Key Patents Covering Bosulif Manufacturing
Bosulif (bosutinib), made by Pfizer, has patents protecting its manufacturing processes, including synthesis of the active ingredient and formulation steps. US Patent 7,342,013 covers methods for preparing bosutinib by reacting 3-cyano-4-(2-methyl-4-quinazolinylamino)aniline with specific acyl chlorides or anhydrides to form the monohydrate form used in tablets [1]. This patent expires May 7, 2027.
US Patent 8,461,173 details scalable manufacturing processes for bosutinib intermediates, focusing on purification and crystallization to achieve high purity, essential for consistent drug production [1]. It expires September 25, 2029.
Formulation and Dosage Form Patents
US Patent 8,987,452 protects tablet manufacturing methods, including granulation, compression, and coating processes to ensure stability and bioavailability of the 400mg and 500mg strengths [1]. Expiration is March 18, 2031.
These overlap with composition-of-matter protection under US 7,417,142 (expires February 28, 2029), which indirectly supports manufacturing by defining the crystalline form produced [1].
When Do These Patents Expire?
| Patent Number | Manufacturing Focus | Assignee | Expiration Date |
|---------------|---------------------|----------|-----------------|
| US 7,342,013 | Core synthesis | Pfizer | May 7, 2027 |
| US 8,461,173 | Intermediate purification | Pfizer | Sep 25, 2029 |
| US 8,987,452 | Tablet formulation | Pfizer | Mar 18, 2031 |
Pediatric exclusivity may add six months to some expirations. Full details and status at DrugPatentWatch.com [1].
Are These Patents Challenged?
Yes, multiple Paragraph IV challenges target these and related patents. In 2022, Dr. Reddy's filed ANDA with Paragraph IV certification against US 7,342,013 and others, prompting Pfizer's infringement suit (settled with entry delayed to 2031 for some) [1][2]. Similar challenges from MSN and Celltrion are ongoing, potentially accelerating generic manufacturing entry [1].
How Do Manufacturing Patents Affect Generics?
Generic makers must design around these by developing non-infringing synthesis routes, like alternative coupling reactions or anhydrous forms. FDA requires bioequivalence, so purification patents limit options even if synthesis differs [2]. Biosimilar pathways (under BPCIA) rarely apply here as Bosulif is small-molecule.
Who Owns and Licenses These Patents?
Pfizer holds all as assignee. No major licenses noted for manufacturing; ArQule (now Pfizer subsidiary) originated early filings [1].
Sources:
[1] DrugPatentWatch.com - Bosulif Patents
[2] FDA Orange Book - Bosulif ANDAs