl 4-(dimethylamino)butanoate; DMG-PEG, polyethylene glycol-dimyristolglycerol; TfR, transferrin receptor