TABLE 2.

Paclitaxel (PTX) formulations

Formulations	Manufacturer	Composition details	Regulatory status
Approved/marketed
Taxol®	Bristol-Myers Squibb	Each ml of sterile nonpyrogenic nonaqueous solution contains 6 mg paclitaxel, 527 mg of purified Cremophor® EL* (polyoxyethylated castor oil) and 49.7% (v/v) dehydrated alcohol, USP. Drug Loading: approximately 1% wt PTX	Approved in 1992 (Weaver, 2014)
Abraxane® (nab-paclitaxel; ABI-007)	Abraxis BioScience, Inc. (now Celgene)	Each single-dose vial contains 100 mg of paclitaxel (bound to human albumin) and approximately 900 mg of human albumin (containing sodium caprylate and sodium acetyl tryptophanate). Each milliliter (ml) of reconstituted suspension contains 5 mg paclitaxel formulated as albumin-bound NPs Drug loading: approximately 10% wt PTX	Approved by FDA in 2005 for metastatic breast. In 2012, approved for lung (NSCLC) and pancreatic cancer [FDA label]
Lipusu®	Luye Pharma Group Ltd.	Liposomes lecithin and cholesterol in a ratio of 87:13 wt% (Steffes et al., 2017; Ye et al., 2013)	Approved in China in 2003 for ovarian cancer, breast cancer, and nonsmall cell lung cancer (Ye et al., 2013)
Apealea® Paclical®	Oasmia Pharmaceutical AB	Micellar paclitaxel containing XR-17 (N-(all-trans-retinoyl)-l-cysteic acid methyl ester sodium salt and N-(13-cis-retinoyl)-l-cysteic acid methyl ester sodium salt t; Vergote et al., 2020) One vial of powder (Greenish yellow to yellow powder) contains 60 mg of paclitaxel. After reconstitution, each ml of solution contains 1 mg of paclitaxel (micellar)	Authorized for marketing by the European Commission in 2018. Apealea® in combination with Carboplatin is approved for the treatment of adult patients with the first relapse of platinum-sensitive epithelial ovarian cancer, primary peritoneal cancer, and fallopian tube cancer. Elevar Therapeutics licensed the global rights for Apealea® except for Nordics, Russia, and select CIS countries.
Genexol PM	Samyang Biopharmaceuticals Corporation	Lyophilized mPEG-PDLLA polymeric micellar formulation of paclitaxel. mPEG-PDLLA [monomethoxy-poly (ethylene glycol)-block-poly (d,l-lactide)] as solubilizer. Prepared with Samyang’s plant cell culture technology and proprietary polymeric micelle technology. Drug loading: approximately 16% wt PTX	Approved in South Korea in 2007
Clinical Trials
EndoTAG-1® (SB05PC)	Medigene SynCore Biotechnology Co., Ltd., Taipei, Taiwan	Paclitaxel [Liposomes containing cationic lipid dioleoyloxypropyltrimethyl ammonium (DOTAP) and neutral lipid (DOPC)] [DOTAP:DOPC:PTX in 50:47:3]	FDA grants orphan drug designation in 2009 Phase 3 clinical trial (NCT03126435 and NCT03002103) for locally advanced and/or metastatic adenocarcinoma of the pancreas
LEP-ETU (Liposome Entrapped Paclitaxel Easy to Use)	Neopharm Labs Sponsored by Insys Therapeutics	Paclitaxel (liposome composed of a 90:5:5 molar ratio of DOPC, cholesterol, and cardiolipin and a final total lipid to drug molar ratio of 33:1).	FDA granted Orphan Drug Designation in 2015 for Ovarian cancer
NK-105	NanoCarrier, Chiba, Japan	Self-assembled micellar formulation from PEG-poly (aspartic acid) (PEG-P[Asp]) modified with 4-phenyl-1-butanol to increase the hydrophobicity NK-105 was formulated as a freeze-dried formulation and administered as an infusion Drug loading: approximately 23% w/w. Average particle size of 85 nm (20–430 nm)	Phase 3 (NCT01644890) for treatment of metastatic breast cancer Phase 3 for recurrent gastric cancer.
Taxoprexin® (docosahexaenoic acid-paclitaxel conjugate)	Luitpold Pharmaceuticals, Inc.	Prodrug of PTX A prodrug composed of the naturally occurring omega-3 fatty acid (docosahexaenoic acid, DHA) covalently conjugated to paclitaxel. Contains 73% parent drug	Phase 3 study (in combination with Carboplatin in patients with Non-Small Cell Lung Cancer; NCT00243867)
Paclical® poliglumex (XYOTAX, CT-2103)	CTI Life Sciences, Ltd	Ester conjugate of α-poly (l)-glutamic acid (PGA) and paclitaxel Prodrug of PTX (consist of 37% parent drug) Reconstitution with 10 ml sterile water for injections yields a solution containing 9 mg/ml paclitaxel, in conjugated form with 5 mg/ml poloxamer 188, 20 mg/ml disodium phosphate, and 16 mg/ml sodium dihydrogen phosphate.	Phase 2 study (in combination with Capecitabine in patients with breast cancer; NCT00265733)
Paclitaxel-hyaluronic acid	Fidia Farmaceutici S.p.A.	Hyaluronic acid-Paclitaxel conjugate	Orphan drug designation in 2021 for treatment of Malignant Mesothelioma Phase I trial (NCT04798703)
ANG1005	Angiochem Inc	Paclitaxel is linked to angiopep-2 (brain peptide vector).	Open-label Phase 3 study n HER2-negative breast cancer patients with the newly diagnosed leptomeningeal disease and previously treated brain metastases. Phase 3 trial (NCT03613181)