Dosing & Uses
Dosage Forms & Strengths
injection, lyophilized powder for reconstitution
- 500mg/single-dose vial
Thyroid Eye Disease
Indicated for thyroid eye disease, regardless of disease activity or duration
10 mg/kg IV initially, followed by 20 mg/kg IV q3 weeks for 7 additional infusions
Dosage Modifications
Renal impairment
- Mild-to-moderate (CrCl 30-89 mL/min): No significant difference in pharmacokinetics observed
Hepatic impairment
- Effect of hepatic impairment on the pharmacokinetics of teprotumumab-trbw is unknown
Safety and efficacy not established
Adverse Effects
>10%
Muscle spasms (25%)
Nausea (17%)
Alopecia (13%)
Diarrhea (12%)
Fatigue (12%)
1-10%
Hyperglycemia (10%)
Hearing impairment (10%)
Dysgeusia (8%)
Headache (8%)
Dry skin (8%)
Postmarketing Reports
Exacerbation of preexisting inflammatory bowel disease
Infusion reactions
Metabolism and nutrition disorders: Diabetic ketoacidosis, hyperosmolar hyperglycemic state (HHS)
Warnings
Contraindications
None
Cautions
Infusion reactions may occur; if an infusion reaction occurs, interrupt or slow infusion rate and use appropriate medical management
May cause exacerbation of preexisting inflammatory bowel disease (IBD); monitor patients with preexisting IBD for flare of disease; discontinue treatment if IBD worsens
Hyperglycemia reported; assess patients for elevated blood glucose and symptoms of hyperglycemia prior to infusion and continue to monitor while on treatment; ensure patients with hyperglycemia or pre-existing diabetes are under appropriate glycemic control before and while receiving therapy
Pregnancy & Lactation
Pregnancy
Based on findings in animals and its mechanism of action, fetal harm may occur when administered to a pregnant woman
Adequate and well-controlled studies have not been conducted in pregnant women
Data are insufficient with use in pregnant women to inform any drug-associated risks for adverse developmental outcomes
Animal data
- In utero teprotumumab exposure in cynomolgus monkeys dosed once weekly with teprotumumab throughout pregnancy resulted in external and skeletal abnormalities
- Teprotumumab exposure may lead to an increase in fetal loss; therefore, do not use during pregnancy
- If patient becomes pregnant during treatment, discontinue treatment and advise patient of the potential risk to the fetus
Contraception
- Advise females of reproductive potential to use effective contraception before initiation, during treatment, and for 6 months following the last dose
Lactation
There is no information regarding the presence of teprotumumab in human milk, the effects on the breastfed infant, or the effects on milk production
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Monoclonal antibody that binds insulin-like growth factor-1 receptor (IGF-1R)
Mechanism of action for thyroid eye disease has not been fully characterized
Teprotumumab-trbw binds to IGF-1R and blocks its activation and signaling
Absorption
Peak plasma concentration: 632 mcg/mL
Trough plasma concentration: 176 mcg/mL
AUC: 138 mg⋅hr/mL
Distribution
Vd: 3.26 L (central); 4.32 L (peripheral)
Metabolism
Metabolism has not been fully characterized
However, teprotumumab-trbw is expected to undergo metabolism via proteolysis
Elimination
Clearance: 0.27 L/day
Half-life: 20 days
Administration
IV Incompatibilities
Do not infuse concomitantly with other agents
IV Compatibilities
0.9% NaCl
No incompatibilities with polyethylene (PE), polyvinyl chloride (PVC), polyurethane (PUR), or polyolefin (PO) bags, and IV administration sets have been observed
IV Preparation
Reconstitution
- Calculate dose and determine number of vials needed; each vial contains 500 mg of teprotumumab antibody
- Reconstitute each vial with 10 mL of sterile water for injection; do not direct the stream of diluent onto the lyophilized powder, which has a cake-like appearance
- Do not shake; gently swirl solution by rotating the vial until powder is dissolved
- Reconstituted solution has a volume of 10.5 mL (final concentration is 47.6 mg/mL); withdraw 10.5 mL of reconstituted solution to obtain 500 mg
Dilution
- Further dilute in 0.9% NaCl
- To maintain a constant volume in the infusion bag, remove the volume equivalent to the amount of the reconstituted to be placed into the infusion bag
- Withdraw required volume from the reconstituted vial(s) and transfer into an IV bag containing 0.9% NaCl to prepare a diluted solution with a total volume of 100 mL (for less than an 1800-mg dose) or 250 mL (for 1800-mg and greater dose)
- Mix diluted solution by gentle inversion; do not shake
Visually inspect for particulate matter and discoloration prior to administration, whenever solution and container permit; solution should appear as a colorless or slightly brown, clear-to-opalescent solution that is free of foreign particulate matter
Discard solution if any particulate matter or discoloration is observed
- Discard vial(s) and all unused contents.
IV Administration
First 2 infusions: Infuse over 90 min
Subsequent infusions: If well tolerated, may reduce infusion time to 60 min; if not well tolerated, keep infusion time at 90 min
Do not administer as an IV push or bolus
Storage
Protect from light
Do not freeze
Unused vials: Refrigerate at 2-8ºC (36-46ºF) in original carton until time of use
Reconstituted vials and diluted solutions
- Store at room temperature (20-25ºC [68-77ºF]) for up to 4 hr OR
- Refrigerate at 2-8ºC (36-46ºF) for up to 48 hr
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Formulary
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