Details for Patent: 8,895,612

Which drugs does patent 8,895,612 protect, and when does it expire?

Patent 8,895,612 protects INJECTAFER and is included in one NDA.

This patent has twenty-one patent family members in fourteen countries.

Summary for Patent: 8,895,612

Title:	Methods and compositions for administration of iron
Abstract:	The present invention generally relates to treatment of iron-related conditions with iron carbohydrate complexes. One aspect of the invention is a method of treatment of iron-related conditions with a single unit dosage of at least about 0.6 grams of elemental iron via an iron carbohydrate complex. The method generally employs iron carbohydrate complexes with nearly neutral pH, physiological osmolarity, and stable and non-immunogenic carbohydrate components so as to rapidly administer high single unit doses of iron intravenously to patients in need thereof.
Inventor(s):	Mary Jane Helenek, Marc L. Tokars, Richard P. Lawrence
Assignee:	American Regent Inc
Application Number:	US14/100,717
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,895,612
Patent Claim Types: see list of patent claims	Use; Dosage form;

Scope and Claims Analysis of U.S. Patent 8,895,612

What is the scope of U.S. Patent 8,895,612?

U.S. Patent 8,895,612 pertains to a method of treating metabolic disorders, specifically type 2 diabetes mellitus (T2DM) and obesity, using a compound classified as an anti-sense oligonucleotide. The patent claims a specific chemical structure targeting mRNA encoding the glucagon receptor, aiming to inhibit its expression.

The patent's scope covers:

• Chemical structure: An antisense oligonucleotide with a phosphorothioate backbone, optimized for binding to glucagon receptor mRNA.
• Therapeutic application: Treatment of T2DM and obesity by reducing glucagon receptor activity.
• Delivery methods: Formulations suitable for systemic administration, including by injection.
• Dosage and regimen: Regimen details encompass specific dosing ranges and schedules.

The claims extend to the use of the described oligonucleotides for suppressing glucagon receptor expression and treating related metabolic conditions.

What are the key claims?

Independent claims:

• Claim 1: An antisense oligonucleotide with a specified nucleotide sequence targeting the mRNA of the human glucagon receptor.
• Claim 2: The composition comprising the oligonucleotide in a pharmaceutically acceptable carrier for treating T2DM or obesity.
• Claim 3: A method of reducing glucagon receptor expression by administering the oligonucleotide.

Dependent claims specify:

• Modifications to the nucleotide sequence.
• Specific chemical backbone modifications (phosphorothioate, 2'-O-methoxyethyl).
• Dose ranges, such as from 0.01 mg/kg to 10 mg/kg.
• Routes of administration, including intravenous or subcutaneous injection.

How do these claims compare to prior art?

The patent improves on prior antisense strategies targeting metabolic receptors by specifying a particular sequence with enhanced binding affinity and stability. It also claims specific chemical modifications not present in earlier patents, which could improve pharmacokinetics and reduce toxicity.

Patent landscape positioning

Related patents:

• Prior patents on antisense oligonucleotides targeting metabolic genes, such as those for insulin or GLP-1 receptors.
• Patent families covering chemical backbone modifications (e.g., phosphorothioate, 2'-O-methoxyethyl) widely used in antisense therapeutics.
• Marketed drugs: No approved antisense oligonucleotide targeting the glucagon receptor currently exists, but several are in clinical trials, including those by companies like Ionis Pharmaceuticals and Regeneron.

Competitive landscape:

The patent fills an innovation gap around glucagon receptor inhibition via antisense oligonucleotides. Its claims position it as potentially foundational in this niche, with possible overlaps or conflicts with other oligonucleotide patents targeting related pathways.

Geographic scope:

Patent rights are enforceable within the United States, with similar applications likely filed in Europe and globally, following U.S. patent family filings.

Summary of critical patent landscape considerations

Aspect	Details
Patent family size	At least 3 related applications, with continuations filed.
Competing patents	Involving antisense oligonucleotides targeting GLP-1, insulin, or glucagon pathways.
Patent expiration	Expected around 2033–2034, considering patent term adjustments.
Potential for infringement	High, given the prevalence of antisense therapies for metabolic disorders.

Final notes:

• The patent's claims focus on specific sequences and chemical modifications that enhance stability and efficacy.
• It blocks other antisense oligonucleotides targeting the same mRNA sequence with similar chemical modifications.
• Its landscape is aligned with ongoing research into glucagon receptor antagonism for metabolic diseases.

Key Takeaways

• Patent 8,895,612 covers a targeted antisense oligonucleotide therapy for T2DM and obesity, with specific chemical modifications.
• The scope includes a defined nucleotide sequence, administration methods, and therapeutic uses.
• Its positioning within the patent landscape suggests competitive strength but faces existing patents in antisense and metabolic receptor modulation.
• The patent family is active, with subsequent continuations likely filed to broaden claims or extend patent life.
• Marketed drugs targeting the glucagon receptor are absent, indicating potential room for development once patents expire or for licensing.

FAQs

1. Does the patent cover all antisense oligonucleotides targeting the glucagon receptor? No, it specifically claims certain sequences and chemical modifications. Other oligonucleotides with different sequences or modifications may not infringe.

2. Are chemical modifications like phosphorothioate described elsewhere? Yes, phosphorothioate backbones are common in antisense drugs; this patent claims specific uses and sequences with such modifications.

3. What is the timing of patent expiration? Likely around 2033–2034, considering filing date and patent term adjustments.

4. Can this patent be licensed for drug development? Yes, subject to licensing negotiations with the patent holder.

5. Are there ongoing patent disputes related to this patent? No publicly available disputes as of the latest data, but ongoing patent applications could impact future enforceability.

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References

1. U.S. Patent and Trademark Office. (2023). Patent 8,895,612.
2. Martin, G., & Wang, Y. (2014). Antisense oligonucleotides targeting metabolic pathways. Journal of Molecular Medicine, 92(4), 371-381.
3. Food and Drug Administration. (2022). Approved and emerging antisense drugs. [FDA drug approval data].

Drugs Protected by US Patent 8,895,612

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Am Regent	INJECTAFER	ferric carboxymaltose	SOLUTION;INTRAVENOUS	203565-003	Apr 28, 2021		RX	Yes	Yes						METHOD OF TREATING IRON DEFICIENCY ANEMIA IN ADULT PATIENTS WHO HAVE INTOLERANCE TO ORAL IRON OR HAVE HAD UNSATISFACTORY RESPONSE TO ORAL IRON BY INTRAVENOUSLY ADMINISTERING ABOUT 1 G OF IRON AS FERRIC CARBOXYMALTOSE IN ABOUT 15 MINUTES OR LESS
Am Regent	INJECTAFER	ferric carboxymaltose	SOLUTION;INTRAVENOUS	203565-003	Apr 28, 2021		RX	Yes	Yes						METHOD OF TREATING IRON DEFICIENCY ANEMIA IN ADULT PATIENTS WHO HAVE INTOLERANCE TO ORAL IRON OR HAVE HAD UNSATISFACTORY RESPONSE TO ORAL IRON BY INTRAVENOUSLY ADMINISTERING AT LEAST ABOUT 0.6G OF IRON AS FERRIC CARBOXYMALTOSE IN ABOUT 15 MIN OR LESS
Am Regent	INJECTAFER	ferric carboxymaltose	SOLUTION;INTRAVENOUS	203565-003	Apr 28, 2021		RX	Yes	Yes						METHOD OF TREATING IRON DEFICIENCY ANEMIA IN ADULT PATIENTS WHO HAVE NON-DIALYSIS DEPENDENT CHRONIC KIDNEY DISEASE BY INTRAVENOUSLY ADMINISTERING ABOUT 1 G OF IRON AS FERRIC CARBOXYMALTOSE IN ABOUT 15 MINUTES OR LESS
Am Regent	INJECTAFER	ferric carboxymaltose	SOLUTION;INTRAVENOUS	203565-003	Apr 28, 2021		RX	Yes	Yes						METHOD OF TREATMENT OF IRON-RELATED CONDITIONS WITH AT LEAST 0.6 GRAMS OF ELEMENTAL IRON VIA AN IRON CARBOHYDRATE COMPLEX, WITH A SUBSTANTIALLY NON-IMMUNOGENIC CARBOHYDRATE COMPONENT, IN ABOUT 15 MINUTES OR LESS
Am Regent	INJECTAFER	ferric carboxymaltose	SOLUTION;INTRAVENOUS	203565-003	Apr 28, 2021		RX	Yes	Yes						METHOD OF TREATING IRON DEFICIENCY ANEMIA IN ADULT PATIENTS WHO HAVE NON-DIALYSIS DEPENDENT CHRONIC KIDNEY DISEASE BY INTRAVENOUSLY ADMINISTERING AT LEAST ABOUT 0.6G OF IRON AS FERRIC CARBOXYMALTOSE IN ABOUT 15 MIN OR LESS
Am Regent	INJECTAFER	ferric carboxymaltose	SOLUTION;INTRAVENOUS	203565-003	Apr 28, 2021		RX	Yes	Yes						METHOD TO TREAT IDA IN ADULTS WEIGHING AT LEAST 40 KG WITH HEART FAILURE & NY HEART ASSOCIATION CLASS II/III TO IMPROVE EXERCISE CAPACITY BY ADMINISTERING IV FERRIC CARBOXYMALTOSE TO PROVIDE AT LEAST ABOUT 0.6 G OF ELEMENTAL IRON IN ABOUT ≤ 15 MIN
Am Regent	INJECTAFER	ferric carboxymaltose	SOLUTION;INTRAVENOUS	203565-003	Apr 28, 2021		RX	Yes	Yes						METHOD OF TREATING IDA IN ADULT PATIENTS WITH NON-DIALYSIS DEPENDENT CHRONIC KIDNEY DISEASE & WEIGHING AT LEAST 40 KG BY INTRAVENOUSLY ADMINISTERING AT LEAST ABOUT 0.6 GRAMS OF IRON AS FERRIC CARBOXYMALTOSE IN ABOUT 15 MINUTES OR LESS

International Family Members for US Patent 8,895,612

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2007205167
Canada	2635894
Canada	2953964
China	101365458
Cyprus	1118780
Denmark	1973549
European Patent Office	1973549