Target intelligence / Profile preview

Thyroxine (T4) (T4)

Target
T4
Molecular classification
Other (hormone, as it is not a receptor, enzyme, transporter, or similar target)
01

Overview

Levothyroxine is the synthetic levo-isomer form of thyroxine (T4), a principal hormone produced by the thyroid gland. It functions as a prohormone for triiodothyronine (T3), its more active metabolite, and is essential for normal metabolism, growth, and neurological development. Levothyroxine is used primarily as a replacement therapy in hypothyroidism (both congenital and acquired), as well as for thyrotropin suppression in certain thyroid cancers. It does not act as a receptor, enzyme, or transporter, but replaces natural hormone and exerts effects via conversion to T3 and activation of nuclear thyroid hormone receptors. It is one of the most prescribed medications worldwide, though inappropriate use and over-replacement can pose significant health risks[1][2][3][4][5][6].

Other names
LevothyroxineL-thyroxineT43,3',5,5'-Tetraiodyl-L-thyronineL-thyroxine sodium saltLT4
02

Mechanism of action

Thyroxine (T4) is a prohormone that is converted to triiodothyronine (T3), the active form. T3 binds to nuclear thyroid hormone receptors to regulate gene transcription and protein synthesis, leading to increased metabolic rate, oxygen consumption, and energy use[1][3][5].

03

Biological functions

Regulation of metabolismGrowth and development (especially in fetal and neonatal brain and skeleton)Regulation of protein synthesisRegulation of energy expenditure
04

Disease associations

HypothyroidismMyxedema comaThyroid hormone deficiencyUsed adjunctively in thyroid cancer
05

Safety considerations

Over-replacement can cause symptoms of hyperthyroidism (arrhythmia, cardiac ischemia, osteoporosis)Not to be used for weight loss in euthyroid patientsPatients with cardiovascular disease, elderly, and pregnant patients require careful dosingMultiple drug and food interactions can affect bioavailability and efficacy
06

Interacting drugs

Includes but not limited to: Amiodarone

10 more in the full profile.

07

Biomarkers

Serum thyrotropin (TSH)Free thyroxine (free T4)Free triiodothyronine (free T3)

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