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Levothyroxine

Generic Name
Levothyroxine
Brand Names
Eltroxin, Ermeza, Euthyrox, Levo-T, Levothroid, Levoxyl, Np Thyroid, Synthroid, Thyquidity, Tirosint, Unithroid
Drug Type
Small Molecule
Chemical Formula
C15H11I4NO4
CAS Number
51-48-9
Unique Ingredient Identifier
Q51BO43MG4

Overview

Levothyroxine is a synthetically produced form of thyroxine, a major endogenous hormone secreted by the thyroid gland. Also known as L-thyroxine or the brand name product Synthroid, levothyroxine is used primarily to treat hypothyroidism, a condition where the thyroid gland is no longer able to produce sufficient quantities of the thyroid hormones T (tetraiodothyronine or thyroxine) and T (triiodothyronine or Liothyronine), resulting in diminished down-stream effects of these hormones. Without sufficient quantities of circulating thyroid hormones, symptoms of hypothyroidism begin to develop such as fatigue, increased heart rate, depression, dry skin and hair, muscle cramps, constipation, weight gain, memory impairment, and poor tolerance to cold temperatures. In response to Thyroid Stimulating Hormone (TSH) release by the pituitary gland, a normally functioning thyroid gland will produce and secrete T, which is then converted through deiodination (by type I or type II 5′-deiodinases) into its active metabolite T. While T is the major product secreted by the thyroid gland, T exerts the majority of the physiological effects of the thyroid hormones; T and T have a relative potency of ~1:4 (T4:T3). T and T act on nearly every cell of the body, but have a particularly strong effect on the cardiac system. As a result, many cardiac functions including heart rate, cardiac output, and systemic vascular resistance are closely linked to thyroid status. Prior to the development of levothyroxine, Thyroid, porcine or desiccated thyroid, used to be the mainstay of treatment for hypothyroidism. However, this is no longer recommended for the majority of patients due to several clinical concerns including limited controlled trials supporting its use. Desiccated thyroid products contain a ratio of T4 to T3 of 4.2:1, which is significantly lower than the 14:1 ratio of secretion by the human thyroid gland. This higher proportion of T3 in desiccated thyroid products can lead to supraphysiologic levels of T3 which may put patients at risk of thyrotoxicosis if thyroid extract therapy is not adjusted according to the serum TSH.

Background

Levothyroxine is a synthetically produced form of thyroxine, a major endogenous hormone secreted by the thyroid gland. Also known as L-thyroxine or the brand name product Synthroid, levothyroxine is used primarily to treat hypothyroidism, a condition where the thyroid gland is no longer able to produce sufficient quantities of the thyroid hormones T (tetraiodothyronine or thyroxine) and T (triiodothyronine or Liothyronine), resulting in diminished down-stream effects of these hormones. Without sufficient quantities of circulating thyroid hormones, symptoms of hypothyroidism begin to develop such as fatigue, increased heart rate, depression, dry skin and hair, muscle cramps, constipation, weight gain, memory impairment, and poor tolerance to cold temperatures. In response to Thyroid Stimulating Hormone (TSH) release by the pituitary gland, a normally functioning thyroid gland will produce and secrete T, which is then converted through deiodination (by type I or type II 5′-deiodinases) into its active metabolite T. While T is the major product secreted by the thyroid gland, T exerts the majority of the physiological effects of the thyroid hormones; T and T have a relative potency of ~1:4 (T4:T3). T and T act on nearly every cell of the body, but have a particularly strong effect on the cardiac system. As a result, many cardiac functions including heart rate, cardiac output, and systemic vascular resistance are closely linked to thyroid status. Prior to the development of levothyroxine, Thyroid, porcine or desiccated thyroid, used to be the mainstay of treatment for hypothyroidism. However, this is no longer recommended for the majority of patients due to several clinical concerns including limited controlled trials supporting its use. Desiccated thyroid products contain a ratio of T4 to T3 of 4.2:1, which is significantly lower than the 14:1 ratio of secretion by the human thyroid gland. This higher proportion of T3 in desiccated thyroid products can lead to supraphysiologic levels of T3 which may put patients at risk of thyrotoxicosis if thyroid extract therapy is not adjusted according to the serum TSH.

Indication

Levothyroxine is indicated as replacement therapy in primary (thyroidal), secondary (pituitary) and tertiary (hypothalamic) congenital or acquired hypothyroidism. It is also indicated as an adjunct to surgery and radioiodine therapy in the management of thyrotropin-dependent well-differentiated thyroid cancer.

Associated Conditions

  • Edematous Fibrosclerotic Panniculopathy (Cellulite)
  • Hypothyroidism
  • Localized Adiposity
  • Myxedema coma
  • Euthyroid Goitre
  • Thyrotropin dependent Well-Differentiated Thyroid Cancer

Clinical Trials

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Title
Posted
Study ID
Phase
Status
Sponsor
2023/09/14
Phase 3
Completed
2023/04/21
Phase 2
Completed
2023/04/07
Phase 2
Completed
2023/02/03
Phase 2
Active, not recruiting
2022/09/02
Phase 2
Recruiting
2022/06/09
Phase 2
Completed
2022/05/23
N/A
Completed
OMER B ABDELBASIT
2022/05/12
Phase 4
Completed
Federico II University
2022/04/07
Phase 3
Recruiting
Fondazione IRCCS Istituto Nazionale dei Tumori, Milano
2022/03/11
N/A
Recruiting

FDA Drug Approvals

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Approved Product
Manufacturer
NDC Code
Route
Strength
Effective Date
A-S Medication Solutions
50090-6880
ORAL
0.112 mg in 1 1
11/8/2023
Mylan Pharmaceuticals Inc.
0378-1811
ORAL
112 ug in 1 1
8/31/2020
Mylan Pharmaceuticals Inc.
0378-1800
ORAL
25 ug in 1 1
8/31/2020
NorthStar RxLLC
72603-664
ORAL
100 ug in 1 1
4/15/2025
REMEDYREPACK INC.
70518-3208
ORAL
50 ug in 1 1
6/2/2025
Major Pharmaceuticals
0904-6956
ORAL
0.15 mg in 1 1
2/4/2020
IBSA Pharma Inc.
71858-0105
ORAL
13 ug in 1 mL
11/30/2023
Bryant Ranch Prepack
63629-2094
ORAL
300 ug in 1 1
7/23/2020
A-S Medication Solutions
50090-5661
ORAL
50 ug in 1 1
7/23/2020
NuCare Pharmaceuticals,Inc.
68071-4866
ORAL
100 ug in 1 1
2/17/2021

EMA Drug Approvals

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NMPA Drug Approvals

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PPB Drug Approvals

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