teplizumab

Absorption: IV administration results in complete bioavailability.

Distribution: Not widely distributed to tissues.

Metabolism/Excretion: Metabolized into small peptides by catabolic pathways; excretion pathway unknown.

Half-Life: 4.5 days.

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
IV	rapid	unknown	unknown

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Active or chronic infection (excluding localized skin infection);
Laboratory or clinical evidence of acute infection with Epstein-Barr virus or cytomegalovirus;
Lymphocyte count <1000 cells/mcL;
Hemoglobin <10 g/dL;
Platelet count <150,000 cells/mcL;
Absolute neutrophil count <1500 cells/mcL;
Elevated ALT or AST >2 times upper limit of normal (ULN) or bilirubin >1.5 times ULN;
OB: Pregnancy.

Use Cautiously in:

Lactation: Safety not established during breastfeeding;
Rep: Women of reproductive potential;
Pedi: Children <8 yr (safety and effectiveness not established).

Adv. Reactions/Side Effects ⬆ ⬇

Derm: rash

F and E: ↓bicarbonate, hypocalcemia

GI: ↑liver enzymes, diarrhea, nausea

Hemat: anemia, leukopenia, lymphopenia, thrombocytopenia, neutropenia

Neuro: headache

Misc: cytokine release syndrome (CRS), HYPERSENSITIVITY REACTIONS (INCLUDING ANGIOEDEMA), infection

Interactions ⬆ ⬇

Drug-drug:

May ↓ effectiveness of vaccines; do not administer inactivated or mRNA vaccines within 2 wk prior to treatment, during treatment, or for 6 wk after treatment completed; do not administered live-attenuated vaccines within 8 wk prior to treatment, during treatment, or up to 52 wk after treatment completed.

Route/Dosage ⬆ ⬇

IV (Adults and Children >8 yr): Day 1: 65 mcg/m² as single dose; Day 2: 125 mcg/m² as single dose; Day 3: 250 mcg/m² as single dose; Day 4: 500 mcg/m² as single dose; Day 5–14: 1030 mcg/m² once daily.

Availability ⬆ ⬇

Solution for injection: 1 mg/mL

Assessment ⬆ ⬇

Monitor for CRS; typically occurs during first 5 days of therapy. If CRS occurs, treat with antipyretic, antihistamine, and/or antiemetic. If severe CRS occurs, consider holding for 1–2 days; then resume remaining doses to complete a 14-day course or discontinue teplizumab depending on liver function tests.
Monitor for serious or chronic active infection prior to, during, and after last dose. If serious infection occurs, treat appropriately and discontinue teplizumab.
Monitor for hypersensitivity reactions (serum sickness, angioedema, urticaria, rash, vomiting, bronchospasm). If hypersensitivity reaction occurs, discontinue teplizumab and treat promptly.

Lab Test Considerations:

Verify negative pregnancy status prior to starting therapy.
Confirm stage 2 type 1 diabetes with ≥two positive pancreatic islet cell autoantibody tests and oral glucose tolerance test indicating dysglycemia without overt hyperglycemia, and verify that clinical history does not suggest type 2 diabetes prior to initiation of therapy.
Monitor CBC with differential before and during therapy. If prolonged (≥1 wk) severe lymphopenia (<500/mcL) occurs, discontinue teplizumab.
Monitor liver enzymes before and during therapy. If ALT or AST >5 times ULN or bilirubin >3 times ULN, discontinue teplizumab.

Implementation ⬆ ⬇

Administer age-appropriate vaccines prior to therapy initiation, live-attenuated ≥8 wk prior, and inactive or mRNA vaccines ≥2 wk prior.
Premedicate prior to the first 5 days of dosing with an NSAID or acetaminophen, antihistamine, and/or antiemetic. May administer multiple doses as indicated.
Do not administer two doses on the same day. If a dose is missed, resume with next scheduled dose to complete therapy over the next 14 consecutive days.

IV Administration:

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of medication. Advise patient to read Patient Information before starting therapy.
Inform patient that vaccinations are not recommended during therapy.
Advise patient to notify health care professional for symptoms of CRS (fever, fatigue, nausea, headache, muscle and joint pain) or serious infection (cellulitis, gastroenteritis, pneumonia, wound infection).
Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care professional before taking other medications.
Rep: May cause fetal harm. Advise women of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding. May interrupt breastfeeding and pump, discarding breast milk, during therapy and for 20 days after last dose. If exposed to teplizumab during pregnancy, encourage patient to contact Provention Bio, Inc.’s adverse event line at 1-844-778-2246.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇