Table 6.
Examples of polymeric micelle-based drug products in clinical trials or approved.
| Product code name | API | Polymer | Physicochemical properties | Development Stage | Comments | Trial code and/or Ref. |
|---|---|---|---|---|---|---|
| Genexol® PM1 | Paclitaxel | mPEG-b-PDLLA | Size: 20–50 nm, LC: 16.7% | Approved in South Korea, Philippines, India, and Vietnam | Enabled higher doses of paclitaxel with decreased toxicity in phase I study, Improved overall response rate (58.5%) compared to that of Taxol® (21–54%) in patients with metastatic breast cancer in phase II study. | [9, 11] NCT00876486 NCT02064829 |
| Nanoxel® M1 | Docetaxel | mPEG-b-PDLLA | Size: 25.4 nm | Approved in South Korea | Comparable efficacy and superior safety profile compared to that of conventional docetaxel formulated in polysorbate 80 (Taxotere) [13] | NCT01336582 NCT02639858 |
| NK1052 | Paclitaxel | mPEG-b-modified P(Asp) | Size: 85 nm LC: 23% | Phase 3 (completed) | Improved plasma AUC of paclitaxel and reduced hypersensitivity reaction compared to conventional paclitaxel [238]. Failed to improve efficacy of paclitaxel in phase III study [307]. | NCT01644890 |
| NC-60043 | Cisplatin | PEG-b-P(Glu) coordination complex | Size: 28 nm LC: 39 % | Phase 3 (completed) | Improved safety profile and patient’s quality of life, while showed modest efficacy in phase II study [309]. | NCT02043288 |
| SP1049C4 | Doxorubicin | Pluronic® L61 and F127 | Size: < 30 nm LC: 8.2 % | Phase 2 (completed) | Shown efficacy of doxorubicin as a single agent in phase II study | [10, 17] |
| NK0125 | SN-38 | PEG-b-P(Glu) covalent drug-copolymer conjugate | Size: 20 nm LC: 20 % | Phase 2 (completed) | Showed efficacy in patients with sensitive relapsed small cell lung cancer and toxicity was manageable. | NCT00951054 NCT00951613 |
| CPC6346 (CriPec®) | Docetaxel | PEG-b-P(HPMAm-Lacn) covalent drug-copolymer conjugate | Size: 66 nm LC: 12 % | Phase 2 (recruiting) | Possible improved safety profile, skin toxicity was seen at high dose in phase I study | NCT02442531 NCT03742713 |
| NK9117 | Doxorubicin | PEG-b-P(Asp) covalent drug-copolymer conjugate | Size: 40 nm | Phase 1 (completed) | Comparable toxicity profile of doxorubicin to free doxorucin, No infusion-related reaction in phase I study | [146] |
| NC-40168 | Oxaliplatin | PEG-b-P(Glu) coordination complex | Size: 40 nm LC: 32 % | Phase 1 (completed) | No results available yet | NCT03168035 |
Developed by Samyang Biopharmaceuticals Corp.
originally developed by NanoCarrier Co., Ltd. and licensed to Nippon Kayaku Co., Ltd.
developed by NanoCarrier Co., Ltd. in collaboration with Orient Europharma Co., Ltd. (drug is bound to the P(Glu) block of the block copolymer via coordination bonds)
originally developed by Supratek Pharma Inc. and acquired by SoftKemo Pharma Corp. (now termed SKC1049)
developed jointly by NanoCarrier Co., Ltd. and Nippon Kayaku Co., Ltd. (SN-38 is chemically conjugated to the P(Glu) block of the copolymer)
developed by Cristal Therapeutics (cdocetaxel is covalently conjugated m-PEG-b-poly[N-(2-hydroxypropyl)methacrylamide lactate] (mPEG-b-p(HPMAm-Lacn) copolymer)
developed by Nippon Kayaku Co., Ltd. (doxorubicin is chemically conjugated to the P(Asp) block of the copolymer, and the free drug is solubilized in the micelles of the resulting conjugate)
developed by NanoCarrier Co., Ltd. (drug is bound to the P(Glu) block of the block copolymer via coordination bonds).