Butorphanol
Clinical Need
Approximately 30 million people in the United States suffer an estimated 163 million migraine attacks each year. Approximately 60 percent of people with migraines have one or more debilitating attacks each month. In 2004, 27 million prescriptions were written for migraines in the United States, translating into $2 billion in sales for antimigraine preparation. Nevertheless, migraines tend to be under-diagnosed and under-treated, with 30 percent of patients ending therapy after their first treatment.
Product Benefit
We have developed a butorphanol tartrate nasal spray for the treatment of acute, moderate-to-severe pain through Phase II clinical development.
ITI’s butorphanol nasal product is designed to act quickly and provide rapid relief for migraine sufferers. Delivered via unit dose devices, this spray allows for more accurate dosing to improve therapeutic outcomes and predictability over existing nasal butorphanol products. In addition, the product’s unit dose delivery device allows for controlled intake and limits abuse potential.
Development Status
ITI has submitted an IND to meet requirements for a Section 505(b)(2) NDA. In addition, we completed three Phase I studies and one Phase II pilot efficacy study that included a total of 119 subjects. These studies demonstrated that in healthy, adult volunteers, intranasal butorphanol was absorbed rapidly, and bioavailability compared to an IV dose was approximately 78% to 80%. In the Phase II study using a dental pain model, intranasal butorphanol provided safe, dose-related pain relief. No clinically serious adverse events were reported. Additional information can be found in our publications.
We also have completed stability work which demonstrates that butorphanol tartrate nasal spray is a stable formulation for two years when stored at ambient room temperature.
As a result of our End-of-Phase 2 meeting with the FDA, butorphanol is ready for its final stage of clinical development.
ITI Publications
Davis GA, Rudy AC, Archer SM, Wermeling DP. Pharmacokinetics of butorphanol tartrate administered from single-dose intranasal sprayer. Am J Health-Syst Pharm 2004;61(2):261-266.
Davis GA, Rudy AC, Archer SM, Wermeling DP. Bioavailability of Intranasal Butorphanol Administered From A Single-Dose Sprayer. Am J Health-Syst Pharm 2005; 62:48-53.
Wermeling DP, Grant GM, Lee A, Alexander N, Rudy AC. Analgesic effects of intranasal butorphanol tartrate administered via a unit-dose device in the dental impaction pain model: a randomized, double-blind, placebo-controlled, parallel-group study. Clin Ther 2005;27(4):430-440.
