Anti-(human Insulin-like Growth Factor I Receptor) (human Monoclonal Heavy Chain)

Anti-(human Insulin-like Growth Factor I Receptor) (human Monoclonal Heavy Chain) Uses, Dosage, Side Effects, Food Interaction and all others data.

Anti-(human Insulin-like Growth Factor I Receptor) (human Monoclonal Heavy Chain) is a fully human IgG1 monoclonal antibody directed against the human insulin-like growth factor-1 receptor. Following a clinical trial in which its efficacy in the treatment of thyroid eye disease (TED) was assessed, it received "breakthrough therapy" designation from the FDA in 2016 and was approved by the FDA in January 2020 for the treatment of TED. Thyroid eye disease is a potentially debilitating complication of Graves' Disease involving inflammation and tissue remodeling behind the eye, and previous treatment options typically involved multiple invasive surgeries - teprotumumab is the first drug ever approved for the treatment of TED and therefore represents a significant step forward in the treatment this disease.

Anti-(human Insulin-like Growth Factor I Receptor) (human Monoclonal Heavy Chain) inhibits the downstream effects of IGF-1R signaling, namely tissue inflammation and remodeling, which are responsible for the various symptoms of thyroid eye disease. Anti-(human Insulin-like Growth Factor I Receptor) (human Monoclonal Heavy Chain) may cause disease flares in patients with pre-existing inflammatory bowel disease (IBD) - patients experiencing an exacerbation should discontinue therapy with teprotumumab. Significant hyperglycemia has been observed in patients receiving treatment with teprotumumab which may require antihyperglycemic medications. Based on its mechanism of action, it is likely that teprotumumab will cause fetal harm in pregnant woman - for this reason, females of child-bearing age should use effective contraception prior to initiation, during therapy, and for 6 months following the last dose of teprotumumab.

Anti-(human Insulin-like Growth Factor I Receptor) (human Monoclonal Heavy Chain)
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
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Interaction With other Medicine
Contradiction
Storage

Trade Name	Anti-(human Insulin-like Growth Factor I Receptor) (human Monoclonal Heavy Chain)
Availability	Prescription only
Generic	Teprotumumab
Teprotumumab Other Names	Immunoglobulin G1, anti-(human insulin-like growth factor I receptor) (human monoclonal heavy chain), disulfide with human monoclonal light chain, dimer, Teprotumumab, teprotumumab-trbw
Related Drugs	Tepezza
Type
Weight	148000.0 Da (approximate)
Protein binding	Data regarding teprotumumab serum protein binding is unavailable at this time.
Groups	Approved, Investigational
Therapeutic Class
Manufacturer
Available Country
Last Updated:	September 19, 2023 at 7:00 am

Uses

Anti-(human Insulin-like Growth Factor I Receptor) (human Monoclonal Heavy Chain) is a fully human monoclonal antibody directed against insulin-like growth factor-1 receptor for the treatment of thyroid eye disease.

Anti-(human Insulin-like Growth Factor I Receptor) (human Monoclonal Heavy Chain) is indicated for the treatment of thyroid eye disease.

Anti-(human Insulin-like Growth Factor I Receptor) (human Monoclonal Heavy Chain) is also used to associated treatment for these conditions: Thyroid Eye Disease

How Anti-(human Insulin-like Growth Factor I Receptor) (human Monoclonal Heavy Chain) works

Graves’ Disease is an autoimmune syndrome involving the thyroid, orbital connective tissues, and some regions of the skin. One manifestation of Graves’ Disease is thyroid-associated ophthalmopathy, or thyroid eye disease, which is characterized by orbital inflammation, tissue remodeling, and fibrosis. As the disease progresses, patients may develop proptosis, strabismus, corneal ulceration, and optic neuropathy. It has been demonstrated that insulin-like growth factor-1 receptors (IGF-1R) are overexpressed by orbital fibroblasts in patients with thyroid eye disease, in addition to being overexpressed on T-cells and B-cells in these patients. It was found that Graves’ Disease IgG molecules could mimic the principal ligand of IGF-1R, insulin-like growth factor-1 (IGF-1), and their binding of IGF-1R induces the expression of chemokines that play roles in tissue remodeling and inflammation. For these reasons, IGF-1R was sought after as a potential therapeutic target for the treatment of thyroid eye disease.

Anti-(human Insulin-like Growth Factor I Receptor) (human Monoclonal Heavy Chain) is a fully human IgG1 monoclonal antibody directed against IGF-1R. It binds to and induces internalization and degradation of these receptors, thus preventing their downstream effects and alleviating symptoms of thyroid eye disease.

Toxicity

Toxicity information, including information regarding overdosage, is currently unavailable. Symptoms of teprotumumab overdose are likely to be consistent with its adverse effect profile.

Food Interaction

No interactions found.

Anti-(human Insulin-like Growth Factor I Receptor) (human Monoclonal Heavy Chain) Disease Interaction

Moderate: diabetes, IBD

Volume of Distribution

Following the standard dosing regimen, the mean central and peripheral volumes of distribution are approximately 3.26 ± 0.87 L and 4.32 ± 0.67 L, respectively.

Elimination Route

In a population of 40 patients receiving standard dosing in two clinical trials of teprotumumab, utilizing a two-compartment pharmacokinetic model, the AUC and C_max were estimated to be 138 ± 34 mg•hr/mL and 632 ± 139 mcg/mL, respectively.