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Table 2 Liposomal formulation present in clinical trials

From: Nanomedicine review: clinical developments in liposomal applications

LF

Active agent

Composition

Size (nm)

Indication

Status

References

ONPATTRO®

Patisiran (siRNA)

DLin-MC3-DMA, Cholesterol, DSPC, PEG2000-C-DMG

–

Hereditary transthyretin amyloidosis

Approved by FDA in August 2018

(Anselmo and Mitragotri 2019)

CPX-351 (Vyxeosâ„¢)

Daunorubicin + cytarabine

DSPC, DSPG, cholesterol (7:2:1) daunorubicin, cytarabine 5:1

100

Acute myeloid leukemia

Approved by FDA in 2017

(Ventola 2017; Lancet et al. 2014; Kaspers et al. 2013; Inman 2017)

Onivyde®

Irinotecan + fluorouracil + folinic acid

PEGylated liposome

80–140

Pancreatic adenocarcinoma

Approved by FDA in 2015

(Pelzer et al. 2017; Tran et al. 2017)

LEP-ETU

Paclitaxel

DOPC, cholesterol, cardiolipin (90:5:5)

Lipid, PTX (33:1)

150

Ovarian cancer

Not approved by FDA

(Bozzuto and Molinari 2015; Bulbake et al. 2017; Slingerland et al. 2017)

Marqibo®

Vincristine

Sphingomyelin, Cholesterol (60:40)

100

Non-Hodgkin’s lymphoma and leukemia

Approved by FDA in August 2012

(Bozzuto and Molinari 2015; Silverman and Deitcher 2013)

Exparel®

Bupivacaine

DEPC, DPPG, cholesterol, tricaprylin

3000–30,000

Pain management

Approved by FDA in 2011

(Bulbake et al. 2017; Yeung et al. 2018)

Mepact®

Mifamurtide

Non-PEGylated liposome, Muramyl tripeptide PE

–

Osteosarcoma

FDA 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 virus

DOPC, DOPE (75:25)

150

Influenza

Approved by European Medicines Agency (EMEA) in 2008

(Bulbake et al. 2017; Gasparini et al. 2013)

Genexol-PM

Paclitaxel

PEG–PLA polymeric micelle

20–50

Breast, lung and ovarian cancer

Approved 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)

150

Hepatitis A

Approved in 2006 and is currently used in Switzerland and Argentina

(Bulbake et al. 2017; Lim et al. 2014)

Lipusu®

Paclitaxel

72 g PC, 10.8 cholesterol in ethanol

400

Gastric, ovarian and lung cancer

Approved by FDA in 2005

(Xu et al. 2013; Ye et al. 2013)

DepoDurâ„¢

Morphine sulfate

Cholesterol, triolein, DOPC, DPPG (11:1:7:1)

17,000–23,000

Pain management

Approved by FDA in 2004

(Bulbake et al. 2017; Carvalho et al. 2007)

Lipo-Dox®

Doxorubicin

DSPC, cholesterol, PEG 2000-DSPE (56:39:5)

20

Breast and ovarian cancer

Approved by FDA in 2012

(Bozzuto and Molinari 2015; Smith et al. 2016)

Myocet®

Doxorubicin + cyclophosphamide

EPC, cholesterol (55:45)

190

Metastatic breast cancer

Approved by EMEA in 2000

(Bozzuto and Molinari 2015; Eitan et al. 2014)

Visudyne®

Verteporphin

EPG, DMPC (3:5)

100

Ocular histoplasmosis

Approved by FDA in 2000

(Bozzuto and Molinari 2015; Jain et al. 2016)

Depocyt®

Cytarabine

Cholesterol, triolein, DOPC, DPPG (11:1:7:1)

20

Neoplastic meningitis

FDA status: discontinued

(Bozzuto and Molinari 2015; Phuphanich et al. 2006)

Abelcet®

Amphotericin B

DMPC, DMPG (7:3)

600–11,000

Invasive fungal infection

Approval FDA in 1995

(Bozzuto and Molinari 2015; Bulbake et al. 2017)

Amphotec®

Amphotericin B

Cholesteryl sulfate

–

FDA status: discontinued

(Clemons and Stevens 2004)

DaunoXome®

Daunorubicin

DSPC, cholesterol, daunorubicin (10:5:1)

45–80

Leukemia

FDA status: discontinued

(Olusanya et al. 2018; Kraft et al. 2014; Kaspers et al. 2013)

Doxil®

Doxorubicin

HSPC, cholesterol, PEG 2000-DSPE (56:39:5)

100

Kaposi’s sarcoma

Approved by FDA in 1995

(Bozzuto and Molinari 2015; Kohli et al. 2014)

AmBisome®

Amphotericin B

HSPC, DSPG, cholesterol, amphotericin B (2:0.8:1:0.4)

45–80

Invasive fungal infection

Approved by FDA in 1997

(Bozzuto and Molinari 2015; Bulbake et al. 2017)

Thermodox®

Doxorubicin

DPPC, MSPC, PEG 2000-DSPE (90:10:14)

175

Hepatocellular carcinoma, solid tumors

Not approved

(Bozzuto and Molinari 2015; Lombardo et al. 2016; Chang and Yeh 2012)

EndoTAG®

Paclitaxel

DOTAP, DOPC, PTX (50:47:3)

180–200

Breast cancer

Not approved

(Bozzuto and Molinari 2015; Bulbake et al. 2017; Strieth et al. 2013)

MM-302

Doxorubicin

DSPE, HER2, PEG

75–110

Breast cancer

Not approved

(Miller et al. 2016)

PTX–LDE

Paclitaxel

135 mg cholesteryl oleate, 333 mg egg PC, 132 mg miglyol 812 N, 6 mg cholesterol, 60 mg PTX

1–1000

Epithelial ovarian carcinoma

Not approved

(Graziani et al. 2017; Jin et al. 2016)

Arikace®

Amikacin

DPPC, cholesterol (2:1)

≈ 300

Lung infections

Not approved

(Rose et al. 2014; Olivier et al. 2017)

MRX34

miR-34a

DOTAP, cholesterol

≈ 110

Advanced solid tumors and hematological malignances

Not approved

(Shi et al. 2017; Beg et al. 2016; Li et al. 2013)

Xemys

Myelin basic proteins

Egg PC, monomannosyl dioleoyl glycerol, α-tocopherol and lactose

–

Multiple sclerosis

Not 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