Drug intelligence / Profile preview

bithionol

Development stage
Preclinical
Lead developer
Champions Oncology
Modality
Small Molecules
Administration
Oral, Topical
01

Overview

Bithionol is a synthetic small molecule formerly used as an antibacterial and anthelmintic agent. It was primarily indicated for the treatment of parasitic infections such as fascioliasis (liver fluke infection) and paragonimiasis (lung fluke infection), and has also been used in veterinary medicine to treat tapeworms in horses[3][4]. Bithionol acts as a potent inhibitor of soluble adenylyl cyclase by binding to its bicarbonate binding site, leading to allosteric inhibition that disrupts the conversion of ATP to cAMP[3][6]. Additional mechanisms include inhibition of estrogen receptor activity and calpain-2 catalytic subunit[1]. Bithionol also exhibits antibacterial, antifungal, algaecidal properties and has shown cytotoxic effects against ovarian cancer cell lines through mechanisms involving reactive oxygen species generation, NF-kB inhibition, and autotaxin inhibition[7][8]. Due to its photosensitizing potential causing serious skin disorders, regulatory approval for human use was withdrawn in 1967; it is no longer marketed for human use but may still be available for research or veterinary applications[1].

Other names
2,2'-thiobis[4,6-dichlorophenol]bis(2-hydroxy-3,5-dichlorophenyl)sulfidebithionolate sodium
02

Targets

sAC (Soluble adenylyl cyclase)

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