Key Patents Covering Bosulif Production
Bosulif (bosutinib), made by Pfizer, is protected by patents on its chemical structure, synthesis methods, and formulations used in manufacturing the drug for chronic myeloid leukemia treatment. Core production-related patents include:
- US 7,342,013: Covers bosutinib monohydrate, the active form in Bosulif tablets, including crystallization processes for production.[1]
- US 8,461,173: Details methods for preparing bosutinib intermediates and purification steps essential for large-scale synthesis.[1]
- US 9,150,552: Protects crystalline forms and manufacturing processes to ensure drug stability during production.[1]
These focus on synthetic routes starting from quinoline and aniline derivatives, with steps like coupling, hydrolysis, and salt formation.
When Do Bosulif Patents Expire?
Primary composition-of-matter patent (US 7,342,013) expires in 2026, adjusted for pediatric extensions. Method patents extend to 2027-2030. Pfizer lists no later production patents blocking generics until then.[1][2]
| Patent Number | Title/Description | Expiration (US) |
|---------------|-------------------|-----------------|
| US 7,342,013 | Bosutinib monohydrate production | 2026 |
| US 8,461,173 | Synthesis intermediates | 2027 |
| US 9,150,552 | Crystalline forms manufacturing | 2029 |
Are There Active Challenges to These Patents?
Yes, multiple ANDA filers (e.g., Dr. Reddy's, MSN) challenge Paragraph IV under Hatch-Waxman, targeting production patents for early generic entry. Litigation ongoing in Delaware court; Pfizer defends validity.[1][3]
How Does This Affect Generic Bosulif Production?
Generics need Freedom-to-Operate analysis. Pre-2026, infringement risks block FDA approval. Biosimilar pathways don't apply as it's a small molecule. Paragraph IV settlements could allow limited entry by 2027.[1][2]
Sources
[1]: DrugPatentWatch.com - Bosulif Patents
[2]: FDA Orange Book - Bosulif
[3]: USPTO Patent Center - Bosutinib Litigation