Drug intelligence / Profile preview

propylthiouracil

Development stage
Approved
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

Propylthiouracil (PTU) is a thionamide antithyroid agent used for the management of hyperthyroidism associated with Graves' disease or toxic multinodular goiter. Its primary mechanism involves the inhibition of thyroid peroxidase (TPO), which prevents the iodination of tyrosine residues on thyroglobulin and the subsequent coupling of iodotyrosines to form T3 and T4. Additionally, PTU is unique among thionamides for its ability to inhibit Type 1 iodothyronine deiodinase (DIO1), thereby reducing the peripheral conversion of thyroxine (T4) to the more potent triiodothyronine (T3). While effective, PTU is associated with a risk of severe hepatotoxicity and agranulocytosis, leading to its use being primarily reserved for patients who cannot tolerate methimazole, those in their first trimester of pregnancy, or those experiencing thyroid storm.

Brand names
Propyl-Thyracil
Other names
6-propyl-2-thiouracil丙硫氧嘧啶
02

Targets

TPO (Thyroid peroxidase)DIO1 (Type I iodothyronine deiodinase)

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