Phase I study of the novel, fully synthetic epothilone sagopilone (ZK-EPO) in patients with solid tumors

Comparative Profiling of the Novel Epothilone, Sagopilone, in Xenografts Derived from Primary Non–Small Cell Lung Cancer

“…Sagopilone has been tested as monotherapy in a phase II clinical trial in platin-resistant NSCLC (25,55,56). Although the number of partial response has only been 5%, Sagopilone has induced SD in 43% to 45%.…”

Highlights of Natural Products in Prostate Cancer Drug Discovery

“…Phase I clinical trials established that the sagopilone side-effect profile was similar to that reported for taxanes, with neuropathy and neutropenia being the most commonly reported toxicities (Arnold et al, 2009, Schmid et al, 2010. A recommended dose for phase II studies was established at 16.53 mg/m 2 , once every 3 weeks (Schmid et al, 2010). Proof-of-concept has already been www.intechopen.com established in patients with platinum-resistant ovarian cancer and androgen-independent PC, and clinical responses have been shown in patients with melanoma and small-cell lung cancer.…”

“…Moreover, sagopilone was not recognized by multidrug-resistant (MDR) cellular efflux mechanisms, and maintained its activity in MDR tumor models. Phase I clinical trials established that the sagopilone side-effect profile was similar to that reported for taxanes, with neuropathy and neutropenia being the most commonly reported toxicities (Arnold et al, 2009, Schmid et al, 2010. A recommended dose for phase II studies was established at 16.53 mg/m 2 , once every 3 weeks (Schmid et al, 2010).…”

“…Proof-of-concept has already been www.intechopen.com established in patients with platinum-resistant ovarian cancer and androgen-independent PC, and clinical responses have been shown in patients with melanoma and small-cell lung cancer. Results are awaited from other ongoing trials (Schmid et al, 2010). Fig.…”

The anti-tumor agent sagopilone shows antiresorptive effects both in vitro and in vivo

“…Sagopilone has shown in vitro and in vivo activity at sub-nanomolar concentrations (IC 50 <1 nM) with balanced tolerability against a broad range of tumor models, including superior activity compared with paclitaxel in many breast cancer cell lines [7,9,10]. Sagopilone has also showed good potential in recently reported phase I and II clinical trials [11][12][13]. Furthermore, sagopilone was shown to have a dual inhibitory effect on bone metastases in the MDA-MB-231(SA) mouse model of breast cancer bone metastasis [14], indicating an inhibitory effect of this compound on both osteoclasts and tumor cells.…”