Details for Patent: 10,016,404

Which drugs does patent 10,016,404 protect, and when does it expire?

Patent 10,016,404 protects JUXTAPID and is included in one NDA.

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

Summary for Patent: 10,016,404

Title:	Methods for treating disorders or diseases associated with hyperlipidemia and hypercholesterolemia while minimizing side effects
Abstract:	The present invention provides methods and compositions for treating hyperlipidemia and/or hypercholesterolemia comprising administering to the subject an effective amount of an MTP inhibitor to inhibit hyperlipidemia and/or hypercholesterolemia in said subject, wherein said administration comprises an escalating series of doses of the MTP inhibitor. In some embodiments the method comprises administering at least three step-wise, increasing dosages of the MTP inhibitor to the subject. In some embodiments, the method further comprises the administration of one or more other lipid modifying compounds.
Inventor(s):	Rader; Daniel J. (Philadelphia, PA)
Assignee:	The Trustees of the University of Pennsylvania (Philadelphia, PA)
Application Number:	15/605,548
Patent Claim Types: see list of patent claims	Use;

Understanding the Scope and Claims of United States Patent 10,016,404: A Detailed Analysis

Introduction

Patent 10,016,404, titled "Methods of Treating Hyperlipidemia or Hypercholesterolemia," is associated with the drug lomitapide, a microsomal triglyceride transfer protein (MTP) inhibitor. This patent is crucial for understanding the treatment of hyperlipidemia, particularly in patients with homozygous familial hypercholesterolemia (HoFH). Here, we delve into the scope, claims, and the broader patent landscape surrounding this invention.

Background on Lomitapide

Lomitapide is a small molecule drug approved for the treatment of HoFH, a genetic condition characterized by extremely high levels of low-density lipoprotein cholesterol (LDL-C)[1].

Patent Overview

Patent Number and Approval

The patent in question, US 10,016,404, was approved on July 10, 2018. It is one of several patents related to lomitapide, each covering different aspects of its use and formulation[1].

Indicated Conditions

This patent specifically addresses methods for treating hyperlipidemia and hypercholesterolemia, particularly in pediatric patients. It highlights the use of lomitapide or its pharmaceutically acceptable salts in these treatments[4].

Scope of the Patent

Mechanism of Action

Lomitapide works by inhibiting the microsomal triglyceride transfer protein (MTP), which is essential for the assembly and secretion of very-low-density lipoprotein (VLDL) in the liver. By inhibiting MTP, lomitapide reduces the levels of LDL-C, total cholesterol (TC), apolipoprotein B (apo B), and non-high-density lipoprotein cholesterol (non-HDL-C)[1].

Claims

The patent claims cover various methods of treating hyperlipidemia and hypercholesterolemia, including:

• Daily Dose Administration: The patent specifies the daily dose of lomitapide and its acceptable salts for pediatric patients.
• Pharmaceutically Acceptable Salts: It includes claims related to the use of pharmaceutically acceptable salts of lomitapide, which are crucial for enhancing the drug's bioavailability and stability.
• Treatment Regimens: The patent outlines different treatment regimens, including the duration and frequency of lomitapide administration[4].

Patent Claims Analysis

Independent Claim Length and Count

Research on patent scope often involves analyzing independent claim length and count. These metrics can indicate the breadth and clarity of the patent claims. For instance, narrower claims with shorter lengths and fewer counts are generally associated with a higher probability of grant and a shorter examination process[3].

Enablement Requirement

The Supreme Court's ruling in Amgen Inc. v. Sanofi emphasizes the importance of the enablement requirement under 35 U.S.C. § 112. This requirement mandates that the patent specification must enable a person skilled in the art to make and use the entire class of inventions claimed. In the context of US 10,016,404, the patent must provide sufficient detail to enable the production and use of lomitapide for treating hyperlipidemia and hypercholesterolemia without requiring an unreasonable amount of experimentation[5].

Broader Patent Landscape

Patent Scope and Quality

Debates over patent quality often focus on the breadth and clarity of patent claims. The purported decrease in patent quality has led to concerns about overly broad patents and increased litigation costs. Metrics such as independent claim length and count help in assessing the scope and quality of patents. For US 10,016,404, the claims must be specific enough to avoid the pitfalls of overly broad claims while ensuring they are clear and enabling[3].

Patent Claims Research Dataset

The USPTO's Patent Claims Research Dataset provides detailed information on claims from US patents and patent applications. This dataset can be used to analyze the trends and metrics of patent scope, including those related to lomitapide patents. It helps in understanding how patent claims evolve during the examination process and how they impact the overall patent landscape[2].

Clinical and Therapeutic Implications

Treatment of HoFH

The primary clinical implication of US 10,016,404 is the treatment of HoFH, a rare and severe form of hypercholesterolemia. Lomitapide, as described in the patent, offers a critical therapeutic option for reducing LDL-C levels in these patients[1].

Pediatric Use

The patent's focus on pediatric patients is significant, as it addresses a critical need for effective treatments in this population. The specified daily doses and treatment regimens are tailored to ensure safety and efficacy in younger patients[4].

Economic and Regulatory Considerations

Patent Expiration and Generic Competition

The patent's expiration date, estimated to be around 2025, is crucial for understanding the future market landscape. Once the patent expires, generic versions of lomitapide could enter the market, potentially reducing costs and increasing access to this life-saving medication[1].

Regulatory Approvals

The approval process for lomitapide involved rigorous clinical trials and regulatory reviews. The patent's claims must align with the regulatory approvals and guidelines set by health authorities, ensuring that the treatment methods described are safe and effective[1].

Key Takeaways

• Patent Scope: US 10,016,404 covers specific methods for treating hyperlipidemia and hypercholesterolemia using lomitapide.
• Claims Analysis: The patent's claims must meet the enablement requirement and avoid being overly broad.
• Clinical Implications: The patent is crucial for treating HoFH and provides treatment options for pediatric patients.
• Regulatory Considerations: The patent's expiration and regulatory approvals are key factors in its economic and therapeutic impact.

FAQs

What is the primary use of lomitapide as described in US 10,016,404?

Lomitapide is used to treat hyperlipidemia and hypercholesterolemia, particularly in patients with homozygous familial hypercholesterolemia (HoFH).

What is the mechanism of action of lomitapide?

Lomitapide inhibits the microsomal triglyceride transfer protein (MTP), reducing the levels of LDL-C, total cholesterol, apolipoprotein B, and non-HDL-C.

What is the significance of the enablement requirement in patent law?

The enablement requirement ensures that the patent specification provides sufficient detail to enable a person skilled in the art to make and use the entire class of inventions claimed without requiring an unreasonable amount of experimentation.

How does the patent landscape impact the availability of generic versions of lomitapide?

The patent's expiration, estimated around 2025, will allow generic versions of lomitapide to enter the market, potentially reducing costs and increasing access to the medication.

What are the clinical implications of US 10,016,404 for pediatric patients?

The patent provides critical treatment options for pediatric patients with hyperlipidemia and hypercholesterolemia, including specified daily doses and treatment regimens tailored for this population.

Sources

1. DrugBank: Lomitapide: Uses, Interactions, Mechanism of Action.
2. USPTO: Patent Claims Research Dataset.
3. SSRN: Patent Claims and Patent Scope.
4. Google Patents: Lomitapide for use in methods of treating hyperlipidemia and hypercholesterolemia in pediatric patients.
5. Vorys: Supreme Court Issues Patent Ruling Curbing Broad Functional Claims in Patents.

Drugs Protected by US Patent 10,016,404

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Chiesi	JUXTAPID	lomitapide mesylate	CAPSULE;ORAL	203858-001	Dec 21, 2012		RX	Yes	No						A DOSING REGIMEN FOR THE TREATMENT OF HYPERCHOLESTEROLEMIA AND HYPERLIPIDEMIA IN PATIENTS WITH HOMOZYGOUS FAMILIAL HYPERCHOLESTEROLEMIA USING AT LEAST THREE STEP-WISE INCREASING DOSES
Chiesi	JUXTAPID	lomitapide mesylate	CAPSULE;ORAL	203858-002	Dec 21, 2012		RX	Yes	No						A DOSING REGIMEN FOR THE TREATMENT OF HYPERCHOLESTEROLEMIA AND HYPERLIPIDEMIA IN PATIENTS WITH HOMOZYGOUS FAMILIAL HYPERCHOLESTEROLEMIA USING AT LEAST THREE STEP-WISE INCREASING DOSES
Chiesi	JUXTAPID	lomitapide mesylate	CAPSULE;ORAL	203858-003	Dec 21, 2012		RX	Yes	No						A DOSING REGIMEN FOR THE TREATMENT OF HYPERCHOLESTEROLEMIA AND HYPERLIPIDEMIA IN PATIENTS WITH HOMOZYGOUS FAMILIAL HYPERCHOLESTEROLEMIA USING AT LEAST THREE STEP-WISE INCREASING DOSES
Chiesi	JUXTAPID	lomitapide mesylate	CAPSULE;ORAL	203858-004	Apr 23, 2015		RX	Yes	No						A DOSING REGIMEN FOR THE TREATMENT OF HYPERCHOLESTEROLEMIA AND HYPERLIPIDEMIA IN PATIENTS WITH HOMOZYGOUS FAMILIAL HYPERCHOLESTEROLEMIA USING AT LEAST THREE STEP-WISE INCREASING DOSES
Chiesi	JUXTAPID	lomitapide mesylate	CAPSULE;ORAL	203858-005	Apr 23, 2015		DISCN	Yes	No						A DOSING REGIMEN FOR THE TREATMENT OF HYPERCHOLESTEROLEMIA AND HYPERLIPIDEMIA IN PATIENTS WITH HOMOZYGOUS FAMILIAL HYPERCHOLESTEROLEMIA USING AT LEAST THREE STEP-WISE INCREASING DOSES
Chiesi	JUXTAPID	lomitapide mesylate	CAPSULE;ORAL	203858-006	Apr 23, 2015		DISCN	Yes	No						A DOSING REGIMEN FOR THE TREATMENT OF HYPERCHOLESTEROLEMIA AND HYPERLIPIDEMIA IN PATIENTS WITH HOMOZYGOUS FAMILIAL HYPERCHOLESTEROLEMIA USING AT LEAST THREE STEP-WISE INCREASING DOSES

International Family Members for US Patent 10,016,404

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	1725234		CA 2014 00002	Denmark
European Patent Office	1725234		C300634	Netherlands
European Patent Office	1725234		PA2014001	Lithuania
European Patent Office	1725234		C20140001 00107	Estonia
European Patent Office	1725234		14C0003	France
European Patent Office	1725234		1490006-2	Sweden