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|Solubility||DMSO>96mg/mL Water<1mg/mL Ethanol>96mg/mL|
|Storage||at -20°C 2 years|
|PD0325901 is MEK inhibitor and non-competitive with ATP, Kiapp of 1 nM against activated MEK1 and MEK2.|
|Solubility (25°C)*||In vitro||DMSO||96 mg/mL (199.09 mM)|
|Water||<1 mg/mL (<1 mM)|
|Ethanol||40 mg/mL (82.95 mM)|
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Phase II clinical trials was published in 2010. The study propose was to evaluate the efficacy of mitogen-activated protein kinase/extracellular signal-related kinase kinase inhibitor PD0325901 in advanced non–small cell lung cancer patients who had experienced treatment failure after, or were refractory to, standard systemic therapy. All patients had received prior systemic therapy (median of two regimens, including epidermal growth factor receptor inhibitors in 26%). Of 13 patients treated on schedule A, three discontinued due to adverse events (blurred vision, fatigue, and hallucinations, respectively). Twenty-one patients received schedule B. Main toxicities included diarrhea, fatigue, rash, vomiting, nausea, and reversible visual disturbances. Hematologic toxicity consisted mainly of mild-to-moderate anemia, without neutropenia. Chemistry abnormalities were rare. Mean (coefficient of variation) PD0325901 trough plasma concentrations were 100 ng/mL (52%) and 173 ng/mL (73%) for schedules A and B, respectively, above the minimum target concentration established in preclinical studies (16.5 ng/mL). There were no objective responses. Seven patients had stable disease. Median (95% confidence interval) progression-free survival was 1.8 months (1.5-1.9) and overall survival was 7.8 months (4.5-13.9). Conclusions: PD0325901 did not meet its primary efficacy end point. Future studies should focus on PD-0325901 schedule, rational combination strategies, and enrichment of patient selection based on mode of action.
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