tremelimumab

High Alert

Unresectable hepatocellular carcinoma (in combination with durvalumab).
Metastatic non-small cell lung cancer (NSCLC) with no sensitizing epidermal growth factor receptor mutations or anaplastic lymphoma kinase genomic tumor aberrations (in combination with durvalumab and platinum-based chemotherapy).

Contraind./Precautions ⬆ ⬇

Contraindicated in:

OB: Pregnancy;
Lactation: Lactation.

Use Cautiously in:

Rep: Women of reproductive potential;
Pedi: Safety and effectiveness not established in children.

Adv. Reactions/Side Effects ⬆ ⬇

CV: edema, immune-mediated myocarditis, immune-mediated pericarditis, immune-mediated vasculitis

Derm: alopecia, pruritus, DRUG REACTION WITH EOSINOPHILIA AND SYSTEMIC SYMPTOMS (DRESS), STEVENS-JOHNSON SYNDROME (SJS), TOXIC EPIDERMAL NECROLYSIS (TEN)

EENT: immune-mediated iritis, immune-mediated uveitis

Endo: hyperglycemia, immune-mediated hypothyroidism, immune-mediated adrenal insufficiency, immune-mediated hyperthyroidism, immune-mediated hypoparathyroidism, immune-mediated hypophysitis, immune-mediated thyroiditis, immune-mediated type 1 diabetes

F and E: hyperkalemia, hypernatremia, hypocalcemia, hypokalemia, hypomagnesemia, hyponatremia

GI: ↑amylase, ↑lipase, ↑liver enzymes, abdominal pain, constipation, diarrhea, hyperbilirubinemia, hypoalbuminemia, nausea, stomatitis, vomiting, GI PERFORATION, IMMUNE-MEDIATED COLITIS, immune-mediated gastritis, IMMUNE-MEDIATED HEPATITIS, immune-mediated pancreatitis

GU: ↑serum creatinine, immune-mediated nephritis

Hemat: anemia, leukopenia, lymphocytopenia, neutropenia, thrombocytopenia, IMMUNE-MEDIATED APLASTIC ANEMIA, immune-mediated hemolytic anemia, immune-mediated hemophagocytic lymphohistiocytosis, immune-mediated thrombocytopenia

Metab: ↓appetite

MS: pain, immune-mediated myositis/polymyositis, IMMUNE-MEDIATED RHABDOMYOLYSIS

Neuro: fatigue, headache, insomnia, autoimmune neuropathy, Guillain-Barré syndrome, IMMUNE-MEDIATED ENCEPHALITIS, IMMUNE-MEDIATED MENINGITIS, immune-mediated myasthenic syndrome/myasthenia gravis, immune-mediated myelitis

Resp: cough, pneumonia, upper respiratory tract infection, IMMUNE-MEDIATED PNEUMONITIS

Misc: fever, INFUSION-RELATED REACTIONS

Interactions ⬆ ⬇

Drug-drug:

None reported.

Availability ⬆ ⬇

Solution for injection: 20 mg/mL

Route/Dosage ⬆ ⬇

Hepatocellular Carcinoma

IV (Adults ≥30 kg): 300 mg as single dose on Day 1 of Cycle 1 (followed by durvalumab); then continue with durvalumab monotherapy every 4 wk until disease progression or unacceptable toxicity.
IV (Adults <30 kg): 4 mg/kg as single dose on Day 1 of Cycle 1 (followed by durvalumab); then continue with durvalumab monotherapy every 4 wk until disease progression or unacceptable toxicity.

Non-Small Cell Lung Cancer

If patients receive <4 cycles of platinum-based chemotherapy, the remaining tremelimumab doses (up to a total of 5) should be administered after the platinum-based chemotherapy phase (in combination with durvalumab) every 4 wk.
IV (Adults ≥30 kg): Cycles 1–4: 75 mg every 3 wk (administered on Day 1 of Cycles 1–4) (in combination with durvalumab and platinum-based chemotherapy); Cycle 5 (Wk 12): No tremelimumab dose is administered (durvalumab is administered); Cycle 6 (Wk 16): 75 mg as single dose on Day 1 of Cycle 6 (in combination with durvalumab); Cycle 7 and beyond: Continue with durvalumab monotherapy every 4 wk until disease progression or unacceptable toxicity.
IV (Adults <30 kg): Cycles 1–4: 1 mg/kg every 3 wk (administered on Day 1 of Cycles 1–4) (in combination with durvalumab and platinum-based chemotherapy); Cycle 5 (Wk 12): No tremelimumab dose is administered (durvalumab is administered); Cycle 6 (Wk 16): 1 mg/kg as single dose on Day 1 of Cycle 6 (in combination with durvalumab); Cycle 7 and beyond: Continue with durvalumab monotherapy every 4 wk until disease progression or unacceptable toxicity.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Binds to cytotoxic T-lymphocyte-associated antigen 4 (CTLA-4) and prevents it from binding to CD80/CD86 ligands. CTLA-4 is a negative regulator of T-cell activation; binding results in augmented T-cell activation and proliferation.

Therapeutic effects:

Improved survival in hepatocellular carcinoma and NSCLC.

Classifications ⬆ ⬇

Therapeutic Classification: antineoplastics

Pharmacologic Classification: monoclonal antibodies, cytotoxic t lymphocyte antigen 4 inhibitors

Pharmacokinetics ⬆ ⬇

Absorption: IV administration results in complete bioavailability.

Distribution: Not widely distributed to tissues.

Metabolism/Excretion: Unknown.

Half-Life: 18.2 days.

Time/Action Profile ⬆ ⬇

ROUTE	ONSET	PEAK	DURATION
IV	unknown	unknown	unknown

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of medication. Advise patient to read Patient Information before starting therapy.
Advise patient to notify health care professional immediately if signs and symptoms of pneumonitis, hepatitis (jaundice, severe nausea or vomiting, pain on right side of abdomen, lethargy, easy bruising or bleeding, dark urine, light-colored stools), colitis, adrenal insufficiency (prolonged or unusual headache, feeling cold, extreme tiredness, constipation, weight gain or loss, deepening voice, dizziness or fainting, ↑ urination , ↑ hunger or thirst, nausea or vomiting, hair loss, abdominal pain, changes in mood or behavior, ↓ sex drive, irritability, forgetfulness), nephritis (↓ urine output, hematuria, ankle edema, loss of appetite, rash, itching, skin blistering), or infusion-related reactions occur.
Advise patient to inform health care professional if other signs and symptoms (neck stiffness, fatigue, excessive bleeding or bruising, confusion, muscle weakness or pain, fever, vision changes, chest pain, shortness of breath, irregular heartbeat, eye pain or redness, mood or behavior changes) occur.
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 use effective contraception and avoid breastfeeding during and for ≥3 mo after last dose of tremelimumab. Advise women of reproductive potential to notify health care professional if pregnancy is planned or suspected.

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Indications ⬇