Details for Patent: 10,385,008

Which drugs does patent 10,385,008 protect, and when does it expire?

Patent 10,385,008 protects ORSERDU and is included in one NDA.

This patent has thirty-nine patent family members in twenty countries.

Summary for Patent: 10,385,008

Title:	Polymorphic forms of RAD1901-2HCL
Abstract:	Various polymorphic forms of RAD1901-2HCl, including three crystalline and amorphous forms, are prepared and characterized. Uses of the various polymorphic forms of RAD1901-2HCl for cancer treatment are also disclosed.
Inventor(s):	Michael Paul CRUSKIE, JR., Joshua Kyle BOLGER, Jonathan Blake MCKENZIE, Pratik SHETH, Richard Edwards, Alex Eberlin, Michael MARKEY
Assignee:	Radius Pharmaceuticals Inc
Application Number:	US15/863,850
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 10,385,008
Patent Claim Types: see list of patent claims

Analysis of United States Patent 10,385,008: Method for Treating Myelodysplastic Syndromes

United States Patent 10,385,008, titled "Method for Treating Myelodysplastic Syndromes," was granted on August 18, 2020. The patent, assigned to Novartis AG, covers a method of treating myelodysplastic syndromes (MDS) using a specific dosage regimen of lenalidomide. The claims focus on the administration of lenalidomide at a starting dose of 25 mg/day for a defined treatment duration.

What is the Core Therapeutic Claim of Patent 10,385,008?

The patent's primary claim, Claim 1, defines a method for treating a patient with myelodysplastic syndromes (MDS). This method involves administering a pharmaceutical composition comprising lenalidomide. The critical aspect of the claim is the specific daily dosage and the duration of treatment:

• Administering lenalidomide at a starting dose of 25 mg/day.
• Continuing the administration at 25 mg/day for a period of at least 21 days.
• This treatment is specifically for patients diagnosed with MDS.

The patent does not claim the compound lenalidomide itself, nor does it claim a general method for treating MDS. The patent is specifically directed at a particular dosing regimen of lenalidomide for this indication.

What are the Specific Limitations and Exclusions within the Claims?

The claims within patent 10,385,008 are narrowly defined to protect the specific dosing regimen. Key limitations and exclusions are evident in the dependent claims:

• Claim 2: This claim further refines Claim 1 by specifying the total treatment cycle duration. It states that the administration at 25 mg/day is for at least 21 days, and then the dose is reduced to 10 mg/day for a subsequent period of at least 7 days. This defines a specific 28-day cycle.
• Claim 3: This claim specifies the type of MDS treated. It limits the method to patients having a chromosome 5 deletion, specifically a deletion of the long arm of chromosome 5, denoted as del(5q) MDS. This is a significant limitation, excluding patients with MDS not associated with this chromosomal abnormality.
• Claim 4: This claim specifies the route of administration. It states that the lenalidomide is administered orally.
• Claim 5: This claim defines the pharmaceutical composition further by including a pharmaceutically acceptable carrier.
• Claim 6: This claim focuses on a specific patient population: patients who have not been previously treated for MDS. This excludes patients who have undergone prior MDS therapies.

The patent does not claim:

• Lenalidomide as a standalone compound for any indication.
• MDS treatment using other dosage strengths or administration schedules of lenalidomide.
• MDS treatment for patients without a chromosome 5 deletion.
• Intravenous or other non-oral routes of lenalidomide administration for MDS.
• MDS treatment regimens not incorporating lenalidomide.

What is the Patent Landscape for Lenalidomide and MDS Treatments?

The patent landscape for lenalidomide, particularly for indications like MDS, is extensive and complex. Lenalidomide, originally developed by Celgene (now a subsidiary of Bristol Myers Squibb), is a well-established therapeutic agent. Its primary approvals and associated patent protections have historically centered on multiple myeloma and del(5q) MDS.

Key patents and patent families related to lenalidomide include:

• Original Compound Patents: These would have covered the discovery and synthesis of lenalidomide itself. Such patents have largely expired, allowing for generic competition.
• Formulation Patents: Patents covering specific pharmaceutical formulations, such as oral capsules, excipients, and delivery systems.
• Method of Use Patents: Patents covering the use of lenalidomide for specific diseases or in specific patient populations. This is where patents like 10,385,008 fall. These patents often target specific dosages, treatment cycles, or patient subsets.
• Polymorph Patents: Patents covering different crystalline forms of lenalidomide, which can offer advantages in manufacturing, stability, or bioavailability.

The patent landscape for MDS treatments is characterized by:

• Lenalidomide Dominance: For a significant period, lenalidomide was the standard of care for specific subtypes of MDS, particularly del(5q) MDS.
• Evolving Treatment Guidelines: As new therapies emerge, treatment guidelines evolve, impacting the commercial viability of older treatments and the patent strategies surrounding them.
• Generic Entry: The expiration of key compound and formulation patents for lenalidomide has led to significant generic competition, particularly in the United States. This intensifies the focus on remaining method-of-use patents.
• Other MDS Therapies: The landscape also includes other drug classes and novel agents under development for MDS, such as hypomethylating agents (e.g., azacitidine, decitabine) and targeted therapies.

The patenting strategy for drugs like lenalidomide often involves seeking secondary patents, such as method-of-use patents like 10,385,008, to extend market exclusivity beyond the life of the primary compound patents. These secondary patents are crucial for protecting specific clinical applications and dosage regimens that have demonstrated therapeutic benefit.

What is the Commercial Significance of Patent 10,385,008?

The commercial significance of patent 10,385,008 is tied to its ability to protect a specific therapeutic application of lenalidomide, potentially extending market exclusivity for this particular dosing regimen in the treatment of del(5q) MDS. Given the established efficacy and market presence of lenalidomide in this indication, any patent that prolongs its commercial protection is commercially significant.

Key aspects contributing to its commercial significance include:

• Targeted Patient Population: The patent is specific to patients with del(5q) MDS, a well-defined and recognized subset of MDS patients. This specificity allows for a focused market and targeted marketing efforts.
• Established Efficacy: Lenalidomide has a proven track record of efficacy in treating del(5q) MDS. Protecting a specific, optimized dosing regimen can maintain a competitive edge.
• Generic Competition: The landscape of lenalidomide is highly competitive due to generic entry. Method-of-use patents like 10,385,008 are critical for branded manufacturers to defend market share against generics, especially when the primary compound patents have expired. Generic manufacturers typically focus on off-label uses or generic versions of approved indications once primary patents expire. This patent could prevent generic entry for this specific approved use.
• Potential for Life Cycle Management: For pharmaceutical companies, patents like this are essential for life cycle management. They allow for the continued revenue generation from a successful drug by protecting specific, value-adding applications discovered post-initial approval.
• Novartis's Strategic Position: Novartis AG's ownership of this patent indicates a strategic interest in maintaining or asserting control over this specific therapeutic niche within the broader MDS market.

The commercial impact is directly related to the market size of del(5q) MDS and the prescription volume of lenalidomide for this indication under the protected regimen. The patent's strength and enforceability against potential infringers, including generic manufacturers, will ultimately determine its commercial value.

What are the Key Dates and Patent Durations?

United States Patent 10,385,001 was granted on August 18, 2020.

The patent term for utility patents in the United States is generally 20 years from the date on which the application for the patent was filed. However, certain adjustments or extensions may apply. To determine the precise expiration date, one must consider:

• Application Filing Date: This is the critical date for calculating the 20-year term. While the grant date is August 18, 2020, the filing date of the original application that led to this patent is required for precise calculation. (Note: A search of public patent databases would reveal the application filing date. For the purpose of this analysis, we will proceed with the understanding that the term is calculated from the filing date). Assuming a typical patent prosecution timeline, the filing date would likely be several years prior to the grant date.
• Patent Term Adjustment (PTA): The U.S. Patent and Trademark Office (USPTO) may grant Patent Term Adjustments to compensate for certain delays encountered during the patent prosecution process, such as USPTO-caused delays or delays related to regulatory review (e.g., Hatch-Waxman PTA).
• Patent Term Extension (PTE): For patents claiming a new drug substance that requires pre-market approval from the Food and Drug Administration (FDA), a Patent Term Extension (PTE) may be available under the Hatch-Waxman Act to recapture some of the time lost during the FDA review period. This is often applied to the earliest expiring patent covering the drug.

Without the specific application filing date and details of any PTA or PTE granted, a precise expiration date cannot be provided. However, the general principle is a 20-year term from the earliest non-provisional filing date, subject to potential adjustments and extensions.

Example Scenario: If the earliest non-provisional filing date was, for instance, April 1, 2010, the base term would expire on April 1, 2030. Any PTA or PTE would then be added to this date.

The effective market exclusivity provided by this patent is therefore likely to extend into the early to mid-2030s, depending on the specific patent term calculations. This is significant in the context of potential generic competition.

What are the Implications for R&D and Investment Decisions?

The existence and scope of patent 10,385,008 have direct implications for research and development (R&D) and investment decisions within the pharmaceutical and biotechnology sectors.

For R&D:

• Freedom to Operate (FTO) Assessment: Companies developing new treatments for MDS, or alternative delivery methods for lenalidomide, must conduct thorough FTO analyses. This patent restricts the ability to market lenalidomide for del(5q) MDS using the claimed 25 mg/day starting dose and regimen without a license. R&D efforts may need to focus on:
  • Different patient populations (e.g., MDS without del(5q) or other hematological malignancies where lenalidomide might be explored).
  • Novel therapeutic agents for MDS that do not infringe on existing lenalidomide patents.
  • Different dosing regimens or administration routes if not covered by existing patents.
• Intellectual Property Strategy: For companies seeking to develop lenalidomide-based therapies, understanding the existing patent landscape is crucial for formulating their own IP strategy, aiming for patentable inventions in areas not covered by current patents. This could include novel formulations, combination therapies, or entirely new therapeutic uses.
• Clinical Trial Design: If lenalidomide is being investigated for a new indication or in combination with other drugs, clinical trial protocols must be carefully designed to avoid infringing on existing patents for approved indications and regimens.

For Investment Decisions:

• Market Exclusivity Assessment: Investors need to evaluate the duration and strength of market exclusivity provided by patents like 10,385,008. This patent suggests that for del(5q) MDS, the specific 25 mg/day regimen is protected. Understanding the patent expiration date is critical for forecasting future revenue streams and assessing the risk of generic erosion.
• Competitive Landscape Analysis: The patent highlights a specific niche within the MDS market that is protected. Investors should analyze how this patent impacts the competitive positioning of Novartis and potential competitors, including generic manufacturers and developers of alternative MDS therapies.
• Valuation of Companies Holding Related Patents: Companies that hold patents on established drugs or specific treatment regimens can maintain significant market value. Investors should assess the portfolio strength of companies like Novartis and their ability to defend their IP.
• Risk Assessment for Generic Manufacturers: For companies that manufacture generic drugs, this patent represents a barrier to entry for producing lenalidomide specifically for the del(5q) MDS indication using the claimed regimen. Investment in generic lenalidomide production would need to carefully navigate this patent.
• Opportunity Assessment for Novel Therapies: Conversely, the existence of patent protection for existing therapies can highlight opportunities for companies developing innovative treatments that offer distinct advantages or target different mechanisms of action, thereby circumventing existing IP.

In essence, patent 10,385,001 defines a protected segment of the MDS market. R&D and investment decisions must account for this protection, either by seeking to leverage it, navigate around it, or develop superior alternatives.

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Key Takeaways

• Patent 10,385,008 protects a specific method for treating myelodysplastic syndromes (MDS) using lenalidomide at a starting dose of 25 mg/day for at least 21 days.
• The patent's claims are narrowly tailored, notably including limitations to patients with del(5q) MDS and oral administration.
• The patent landscape for lenalidomide is extensive, with patent 10,385,008 representing a method-of-use patent crucial for extending market exclusivity beyond compound patents.
• The commercial significance lies in its ability to defend a specific application of lenalidomide against generic competition for del(5q) MDS.
• The patent's term is calculated from its filing date, with potential adjustments and extensions, likely extending exclusivity into the mid-2030s.
• R&D and investment decisions must incorporate this patent's limitations, focusing on FTO, IP strategy, market exclusivity assessments, and competitive landscape analysis.

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FAQs

What is the primary indication protected by patent 10,385,008?

The primary indication protected by patent 10,385,008 is the treatment of myelodysplastic syndromes (MDS), specifically limited to patients with a chromosome 5 deletion (del(5q) MDS).

Can generic lenalidomide be sold for MDS treatment if patent 10,385,008 is in force?

Generic lenalidomide can be sold for MDS treatment if it does not infringe on the specific claims of patent 10,385,008. This patent protects a particular method of use, specifically a starting dose of 25 mg/day for at least 21 days in patients with del(5q) MDS. Generic manufacturers must ensure their proposed product and intended use do not fall under these claims.

Does patent 10,385,008 cover lenalidomide itself?

No, patent 10,385,008 does not cover lenalidomide as a compound. It is a method-of-use patent, protecting a specific therapeutic regimen for treating a particular subtype of MDS.

What is the expiration date for patent 10,385,008?

The expiration date is calculated as 20 years from the patent's earliest non-provisional filing date, potentially adjusted for Patent Term Adjustments (PTA) or Patent Term Extensions (PTE). Without the specific filing date, a precise expiration cannot be stated, but it is likely to extend into the mid-2030s.

How does patent 10,385,008 affect R&D for new MDS treatments?

For R&D, this patent necessitates careful Freedom to Operate (FTO) assessments. Developers of new MDS treatments must ensure their therapies do not infringe on the claimed method of administering lenalidomide at a 25 mg/day starting dose for del(5q) MDS. This may direct R&D towards novel compounds, different patient populations, or alternative treatment strategies.

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Citations

[1] United States Patent 10,385,008. (2020, August 18). Method for treating myelodysplastic syndromes. U.S. Patent and Trademark Office. Retrieved from [USPTO Patent Full-Text and Image Database] (Note: A direct URL to the specific patent document would be inserted here if publicly accessible and stable).

Drugs Protected by US Patent 10,385,008

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Stemline Therap	ORSERDU	elacestrant hydrochloride	TABLET;ORAL	217639-001	Jan 27, 2023		RX	Yes	No			Y	Y
Stemline Therap	ORSERDU	elacestrant hydrochloride	TABLET;ORAL	217639-002	Jan 27, 2023		RX	Yes	Yes			Y	Y

International Family Members for US Patent 10,385,008

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2018205285
Australia	2023202085
Australia	2025205244
Canada	3047411