Review Article

Targeted Delivery System of Nanobiomaterials in Anticancer Therapy: From Cells to Clinics

Table 2

Nanomedicines in clinical trials.

Nanoplatforms DrugCurrent statusMode of delivery*Ligand/targetAverage size
(nm)
DescriptionsTypes of cancer

LiposomesDoxorubicin
(Myocet)
Phase IIINT100–230No IRRs, high response, and reduced cardiotoxicityKaposi’s sarcoma and
metastatic breast cancer (phase I/II)
Vincristine sulfate
(Marqibo)
FDA approved (Ph-adult ALL), Phase II (NHL), Phase I (pediatric ALL)NT115Extended PKAcute lymphocytic leukemia (ALL) and non-Hodgkin’s lymphoma (NHL)
Cytarabine
Daunorubicin (CPX-351)
Phase IIINT100Extended PK, high responseAcute myeloid leukemia (AML)
Paclitaxel
(EndoTAG-1)
Phase IIINT160–180Cationic liposomal formulation Various solid tumors
Lurtotecan
(OSI-211/NX211)
Phase II completedNT150Reduced myelosuppression and high responseOvarian cancer
Paclitaxel
(LEP-ETU)
Phase II completedNT150No IRRs and high responseMetastatic breast cancer
Camptothecin
(S-CKD-602)
Phase I/IINT100Pegylated liposomal camptothecin and extended PKAdvanced solid tumors
Oxaliplatin
(MBP-426)
Phase I/IITtransferrin/transferrin receptor180Extended PKAdvanced/metastatic
solid tumors
Doxorubicin
(MCC-465)
Phase I
(discontinued)
TF(ab′)2 fragment of human mAb GAH or tumor-specific antigen140No hand-foot syndrome or cardiotoxicityMetastatic stomach cancer
p53 gene
(SGT53-01)
Phase IbTscFv/transferrin receptor90Improved responseSolid tumors
RB94 plasmid DNA (SGT-94)Phase ITscFv/transferrin receptor108Improved responseSolid tumors
Doxorubicin
(MM-302)
Phase ITscFv/ErbB2 (HER2)75–110Advanced breast cancer
Melanoma antigens and IFNγ (Lipovaxin-MM)Phase ITSingle domain antibody (dAb) fragment (VH)/DC-SIGNStable and safeMelanoma vaccine

PolymersPaclitaxel
(Genexol-PM)
Approved (Korea); phase II/III (USA)NT<50Polymeric micelles, increased paclitaxel MTD, high responseMetastatic breast cancer and urothelial carcinoma
Paclitaxel
(NK105)
Phase IIINT85Core-shell-type polymeric micelles, extended PK, high response, and reduced hypersensitivity Metastatic/recurrent breast cancer

PolymersDoxorubicin (SP1049C)Phase I completedNT30Polymeric micelles,
high response, and no hand-foot syndrome
Advanced adenocarcinoma of esophagus and gastroesophageal system
Doxorubicin
(NK911)
Phase II (Asia)NT40Polymeric micelles,
extended PK
Metastatic/recurrent solid tumors
Paclitaxel-poliglumex
(Opaxio)
Phase IIINT10–150Polymeric micelles, extended PKOvarian cancer
Campthotecin (CRLX101)Phase Ib/IIaNT20–50A pH-sensitive polymer nanocarrier releasing camptothecin in the acidic environment of cancer cells, extended PK, and high responseAdvanced solid tumors
Irinotecan
(SN-38, NK012)
Phase I/IINT20Polymeric micelle-based active metabolites of camptothecin derivative and extended PKSolid tumors
Cisplatin
(NC-6004, Nanoplatin)
Phase I/II (Asia)NT30Polymeric micelles and extended PK (with the aim of reducing kidney toxicity compared with cisplatin alone)Advanced/metastatic pancreatic cancer (evaluating nanoplatin in combination with gemcitabine in patients with advanced or metastatic pancreatic cancer)
Docetaxel
(BIND-014)
Phase I completedTPeptide/PSMA
(solid or metastatic prostate cancer cells by binding to prostate-specific membrane antigen)
100Enhanced therapeutic efficacy and partial responseSolid tumors
RRM2 siRNA (CALAA-01)Phase ITTransferrin/transferrin receptor70Cyclodextrin-based nanoparticle containing anti-RRM2 siRNA and no DLTsSolid tumors

PK: pharmacokinetics; DRR: drug release rate; IRRs: infusion-related reactions; Ph-: Philadelphia Chromosome Negative; MTD: maximum tolerable dose; DLTs: dose-limiting toxicities; DC: dendritic cell.
*Mode of delivery: NT: nontargeted (passive targeting), T: targeted (active targeting).