{"id":"02501","slug":"non-steroidal-androgen--02501","source":{"id":"02501","dataset":"techtransfer","title":"Non-Steroidal Androgen Receptor Antagonists for Advanced Prostate Cancer Therapy","description_":"

This invention features a new class of non-steroidal compounds designed to act as highly potent androgen receptor antagonists. They offer a powerful therapeutic strategy to inhibit prostate cancer cell growth, specifically targeting strains resistant to current standard-of-care treatments.

Description

The technology encompasses a unique series of non-steroidal analogs structured to bind effectively to the androgen receptor (AR) and suppress its biological activity. These molecules utilize specialized chemical frameworks to optimize their binding affinity and metabolic stability. By altering the core architecture compared to conventional treatments, these compounds avoid the molecular vulnerabilities that typically allow mutating cancer cells to develop resistance.\r\n\r\nIn vitro screening demonstrates that these novel agents significantly suppress AR-mediated transcription and cell proliferation in both standard and enzalutamide-resistant prostate cancer cell lines. They exhibit nanomolar potency (IC50 values) in reducing the expression of Prostate-Specific Antigen (PSA) and driving down tumor cell viability. Furthermore, structural modifications, such as evaluating specific enantiomeric forms, have allowed the fine-tuning of their pharmacokinetic profile, balancing strong therapeutic efficacy with optimal metabolic clearance.

Applications

- Advanced Oncology Therapeutics: Development of next-generation oral therapeutics specifically for metastatic castration-resistant prostate cancer (mCRPC).\r
- Combination Drug Regimens: Implementation alongside existing standards of care like abiraterone or enzalutamide to maximize tumor suppression.\r
- Androgen-Driven Disorder Treatments: Expansion into clinical therapies for other conditions mediated by hyperactive androgen receptors.\r
- Diagnostic and Research Assays: Employment as highly selective control reagents or chemical probes in academic and corporate AR signaling research.

Advantages

- Overcomes Treatment Resistance: Demonstrates robust efficacy against enzalutamide-resistant prostate cancer cell models.\r
- High Anti-Androgenic Potency: Achieves significant suppression of androgen receptor activity and PSA levels at nanomolar concentrations.\r
- Non-Steroidal Advantage: Minimizes the broad off-target metabolic or hormonal side effects frequently associated with traditional steroidal agents.\r
- Optimized Metabolic Stability: Engineered with structural modifications that improve half-life and resistance to rapid enzymatic breakdown.\r
- Flexible Combinatorial Potential: Fully compatible with existing therapeutic regimens, such as androgen deprivation therapy (ADT) or modern anti-androgens.

Invention Readiness

In vivo and In vitro data. Preclinical efficacy and pharmacology data have been validated by third parties.

IP Status

https://patents.google.com/patent/US10004730B2; https://patents.google.com/patent/US10882834B2; https://patents.google.com/patent/US10544110B2; https://patents.google.com/patent/US10980806B2; https://patents.google.com/patent/US9708276B2; https://patents.google.com/patent/US9981974B2

","tags":["Precision medicine"],"file_number":"02501","collections":[],"meta_description":"Non-steroidal androgen receptor antagonists deliver potent, resistance-guarded therapy for metastatic prostate cancer with favorable safety and PK.","image_url":"","apriori_judge_output":"{\"scores\":{\"novelty\":2.0,\"potential_impact\":3.0,\"readiness\":2.0,\"scalability\":2.0,\"timeliness\":2.0},\"weighted_score\":2.22,\"risks\":[\"Outdated (2011) with preclinical readiness; clinical translation risk high; potential redundancy with existing AR antagonists; safety/PK gaps; limited in vivo models for current standards; lack of published clinical data; regulatory path unclear.\"],\"one_sentence_take\":\"Moderate novelty with historically developed AR antagonists; preclinical readiness in 2011, limited timeliness and translational clarity for current prostate cancer needs.\"}","lead_inventor_name":"Zhou Wang","lead_inventor_dept":"Med-Urology","technology_type":"Therapeutic Modality","technology_subtype":"Small Molecule","therapeutic_areas":["Oncology"],"therapeutic_indications":["Prostate cancer / adenocarcinoma"],"custom_tags":[],"all_tech_innovators":["Paul A. Johnston","John S. Lazo","Joel B. Nelson","Minh Mindy Bao Nguyen","Zhou Wang"],"date_submitted":"2011-06-10","technology_readiness_level":"4. Pre-clinical development"},"highlight":{},"matched_queries":null,"score":0.0}