Drug intelligence / Profile preview

methylthiouracil

Development stage
Discontinued
Lead developer
Changzhou Kangpu Pharmaceutical
Modality
Small Molecules
Administration
Oral
01

Overview

Methylthiouracil is a small molecule antithyroid drug belonging to the thionamide class, introduced in the mid-1940s for the treatment of hyperthyroidism, including Graves' disease. It acts primarily by inhibiting thyroid peroxidase, an enzyme essential for thyroid hormone synthesis. This inhibition reduces the production of thyroxine (T4) and triiodothyronine (T3), leading to decreased thyroid hormone levels. Methylthiouracil has also demonstrated anti-inflammatory effects in vitro and in vivo and was found effective in a murine model of sepsis. While it is no longer widely used clinically in most countries, it may still be available or used to a limited extent in some regions[1][5][6][8]. Methylthiouracil is classified as an experimental drug and is not approved or marketed widely today; its use has largely been replaced by other thionamides such as propylthiouracil and methimazole due to safety concerns[2][5]. It can cause adverse effects including agranulocytosis, skin reactions, joint pain, and potential carcinogenicity[3]. The compound crosses the placenta and can be excreted into breast milk[4].

Other names
methylthiouracilemethylthiouracilummetiltiouracilo
02

Targets

TPO (Thyroid peroxidase)

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