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Table 2 Liposomal formulation present in clinical trials

From: Nanomedicine review: clinical developments in liposomal applications

LFActive agentCompositionSize (nm)IndicationStatusReferences
ONPATTRO®Patisiran (siRNA)DLin-MC3-DMA, Cholesterol, DSPC, PEG2000-C-DMGHereditary transthyretin amyloidosisApproved by FDA in August 2018(Anselmo and Mitragotri 2019)
CPX-351 (Vyxeos™)Daunorubicin + cytarabineDSPC, DSPG, cholesterol (7:2:1) daunorubicin, cytarabine 5:1100Acute myeloid leukemiaApproved by FDA in 2017(Ventola 2017; Lancet et al. 2014; Kaspers et al. 2013; Inman 2017)
Onivyde®Irinotecan + fluorouracil + folinic acidPEGylated liposome80–140Pancreatic adenocarcinomaApproved by FDA in 2015(Pelzer et al. 2017; Tran et al. 2017)
LEP-ETUPaclitaxelDOPC, cholesterol, cardiolipin (90:5:5)
Lipid, PTX (33:1)
150Ovarian cancerNot approved by FDA(Bozzuto and Molinari 2015; Bulbake et al. 2017; Slingerland et al. 2017)
Marqibo®VincristineSphingomyelin, Cholesterol (60:40)100Non-Hodgkin’s lymphoma and leukemiaApproved by FDA in August 2012(Bozzuto and Molinari 2015; Silverman and Deitcher 2013)
Exparel®BupivacaineDEPC, DPPG, cholesterol, tricaprylin3000–30,000Pain managementApproved by FDA in 2011(Bulbake et al. 2017; Yeung et al. 2018)
Mepact®MifamurtideNon-PEGylated liposome, Muramyl tripeptide PEOsteosarcomaFDA denied approval 2007. This medicine is authorized for use in the European Union(Shi et al. 2017; Sinatra et al. 2014)
Inflexal V®Inactivated hemagglutinin of A or B influenza virusDOPC, DOPE (75:25)150InfluenzaApproved by European Medicines Agency (EMEA) in 2008(Bulbake et al. 2017; Gasparini et al. 2013)
Genexol-PMPaclitaxelPEG–PLA polymeric micelle20–50Breast, lung and ovarian cancerApproved in Korea and marketed in Europe in 2007(Ahn et al. 2014; Tran et al. 2017)
Epaxal®Inactivated hepatitis A virus (strain RGSB)DOPC, DOPE (75:25)150Hepatitis AApproved in 2006 and is currently used in Switzerland and Argentina(Bulbake et al. 2017; Lim et al. 2014)
Lipusu®Paclitaxel72 g PC, 10.8 cholesterol in ethanol400Gastric, ovarian and lung cancerApproved by FDA in 2005(Xu et al. 2013; Ye et al. 2013)
DepoDur™Morphine sulfateCholesterol, triolein, DOPC, DPPG (11:1:7:1)17,000–23,000Pain managementApproved by FDA in 2004(Bulbake et al. 2017; Carvalho et al. 2007)
Lipo-Dox®DoxorubicinDSPC, cholesterol, PEG 2000-DSPE (56:39:5)20Breast and ovarian cancerApproved by FDA in 2012(Bozzuto and Molinari 2015; Smith et al. 2016)
Myocet®Doxorubicin + cyclophosphamideEPC, cholesterol (55:45)190Metastatic breast cancerApproved by EMEA in 2000(Bozzuto and Molinari 2015; Eitan et al. 2014)
Visudyne®VerteporphinEPG, DMPC (3:5)100Ocular histoplasmosisApproved by FDA in 2000(Bozzuto and Molinari 2015; Jain et al. 2016)
Depocyt®CytarabineCholesterol, triolein, DOPC, DPPG (11:1:7:1)20Neoplastic meningitisFDA status: discontinued(Bozzuto and Molinari 2015; Phuphanich et al. 2006)
Abelcet®Amphotericin BDMPC, DMPG (7:3)600–11,000Invasive fungal infectionApproval FDA in 1995(Bozzuto and Molinari 2015; Bulbake et al. 2017)
Amphotec®Amphotericin BCholesteryl sulfateFDA status: discontinued(Clemons and Stevens 2004)
DaunoXome®DaunorubicinDSPC, cholesterol, daunorubicin (10:5:1)45–80LeukemiaFDA status: discontinued(Olusanya et al. 2018; Kraft et al. 2014; Kaspers et al. 2013)
Doxil®DoxorubicinHSPC, cholesterol, PEG 2000-DSPE (56:39:5)100Kaposi’s sarcomaApproved by FDA in 1995(Bozzuto and Molinari 2015; Kohli et al. 2014)
AmBisome®Amphotericin BHSPC, DSPG, cholesterol, amphotericin B (2:0.8:1:0.4)45–80Invasive fungal infectionApproved by FDA in 1997(Bozzuto and Molinari 2015; Bulbake et al. 2017)
Thermodox®DoxorubicinDPPC, MSPC, PEG 2000-DSPE (90:10:14)175Hepatocellular carcinoma, solid tumorsNot approved(Bozzuto and Molinari 2015; Lombardo et al. 2016; Chang and Yeh 2012)
EndoTAG®PaclitaxelDOTAP, DOPC, PTX (50:47:3)180–200Breast cancerNot approved(Bozzuto and Molinari 2015; Bulbake et al. 2017; Strieth et al. 2013)
MM-302DoxorubicinDSPE, HER2, PEG75–110Breast cancerNot approved(Miller et al. 2016)
PTX–LDEPaclitaxel135 mg cholesteryl oleate, 333 mg egg PC, 132 mg miglyol 812 N, 6 mg cholesterol, 60 mg PTX1–1000Epithelial ovarian carcinomaNot approved(Graziani et al. 2017; Jin et al. 2016)
Arikace®AmikacinDPPC, cholesterol (2:1)≈ 300Lung infectionsNot approved(Rose et al. 2014; Olivier et al. 2017)
MRX34miR-34aDOTAP, cholesterol≈ 110Advanced solid tumors and hematological malignancesNot approved(Shi et al. 2017; Beg et al. 2016; Li et al. 2013)
XemysMyelin basic proteinsEgg PC, monomannosyl dioleoyl glycerol, α-tocopherol and lactoseMultiple sclerosisNot approved(Jr et al. 2016)
  1. LF liposomal formulation, siRNA small interfering RNA, DLin-MC3-DMA (6Z,9Z,28Z,31Z)-heptatriaconta-6,9,28,31-tetraen-19-yl-4-(dimethylamino)butanoate, PEG2000-C-DMG α-(30-{[1,2-di(myristyloxy)propanoxy] carbonylamino}propyl)-ω-methoxy polyoxyethylene, DSPC distearoyl phosphatidylcholine, DSPG distearoyl phosphatidylglycerol, DOPC dioleoyl phosphatidylcholine, DPPG dipalmitoyl phosphatidylglycerol, DOPE dioleoyl phosphatidylethanolamine, PC phosphatidylcholine, PEG 2000-DSPE polyethylene glycol 2000-distearoyl phosphatidylethanolamine, EPC ethyl phosphatidylcholine, EPG ethyl phosphatidylglycerol, DMPC dimyristoyl phosphatidylcholine, DMPG dimyristoyl phosphatidylglycerol, HSPC hydrogenated soybean phosphatidylcholine, MSPC monostearoyl phosphatidylcholine, DOTAP dioleoyl trimethylammonium-propane, HER2 human epidermal growth factor receptor 2, DPPC dipalmitoyl phosphatidylcholine, PTX paclitaxel, IU investigational use