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2012.04.04

Results of First Phase I Clinical Study for Intranasal Zolmitriptan Formulation (Migraine Drug)

Shin Nippon Biomedical Laboratories, Ltd. (SNBL) is currently developing an intranasal form of zolmitriptan (TRZ), a drug for relief of migraine headaches*1. SNBL today announces the completion and results of the first Phase I clinical study of TRZ.

[Summary]

The safety and pharmacokinetics of TRZ in 16 male and female healthy adult volunteers were evaluated by single administration of each of the three doses of TRZ (0.75, 1.5 and 3.0 mg), marketed zolmitriptan tablet (5 mg) and marketed zolmitriptan nasal spray (5 mg) at weekly intervals. The results were as follows:

1.Quick absorption of TRZ was confirmed. The concentration of zolmitriptan in blood increased swiftly after administration of TRZ, reaching maximum concentration (Cmax*2) within 20 minutes after administration. On the other hand, marketed zolmitriptan tablet and nasal spray showed Cmax at 120 minutes after administration. (See Figure)

2.Higher zolmitriptan absorption was shown in TRZ compared with the marketed drugs. Relative bioavailability*3 of TRZ was 136% compared with tablet and 182% compared with nasal spray.

3.Stable absorption of TRZ was demonstrated. The Cmax and AUC*4 of TRZ were dose dependent across the delivered doses.

4.TRZ was well tolerated in healthy volunteers.

Combined with the clinical results obtained for SNBL's nasal granisetron formulation (TRG), the results of this clinical study demonstrates the capability of SNBL's novel nasal drug delivery platform technology (μco™ System*5) to deliver a with a wide variety of drug compounds. Based on these results, SNBL expects more opportunities to partner with pharmaceutical companies to utilize μco™ System for a compound in development or for life-cycle-management*6 of existing drug products.

The effect of this study on the earnings of SNBL's current term is minimal.

trz_英グラフ.bmp

Figure: (Left) Mean blood concentration of zolmitriptan after administration of TRZ and marketed zolmitriptan products in healthy adult volunteers. (Right) Dose dependence of mean Cmax and AUCinf after administration of TRZ.

[References]
*1 Migraine headaches: Migraine headache is characterized by a thrusting pain that occurs on either side at the temple; it can also be accompanied by nausea. In severe cases, the pain is sufficient to have a significant impact on the regular lifestyle of patients. In the US, 28 million people (around 10% of the entire population) suffer from migraine headaches, while there are 8.4 million patients in Japan. The majority of migraine patients are between 20 and 40 years of age - at the height of their professional and personal lives - and these patients live in fear of the next strong migraine attack. Unmet needs remain among patients for a migraine drug with quick and consistent action that is also portable and easy to use.

*2 Cmax: Maximum drug concentration in the blood reached after dosing.

*3 Relative Bioavailability: Fraction of an administered dose of unchanged drug that reaches the systemic circulation when compared with another formulation of the same dose.

*4 AUC: Area Under the blood concentration time Curve of blood concentration vs time graph. This characterizes the total amount of drug that was absorbed by the body.

*5 μco™ System: SNBL's novel nasal drug delivery system consisting of a carrier formulation technology and intranasal devices.

*6 Life-cycle-management: A strategy to maximize the sales of the product at an appropriate time of the product life-cycle.

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