Related Experiment Video
Updated: Jul 9, 2026

A New Technique for Quantitative Analysis of Hair Loss in Mice Using Grayscale Analysis
Published on: March 9, 2015
Novel Dual Soft Drug Strategy Enables Development of Topical Androgen Receptor Antagonists with Enhanced Efficacy and
Yan Zhang1,2,3, Wenqiang Zhang1, Feng Tang2,3
1School of Science, China Pharmaceutical University, 639 Longmian Avenue, Nanjing 211198, China.
Abstract:
Reconciling therapeutic efficacy with a low risk of systemic toxicity persists as a critical hurdle in developing topical AR antagonists for AGA. Our first-generation soft drug AR antagonist 14-P1 showed pyrilutamide-comparable efficacy with enhanced pharmacokinetics and safety, yet required high dosing due to suboptimal AR antagonism. Here, structural optimization of 14-P1 focused on enhancing intrinsic AR antagonism through thiohydantoin scaffold refinement. Additionally, the implementation of a dual soft drug design strategy yielded the best-performing candidate 39, demonstrating potent AR antagonism (IC50 = 20.6 ± 2.3 nM) and favorable PK profiles. In a hair-growth mouse model, 0.5% 39 achieved comparable efficacy to 0.5% pyrilutamide with accelerated response kinetics (14-day vs 21-day onset) and preserved safety. This dual metabolic inactivation strategy successfully reconciles therapeutic potency with a low risk of systemic toxicity, providing a paradigm for next-generation topical AR antagonist development.
Related Concept Videos
Structure-Activity Relationships and Drug Design
SAR studies the intricate relationship between a drug's chemical structure and biological activity. It focuses on understanding how modifications to a drug's structure can influence its...
Drug-Receptor Interaction: Agonist
Agonists can bind to receptors in different ways. Some agonists bind directly to the receptor's active site, mimicking the endogenous ligand's action.
Principles of Drug Action
Drugs can be agonists or antagonists. Like the endogenous ligands, agonists always bind and activate the target to produce a cellular response. Agonist binding induces a conformational change which in turn...
Modified-Release Drug Delivery Systems: Site-Targeted
Transdermal Drug Delivery Systems
Pharmacogenomics: Identification of New Drug Targets
