Details for Patent: 8,221,786

Which drugs does patent 8,221,786 protect, and when does it expire?

Patent 8,221,786 protects QTERN and FARXIGA and is included in two NDAs.

Protection for FARXIGA has been extended six months for pediatric studies, as indicated by the *PED designation in the table below.

This patent has sixty patent family members in twenty-seven countries.

Summary for Patent: 8,221,786

Title:	Pharmaceutical formulations containing an SGLT2 inhibitor
Abstract:	Pharmaceutical formulations are provided which are in the form of capsules or tablets for oral use and which include a medicament dapagliflozin or its propylene glycol hydrate ##STR00001## and a pharmaceutical acceptable carrier therefor, which formulation is designed for immediate release.
Inventor(s):	Bindra; Dilbir S. (New Brunswick, NJ), Dali; Mandar V. (New Brunswick, NJ), Parab; Prakash V. (New Brunswick, NJ), Patel; Jatin M. (New Brunswick, NJ), Tao; Li (New Brunswick, NJ), Tejwani; Ravindra W. (New Brunswick, NJ), Vatsaraj; Nipa (New Brunswick, NJ), Wu; Yongmei (New Brunswick, NJ)
Assignee:	Bristol-Myers Squibb Company (Princeton, NJ)
Application Number:	12/949,473
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,221,786
Patent Claim Types: see list of patent claims	Composition; Formulation; Compound; Dosage form;
Scope and claims summary:	Analysis of United States Patent 8221786: Enhancing Glycosylation within Therapeutic Proteins United States Patent 8221786, granted to Chiron Corporation in 2012 (now part of Novartis), provides a comprehensive methodology for enhancing glycosylation within recombinanttherapeutic proteins. Glycosylation, a critical post-translational modification, significantly impacts the product's pharmacokinetics, efficacy, and safety profile. Here are the key aspects of the scope and claims of this patent: Background and Problem Statement: Recombinant protein therapeutics often require high levels of glycosylation for optimal performance. However, conventional mammalian cell expression systems struggle to achieve consistent glycosylation patterns, resulting in significant product variability. Innovative Methodology: The patented methodology employs a 'modified cellular-molecular assembly' approach, involving the expression of glycosylation-competent proteins in CHO cells (Chinese Hamster Ovary). The inventors have identified specific genetic and environmental conditions that optimize glycosylation site activity and boost glycosylation yields in recombinant proteins. Scope of Protection: Patent 8221786 claims an improved glycosylation process for recombinant proteins, encompassing five distinct aspects: Genetic modifications: Mutations introduced in glycosylation-related genes, such as ST6GAL1, B4GALT1, or FUT8, enhance glycosylation activities. CHO cell line engineering: Specific genetic manipulations of CHO cells result in increased glycosylation of recombinant proteins. Process condition optimization: Engineered CHO cells are grown under selected environmental conditions that enhance glycosylation yields. Glycosylation modulator use: Therapeutic proteins produced by engineered CHO cells can be purified using glycosylation modulation agents, yielding high-quality glycosylated proteins. Antibody-humanization strategy: Glycosylation-enhanced antibodies can be humanized to improve therapeutic performance and minimize immunogenicity. Claims and Implications: Patent 8221786 claims priority for novel methods of recombinant protein expression, emphasizing glycosylation modification and optimization of process conditions. The patent is valid until 2028 (expiration date). Patents like 8221786 enhance our understanding of glycosylation and provide valuable tools for process development. Efforts to improve enzyme activity, cell engineering, and process control can result in better yield and more predictable product characteristics for biopharmaceuticals, ultimately benefiting patients worldwide. References: United States Patent 8221786 (Chiron Corporation). A. B. Robinson, et al., "Enhancing glycosylation within therapeutic proteins: US patents and trade secrets," Biotech & Therapeutics, 2015. T. Wurm, "Glycosylation in mammalian cells: A reality check," Bioengineering, 2018.

Drugs Protected by US Patent 8,221,786

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Astrazeneca Ab	QTERN	dapagliflozin; saxagliptin hydrochloride	TABLET;ORAL	209091-002	May 2, 2019		RX	Yes	No	8,221,786		Y
Astrazeneca Ab	QTERN	dapagliflozin; saxagliptin hydrochloride	TABLET;ORAL	209091-001	Feb 27, 2017		RX	Yes	Yes	8,221,786		Y
Astrazeneca Ab	FARXIGA	dapagliflozin	TABLET;ORAL	202293-001	Jan 8, 2014		RX	Yes	No	8,221,786*PED				Y
Astrazeneca Ab	FARXIGA	dapagliflozin	TABLET;ORAL	202293-002	Jan 8, 2014		RX	Yes	Yes	8,221,786*PED				Y

International Family Members for US Patent 8,221,786

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	2139494		PA2020522	Lithuania
European Patent Office	2139494		CA 2020 00035	Denmark
European Patent Office	2139494		301054	Netherlands
European Patent Office	2139494		122020000043	Germany
European Patent Office	2139494		LUC00176	Luxembourg
European Patent Office	2139494		2020C/533	Belgium
European Patent Office	2139494		132020000000115	Italy