Discovery of an Androgen Receptor Degrader Featuring a Pyridazinyl Glutarimide CRBN-Binding Motif for Transdermal Treatment of Androgenetic Alopecia

    May 2026 in “ Journal of Medicinal Chemistry ”
    X Wang, Ling Ge, Yawei Yu … Chong Qin
    Studysummary In this study, the authors developed a novel PROTAC named dAR-6–1, which demonstrated superior hair regeneration in an AGA mouse model compared to minoxidil, highlighting its promise as a therapy due to potent AR degradation and excellent skin permeability.
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    Research cited in this study 19

    1. Discovery of a Novel Non-Invasive AR PROTAC Degrader for the Topical Treatment of Androgenetic Alopecia Journal of Medicinal Chemistry · 2024
    2. A Top-Down Design Approach for Generating a Peptide PROTAC Drug Targeting Androgen Receptor for Androgenetic Alopecia Therapy Journal of medicinal chemistry · 2024
    3. Local and Systemic Mechanisms That Control the Hair Follicle Stem Cell Niche Nature Reviews Molecular Cell Biology · 2023
    4. Androgenetic Alopecia: Therapy Update Drugs · 2023
    5. The AR/miR-221/IGF-1 Pathway Mediates the Pathogenesis of Androgenetic Alopecia International Journal of Biological Sciences · 2023
    6. Protac Degraders of Androgen Receptor-Integrated Dissolving Microneedles for Androgenetic Alopecia and Recrudescence Treatment via Single Topical Administration Small methods · 2022
    7. Efficacy of Asymmetric siRNA Targeting Androgen Receptors for the Treatment of Androgenetic Alopecia Molecular Pharmaceutics · 2022
    8. Oral Minoxidil Use in Androgenetic Alopecia and Telogen Effluvium Archives of Dermatological Research · 2022
    9. Bicalutamide and the New Perspectives for Female Pattern Hair Loss Treatment: What Dermatologists Should Know Journal of Cosmetic Dermatology · 2022
    10. Topical Treatment for Scarring and Non-Scarring Alopecia: An Overview of the Current Evidence Clinical, Cosmetic and Investigational Dermatology · 2021
    11. Current Advances in Stem Cell-Based Therapies for Hair Regeneration European Journal of Pharmacology · 2020
    12. Minoxidil And Its Use In Hair Disorders: A Review Drug Design Development and Therapy · 2019
    13. Androgen Modulation of Wnt/β-Catenin Signaling in Androgenetic Alopecia Archives of Dermatological Research · 2018
    14. Alopecia and the Metabolic Syndrome Clinics in Dermatology · 2017
    15. Transdermal Permeation of Drugs in Various Animal Species Pharmaceutics · 2017
    16. The Effectiveness of Treatments for Androgenetic Alopecia: A Systematic Review and Meta-Analysis Journal of The American Academy of Dermatology · 2017
    17. Molecular Basis of Androgenetic Alopecia: From Androgen to Paracrine Mediators Through Dermal Papilla Journal of Dermatological Science · 2010
    18. Towards a Molecular Understanding of Hair Loss and Its Treatment Trends in Molecular Medicine · 2001
    19. Different Levels of 5α-Reductase Type I and II, Aromatase, and Androgen Receptor in Hair Follicles of Women and Men with Androgenetic Alopecia Journal of Investigative Dermatology · 1997