Action and Spectrum

Teprotumumab is a monoclonal antibody that is being investigated for the treatment of thyroid eye disease (TED), also known as Graves’ orbitopathy. It works by inhibiting the activity of the insulin-like growth factor 1 receptor (IGF-1R), which is thought to play a role in the development and progression of TED. 

Teprotumumab is administered intravenously (through a vein) in eight infusions over 16 weeks. The specific actions and spectrum of teprotumumab still need to be fully understood. Still, it is thought to work by reducing inflammation and swelling in the muscles and tissues around the eye, which can improve the appearance of the eye and alleviate symptoms such as double vision and difficulty closing the eyelids. 

Teprotumumab is currently being investigated in clinical trials and has not yet been approved for use by regulatory agencies such as the US Food and Drug Administration (FDA). If approved, it would be used as a treatment for TED in individuals who have not responded to other therapies. As with any medication, discussing the potential risks and benefits with a healthcare provider before starting treatment with teprotumumab is essential. 

Drug Interaction

Adverse Reaction

Frequency defined:  

>10% 

Nausea 

Diarrhea 

Muscle spasm 

Alopecia 

fatigue 

1-10% 

Hearing impairment 

Headache 

Hyperglycemia 

Dysgeusia 

Dry skin 

Post-marketing reports 

Infusion reactions 

Diabetic ketoacidosis 

Exacerbation of preexisting inflammatory bowel disease 

Black Box Warning

Contraindication / Caution

Teprotumumab is a monoclonal antibody that is being investigated for the treatment of thyroid eye disease (TED). As it is currently being studied in clinical trials, the full range of potential cautions and risks associated with teprotumumab is not yet known. 

However, as with any medication, it is essential to discuss the potential risks and benefits with a healthcare provider before starting treatment with teprotumumab. Some potential cautions and side effects that have been observed in clinical trials of teprotumumab include: 

• Infusion reactions: Teprotumumab is administered intravenously (through a vein), and some individuals may experience infusion reactions during treatment. These reactions may include symptoms such as fever, chills, nausea, vomiting, and difficulty breathing. 
• Muscle weakness: Teprotumumab may cause muscle weakness, particularly in the legs and feet. This may affect an individual’s ability to walk or perform other activities. 
• Eye problems: Teprotumumab may cause eye problems, such as dry eye, double vision, or a loss of vision. It is essential to report any changes in vision to a healthcare provider. 
• Thyroid hormone levels: Teprotumumab may affect thyroid hormone levels, and monitoring thyroid function during treatment is essential. 

Again, these are potential cautions and side effects that have been observed in clinical trials of teprotumumab. 

Pregnancy / Lactation

Pregnancy consideration: Insufficient data available 

Lactation: Excretion of the drug in human breast milk is unknown 

Pregnancy category: 

Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester.   

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: There is no data available for the drug under this category 

Pharmacology

Mechanism of action 

Teprotumumab is a monoclonal antibody that is used to treat thyroid eye disease, a condition characterized by inflammation and swelling of the tissues around the eye. Teprotumumab works by targeting and inhibiting the action of insulin-like growth factor-1 receptor (IGF-1R), a protein that is involved in the growth and survival of cells. 

IGF-1R is expressed on the surface of many types of cells, including cells of the eye muscles and fat. In thyroid eye disease, IGF-1R signaling is thought to contribute to the inflammation and tissue swelling that occurs. By inhibiting IGF-1R, teprotumumab reduces inflammation and swelling, which can help improve symptoms of thyroid eye disease. 

Teprotumumab is given as an intravenous infusion, and it has been shown to be effective at improving symptoms of thyroid eye disease in clinical studies. However, like all medications, it can cause side effects, including muscle and joint pain, nausea, and high blood sugar. It is essential to carefully weigh the potential benefits and risks of teprotumumab before starting treatment.  

Pharmacokinetics 

Absorption 

It appears that the drug has a high peak plasma concentration and a long half-life, which suggests that it is slowly absorbed and eliminated from the body.  

Distribution 

The volume of distribution (Vd) is also relatively large, with a central Vd of 3.26 L and a peripheral Vd of 4.32 L. This suggests that the drug is widely distributed throughout the body. 

Metabolism 

It is not clear from the information provided how the drug is metabolized. It is stated that the metabolism of the drug has not been fully characterized.  

Elimination/excretion

The elimination half-life of the drug is 20 days, and the clearance is 0.27 L/day. This suggests that the drug is eliminated from the body slowly. 

Adminstartion

IV Contradictions 

Do not administer simultaneously with other agents. 

0.9% NaCl IV compatibilities  

No incompatibilities with IV administration set or bags made of polyethylene (PE), polyvinyl chloride (PVC), polyurethane (PUR), or polyolefin (PO) 

Patient Information Leaflet

Patient information leaflet 

Generic Name: teprotumumab 

Pronounced: [ TEP-roe-TOOM-ue-mab ] 

Why do we use teprotumumab? 

Teprotumumab is a monoclonal antibody that is being investigated for the treatment of thyroid eye disease (TED), also known as Graves’ orbitopathy. TED is a condition that causes inflammation and swelling in the muscles and tissues around the eye, leading to bulging of the eye, double vision, and difficulty closing the eyelids. It is often associated with an overactive thyroid gland, which produces an excess of thyroid hormone. 

Teprotumumab works by inhibiting the activity of insulin-like growth factor 1 receptor (IGF-1R), which is thought to play a role in the development and progression of TED. It is administered intravenously (through a vein) in a series of eight infusions over 16 weeks