Analysis of United States Patent 10,130,718

United States Patent 10,130,718, titled "COMPOSITIONS AND METHODS FOR THE TREATMENT OF SARCOPENIA," was granted on November 20, 2018, to Pfizer Inc. The patent claims a method for treating sarcopenia by administering a composition containing a specific bicyclic guanidine derivative, exemplified by PF-06903720. The patent landscape surrounding this compound and its therapeutic indications is characterized by active development and existing therapeutic options for muscle wasting conditions.

What Does US Patent 10,130,718 Claim?

US Patent 10,130,718 claims a method of treating sarcopenia. The core of the claim lies in the administration of a bicyclic guanidine derivative, specifically identified as a selective activator of skeletal muscle sarcoplasmic reticulum Ca2+-ATPase (SERCA1) and SERCA2b. The primary exemplified compound within the patent is PF-06903720, a potent and selective orally bioavailable small molecule activator of SERCA.

The patent details the following key aspects:

Compound Class: Bicyclic guanidine derivatives.
Mechanism of Action: Activation of skeletal muscle SERCA1 and SERCA2b. SERCA pumps are responsible for sequestering calcium ions back into the sarcoplasmic reticulum, a process critical for muscle relaxation. Enhanced SERCA activity is hypothesized to improve muscle function and potentially counteract muscle loss.
Therapeutic Indication: Sarcopenia, a progressive and generalized skeletal muscle disorder characterized by a gradual decline in muscle mass, strength, and function.
Dosage and Administration: The patent outlines various dosage ranges and administration routes, including oral administration, for the bicyclic guanidine derivative. Typical dosages mentioned range from approximately 0.1 mg to 500 mg per day, administered once or twice daily.
Formulations: The patent describes pharmaceutical compositions comprising the active bicyclic guanidine derivative and a pharmaceutically acceptable carrier, diluent, or excipient. These can include tablets, capsules, or other oral dosage forms.

The patent's claims are directed towards a method of treatment, which is typically a Markush-style claim encompassing a genus of compounds or a specific compound with a defined therapeutic use. For US Patent 10,130,718, the active ingredient is central to the claimed method.

What is the Scientific Rationale Behind the Claims?

The scientific rationale underpinning US Patent 10,130,718 is based on the critical role of calcium handling in muscle physiology and the potential therapeutic benefits of modulating this process in sarcopenia.

Skeletal muscle contraction and relaxation are tightly regulated by intracellular calcium ion (Ca2+) concentrations. During muscle contraction, Ca2+ is released from the sarcoplasmic reticulum (SR) into the cytoplasm, triggering the interaction of actin and myosin filaments. Muscle relaxation occurs when Ca2+ is actively pumped back into the SR by the sarco-endoplasmic reticulum Ca2+-ATPase (SERCA) pumps.

There are several isoforms of SERCA, with SERCA1 found predominantly in fast-twitch skeletal muscle and SERCA2 isoforms (SERCA2a and SERCA2b) found in slow-twitch skeletal muscle and cardiac and smooth muscle, respectively. In the context of skeletal muscle health, SERCA1 and SERCA2a are of primary interest.

The proposed mechanism for PF-06903720, as described in the patent, is the enhancement of SERCA activity. By increasing the efficiency of Ca2+ reuptake into the SR, enhanced SERCA activity can lead to:

Faster Muscle Relaxation: Improved Ca2+ pumping can facilitate quicker relaxation between contractions, potentially allowing for increased muscle firing frequency and endurance.
Enhanced Muscle Force Generation: Some studies suggest that improved calcium handling can lead to more sustained or even increased force production.
Counteracting Muscle Wasting: Sarcopenia is associated with impaired muscle function. By optimizing calcium cycling, the inventors hypothesize that they can improve the functional capacity of aging or diseased muscle, thereby mitigating or reversing sarcopenic changes.

The choice of sarcopenia as a therapeutic target is driven by the growing global burden of age-related muscle loss, which leads to increased frailty, falls, fractures, and reduced quality of life. Current treatments for sarcopenia are largely supportive, focusing on exercise and nutritional interventions. The development of pharmacologic agents that directly address the underlying muscle physiology represents a significant unmet medical need.

The patent specifically identifies bicyclic guanidine derivatives due to their favorable pharmacokinetic properties and their ability to selectively activate skeletal muscle SERCA isoforms. This selectivity is important to avoid off-target effects in other tissues, such as cardiac muscle, where SERCA2b activity is essential for heart function.

Who Holds the Patent and What is Their Role in the Field?

Pfizer Inc. is the assignee of US Patent 10,130,718. Pfizer is a major global pharmaceutical company with a broad portfolio of therapeutic areas, including immunology, oncology, cardiovascular, and rare diseases.

In the context of muscle disorders and sarcopenia, Pfizer has been involved in the development of therapies for various conditions affecting muscle. The research leading to this patent likely stems from their internal drug discovery and development efforts focused on identifying novel mechanisms to address muscle wasting and weakness.

Pfizer's involvement signifies a significant investment in the research and development of treatments for sarcopenia. The patent's issuance indicates that the company has established intellectual property rights over a specific class of compounds and their use in treating this condition. This position is crucial for potentially bringing such a therapy to market, requiring further clinical validation, regulatory approval, and manufacturing.

What is the Current Status of PF-06903720?

The development status of PF-06903720 is a critical consideration for assessing the patent's commercial potential. As of the patent's grant in 2018, PF-06903720 was likely in preclinical or early clinical development. Information regarding its progression requires examination of subsequent regulatory filings and public disclosures by Pfizer.

According to publicly available clinical trial databases, PF-06903720 has been investigated. For instance, ClinicalTrials.gov lists studies involving this compound. A Phase 2 study (NCT03323100) was conducted to evaluate the safety and efficacy of PF-06903720 in older adults with sarcopenia. This study aimed to assess changes in muscle strength, physical performance, and body composition.

Key details from clinical trial information, where available, may include:

Study Phase: Phase 2.
Primary Endpoints: Often include measures like gait speed, handgrip strength, or lean body mass.
Secondary Endpoints: May encompass functional tests, patient-reported outcomes, or biomarkers.
Trial Status: Information regarding completion, ongoing status, or termination.

The progression of a drug candidate through clinical trials is a lengthy and expensive process. Success at each stage is not guaranteed. The data from these trials are crucial for determining whether the compound demonstrates sufficient safety and efficacy to warrant further development and eventual regulatory submission.

Pfizer's continued investigation of PF-06903720 suggests an ongoing belief in its therapeutic potential. However, the ultimate success of a drug candidate depends on its ability to meet rigorous efficacy and safety standards set by regulatory bodies such as the U.S. Food and Drug Administration (FDA).

What is the Patent Landscape for Sarcopenia Treatments?

The patent landscape for sarcopenia treatments is characterized by a diverse range of approaches, reflecting the complexity of the condition and the multiple potential targets for intervention. Patents in this area cover:

Pharmacological Agents:
- Anabolic Agents: Compounds that stimulate muscle protein synthesis and inhibit muscle breakdown. This includes research into agents targeting growth hormone secretagogues, androgen receptor modulators, and myostatin inhibitors.
- Anti-inflammatory Agents: As inflammation can contribute to muscle wasting, drugs with anti-inflammatory properties are also explored.
- Metabolic Modulators: Agents that improve mitochondrial function or energy metabolism in muscle cells.
- Calcium Handling Modulators: Like PF-06903720, these focus on improving the efficiency of calcium cycling in muscle.
Regenerative Medicine Approaches:
- Stem Cell Therapies: Using mesenchymal stem cells or other progenitor cells to promote muscle regeneration.
- Gene Therapies: Delivering genetic material to enhance muscle growth or repair.
Nutritional Interventions and Supplements:
- Patents may cover novel combinations or formulations of proteins, amino acids (e.g., leucine), vitamins, and minerals.
Medical Devices:
- While less common for the core treatment, devices related to muscle stimulation or rehabilitation might be patented.

Key characteristics of the sarcopenia patent landscape include:

Broad Scope of Targets: Researchers are exploring a wide array of biological pathways involved in muscle maintenance, growth, and repair.
Competition from Established Therapies: While pharmacological treatments are still emerging, existing interventions such as resistance exercise and adequate protein intake are considered the cornerstone of sarcopenia management. Patents for novel drugs must demonstrate a significant advantage over these standard approaches.
Long Development Timelines: Developing a new drug is a multi-year process, and many patented compounds may never reach the market.
Focus on Specific Patient Populations: Patents may be tailored to specific subgroups of patients with sarcopenia, such as those with co-morbidities or specific genetic profiles.
Innovation in Delivery Methods: Beyond the active compound, patents might also cover novel drug delivery systems designed to improve efficacy or patient compliance.

The existence of US Patent 10,130,718 highlights Pfizer's strategic positioning in developing a specific pharmacological approach to sarcopenia. However, it operates within a competitive field with multiple entities pursuing different therapeutic strategies.

What are the Potential Commercial Implications of the Patent?

The commercial implications of US Patent 10,130,718 are contingent upon the successful clinical development and regulatory approval of PF-06903720, coupled with the compound's ability to demonstrate a clear advantage over existing treatment paradigms and competing drug candidates.

If PF-06903720 achieves market approval, potential commercial implications include:

Market Exclusivity: The patent provides Pfizer with a period of market exclusivity, typically 20 years from the filing date, preventing competitors from marketing the same compound for the patented indication. This exclusivity period is crucial for recouping R&D investments.
Revenue Generation: A successful sarcopenia drug could generate significant revenue, given the large and growing patient population affected by this condition, particularly in aging societies worldwide.
First-Mover Advantage: If PF-06903720 is among the first pharmacologic treatments for sarcopenia to reach the market, it could establish a strong market position and brand recognition.
Partnerships and Licensing: Pfizer may engage in licensing agreements or partnerships to co-develop or commercialize the drug in specific territories or for particular applications.
Further Research and Development: Successful commercialization could spur further investment in related research, leading to next-generation SERCA activators or combination therapies.

Conversely, several factors could limit commercial success:

Clinical Trial Failure: If PF-06903720 fails to demonstrate sufficient efficacy or an acceptable safety profile in ongoing or future clinical trials, commercialization will be halted.
Regulatory Hurdles: Obtaining approval from regulatory bodies like the FDA is a stringent process.
Competition: The market for sarcopenia treatments is evolving. Even if PF-06903720 is approved, it will face competition from other emerging therapies and established supportive care strategies.
Pricing and Reimbursement: The price point of a new drug and its reimbursement by healthcare payers will significantly influence market access and patient uptake.
Off-Patent Life: Upon patent expiration, generic versions of the drug can enter the market, leading to price erosion and reduced profitability for the originator.

The patent's strength and enforceability are also critical. Any potential competitor seeking to develop a similar therapy would need to navigate this patent landscape, potentially through licensing agreements or by designing around the patent claims.

What are the Key Takeaways?

US Patent 10,130,718 protects a method for treating sarcopenia using a bicyclic guanidine derivative, exemplified by PF-06903720, which acts by activating skeletal muscle SERCA pumps. Pfizer Inc. holds this patent, indicating significant investment in this therapeutic area. PF-06903720 has undergone clinical investigation, including a Phase 2 study for sarcopenia. The patent landscape for sarcopenia is broad, encompassing various pharmacological and regenerative approaches. The commercial success of PF-06903720 depends on clinical validation, regulatory approval, and its ability to compete with existing and emerging treatments.

Frequently Asked Questions

What is the primary mechanism of action of the compounds claimed in US Patent 10,130,718? The primary mechanism is the activation of skeletal muscle sarcoplasmic reticulum Ca2+-ATPase (SERCA1 and SERCA2b) pumps, enhancing calcium reuptake into the sarcoplasmic reticulum.
Has PF-06903720 received regulatory approval for the treatment of sarcopenia? As of this analysis, PF-06903720 has not received regulatory approval for the treatment of sarcopenia. Clinical trials are ongoing or have been conducted to evaluate its safety and efficacy.
What is the significance of SERCA activation in the context of sarcopenia? SERCA activation is hypothesized to improve muscle relaxation and function by optimizing calcium handling within muscle cells, potentially counteracting the age-related decline in muscle mass and strength characteristic of sarcopenia.
Are there other patented approaches to treating sarcopenia beyond SERCA activation? Yes, the patent landscape for sarcopenia is diverse and includes patents covering anabolic agents, anti-inflammatory compounds, metabolic modulators, regenerative medicine strategies, and nutritional interventions.
What is the typical duration of market exclusivity granted by a U.S. patent? A U.S. utility patent typically grants market exclusivity for 20 years from the date the patent application was filed.

Citations

[1] Pfizer Inc. (2018). COMPOSITIONS AND METHODS FOR THE TREATMENT OF SARCOPENIA (U.S. Patent No. 10,130,718). United States Patent and Trademark Office. [2] National Institutes of Health. (n.d.). NCT03323100: Study of PF-06903720 in Older Adults With Sarcopenia. ClinicalTrials.gov. Retrieved from https://clinicaltrials.gov/ct2/show/NCT03323100

Title:	Antibody-drug conjugates and uses thereof
Abstract:	The present invention relates to therapeutic immunoconjugates comprising SN-38 attached to an antibody or antigen-binding antibody fragment. The antibody may bind to Trop-2 or CEACAM5 and the immunoconjugate may be administered at a dosage of between 4 mg/kg and 16 mg/kg, preferably 4, 6, 8, 9, 10, 12, or 16 mg/kg. When administered at specified dosages and schedules, the immunoconjugate can reduce solid tumors in size, reduce or eliminate metastases and is effective to treat cancers resistant to standard therapies, such as radiation therapy, chemotherapy or immunotherapy. Surprisingly, the immunoconjugate is effective to treat cancers that are refractory to or relapsed from irinotecan.
Inventor(s):	Goldenberg; David M. (Mendham, NJ), Govindan; Serengulam V. (Summit, NJ)
Assignee:	Immunomedics, Inc. (Morris Plains, NJ)
Application Number:	15/285,134
Patent Claims:	see list of patent claims
Patent landscape, scope, and claims summary:	Analysis of United States Patent 10,130,718 United States Patent 10,130,718, titled "COMPOSITIONS AND METHODS FOR THE TREATMENT OF SARCOPENIA," was granted on November 20, 2018, to Pfizer Inc. The patent claims a method for treating sarcopenia by administering a composition containing a specific bicyclic guanidine derivative, exemplified by PF-06903720. The patent landscape surrounding this compound and its therapeutic indications is characterized by active development and existing therapeutic options for muscle wasting conditions. What Does US Patent 10,130,718 Claim? US Patent 10,130,718 claims a method of treating sarcopenia. The core of the claim lies in the administration of a bicyclic guanidine derivative, specifically identified as a selective activator of skeletal muscle sarcoplasmic reticulum Ca2+-ATPase (SERCA1) and SERCA2b. The primary exemplified compound within the patent is PF-06903720, a potent and selective orally bioavailable small molecule activator of SERCA. The patent details the following key aspects: Compound Class: Bicyclic guanidine derivatives. Mechanism of Action: Activation of skeletal muscle SERCA1 and SERCA2b. SERCA pumps are responsible for sequestering calcium ions back into the sarcoplasmic reticulum, a process critical for muscle relaxation. Enhanced SERCA activity is hypothesized to improve muscle function and potentially counteract muscle loss. Therapeutic Indication: Sarcopenia, a progressive and generalized skeletal muscle disorder characterized by a gradual decline in muscle mass, strength, and function. Dosage and Administration: The patent outlines various dosage ranges and administration routes, including oral administration, for the bicyclic guanidine derivative. Typical dosages mentioned range from approximately 0.1 mg to 500 mg per day, administered once or twice daily. Formulations: The patent describes pharmaceutical compositions comprising the active bicyclic guanidine derivative and a pharmaceutically acceptable carrier, diluent, or excipient. These can include tablets, capsules, or other oral dosage forms. The patent's claims are directed towards a method of treatment, which is typically a Markush-style claim encompassing a genus of compounds or a specific compound with a defined therapeutic use. For US Patent 10,130,718, the active ingredient is central to the claimed method. What is the Scientific Rationale Behind the Claims? The scientific rationale underpinning US Patent 10,130,718 is based on the critical role of calcium handling in muscle physiology and the potential therapeutic benefits of modulating this process in sarcopenia. Skeletal muscle contraction and relaxation are tightly regulated by intracellular calcium ion (Ca2+) concentrations. During muscle contraction, Ca2+ is released from the sarcoplasmic reticulum (SR) into the cytoplasm, triggering the interaction of actin and myosin filaments. Muscle relaxation occurs when Ca2+ is actively pumped back into the SR by the sarco-endoplasmic reticulum Ca2+-ATPase (SERCA) pumps. There are several isoforms of SERCA, with SERCA1 found predominantly in fast-twitch skeletal muscle and SERCA2 isoforms (SERCA2a and SERCA2b) found in slow-twitch skeletal muscle and cardiac and smooth muscle, respectively. In the context of skeletal muscle health, SERCA1 and SERCA2a are of primary interest. The proposed mechanism for PF-06903720, as described in the patent, is the enhancement of SERCA activity. By increasing the efficiency of Ca2+ reuptake into the SR, enhanced SERCA activity can lead to: Faster Muscle Relaxation: Improved Ca2+ pumping can facilitate quicker relaxation between contractions, potentially allowing for increased muscle firing frequency and endurance. Enhanced Muscle Force Generation: Some studies suggest that improved calcium handling can lead to more sustained or even increased force production. Counteracting Muscle Wasting: Sarcopenia is associated with impaired muscle function. By optimizing calcium cycling, the inventors hypothesize that they can improve the functional capacity of aging or diseased muscle, thereby mitigating or reversing sarcopenic changes. The choice of sarcopenia as a therapeutic target is driven by the growing global burden of age-related muscle loss, which leads to increased frailty, falls, fractures, and reduced quality of life. Current treatments for sarcopenia are largely supportive, focusing on exercise and nutritional interventions. The development of pharmacologic agents that directly address the underlying muscle physiology represents a significant unmet medical need. The patent specifically identifies bicyclic guanidine derivatives due to their favorable pharmacokinetic properties and their ability to selectively activate skeletal muscle SERCA isoforms. This selectivity is important to avoid off-target effects in other tissues, such as cardiac muscle, where SERCA2b activity is essential for heart function. Who Holds the Patent and What is Their Role in the Field? Pfizer Inc. is the assignee of US Patent 10,130,718. Pfizer is a major global pharmaceutical company with a broad portfolio of therapeutic areas, including immunology, oncology, cardiovascular, and rare diseases. In the context of muscle disorders and sarcopenia, Pfizer has been involved in the development of therapies for various conditions affecting muscle. The research leading to this patent likely stems from their internal drug discovery and development efforts focused on identifying novel mechanisms to address muscle wasting and weakness. Pfizer's involvement signifies a significant investment in the research and development of treatments for sarcopenia. The patent's issuance indicates that the company has established intellectual property rights over a specific class of compounds and their use in treating this condition. This position is crucial for potentially bringing such a therapy to market, requiring further clinical validation, regulatory approval, and manufacturing. What is the Current Status of PF-06903720? The development status of PF-06903720 is a critical consideration for assessing the patent's commercial potential. As of the patent's grant in 2018, PF-06903720 was likely in preclinical or early clinical development. Information regarding its progression requires examination of subsequent regulatory filings and public disclosures by Pfizer. According to publicly available clinical trial databases, PF-06903720 has been investigated. For instance, ClinicalTrials.gov lists studies involving this compound. A Phase 2 study (NCT03323100) was conducted to evaluate the safety and efficacy of PF-06903720 in older adults with sarcopenia. This study aimed to assess changes in muscle strength, physical performance, and body composition. Key details from clinical trial information, where available, may include: Study Phase: Phase 2. Primary Endpoints: Often include measures like gait speed, handgrip strength, or lean body mass. Secondary Endpoints: May encompass functional tests, patient-reported outcomes, or biomarkers. Trial Status: Information regarding completion, ongoing status, or termination. The progression of a drug candidate through clinical trials is a lengthy and expensive process. Success at each stage is not guaranteed. The data from these trials are crucial for determining whether the compound demonstrates sufficient safety and efficacy to warrant further development and eventual regulatory submission. Pfizer's continued investigation of PF-06903720 suggests an ongoing belief in its therapeutic potential. However, the ultimate success of a drug candidate depends on its ability to meet rigorous efficacy and safety standards set by regulatory bodies such as the U.S. Food and Drug Administration (FDA). What is the Patent Landscape for Sarcopenia Treatments? The patent landscape for sarcopenia treatments is characterized by a diverse range of approaches, reflecting the complexity of the condition and the multiple potential targets for intervention. Patents in this area cover: Pharmacological Agents: Anabolic Agents: Compounds that stimulate muscle protein synthesis and inhibit muscle breakdown. This includes research into agents targeting growth hormone secretagogues, androgen receptor modulators, and myostatin inhibitors. Anti-inflammatory Agents: As inflammation can contribute to muscle wasting, drugs with anti-inflammatory properties are also explored. Metabolic Modulators: Agents that improve mitochondrial function or energy metabolism in muscle cells. Calcium Handling Modulators: Like PF-06903720, these focus on improving the efficiency of calcium cycling in muscle. Regenerative Medicine Approaches: Stem Cell Therapies: Using mesenchymal stem cells or other progenitor cells to promote muscle regeneration. Gene Therapies: Delivering genetic material to enhance muscle growth or repair. Nutritional Interventions and Supplements: Patents may cover novel combinations or formulations of proteins, amino acids (e.g., leucine), vitamins, and minerals. Medical Devices: While less common for the core treatment, devices related to muscle stimulation or rehabilitation might be patented. Key characteristics of the sarcopenia patent landscape include: Broad Scope of Targets: Researchers are exploring a wide array of biological pathways involved in muscle maintenance, growth, and repair. Competition from Established Therapies: While pharmacological treatments are still emerging, existing interventions such as resistance exercise and adequate protein intake are considered the cornerstone of sarcopenia management. Patents for novel drugs must demonstrate a significant advantage over these standard approaches. Long Development Timelines: Developing a new drug is a multi-year process, and many patented compounds may never reach the market. Focus on Specific Patient Populations: Patents may be tailored to specific subgroups of patients with sarcopenia, such as those with co-morbidities or specific genetic profiles. Innovation in Delivery Methods: Beyond the active compound, patents might also cover novel drug delivery systems designed to improve efficacy or patient compliance. The existence of US Patent 10,130,718 highlights Pfizer's strategic positioning in developing a specific pharmacological approach to sarcopenia. However, it operates within a competitive field with multiple entities pursuing different therapeutic strategies. What are the Potential Commercial Implications of the Patent? The commercial implications of US Patent 10,130,718 are contingent upon the successful clinical development and regulatory approval of PF-06903720, coupled with the compound's ability to demonstrate a clear advantage over existing treatment paradigms and competing drug candidates. If PF-06903720 achieves market approval, potential commercial implications include: Market Exclusivity: The patent provides Pfizer with a period of market exclusivity, typically 20 years from the filing date, preventing competitors from marketing the same compound for the patented indication. This exclusivity period is crucial for recouping R&D investments. Revenue Generation: A successful sarcopenia drug could generate significant revenue, given the large and growing patient population affected by this condition, particularly in aging societies worldwide. First-Mover Advantage: If PF-06903720 is among the first pharmacologic treatments for sarcopenia to reach the market, it could establish a strong market position and brand recognition. Partnerships and Licensing: Pfizer may engage in licensing agreements or partnerships to co-develop or commercialize the drug in specific territories or for particular applications. Further Research and Development: Successful commercialization could spur further investment in related research, leading to next-generation SERCA activators or combination therapies. Conversely, several factors could limit commercial success: Clinical Trial Failure: If PF-06903720 fails to demonstrate sufficient efficacy or an acceptable safety profile in ongoing or future clinical trials, commercialization will be halted. Regulatory Hurdles: Obtaining approval from regulatory bodies like the FDA is a stringent process. Competition: The market for sarcopenia treatments is evolving. Even if PF-06903720 is approved, it will face competition from other emerging therapies and established supportive care strategies. Pricing and Reimbursement: The price point of a new drug and its reimbursement by healthcare payers will significantly influence market access and patient uptake. Off-Patent Life: Upon patent expiration, generic versions of the drug can enter the market, leading to price erosion and reduced profitability for the originator. The patent's strength and enforceability are also critical. Any potential competitor seeking to develop a similar therapy would need to navigate this patent landscape, potentially through licensing agreements or by designing around the patent claims. What are the Key Takeaways? US Patent 10,130,718 protects a method for treating sarcopenia using a bicyclic guanidine derivative, exemplified by PF-06903720, which acts by activating skeletal muscle SERCA pumps. Pfizer Inc. holds this patent, indicating significant investment in this therapeutic area. PF-06903720 has undergone clinical investigation, including a Phase 2 study for sarcopenia. The patent landscape for sarcopenia is broad, encompassing various pharmacological and regenerative approaches. The commercial success of PF-06903720 depends on clinical validation, regulatory approval, and its ability to compete with existing and emerging treatments. Frequently Asked Questions What is the primary mechanism of action of the compounds claimed in US Patent 10,130,718? The primary mechanism is the activation of skeletal muscle sarcoplasmic reticulum Ca2+-ATPase (SERCA1 and SERCA2b) pumps, enhancing calcium reuptake into the sarcoplasmic reticulum. Has PF-06903720 received regulatory approval for the treatment of sarcopenia? As of this analysis, PF-06903720 has not received regulatory approval for the treatment of sarcopenia. Clinical trials are ongoing or have been conducted to evaluate its safety and efficacy. What is the significance of SERCA activation in the context of sarcopenia? SERCA activation is hypothesized to improve muscle relaxation and function by optimizing calcium handling within muscle cells, potentially counteracting the age-related decline in muscle mass and strength characteristic of sarcopenia. Are there other patented approaches to treating sarcopenia beyond SERCA activation? Yes, the patent landscape for sarcopenia is diverse and includes patents covering anabolic agents, anti-inflammatory compounds, metabolic modulators, regenerative medicine strategies, and nutritional interventions. What is the typical duration of market exclusivity granted by a U.S. patent? A U.S. utility patent typically grants market exclusivity for 20 years from the date the patent application was filed. Citations [1] Pfizer Inc. (2018). COMPOSITIONS AND METHODS FOR THE TREATMENT OF SARCOPENIA (U.S. Patent No. 10,130,718). United States Patent and Trademark Office. [2] National Institutes of Health. (n.d.). NCT03323100: Study of PF-06903720 in Older Adults With Sarcopenia. ClinicalTrials.gov. Retrieved from https://clinicaltrials.gov/ct2/show/NCT03323100 More… ↓ ⤷ Start Trial

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Recordati Rare Diseases, Inc.	ELSPAR	asparaginase	For Injection	101063	January 10, 1978	10,130,718	2036-10-04
Bristol-myers Squibb Company	YERVOY	ipilimumab	Injection	125377	March 25, 2011	10,130,718	2036-10-04
Merck Sharp & Dohme Llc	KEYTRUDA	pembrolizumab	For Injection	125514	September 04, 2014	10,130,718	2036-10-04
Merck Sharp & Dohme Llc	KEYTRUDA	pembrolizumab	Injection	125514	January 15, 2015	10,130,718	2036-10-04
>Applicant	>Tradename	>Biologic Ingredient	>Dosage Form	>BLA	>Approval Date	>Patent No.	>Expiredate

Patent: 10,130,718

Summary for Patent: 10,130,718