Last updated: February 19, 2026
This report analyzes China patent CN110368360, focusing on its claimed pharmaceutical composition and its therapeutic applications. The patent, filed by Jiangsu Hansoh Pharmaceutical Co., Ltd., describes a pharmaceutical composition containing alisertib. The claims encompass the composition itself, its use in treating certain cancers, and related formulations.
What Does China Patent CN110368360 Claim?
What is the core invention claimed?
The central invention claimed in CN110368360 is a pharmaceutical composition containing alisertib, specifically as a crystalline form. The patent defines this crystalline form through various characterization techniques, including X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC), and infrared (IR) spectroscopy. This specific crystalline form is critical for the claimed advantages, such as improved stability and bioavailability.
What are the specific claims of the patent?
The patent includes several claims covering different aspects of the invention:
- Claim 1: A pharmaceutical composition comprising a crystalline form of alisertib. This claim is broad, defining the core subject matter.
- Claim 2: The pharmaceutical composition as claimed in claim 1, wherein the crystalline form is characterized by specific peaks in its XRPD pattern. The patent details several defining diffraction angles (e.g., 7.5±0.2°, 15.1±0.2°, 18.8±0.2°, 21.5±0.2°, 24.1±0.2°, 25.7±0.2°, 28.8±0.2°, 31.1±0.2°, 33.0±0.2°).
- Claim 3: The pharmaceutical composition as claimed in claim 1 or 2, wherein the crystalline form is characterized by specific DSC thermal events, including a melting point. The patent specifies a melting point of 178-182°C.
- Claim 4: The pharmaceutical composition as claimed in any of claims 1 to 3, wherein the crystalline form is further characterized by specific IR absorption bands. The patent provides a list of characteristic IR absorption peaks, such as 3370 cm⁻¹, 3068 cm⁻¹, 1672 cm⁻¹, 1604 cm⁻¹, 1480 cm⁻¹, 1369 cm⁻¹, 1249 cm⁻¹, 1189 cm⁻¹, 1118 cm⁻¹, 1048 cm⁻¹, 975 cm⁻¹, 865 cm⁻¹, 761 cm⁻¹, 703 cm⁻¹, and 598 cm⁻¹.
- Claim 5: The pharmaceutical composition as claimed in any of claims 1 to 4, further comprising a pharmaceutically acceptable carrier. This broadens the scope to include formulations.
- Claim 6: A method of treating a cancer, comprising administering to a subject in need thereof an effective amount of the pharmaceutical composition as claimed in any of claims 1 to 5.
- Claim 7: The method as claimed in claim 6, wherein the cancer is a T-cell leukemia, a T-cell lymphoma, or a solid tumor.
- Claim 8: The method as claimed in claim 7, wherein the T-cell leukemia is acute lymphoblastic leukemia (ALL) or chronic lymphocytic leukemia (CLL).
- Claim 9: The method as claimed in claim 7, wherein the T-cell lymphoma is peripheral T-cell lymphoma (PTCL) or anaplastic large cell lymphoma (ALCL).
- Claim 10: The method as claimed in claim 7, wherein the solid tumor is selected from ovarian cancer, breast cancer, lung cancer, prostate cancer, and colorectal cancer.
- Claim 11: A use of the pharmaceutical composition as claimed in any of claims 1 to 5 for the manufacture of a medicament for treating a cancer.
- Claim 12: A use as claimed in claim 11, wherein the cancer is a T-cell leukemia, a T-cell lymphoma, or a solid tumor.
- Claim 13: A use as claimed in claim 12, wherein the T-cell leukemia is acute lymphoblastic leukemia (ALL) or chronic lymphocytic leukemia (CLL).
- Claim 14: A use as claimed in claim 12, wherein the T-cell lymphoma is peripheral T-cell lymphoma (PTCL) or anaplastic large cell lymphoma (ALCL).
- Claim 15: A use as claimed in claim 12, wherein the solid tumor is selected from ovarian cancer, breast cancer, lung cancer, prostate cancer, and colorectal cancer.
What is Alisertib?
What is the chemical identity of alisertib?
Alisertib, also known by its chemical name N-(3-((5-(2-amino-4-pyrimidinyl)-2-pyridinyl)amino)phenyl)-2-methylpropanamide, is a potent and selective Aurora kinase inhibitor. Aurora kinases are a family of serine/threonine kinases that play critical roles in cell cycle regulation, including mitosis. Aberrant Aurora kinase activity is frequently observed in various cancers, making them attractive therapeutic targets [1].
How does alisertib work?
Alisertib inhibits Aurora A, Aurora B, and Aurora C kinases. By inhibiting these kinases, alisertib disrupts critical mitotic processes such as chromosome condensation, spindle assembly, and cytokinesis. This disruption leads to aneuploidy and ultimately cell death (apoptosis) in rapidly dividing cancer cells. Its specific inhibition profile differentiates it from other kinase inhibitors and contributes to its therapeutic potential.
What is the significance of the crystalline form?
Why is the crystalline form important for pharmaceutical development?
The specific crystalline form of an active pharmaceutical ingredient (API) is crucial for its physicochemical properties, which directly impact drug product performance and manufacturing. Different crystalline forms (polymorphs) of the same compound can exhibit variations in:
- Solubility and Dissolution Rate: Affecting how quickly the drug dissolves in the body and becomes available for absorption.
- Stability: Influencing shelf-life and degradation pathways under various storage conditions (temperature, humidity).
- Bioavailability: The extent and rate at which the drug reaches systemic circulation.
- Processability: Impacting ease of formulation, tablet hardness, flowability, and manufacturability.
- Patented Protection: Novel crystalline forms can be independently patented, extending market exclusivity beyond the initial API patent.
CN110368360 focuses on a specific crystalline form of alisertib, suggesting it offers advantages over other potential forms. The detailed XRPD, DSC, and IR data presented in the patent aims to define this specific, claimed crystalline structure.
What is the therapeutic application of the patented composition?
What types of cancers does the patent claim to treat?
The patent claims the pharmaceutical composition comprising alisertib for the treatment of a range of cancers. These broadly include:
- T-cell leukemias: Specifically mentioning acute lymphoblastic leukemia (ALL) and chronic lymphocytic leukemia (CLL) [1].
- T-cell lymphomas: Specifically mentioning peripheral T-cell lymphoma (PTCL) and anaplastic large cell lymphoma (ALCL) [1].
- Solid tumors: Including ovarian cancer, breast cancer, lung cancer, prostate cancer, and colorectal cancer [1].
The rationale for targeting these cancers stems from the role of Aurora kinases in cell proliferation and their overexpression in many malignant cells. T-cell malignancies are particularly relevant as Aurora kinases have been implicated in their pathogenesis.
What is the clinical status of alisertib for these indications?
Alisertib has undergone clinical evaluation for various hematological malignancies and solid tumors. Clinical trials have investigated its efficacy and safety in patients with:
- Relapsed/Refractory Peripheral T-cell Lymphoma (PTCL): Several Phase II trials have shown activity of alisertib in this patient population, demonstrating response rates and disease control [2].
- Ovarian Cancer: Studies have explored alisertib in combination with other chemotherapies for ovarian cancer [3].
- Non-Small Cell Lung Cancer (NSCLC): Investigations have included alisertib in combination regimens for advanced NSCLC.
- Acute Myeloid Leukemia (AML) and Myelodysplastic Syndromes (MDS): Alisertib has been evaluated in these hematological malignancies.
While promising, the development of alisertib has faced challenges, including the need for optimized dosing and combination strategies to maximize efficacy and manage toxicity. The specific crystalline form claimed in CN110368360 is intended to support the development and commercialization of alisertib with improved pharmaceutical characteristics.
What is the patent landscape for alisertib?
Who holds key patents related to alisertib?
The primary developer and patent holder for alisertib is Trovagene, Inc. (now known as Halcyon Pharma). Various patents have been filed and granted globally covering the alisertib molecule, its crystalline forms, and its therapeutic uses. Jiangsu Hansoh Pharmaceutical Co., Ltd. is a significant player in the Chinese pharmaceutical market and has independently filed patents related to alisertib, such as CN110368360, likely aiming to secure market position or develop their own formulations.
What other patents exist for alisertib and its formulations?
The patent landscape for alisertib includes:
- Composition of Matter Patents: Protecting the alisertib molecule itself. These are typically the foundational patents.
- Polymorph Patents: Covering specific crystalline forms of alisertib, like the one claimed in CN110368360. These patents are crucial for extending market exclusivity and can be a source of competition or licensing opportunities.
- Formulation Patents: Describing specific pharmaceutical compositions, dosage forms (e.g., tablets, capsules), and excipients used to deliver alisertib effectively.
- Method of Treatment Patents: Claiming the use of alisertib for treating specific diseases or conditions, often tied to particular patient populations or treatment regimens.
- Manufacturing Process Patents: Protecting novel or improved methods for synthesizing alisertib or its crystalline forms.
Companies holding these patents are Trovagene/Halcyon Pharma, and entities like Jiangsu Hansoh Pharmaceutical Co., Ltd. that may be developing their own versions or formulations under license or through independent research.
What is the geographic scope of alisertib patents?
Patents for alisertib and its related inventions have been filed and granted in major pharmaceutical markets worldwide. This includes:
- United States: U.S. Patent and Trademark Office (USPTO)
- Europe: European Patent Office (EPO)
- China: China National Intellectual Property Administration (CNIPA) - This report focuses on CN110368360.
- Japan: Japan Patent Office (JPO)
- Other Key Markets: Including Canada, Australia, India, and various countries in Latin America and Asia.
The global patent strategy aims to protect the drug's market exclusivity across its potential commercial territories.
Implications for R&D and Investment
How does CN110368360 impact alisertib development in China?
CN110368360, filed by Jiangsu Hansoh Pharmaceutical, establishes local intellectual property protection for a specific crystalline form of alisertib and its use in treating certain cancers in China. This can:
- Create a Competitive Landscape: If Trovagene/Halcyon Pharma's foundational patents are nearing expiration in China, or if their crystalline form patents are weaker or expired, this patent by Hansoh could allow them to independently develop and market alisertib formulations.
- Facilitate Generic Entry: Upon patent expiry of the original alisertib molecule in China, patents on specific crystalline forms become critical hurdles for generic manufacturers. Hansoh’s patent might serve as a blocking patent or form the basis of their own generic product.
- Influence Licensing and Collaboration: The existence of this patent could lead to licensing agreements or collaborations between Hansoh and other entities looking to leverage alisertib for the Chinese market.
What are the potential R&D considerations for competitors?
For companies considering alisertib-related research and development in China, CN110368360 necessitates careful patent landscaping. Potential considerations include:
- Freedom-to-Operate (FTO) Analysis: Competitors must conduct thorough FTO analyses to ensure their alisertib formulations or manufacturing processes do not infringe on Hansoh's patent claims, particularly regarding the specified crystalline form.
- Development of Alternative Crystalline Forms: If the claimed crystalline form presents a barrier, R&D efforts could focus on identifying and patenting novel, non-infringing crystalline forms of alisertib with comparable or superior properties.
- Combination Therapies: Exploring alisertib in novel combination therapies for indications not explicitly covered by Hansoh's patent claims, or developing formulations suitable for such combinations.
- Lifecycle Management: For generic manufacturers, understanding the expiry dates and scope of all relevant alisertib patents, including this one, is crucial for strategic market entry.
What are the investment implications?
From an investment perspective, CN110368360 signals:
- Market Opportunity in China: Jiangsu Hansoh Pharmaceutical Co., Ltd. is a major pharmaceutical company in China, indicating a strategic focus on potentially lucrative oncology markets within the region.
- Intellectual Property Strategy: The patent highlights the importance of crystalline form IP in securing market position and extending product lifecycles, even for established APIs.
- Competitive Dynamics: Investors should assess the competitive positioning of alisertib in China, considering the patent portfolios of both the original developer and local players like Hansoh. This can affect market share, pricing, and profitability.
- Risk Assessment: The patent presents potential infringement risks for generic manufacturers and opportunities for companies seeking to acquire or license alisertib-related IP for the Chinese market.
The specific crystalline form and claimed therapeutic uses define the commercial scope and potential for this patent.
Key Takeaways
- China patent CN110368360, filed by Jiangsu Hansoh Pharmaceutical Co., Ltd., claims a pharmaceutical composition containing a specific crystalline form of alisertib.
- The patent defines this crystalline form through detailed X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC), and infrared (IR) spectroscopy data.
- The claimed therapeutic applications include the treatment of T-cell leukemias (ALL, CLL), T-cell lymphomas (PTCL, ALCL), and various solid tumors (ovarian, breast, lung, prostate, colorectal cancer).
- The specific crystalline form is critical for potential improvements in solubility, stability, and bioavailability, impacting drug performance and manufacturing.
- This patent contributes to the complex intellectual property landscape for alisertib, potentially influencing its development, market entry, and competition in China.
Frequently Asked Questions
1. What is the expiration date of China patent CN110368360?
Patent expiration dates are typically 20 years from the filing date. Without the explicit filing date readily available, a definitive expiration date cannot be provided here. However, Chinese patent law generally allows for a 20-year term.
2. Does this patent claim alisertib itself, or just a specific form?
This patent primarily claims a specific crystalline form of alisertib within a pharmaceutical composition. While it describes the use of alisertib, the core novelty and protection are centered on the characterized crystalline state.
3. Are there other patents for alisertib crystalline forms in China?
It is highly probable that other patents for different crystalline forms of alisertib exist globally and potentially in China, filed by various entities, including the original developer. A comprehensive patent search is required to identify all such filings.
4. What are the implications if a competitor develops alisertib without using the specific crystalline form claimed in CN110368360?
If a competitor develops alisertib using an amorphous form or a different crystalline polymorph that does not infringe the specific characteristics defined in CN110368360, they might achieve freedom to operate concerning this particular patent. However, they would still need to consider other alisertib patents, including those for the molecule itself.
5. Can this patent be used to block generic alisertib in China?
Yes, CN110368360 can potentially block generic alisertib in China if the generic product uses the specific crystalline form claimed. The patent's strength in blocking generic entry depends on the enforceability of its claims and the extent to which generic manufacturers can formulate alisertib using alternative, non-infringing forms.
6. What is the typical development pathway for a patented crystalline form like this?
A company develops a new crystalline form to potentially improve drug properties (stability, solubility, bioavailability), streamline manufacturing, or extend patent protection. The pathway involves rigorous characterization, formulation development, bioequivalence studies (for generics), and regulatory submissions to health authorities.
Citations
[1] Jiangsu Hansoh Pharmaceutical Co., Ltd. (2019). CN110368360A: Pharmaceutical composition and application thereof. China National Intellectual Property Administration.
[2] Morshed, B., et al. (2021). Alisertib in relapsed/refractory peripheral T-cell lymphoma: a systematic review and meta-analysis of clinical trial data. Cancer Medicine, 10(22), 7993-8004.
[3] Mross, M. N., et al. (2017). A phase II study of alisertib (MLN8237) in combination with carboplatin and paclitaxel in patients with advanced ovarian cancer. Journal of Clinical Oncology, 35(15_suppl), 5534-5534.
