Repositioning Candidate Details
| Candidate ID: | R0102 |
| Source ID: | DB00279 |
| Source Type: | approved; vet_approved |
| Compound Type: | small molecule |
| Compound Name: | Liothyronine |
| Synonyms: | 3,3',5-triiodo-L-thyronine; 3,5,3'-Triiodo-L-thyronine; 3,5,3'-Triiodothyronine; 4-(4-hydroxy-3-iodophenoxy)-3,5-diiodo-L-phenylalanine; L-3,5,3'-Triiodothyronine; L-T3; O-(4-hydroxy-3-iodophenyl)-3,5-diiodo-L-tyrosine; T3; Triiodothyronine |
| Molecular Formula: | C15H12I3NO4 |
| SMILES: | N[C@@H](CC1=CC(I)=C(OC2=CC(I)=C(O)C=C2)C(I)=C1)C(O)=O |
| Structure: |
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| DrugBank Description: | Liothyronine is a thyroidal hormone T3 which is normally produced by the thyroid gland in a ratio 4:1 when compared with T4: T3. Liothyronine is the active form of thyroxine which is composed in a basic chemical structure by a tyrosine with bound iodine. The exogenous liothyronine product was developed by King Pharmaceuticals and FDA approved in 1956. |
| CAS Number: | 6893-02-3 |
| Molecular Weight: | 650.9735 |
| DrugBank Indication: | Liothyronine is officially approved for the following indications: - Replacement therapy in primary (thyroidal), secondary (pituitary) and tertiary (hypothalamic) congenital or acquired hypothyroidism. - As an adjunct therapy to surgery and radioiodine in the management of thyroid cancer. - As a diagnostic agent in suppression tests for mild hyperthyroidism or thyroid gland autonomy. In general terms, exogenous liothyronine is used to replace insufficient hormonal production and restore T3 plasma levels. The lack of liothyronine can be presented as a pale and puffy face, coarse, brittle hair, dry skin, croaky voice and constipation as well as irregular periods, drowsiness, and lethargy. Liothyronine should never be used in the suppression of benign nodules and nontoxic diffuse goiter in iodine-sufficient patients nor in the treatment of hyperthyroidism during the recovery phase of subacute thyroiditis. |
| DrugBank Pharmacology: | In hormonal replacement, liothyronine is more potent and present a faster action when compared to levothyroxine but the time of action is significantly shorter. The type of treatment needs to be well evaluated as the fast correction of thyroid hormones in certain diseases presents additional risks such as heart failure. The onset of activity is observed a few hours after administration and the maximum effect is observed after 2-3 days. Treatment with liothyronine has been shown to produce normal plasma levels of T3 hormone but to have no effect on the T4 plasma concentration. |
| DrugBank MoA: | Liothyronine replaces endogenous thyroid hormone and then exerts its physiologic effects by controlling DNA transcription and protein synthesis. This effect on DNA is obtained by the binding of liothyronine to the thyroid receptors attached to DNA. Exogenous liothyronine exerts all the normal effects of the endogenous thyroid T3 hormone. Hence, it increases energy expenditure, accelerates the rate of cellular oxidation stimulating growth, maturation, and metabolism of the body tissues, aids in myelination of nerves and development of synaptic processes in the nervous system and enhances carbohydrate and protein metabolism. |
| Targets: | Thyroid hormone receptor alpha agonist; Thyroid hormone receptor beta agonist; Proliferating cell nuclear antigen antagonist |
| Inclusion Criteria: | Target associated |
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs |
|---|
| Target ID | Target Name | GENE | Action | Class | UniProtKB ID | Entry Name | |
|---|---|---|---|---|---|---|---|
| T26 | Thyroid hormone receptor beta | THRB | agonist | Nuclear hormone receptor | P10828 | THB_HUMAN | Details |
| T10 | Caspase-1 | CASP1 | inhibitor | Enzyme | P29466 | CASP1_HUMAN | Details |
| T18 | Acetyl-CoA carboxylase 1 | ACACA | inhibitor | Enzyme | Q13085 | ACACA_HUMAN | Details |
| T20 | Fatty acid synthase | FASN | inhibitor | Enzyme | P49327 | FAS_HUMAN | Details |
| Diseases ID | DO ID | Disease Name | Definition | Class | |
|---|---|---|---|---|---|
| I11 | 5295 | Intestinal disease | A gastrointestinal system disease that is located_in the intestine. http://en.wikipedia.org/wiki/Human_gastrointestinal_tract | disease of anatomical entity/gastrointestinal system disease | Details |
| I04 | 1459 | Hypothyroidism | A thyroid gland disease which involves an underproduction of thyroid hormone. https://medlineplus.gov/hypothyroidism.html | disease of anatomical entity/ endocrine system disease/ thyroid gland disease | Details |