Drug intelligence / Profile preview

adjudin

Development stage
Preclinical
Lead developer
Population Council
Modality
Small Molecules
Administration
Oral, Intraperitoneal
01

Overview

Adjudin is an **indazole-based compound** and an **analog of lonidamine** that was initially developed as a potential **non-hormonal male contraceptive**. It acts as a **testis-specific adherens junction disruption inducer**, primarily targeting the **ectoplasmic specialization (ES)** at the Sertoli-spermatid interface. By disrupting actin microfilament bundles at the ES, adjudin causes **premature germ cell exfoliation** from the seminiferous epithelium, leading to reversible infertility without affecting testosterone, FSH, or LH levels. Studies have shown effectiveness in rats, rabbits, and dogs, with complete reversible infertility achieved within 5 weeks and fertility recovery by 11 weeks post-treatment. Beyond contraceptive applications, adjudin has demonstrated **anti-cancer properties** by inducing apoptosis through caspase-3-dependent pathways, triggering mitochondrial dysfunction, and reducing ATP levels in cancer cells. It has shown efficacy against multiple cancer cell lines including lung, prostate, gastric, breast, hepatoma, and pancreatic cancers both in vitro and in vivo. Additional biological activities include **anti-inflammatory effects in the brain**, **anti-neurodegeneration properties**, and **anti-ototoxicity** against gentamicin-induced damage. The compound acts as a **mitochondria-targeting drug** and **chloride channel blocker**.

Other names
1-(2,4-dichlorobenzyl)-1H-indazole-3-carbohydrazide1-[(2,4-dichlorophenyl)methyl]indazole-3-carbohydrazide
02

Targets

HK2 (Hexokinase Type II)ClC (CLC chloride channel family)Actin filament proteinsABCG2 (Breast cancer resistance protein)

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