AR-targeted Therapy Development
The androgen receptor (AR) is a ligand-activated transcription factor that plays a critical role in normal mammary gland development and function. In breast cancer, AR can exhibit both tumor-suppressive and tumor-promoting effects, depending on the molecular context. At Alfa Cytology, we specialize in the preclinical discovery of AR inhibitors and promotes the development of new therapies for breast cancer.
Introduction to AR-targeted Therapy for Breast Cancer
In ER-positive/HER2-negative tumors, AR activation has been shown to inhibit cell proliferation and counteract the effects of estrogen signaling. Conversely, in TNBC, AR can promote tumor growth and metastasis by activating pro-survival pathways and inducing an immunosuppressive tumor microenvironment.
Fig.1 AR signalling pathways and therapeutic targets of AR. (Ayoub N. M., et al. 2022)
AR-targeted Therapy Development for Breast Cancer
While significant advancements have been made in the treatment of hormone receptor-positive and HER2-positive breast cancers, the triple-negative breast cancer (TNBC) subtype remains a major clinical challenge. In this context, the androgen receptor (AR) has emerged as a promising target for novel breast cancer interventions. Researchers develop novel AR-targeted therapies for breast cancer.
| NCT number | Category | AR agent | Phase |
| NCT03444025 | ADT | Goserelin | |
| NCT01352091 | ADT | Goserelin | |
| NCT03878524 | CYP17-lyase inhibitor/antiandrogen | Abiraterone/Enzalutamide | |
| NCT02953860 | Antiandrogen | Enzalutamide | |
| NCT02955394 | Antiandrogen | Enzalutamide | |
| NCT02676986 | Antiandrogen | Enzalutamide | |
| NCT00755885 | CYP17-lyase inhibitor | Abiraterone acetate | |
| NCT01990209 | CYP17-lyase inhibitor | Orteronel | |
| NCT01616758 | SARM | Enobosarm | |
| NCT02463032 | SARM | Enobosarm | |
| NCT02144051 | Antisense oligonucleotides | AZD5312 |
Our Services
As a leading preclinical CRO, Alfa Cytology is committed to advancing the development of innovative cancer therapies, including novel AR-targeted therapies for breast cancer. Our state-of-the-art facilities and multidisciplinary team of experts provide comprehensive services to support the entire drug development process, from target identification and validation to preclinical studies and biomarker development.
Directly Targeting the AR
- AR Agonist Development
Steroid-Based AR Agonists
Nonsteroidal AR Agonists
Polycyclic AR Agonists - AR Antagonist Development
Androgen-Competitive Antagonists - PROTAC AR Degrader Development
Indirectly Targeting the AR
- mRNA Development Targeting the AR
Antisense Oligonucleotides
Small Interfering RNA - CYP17 Inhibitor Development
- luteinizing Hormone Releasing Hormone (LHRH) Agonist Development
- Heat Shock Protein 90 (Hsp90) Inhibitor Development
Alfa Cytology provides development services for AR-targeted therapies, covering drug design, screening, and efficacy research to find ideal drug candidates for you and accelerate preclinical research on your breast cancer therapeutics. To learn more about our capabilities in AR-targeted therapy development for breast cancer or to discuss potential collaborative opportunities, please don't hesitate to contact us.
Reference
- Kolyvas, E.A., Caldas, C., and et al. Androgen receptor function and targeted therapeutics across breast cancer subtypes. Breast Cancer Res. 2022, 24, 79.