. Author manuscript; available in PMC: 2008 Nov 22.

Published in final edited form as: Adv Drug Deliv Rev. 2008 Feb 8;60(8):886–898. doi: 10.1016/j.addr.2007.11.009

Table 1.

Summary of clinical studies of PG-TXL (CT-2103)

Effect Studied	Status	Results	References
Safety and Pharmacokinetics	Phase Ia (n = 19 on 3- weekly schedule); Phase Ib (n = 11 on 2-weekly schedule)	Phase Ia: MTD, 233 mg/m²; DLT, neutropenia. Phase 1b: MTD, 177 mg/m²; DLT, neuropathy. Observed prolonged plasma half-life (>100 h) and low steady-state volume of distribution, indicating a distribution of PG-TXL restricted to plasma and extracellular fluids	[29]
Safety	Phase I (n = 22) PG-TXL used in combination with carboplatin; solid tumors	MTD, 250 mg/m²; DLTs, neutropenia and thrombocytopenia. 3 patients with ovarian cancer had partial responses	[30]
Safety	Phase I (n = 21) PG-TXL plus concurrent radiation; esophageal and gastric cancer	MTD, 70 mg/m²/week; DLTs, gastritis, esophagitis, eutropenia. 4 of 12 patients with loco-regional disease had a complete response; 7 patients had a partial response	[31]
Safety and Efficacy	Phase II (n = 99) patients with heavily pretreated ovarian cancer	Efficacy: Response rate in platinum-sensitive patients, 28%; in platinum-resistant patients, 10%. Toxicity: grade 3 neutropenia (15%); grade 4 neutropenia (9%); grade 2 neuropathy(15%); grade 3 neuropathy (15%)	[32]
Safety and Efficacy	Phase II (n = 18) patients with metastatic breast cancer	Efficacy: objective response 22%. Toxicity: grade 3/4 hypersensitivity reaction (22%); grade3/4 neuropathy (22%). The study was terminated due to unexpected high incident of hypersensitivity reaction	[33]
Safety and Efficacy	Phase II (n = 21) patients with androgen independent prostate cancer	Efficacy: 2 previously treated and 1 untreated pts responded based on a 50% PSA reduction. Toxicity: hypersensitivity reaction (1 pts), grade2/3 neuropathy (7 pts), grade 3/4 neutropenia (8 pts) and grade 3 thrombocytopenia (1 pts)	[34]
Efficacy	Phase III (n = 400) CT-2103 plus carboplatin compared to Taxol® plus carboplatin; STELLAR 3 trial in PS2 pts with NSCLC	Efficacy: no difference in the duration of overall survival. Women with estrogen >30 pg/dl had a significant survival benefit when receiving CT-2103 compared to women in control arm (10.2 vs. 5.5 mo; p = 0.039).	[18, 35, 36]
Efficacy	Phase III (n = 477) CT-2103 as a single agent compared to gemcitabine or vinorelbine; STELLAR4 trial in PS2 patients with NSCLC	Efficacy: no difference in the duration of overall survival. Combined analysis of STELLAR 3&4 shows median survival advantage for CT-2103 treated women <55 years old (10.0 vs. 5.2 mo, p = 0.038) compared with women in the control arm	[18, 35, 36]
Efficacy	Phase III (n = 850) CT-2103 as a single agent compared to docetaxel; STELLAR 2 trial in PS0-2 patients with NSCLC	Efficacy: no difference in the duration of overall survival as compared to the control arm	[18, 35]