Pharmaceutical patent analyst最新文献

Introduction: Proteolysis Targeting Chimeras (PROTACs) represents a groundbreaking advancement in drug discovery and targeted protein degradation. Unlike traditional small-molecule inhibitors, PROTACs leverage the cell's natural protein degradation machinery to selectively degrade pathogenic proteins, offering significant therapeutic potential for previously undruggable targets and complex diseases such as cancer and neurodegenerative disorders. Understanding the regulatory landscape governing their approval is crucial as their development accelerates.

Areas covered: This review provides an overview of recent patents, regulatory considerations, emerging concerns, and future perspectives of PROTACs in cancer management.

Expert opinion: From a regulatory perspective, PROTACs present unique challenges and opportunities. Their dual-functional nature requires a nuanced approach to classification and approval, blending small-molecule and biologic regulatory frameworks. Specific guidelines addressing pharmacokinetic and pharmacodynamic profiles are needed. Comprehensive preclinical evaluation and robust clinical trial designs are essential to manage off-target effects and immunogenic responses. The collaboration between regulatory bodies, academia, and industry is crucial for establishing a clear pathway for PROTAC approval. Future considerations must account for advancements in PROTAC technology to ensure safe and effective therapies reach patients. While PROTACs hold immense promise, their regulatory journey requires tailored guidelines and rigorous evaluation to realize their full potential.

A snapshot of noteworthy recent developments in the patent literature of relevance to pharmaceutical and medical research and development.

Claudin-18.2 is an overexpressed molecule in gastric cancer, which is why it is considered a potential therapeutic target. WO2024082060 describes trispecific antibodies directed against CDLN-18.2/CD3/CD28, and gastric cancer treatment method. These antibodies exhibit cytotoxic activity, in coculture with primary human CD3+ T lymphocytes, against gastric cancer cells expressing CLDN-18.2, as well as an inhibition of tumor growth rate in a murine model of gastric cancer. The trispecific structure, in particular the CD3 and CD28 binding domains, induce optimal co-stimulation of effector T cells, suggesting that these antibodies are potential candidates for clinical trials for the treatment of gastric cancer associated with high levels of CDLN-18.2 expression.

A snapshot of noteworthy recent developments in the patent literature of relevance to pharmaceutical and medical research and development.

Quinoline inhibitors are appealing medicinal products for a range of illnesses and problems. It is bicyclic heterocyclic scaffold has been intensively employed in pharmacological research and is well known for its wide range of biological purposes. Biological activities exhibited by quinoline derivatives, such as anti-inflammatory properties, antioxidant, antimicrobial, anti-tubercular, antidiabetic, anti-malarial and others are covered in detail in this review. The IC₅₀ of patented inhibitors might range from nm to μM range, based on the experiments used. It presents an outline of patents file between 2002 and 2023 concerning to biological activities by quinoline derivatives. As a result, it is critical to develop additional chemical quinoline core alterations for novel chemical compounds and enhanced pharmacological impacts.

Aim: the activity of patent claims by Mexican pharmaceutical companies is unknown. Objective: analyse the trend in patents of Mexican pharmaceutical companies. Method: a search for patents was carried out in the patent database of the Mexican Institute of Industrial Property, using the list of Mexican pharmaceutical companies belonging to the Mexican Association of Pharmaceutical Research Industries, and the codes A61K, A61P and C07 of the International Patent Classification. Results: the leading companies in patent applications were Liomont, Senosiain and RIMSA; however, Mexican pharmaceutical companies claim very few patents, only 266 patent applications in the period 2000-2020, with a technological factor with a value of zero, and a commercial factor of little value. Conclusion: Mexican pharmaceutical companies lack a robust patent system, without growth, and with a low percentage of patents with high commercial value.

Pancreatic adenocarcinoma, a devastating disease, has the worst cancer prognosis in humans. It often develops resistance to common chemotherapy medications, such as gemcitabine, taxol and 5-fluorouracil. The dense stroma limits therapeutic efficacy in treating this disease. Low or limited drug loading capacity is another problem with current chemotherapeutic agents. There is a need to develop novel approaches to overcome these issues. Hence, an innovative approach has been proposed to co-deliver both hydrophilic (Gemcitabine) and hydrophobic (Paclitaxel) drugs in a single carrier using lipid bilayer-mesoporous silica nanoparticles (LB-MSNP). MSNPs offer effective drug delivery due to their superior bioavailability and physicochemical properties. Further, in order to achieve clinical translation and regulatory approval, toxicity and biodegradability of MSNPs must be resolved.

Post-surgery cancer recurrence is one of the reasons for increased cancer cases. The effective usage of the enhanced permeability and retention effect of a nanocarrier infused with the bioresponsive release mechanism of checkpoint inhibitors (aPD1 and aCTLA4) can become a boon to mankind. DNA nanococoons (DNCs) comprising cytosine-phosphorothioate-guanine oligodeoxynucleotides (CpG-ODNs) with potent immunostimulatory effects can significantly enhance anti-cancer activity. Triglycerylmonostearate (TGMS) with enzymatic cleavage potential at the wound sites of tumor resection, upon caging with restriction enzyme (HhaI) followed by attaching to DNCs, makes the immunotherapy bioresponsive. Hhal-TGMS-DNCs-aPD1 triggered by the inflammation at the wound site undergoes enzymatic cleavage, releases the restriction enzyme, converts DNCs to CpG ODNs sequentially and with sustained aPD1 release exerts an appreciable anti-cancer effect.