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Zelrix: a novel transdermal formulation of sumatriptan.
Mark Pierce1, Thomas Marbury, Carol O'Neill
1NuPathe-Research and Development, Conshohocken, PA 19428, USA.
Headache
|May 15, 2009
Summary
Zelrix, a novel sumatriptan transdermal patch, offers migraine relief by delivering therapeutic plasma levels comparable to other sumatriptan formulations. This iontophoretic patch was well-tolerated, showing mild skin reactions and avoiding gastrointestinal disturbances common in migraineurs.
Area of Science:
- Pharmacology and Drug Delivery
- Neurology and Headache Disorders
- Clinical Trials and Therapeutics
Background:
- Migraine is a debilitating neurological disorder often accompanied by gastrointestinal symptoms that complicate oral medication efficacy.
- Current sumatriptan formulations include oral, nasal, and subcutaneous options, but non-invasive, parenteral delivery methods are needed.
- Triptans, such as sumatriptan, target the trigeminal nerve pathway implicated in migraine pathophysiology.
Purpose of the Study:
- To evaluate the pharmacokinetic and tolerability profiles of Zelrix, a novel iontophoretic transdermal sumatriptan formulation.
- To compare the delivery of sumatriptan via transdermal patch to oral, subcutaneous, and nasal routes.
- To assess the safety and local skin reactions associated with the transdermal sumatriptan patch.
Main Methods:
- A Phase I, single-center, open-label, crossover study was conducted in healthy volunteers.
- Five treatment arms were compared: sumatriptan 100 mg oral, 6 mg subcutaneous, 20 mg nasal spray, and two Zelrix transdermal patch formulations (Zelrix I and II).
- Pharmacokinetic parameters including Cmax and AUC, along with tolerability and skin reactions, were assessed for each delivery method.
Main Results:
- Zelrix transdermal patches achieved sumatriptan plasma concentrations within the range of other formulations, reaching 10 ng/mL in approximately 30 minutes.
- Peak plasma concentrations (Cmax) for Zelrix were lower than subcutaneous sumatriptan, potentially reducing triptan-like sensations.
- Both Zelrix formulations were well-tolerated, with mild and transient skin reactions (erythema) at the patch site.
Conclusions:
- Iontophoretic transdermal sumatriptan (Zelrix) provides consistent drug delivery, achieving therapeutic plasma levels comparable to existing sumatriptan formulations.
- The transdermal delivery system offers a potentially beneficial alternative for migraineurs, bypassing gastrointestinal disturbances.
- Zelrix demonstrated a favorable tolerability profile with mild, transient adverse events, suggesting its potential utility in migraine management.
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