Colorectal cancer, metastatic (microsatellite instability-high [MSI-H] or mismatch repair deficient [dMMR]): Note: FDA approval for MSI-H or dMMR metastatic colorectal cancer is through an accelerated process; continued approval is dependent upon verification of clinical benefit in further trials.
Children ≥12 years and Adolescents: IV: 1 mg/kg every 3 weeks (in combination with nivolumab) for up to 4 doses.
Melanoma, unresectable or metastatic: Note: May be used as a single agent or in combination with nivolumab.
Children ≥12 years and Adolescents: IV: 3 mg/kg every 3 weeks for a maximum of 4 doses (or fewer if unacceptable toxicity occurs).
Solid tumors, relapsed/refractory: Very limited data available:
Combination therapy with nivolumab:
Children ≥4 years and Adolescents: IV: 1 mg/kg every 3 weeks (in combination with nivolumab) for 4 doses (or less if unacceptable toxicity occurs) (Ref).
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
Dosing adjustment for toxicity:
Children ≥12 years and Adolescents:
Note: No dosage reductions of ipilimumab are recommended. When ipilimumab is given in combination with nivolumab, withhold or permanently discontinue both ipilimumab and nivolumab for an adverse reaction meeting dosage modification recommendations. Refer to Nivolumab monograph for information on nivolumab dosage adjustment for toxicity. Other concomitant combination therapy medications may also require treatment interruption, dosage reduction, and/or discontinuation.
Immune-mediated adverse reactions (general information): Withhold ipilimumab for severe (grade 3) immune-mediated adverse reactions. Permanently discontinue ipilimumab for life-threatening (grade 4) immune-mediated adverse reactions, recurrent severe (grade 3) immune-mediated reactions that require systemic immunosuppressive treatment, persistent moderate (grade 2) or severe (grade 3) reactions lasting 12 weeks or longer beyond the last ipilimumab dose (excluding endocrinopathies), or inability to reduce corticosteroid dose to prednisone ≤10 mg/day (or equivalent) within 12 weeks of initiating corticosteroids. If ipilimumab treatment interruption or discontinuation is required, administer systemic corticosteroid therapy (1 to 2 mg/kg/day prednisone [or equivalent]) until improvement to ≤ grade 1; upon improvement to grade 1 or lower, initiate corticosteroid taper and continue to taper over at least 1 month. Consider administration of other systemic immunosuppressants if immune-mediated adverse reaction is not controlled with corticosteroid therapy. Systemic corticosteroids may not be necessary for certain adverse reactions. Hormone replacement therapy may be required for endocrinopathies (if clinically indicated). See table for additional dosage modification guidance.
Adverse reaction |
Severity |
Ipilimumab dosage modification |
---|---|---|
a SJS = Stevens-Johnson syndrome; TEN = toxic epidermal necrolysis; DRESS = drug rash with eosinophilia and systemic symptoms. | ||
Immune-mediated adverse reactions | ||
Cardiovascular toxicity: Myocarditis |
Grade 2, 3, or 4 |
Permanently discontinue ipilimumab. |
Dermatologic toxicity |
Mild to moderate nonbullous/exfoliative rash |
May be managed with topical emollients and/or topical corticosteroids. Withhold or permanently discontinue ipilimumab depending on severity. |
Exfoliative dermatologic conditions: Suspected SJS, TEN, or DRESSa |
Withhold ipilimumab. | |
Confirmed SJS, TEN, or DRESS |
Permanently discontinue ipilimumab. | |
Endocrinopathies |
Grade 2 |
Depending on clinical severity, consider withholding until symptom improvement with hormone replacement. Resume once acute symptoms have resolved. |
Grade 3 or 4 |
Withhold ipilimumab if not clinically stable. Moderate and life-threatening endocrinopathy may require long-term hormone replacement therapy (eg, adrenal or thyroid hormone therapy). | |
Adrenal insufficiency |
Withhold or discontinue ipilimumab (depending on the severity). Initiate medical management as clinically indicated. | |
Hypophysitis |
Withhold or discontinue ipilimumab (depending on the severity). | |
Hyperthyroidism |
Withhold or discontinue ipilimumab (depending on the severity). Initiate medical management as clinically indicated. | |
Hypothyroidism |
Withhold ipilimumab (depending on the severity). Initiate thyroid hormone replacement therapy as clinically indicated. | |
GI toxicity: Colitis |
Grade 2 |
Withhold ipilimumab; resume ipilimumab after complete or partial (to grade 0 or 1) resolution after corticosteroid taper. Permanently discontinue ipilimumab if no complete or partial response within 12 weeks of last ipilimumab dose, or if unable to reduce prednisone to <10 mg/day (or equivalent) within 12 weeks of corticosteroid initiation. |
Grade 3 or 4 |
Permanently discontinue ipilimumab. | |
Neurologic toxicities |
Grade 2 |
Withhold ipilimumab; resume ipilimumab after complete or partial (to grade 0 or 1) resolution after corticosteroid taper. Permanently discontinue ipilimumab if no complete or partial response within 12 weeks of last ipilimumab dose, or if unable to reduce prednisone to <10 mg/day (or equivalent) within 12 weeks of corticosteroid initiation. |
Grade 3 or 4 |
Permanently discontinue ipilimumab. | |
Ophthalmic toxicity |
Grade 2, 3, or 4 that does not improve to grade 1 within 2 weeks while receiving topical therapy or that requires systemic treatment |
Permanently discontinue ipilimumab. |
Vogt-Koyanagi-Harada-like syndrome |
May require systemic corticosteroids to reduce the risk of permanent vision loss. | |
Pancreatitis |
Grade 3 or 4 amylase or lipase increases |
Permanent ipilimumab discontinuation is recommended (Weber 2012). |
Pulmonary toxicity: Pneumonitis |
Grade 2 |
Withhold ipilimumab; resume ipilimumab after complete or partial (to grade 0 or 1) resolution after corticosteroid taper. Permanently discontinue ipilimumab if no complete or partial response within 12 weeks of last ipilimumab dose, or if unable to reduce prednisone to <10 mg/day (or equivalent) within 12 weeks of corticosteroid initiation. |
Grade 3 or 4 |
Permanently discontinue ipilimumab. | |
Other adverse reactions | ||
Infusion reactions |
Grade 1 or 2 |
Interrupt or slow the rate of ipilimumab infusion. |
Grade 3 or 4 |
Permanently discontinue ipilimumab. |
Children ≥12 years and Adolescents:
Baseline kidney impairment:
GFR ≥15 mL/minute/1.73 m2: There are no dosage adjustments provided in the manufacturer's labeling; however, GFR ≥15 mL/minute/1.73 m2 had no clinically important effect on ipilimumab clearance.
GFR <15 mL/minute/1.73 m2: There are no dosage adjustments provided in the manufacturer's labeling.
Nephrotoxicity during treatment:
Immune-mediated nephritis with kidney dysfunction: If ipilimumab treatment interruption or discontinuation is required, administer systemic corticosteroids (1 to 2 mg/kg/day prednisone [or equivalent]) or other appropriate therapy for immune-mediated adverse reactions until improvement to grade 1 or lower, then follow with a corticosteroid taper.
Grade 2 or grade 3 serum creatinine elevation: Withhold ipilimumab; resume ipilimumab after complete or partial (to grade 0 or 1) resolution after corticosteroid taper. Permanently discontinue ipilimumab if no complete or partial response within 12 weeks of last ipilimumab dose, or if unable to reduce prednisone to <10 mg/day (or equivalent) within 12 weeks of corticosteroid initiation.
Grade 4 serum creatinine elevation: Permanently discontinue ipilimumab.
Children ≥12 years and Adolescents:
Baseline hepatic impairment:
Mild impairment (total bilirubin >1 to 1.5 times ULN or AST >ULN): There are no dosage adjustments provided in the manufacturer's labeling; however, mild impairment had no clinically important effect on ipilimumab clearance.
Moderate or severe impairment (total bilirubin >1.5 times ULN and any AST): There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).
Hepatotoxicity during treatment:
If ipilimumab treatment interruption or discontinuation is required, administer systemic corticosteroids (1 to 2 mg/kg/day prednisone [or equivalent]) or other appropriate therapy for immune-mediated adverse reactions until improvement to grade 1 or lower, then follow with a corticosteroid taper. Permanently discontinue ipilimumab if no complete or partial response within 12 weeks of last ipilimumab dose, or if unable to reduce prednisone to <10 mg/day (or equivalent) within 12 weeks of corticosteroid initiation.
If transaminases do not decrease within 48 hours of steroid initiation, consider adding mycophenolate mofetil; may begin tapering corticosteroid (over 1 month) when LFTs show sustained improvement or return to baseline (Ref).
Immune-mediated hepatitis without tumor involvement of the liver or hepatitis with tumor involvement of the liver/non-hepatocellular carcinoma:
AST or ALT >3 to ≤5 times ULN or total bilirubin >1.5 to ≤3 times ULN: Withhold ipilimumab; resume ipilimumab with complete or partial resolution (to grade 0 or 1) of hepatitis after corticosteroid taper.
AST or ALT >5 times ULN or total bilirubin >3 times ULN: Permanently discontinue ipilimumab.
Immune-mediated hepatitis with tumor involvement of the liver/hepatocellular carcinoma (applies to hepatocellular carcinoma ipilimumab/nivolumab combination treatment): Note: When receiving combination therapy with ipilimumab and nivolumab, withhold or permanently discontinue both ipilimumab and nivolumab for adverse reactions meeting dosage modification recommendations (refer to Nivolumab monograph for information on nivolumab dosage adjustment for toxicity). If AST and ALT are ≤ ULN at baseline, follow recommendations for hepatitis without tumor involvement of the liver.
If baseline AST or ALT >1 to ≤3 times ULN and increases to >5 to ≤10 times ULN or baseline AST or ALT >3 to ≤5 times ULN and increases to >8 to ≤10 times ULN: Withhold treatment. Resume treatment with complete or partial resolution (to grade 0 or 1) of hepatitis after corticosteroid taper.
AST or ALT >10 times ULN or total bilirubin >3 times ULN: Discontinue permanently.
(For additional information see "Ipilimumab: Drug information")
Colorectal cancer, metastatic, microsatellite instability-high or mismatch repair deficient: IV: 1 mg/kg once every 3 weeks (in combination with nivolumab) for 4 combination doses, followed by nivolumab monotherapy until disease progression or unacceptable toxicity (Ref).
Esophageal carcinoma, squamous cell, unresectable advanced or metastatic; first-line therapy: IV: 1 mg/kg once every 6 weeks (in combination with nivolumab) until disease progression or unacceptable toxicity, or up to 2 years (Ref).
Hepatocellular carcinoma: IV: 3 mg/kg once every 3 weeks (in combination with nivolumab) for 4 combination doses, followed by nivolumab monotherapy until disease progression or unacceptable toxicity (Ref).
Malignant pleural mesothelioma, unresectable; first-line therapy: IV: 1 mg/kg once every 6 weeks (in combination with nivolumab) until disease progression, unacceptable toxicity, or for up to 2 years in patients without disease progression (Ref).
Melanoma, adjuvant treatment: IV: 10 mg/kg every 3 weeks for up to 4 doses, followed by 10 mg/kg every 12 weeks for up to 3 years unless disease progression or unacceptable toxicity occur (Ref).
Off-label dosing: IV: 3 mg/kg once every 3 weeks for 4 doses (induction), followed by 3 mg/kg once every 12 weeks for up to 4 additional doses (maintenance) or until disease progression or unacceptable toxicity for up to a maximum of 60 weeks (Ref).
Melanoma, unresectable or metastatic, single-agent therapy: IV: 3 mg/kg every 3 weeks for a maximum of 4 doses (Ref).
Melanoma, unresectable or metastatic, combination therapy: IV: 3 mg/kg every 3 weeks (in combination with nivolumab) for a maximum of 4 combination doses (or until unacceptable toxicity, whichever occurs first); followed by nivolumab monotherapy until disease progression or unacceptable toxicity (Ref).
Melanoma, with brain metastases (off-label use): IV: 3 mg/kg once every 3 weeks (in combination with nivolumab) for 4 combination doses, followed by nivolumab monotherapy; total duration of nivolumab therapy is up to 24 months, or until disease progression or unacceptable toxicity (Ref).
Merkel cell carcinoma, unresectable, recurrent, or stage IV (off-label use): IV: 1 mg/kg once every 6 weeks (in combination with nivolumab) until disease progression or unacceptable toxicity (Ref).
Non–small cell lung cancer, metastatic, PD-L1-expressing: IV: 1 mg/kg once every 6 weeks (in combination with nivolumab) until disease progression, unacceptable toxicity, or up to 2 years in patients without disease progression (Ref).
Non–small cell lung cancer, metastatic or recurrent: IV: 1 mg/kg once every 6 weeks (in combination with nivolumab and 2 cycles of histology-based platinum-doublet chemotherapy) until disease progression, unacceptable toxicity, or up to 2 years in patients without disease progression (Ref).
Renal cell cancer, advanced, first-line combination therapy:
Note: May be used in combination with nivolumab in patients with intermediate- or poor-risk disease, and the combination may also be considered (off label) in patients with favorable-risk disease (Ref).
IV: 1 mg/kg once every 3 weeks (in combination with nivolumab) for a maximum of 4 combination doses, followed by nivolumab monotherapy until disease progression or unacceptable toxicity (Ref).
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
Kidney impairment at baseline:
GFR ≥15 mL/minute/1.73 m2: There are no dosage adjustments provided in the manufacturer's labeling; however, GFR ≥15 mL/minute/1.73 m2 had no clinically important effect on ipilimumab clearance.
GFR <15 mL/minute/1.73 m2: There are no dosage adjustments provided in the manufacturer's labeling.
Kidney toxicity during treatment:
Immune-mediated nephritis with kidney dysfunction: If ipilimumab treatment interruption or discontinuation is required, administer systemic corticosteroids (1 to 2 mg/kg/day prednisone [or equivalent]) or other appropriate therapy for immune-mediated adverse reactions until improvement to grade 1 or lower, then follow with a corticosteroid taper.
Grade 2 or grade 3 serum creatinine elevation: Withhold ipilimumab; resume ipilimumab after complete or partial (to grade 0 or 1) resolution after corticosteroid taper. Permanently discontinue ipilimumab if no complete or partial response within 12 weeks of last ipilimumab dose, or if unable to reduce prednisone to <10 mg/day (or equivalent) within 12 weeks of corticosteroid initiation.
Grade 4 serum creatinine elevation: Permanently discontinue ipilimumab.
Hepatic impairment at baseline:
Mild impairment (total bilirubin >1 to 1.5 x ULN or AST >ULN): There are no dosage adjustments provided in the manufacturer's labeling; however, mild impairment had no clinically important effect on ipilimumab clearance.
Moderate or severe impairment (total bilirubin >1.5 x ULN and any AST): There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).
Hepatotoxicity during treatment:
If ipilimumab treatment interruption or discontinuation is required, administer systemic corticosteroids (1 to 2 mg/kg/day prednisone [or equivalent]) or other appropriate therapy for immune-mediated adverse reactions until improvement to grade 1 or lower, then follow with a corticosteroid taper. Permanently discontinue ipilimumab if no complete or partial response within 12 weeks of last ipilimumab dose, or if unable to reduce prednisone to <10 mg/day (or equivalent) within 12 weeks of corticosteroid initiation.
If transaminases do not decrease within 48 hours of steroid initiation, consider adding mycophenolate mofetil; may begin tapering corticosteroid (over 1 month) when LFTs show sustained improvement or return to baseline (Ref).
Immune-mediated hepatitis without tumor involvement of the liver or hepatitis with tumor involvement of the liver/non-hepatocellular carcinoma:
AST or ALT >3 up to 5 times ULN or total bilirubin >1.5 up to 3 times ULN: Withhold ipilimumab; resume ipilimumab with complete or partial resolution (to grade 0 or 1) of hepatitis after corticosteroid taper.
AST or ALT >5 times ULN or total bilirubin >3 times ULN: Permanently discontinue ipilimumab.
Immune-mediated hepatitis with tumor involvement of the liver/hepatocellular carcinoma (applies to hepatocellular carcinoma ipilimumab/nivolumab combination treatment): Note: When receiving combination therapy with ipilimumab and nivolumab, withhold or permanently discontinue both ipilimumab and nivolumab for adverse reactions meeting dosage modification recommendations (refer to Nivolumab monograph for information on nivolumab dosage adjustment for toxicity). If AST and ALT are ≤ ULN at baseline, follow recommendations for hepatitis without tumor involvement of the liver.
If baseline AST or ALT >1 up to 3 times ULN and increases to >5 up to 10 times ULN or baseline AST or ALT >3 up to 5 times ULN and increases to >8 up to 10 times ULN: Withhold treatment. Resume treatment with complete or partial resolution (to grade 0 or 1) of hepatitis after corticosteroid taper.
AST or ALT >10 times ULN or total bilirubin >3 times ULN: Discontinue permanently.
Additional recommendations:
Grade 2 immune-mediated hepatitis: Withhold immune checkpoint inhibitor (ICI); if no improvement within 3 to 5 days after ICI is withheld, consider initiation of corticosteroids (prednisone 0.5 to 1 mg/kg/day or equivalent) (Ref).
Grade 3 or 4 immune-mediated hepatitis: Withhold ICI; initiate corticosteroids (methylprednisolone 1 to 2 mg/kg or equivalent) (Ref). Based on data from a retrospective cohort study in patients with grade 3 or 4 immune-mediated hepatitis, initial treatment with methylprednisolone 1 mg/kg/day demonstrated similar time to ALT normalization (compared with higher methylprednisolone doses), while reducing the potential for corticosteroid-related complications (Ref).
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.
>10%:
Dermatologic: Pruritus (31% to 45%), skin rash (15% to 50%)
Endocrine & metabolic: Endocrine disease (4% to 28%), hyperglycemia (26%), hypocalcemia (20%), hyponatremia (26%), weight loss (7% to 32%)
Gastrointestinal: Colitis (8% to 31%), decreased appetite (14% to 24%), diarrhea (32% to 49%; grades ≥3: 5% to 10%), increased serum amylase (15% to 17%), increased serum lipase (24% to 26%), nausea (25% to 31%; grades ≥3: ≤2%), vomiting (13% to 17%; grades ≥3: ≤2%)
Hematologic & oncologic: Anemia (41%; grades 3/4: 6%), lymphocytopenia (29%; grades 3/4: 4%)
Hepatic: Hepatitis (4% to 15%), increased serum alanine aminotransferase (29% to 46%), increased serum alkaline phosphatase (17% to 23%), increased serum aspartate aminotransferase (29% to 38%), increased serum bilirubin (11%)
Nervous system: Fatigue (41% to 51%), headache (33%)
Neuromuscular & skeletal: Arthralgia (16%), musculoskeletal pain (36%)
Renal: Increased serum creatinine (10% to 17%)
Respiratory: Cough (22%; including productive cough), dyspnea (17%; including dyspnea on exertion), upper respiratory tract infection (17%)
Miscellaneous: Fever (18%)
1% to 10%:
Cardiovascular: Hypertension (9%)
Dermatologic: Urticaria (2%), vitiligo (4% to 5%) (SITC [Brahmer 2021])
Endocrine & metabolic: Adrenocortical insufficiency (≤2%), Cushing syndrome (≤2%), hyperthyroidism (1%), hypothyroidism (5%), pituitary insufficiency (≤2%)
Gastrointestinal: Pancreatitis (1%)
Genitourinary: Hypogonadism (≤2%)
Hematologic & oncologic: Cytopenia (3%), eosinophilia (2%)
Hypersensitivity: Infusion-related reaction (3%)
Immunologic: Antibody development (1%)
Nervous system: Insomnia (10%), neuropathy (2%)
Renal: Acute kidney injury (2%) (SITC [Brahmer 2021]; Isik 2021)
Respiratory: Pneumonitis (1%) (SITC [Brahmer 2021])
<1%:
Cardiovascular: Arteritis (temporal), myocarditis, pericarditis, peripheral vascular disease, vasculitis
Dermatologic: Erythema multiforme, psoriasis
Endocrine & metabolic: Thyroiditis
Gastrointestinal: Duodenitis, esophagitis, gastritis, ulcerative bowel lesion
Hematologic & oncologic: Aplastic anemia, lymphadenitis (histiocytic necrotizing [Kikuchi lymphadenitis])
Hypersensitivity: Hypersensitivity angiitis
Immunologic: Organ transplant rejection (solid), sarcoidosis
Infection: Systemic inflammatory response syndrome
Nervous system: Demyelinating disease, encephalitis, Guillain-Barre syndrome, meningitis, motor dysfunction, myasthenia (myasthenic syndrome), myasthenia gravis, paresis (nerve)
Neuromuscular & skeletal: Arthritis, myelitis, myositis (including orbital), polymyalgia rheumatica, polymyositis, rhabdomyolysis
Ophthalmic: Blepharitis, conjunctivitis, episcleritis, Graves ophthalmopathy, iritis, scleritis, uveitis
Otic: Hypoacusis (neurosensory)
Renal: Kidney failure
Respiratory: Acute respiratory distress syndrome
Frequency not defined: Miscellaneous: Vogt-Koyanagi-Harada disease
Postmarketing:
Cardiovascular: Capillary leak syndrome (Hodi 2010)
Dermatologic: Pemphigoid (SITC [Brahmer 2021]), Stevens-Johnson syndrome (SITC [Brahmer 2021]), toxic epidermal necrolysis (SITC [Brahmer 2021])
Endocrine & metabolic: Hypophysitis (Hodi 2010), type 1 diabetes mellitus (SITC [Brahmer 2021])
Gastrointestinal: Abdominal pain (Hodi 2010), cholangitis (SITC [Brahmer 2021]), cholecystitis (SITC [Brahmer 2021]), constipation (Hodi 2010), xerostomia (SITC [Brahmer 2021])
Hematologic & oncologic: Hemophagocytic lymphohistiocytosis (SITC [Brahmer 2021]; Hantel 2018), neutropenia (SITC [Brahmer 2021]), pure red cell aplasia (SITC [Brahmer 2021])
Hepatic: Hepatotoxicity (Chalasani 2021)
Hypersensitivity: Drug reaction with eosinophilia and systemic symptoms
Immunologic: Dermatomyositis (Yamaguchi 2016), graft-versus-host disease, Sjögren disease (SITC [Brahmer 2021])
Neuromuscular & skeletal: Myalgia (SITC [Brahmer 2021])
Ophthalmic: Dry eye syndrome (SITC [Brahmer 2021])
Respiratory: Bronchiolitis obliterans organizing pneumonia (Barjaktarevic 2013)
There are no contraindications listed in the manufacturer's US labeling.
Canadian labeling: Hypersensitivity to ipilimumab or any component of the formulation; active life-threatening autoimmune disease, or with organ transplantation graft where further immune activation is potentially imminently life-threatening
Concerns related to adverse effects:
• Adverse reactions (immune-mediated): Ipilimumab blocks T-cell inhibitory signals induced by the CTLA-4 pathway, thus removing inhibition of the immune response with the potential for induction of immune-mediated adverse reactions. Severe and fatal immune-mediated adverse effects may occur in any organ system or tissue. Reactions generally occur during treatment (may occur at any time after treatment initiation); reactions may also occur after ipilimumab discontinuation. Early identification and management of immune-mediated adverse reactions are necessary to ensure ipilimumab safety. Medically manage immune-mediated adverse reactions promptly and refer for specialty consultation as appropriate. Depending on the severity, withhold or permanently discontinue ipilimumab. In general, if treatment interruption or discontinuation are required, administer systemic corticosteroid therapy (1 to 2 mg/kg/day prednisone [or equivalent]) until improvement to ≤ grade 1. Upon improvement to grade 1 or lower, initiate corticosteroid taper and continue to taper over at least 1 month. Consider administration of other systemic immunosuppressants if immune-mediated adverse reaction is not controlled with corticosteroid therapy.
• Dermatologic toxicity: Ipilimumab may cause immune-mediated rash or dermatitis, including bullous and exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis, and drug reaction with eosinophilia and systemic symptoms (DRESS). Immune-mediated rash (including grade 2 or higher events) occurred with both single-agent ipilimumab and when used in combination with nivolumab. Higher ipilimumab doses were generally associated with an increased incidence of immune-mediated rash. Systemic corticosteroids were often used to manage immune-mediated rash; reactions resolved in a majority of those patients. In cases where ipilimumab was withheld and patients reinitiated treatment after symptom improvement, some of those patients experienced immune-mediated dermatologic toxicity recurrence.
• Endocrinopathies: Immune-mediated endocrinopathies have occurred with single-agent ipilimumab and when used in combination with nivolumab, including grades 2 to 4 or fatal events. Some endocrinopathies have resulted in long-term hormone replacement therapy, hospitalizations, and management with systemic corticosteroids. Some patients reported resolution of endocrinopathy.
- Adrenal insufficiency: Adrenal insufficiency, including grades 2 to 4, has occurred with single-agent ipilimumab and when used in combination with nivolumab. Adrenal insufficiency led to ipilimumab/nivolumab treatment interruption or discontinuation in a small number of patients. Most patients with adrenal insufficiency due to ipilimumab in combination with nivolumab received hormone replacement therapy and systemic corticosteroids. Adrenal insufficiency resolved in some patients. Some patients experienced a recurrence when ipilimumab and/or nivolumab treatment was restarted after symptom improvement.
- Diabetes mellitus: Type 1 diabetes (including grade 2 to 4 events) has also been observed with ipilimumab in combination with nivolumab. Diabetes led to ipilimumab/nivolumab treatment interruption or discontinuation in some cases and systemic corticosteroids were required in some cases. Diabetes resolved in about one quarter of patients. Diabetes did not recur in patients whose treatment was restarted after symptom improvement.
- Hypophysitis: Ipilimumab may cause immune-mediated hypophysitis, which may present with acute symptoms associated with mass effect, including headache, photophobia, or visual field defects. Hypophysitis may lead to hypopituitarism. Initiate hormone replacement as clinically indicated and, depending on the severity, withhold or discontinue ipilimumab; may also require treatment with systemic corticosteroids. Hypophysitis resolved in over half of patients. Some patients experienced a recurrence when treatment was restarted after symptom improvement.
- Thyroid disorders: Immune-mediated hyperthyroidism, hypothyroidism, and thyroiditis have occurred with single-agent ipilimumab and when used in combination with nivolumab. Grades 2 and 3 hyperthyroidism have been observed. Although ipilimumab/nivolumab treatment interruption was necessary in some patients, no patients required ipilimumab discontinuation for hyperthyroidism. A thyroid synthesis inhibitor and/or systemic corticosteroids were necessary to manage hyperthyroidism in ~20% of patients. Hyperthyroidism resolved in most patients. Some patients experienced a recurrence when ipilimumab and/or nivolumab treatment was restarted after symptom improvement. Hypothyroidism (or thyroiditis resulting in hypothyroidism), including grade 2 and 3 events has been observed. Hypothyroidism led to ipilimumab/nivolumab treatment interruption or discontinuation in some patients. Most patients were managed with thyroid hormone replacement therapy; systemic corticosteroids were required in some patients. Hypothyroidism resolved in approximately one quarter of patients. Recurrence of hypothyroidism occurred rarely when ipilimumab and/or nivolumab treatment was restarted after symptom improvement. Thyroiditis has been reported with ipilimumab when used as a single-agent and when used in combination with nivolumab, including grade 2 and 3 thyroiditis. Thyroiditis led to ipilimumab/nivolumab treatment interruption or discontinuation in some cases; some patients required systemic corticosteroids. Thyroiditis resolved in a majority of patients. Thyroiditis did not recur in patients whose treatment was restarted after symptom improvement.
- Other endocrinopathies: Cushing syndrome, hypogonadism, hypopituitarism, thyroidism, and Graves ophthalmopathy have also been reported.
• GI toxicity: Ipilimumab may cause immune-mediated colitis, which may be fatal. Immune-mediated colitis (including grades 2 to 4 and fatal events) has occurred with single-agent ipilimumab and when used in combination with nivolumab. Systemic corticosteroids were necessary in 60% to 100% of patients with immune-mediated colitis (which resolved in 76% to 95% of these patients); some patients required coadministration of an additional immunosuppressant (with corticosteroids). Upon ipilimumab reinitiation (following therapy interruption for colitis and subsequent resolution), recurrence of colitis commonly occurred. Cytomegalovirus infection/reactivation has been reported in patients with corticosteroid-refractory immune-mediated diarrhea/colitis. In cases of corticosteroid-refractory diarrhea/colitis, consider repeating infectious workup to exclude alternative etiologies. Pancreatitis (including increased serum amylase and lipase levels), duodenitis, and gastritis, have also been reported (rarely).
• Hepatotoxicity: Immune-mediated hepatitis (including grades 2 to 4 and fatal events) has occurred with single-agent ipilimumab and when used in combination with nivolumab. Hepatitis has led to ipilimumab treatment interruption and discontinuation. Systemic corticosteroids were used to manage immune-mediated hepatitis in many patients (which resolved in most of these patients); additional immunosuppressants were necessary in some cases. Upon ipilimumab reinitiation (following therapy interruption for colitis and subsequent resolution), recurrence of hepatitis occurred in some patients.
• Infusion-related reactions: Infusion-related reactions may occur with ipilimumab; may be severe.
• Nephrotoxicity: Immune-mediated nephritis with renal dysfunction (including grade 2 to 4 events) has occurred with ipilimumab when used in combination with nivolumab, and has led to ipilimumab or nivolumab treatment interruption or discontinuation in some patients. Systemic corticosteroids were used to manage immune-mediated nephritis. Nephritis with renal dysfunction resolved in two-thirds of patients. Nephritis recurred in some patients whose treatment was restarted after symptom improvement.
• Ocular toxicity: Immune-mediated blepharitis, episcleritis, iritis, orbital myositis, scleritis, and uveitis have been observed (rarely) with ipilimumab. Some cases may be associated with retinal detachment. If uveitis occurs in combination with other immune-mediated adverse reactions, consider a Vogt-Koyanagi-Harada-like syndrome, which has been observed with ipilimumab.
• Pulmonary toxicity: Immune-mediated pneumonitis (including grade 2 to 4 events) has occurred with ipilimumab when used in combination with nivolumab; some cases were fatal. Pneumonitis has led to ipilimumab and nivolumab treatment interruption or discontinuation. Systemic corticosteroids were used to treat immune-mediated pneumonitis; some patients required coadministration of another immunosuppressant (with corticosteroids) to manage pneumonitis. Pneumonitis resolved in a majority of patients. In patients receiving ipilimumab with nivolumab for the treatment of non-small cell lung cancer, the median duration of pneumonitis was 1.5 months (range: 5 days to >25 months). Some patients experienced recurrence when treatment was restarted after symptom improvement.
• Other immune-mediated toxicities: Other clinically significant immune-mediated adverse reactions have been observed (rarely although sometimes fatal) with ipilimumab (either as a single agent or in combination with nivolumab), including autoimmune neuropathy, meningitis, encephalitis, neurosensory hypoacusis, myelitis and demyelination, myasthenic syndrome/myasthenia gravis, Guillain-Barré syndrome, nerve paresis, motor dysfunction, angiopathy, myocarditis, pericarditis, temporal arteritis, vasculitis, arthritis, myositis, polymyalgia rheumatica, polymyositis, rhabdomyolysis, aplastic anemia, conjunctivitis, cytopenias, eosinophilia, histiocytic necrotizing lymphadenitis (Kikuchi lymphadenitis), hypersensitivity vasculitis, psoriasis, sarcoidosis, systemic inflammatory response syndrome, and solid organ transplant rejection.
Disease-related concerns:
• Hematopoietic stem cell transplant: Serious and potentially fatal graft-vs-host disease (GVHD) can occur in patients receiving ipilimumab either before or after allogeneic hematopoietic stem cell transplantation (HSCT). These complications may occur despite intervening therapy between CTLA-4 receptor blocking antibody and allogeneic HSCT. Monitor for evidence of GVHD and manage promptly. Consider the benefit versus risks of ipilimumab treatment following allogeneic HSCT.
• Myasthenia gravis: Checkpoint inhibitors may worsen or precipitate new myasthenia gravis (MG), especially within the first 16 weeks of treatment; use with caution. Patients with well-controlled MG may be considered for checkpoint inhibitor therapy if MG treatment is maintained (or reinitiated in patients whose MG is in remission), combination therapy (eg, anti–CTLA-4 with anti–PD-a/PD-L1 monoclonal antibodies) is avoided, and respiratory and bulbar function are closely followed. In patients who develop overt MG during checkpoint inhibitor therapy, early aggressive treatment with plasma exchange or IVIG in combination with high-dose corticosteroids may be required (AAN [Narayanaswami 2021]).
Special populations:
• Older adults: In patients with non-small cell lung cancer (NSCLC) who received ipilimumab/nivolumab or ipilimumab/nivolumab with platinum-based doublet chemotherapy, patients ≥75 years of age experienced a higher discontinuation rate due to adverse reactions relative to all patients with NSCLC who received ipilimumab/nivolumab. In the esophageal squamous cell carcinoma (ESCC) ipilimumab/nivolumab study, patients ≥75 years of age experienced a higher discontinuation rate due to adverse reactions relative to all patients with ESCC who received ipilimumab/nivolumab. In the malignant pleural mesothelioma study of ipilimumab in combination with nivolumab, patients ≥75 years of age experienced a higher rate of serious adverse reactions and discontinuation due to adverse reactions.
Dosage form specific issues:
• Polysorbate 80: Some dosage forms may contain polysorbate 80 (also known as Tweens). Hypersensitivity reactions, usually a delayed reaction, have been reported following exposure to pharmaceutical products containing polysorbate 80 in certain individuals (Isaksson 2002; Lucente 2000; Shelley 1995). Thrombocytopenia, ascites, pulmonary deterioration, and renal and hepatic failure have been reported in premature neonates after receiving parenteral products containing polysorbate 80 (Alade 1986; CDC 1984). See manufacturer's labeling.
Other warnings/precautions:
• Appropriate use: Select patients for first-line ipilimumab/nivolumab treatment of metastatic NSCLC based on PD-L1 expression. Information on tests to detect PD-L1 expression may be found at http://www.fda.gov/companiondiagnostics.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Solution, Intravenous [preservative free]:
Yervoy: 50 mg/10 mL (10 mL); 200 mg/40 mL (40 mL) [contains polysorbate 80]
No
Solution (Yervoy Intravenous)
50 mg/10 mL (per mL): $1,023.90
200 mg/40 mL (per mL): $1,023.90
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Solution, Intravenous:
Yervoy: 5 mg/mL (10 mL, 40 mL) [contains polysorbate 80]
IV: Infuse over 30 minutes (refer to specific protocols); administer through a sterile, non-pyrogenic, low protein-binding in-line filter. Do not administer with other medications. Flush with NS or D5W after each ipilimumab infusion.
Combination therapy with nivolumab: When administered in combination with nivolumab, infuse nivolumab first followed by ipilimumab on the same day. Use separate infusion bags and filters for each infusion.
IV: Infuse through a sterile, nonpyrogenic, low protein-binding in-line filter. Do not administer with other medications. Flush with NS or D5W after each ipilimumab infusion.
Colorectal cancer (metastatic), esophageal squamous cell carcinoma, hepatocellular carcinoma, malignant pleural mesothelioma, melanoma (unresectable/metastatic), non–small cell lung cancer, or renal cell carcinoma (advanced): Infuse over 30 minutes.
Melanoma (adjuvant treatment): Infuse over 90 minutes.
Monitor for infusion reactions. Interrupt or slow the infusion for grade 1 or 2 infusion-related reactions; permanently discontinue for grade 3 or 4 infusion-related reactions.
Combination therapy with nivolumab: When administered in combination with nivolumab, infuse nivolumab first, followed by ipilimumab (on the same day as nivolumab). Use separate infusion bags and filters for each infusion.
Combination therapy with nivolumab and platinum-based doublet chemotherapy: When administered in combination with nivolumab and platinum-based doublet chemotherapy, infuse nivolumab first, followed by ipilimumab, and then the platinum-based doublet chemotherapy (all on the same day). Use separate infusion bags and filters for each infusion.
Store intact vials at 2°C to 8°C (36°F to 46°F); do not freeze. Protect from light. Do not shake. Prior to preparation, allow vials to sit at room temperature for ~5 minutes. Solutions diluted for infusion in NS or D5W are stable for up to 24 hours (from time of preparation to time of infusion) refrigerated or at room temperature.
An FDA-approved patient medication guide, which is available with the product information and at https://www.accessdata.fda.gov/drugsatfda_docs/label/2023/125377s129lbl.pdf#page=72, must be dispensed with this medication.
Indications including pediatric patients:
Treatment of microsatellite instability-high (MSI-H) or mismatch repair deficient (dMMR) metastatic colorectal cancer (CRC) that has progressed following treatment with a fluoropyrimidine, oxaliplatin, and irinotecan, in combination with nivolumab; treatment of unresectable or metastatic melanoma as a single agent or in combination with nivolumab (All indications: FDA approved in ages ≥12 years and adults). Note: FDA approval for MSI-H or dMMR metastatic CRC is through an accelerated process; continued approval is dependent upon verification of clinical benefit in further trials.
Indications approved only in adults:
Adjuvant treatment of cutaneous melanoma in patients with pathologic involvement of regional lymph nodes of more than 1 mm who have undergone complete resection, including total lymphadenectomy; treatment of intermediate or poor risk, previously untreated advanced renal cell carcinoma (in combination with nivolumab); treatment of hepatocellular carcinoma (in combination with nivolumab) in patients who have been previously treated with sorafenib; first-line treatment of metastatic non-small cell lung cancer (in combination with nivolumab) in patients whose tumors express PD-L1 (≥1%) as determined by an approved test, and with no EGFR or ALK genomic tumor aberrations; first-line treatment of metastatic or recurrent non-small cell lung cancer (in combination with nivolumab and 2 cycles of platinum doublet chemotherapy) in patients with no EGFR or ALK genomic tumor aberrations; first-line treatment of unresectable malignant pleural mesothelioma (in combination with nivolumab); first-line treatment of unresectable advanced or metastatic esophageal squamous cell carcinoma (in combination with nivolumab) (All indications: FDA approved in adults).
Ipilimumab may be confused with dostarlimab, dupilumab, idaruCIZUmab, isatuximab, nivolumab, tremelimumab.
The Institute for Safe Medication Practices (ISMP) includes this medication among its list of drug classes (chemotherapeutic agent, parenteral and oral) which have a heightened risk of causing significant patient harm when used in error (High-Alert Medications in Acute Care, Community/Ambulatory Care, and Long-Term Care Settings).
None known.
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the drug interactions program by clicking on the “Launch drug interactions program” link above.
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the drug interactions program
Acetaminophen: May diminish the therapeutic effect of Immune Checkpoint Inhibitors (Anti-PD-1, -PD-L1, and -CTLA4 Therapies). Risk C: Monitor therapy
Antibiotics: May diminish the therapeutic effect of Immune Checkpoint Inhibitors (Anti-PD-1, -PD-L1, and -CTLA4 Therapies). Risk C: Monitor therapy
Corticosteroids (Systemic): May diminish the therapeutic effect of Immune Checkpoint Inhibitors (Anti-PD-1, -PD-L1, and -CTLA4 Therapies). Management: Carefully consider the need for corticosteroids, at doses of a prednisone-equivalent of 10 mg or more per day, during the initiation of immune checkpoint inhibitor therapy. Use of corticosteroids to treat immune related adverse events is still recommended Risk D: Consider therapy modification
Inhibitors of the Proton Pump (PPIs and PCABs): May diminish the therapeutic effect of Immune Checkpoint Inhibitors (Anti-PD-1, -PD-L1, and -CTLA4 Therapies). Risk C: Monitor therapy
Ketoconazole (Systemic): Immune Checkpoint Inhibitors (Anti-PD-1, -PD-L1, and -CTLA4 Therapies) may enhance the hepatotoxic effect of Ketoconazole (Systemic). Risk C: Monitor therapy
Vemurafenib: Ipilimumab may enhance the hepatotoxic effect of Vemurafenib. Management: Consider alternatives to this combination when possible. Use of this combination should only be undertaken with extra close monitoring of liver function (hepatic transaminases and bilirubin) and signs/symptoms of hepatotoxicity. Risk D: Consider therapy modification
Verify pregnancy status prior to treatment initiation in patients who could become pregnant. Patients who could become pregnant should use effective contraception during treatment and for 3 months following the last ipilimumab dose.
Pituitary dysfunction, secondary to autoimmune hypophysitis, may occur with ipilimumab therapy; male and female fertility may be impaired (Grunewald 2015).
Ipilimumab is a humanized monoclonal antibody (IgG1). Human IgG crosses the placenta. Fetal exposure is dependent upon the IgG subclass, maternal serum concentrations, placental integrity, newborn birth weight, and gestational age, generally increasing as pregnancy progresses. The lowest exposure would be expected during the period of organogenesis and the highest during the third trimester (Clements 2020; Palmeira 2012; Pentsuk 2009).
Outcome data following maternal use of ipilimumab during pregnancy are limited (Bucheit 2020; Burotto 2018; Mehta 2018; Menzer 2018; Mittra 2021). Based on the mechanism of action and data from animal reproduction studies, in utero exposure to ipilimumab may disrupt maternal tolerance to the fetus, increasing the risk of abortion or stillbirth. Based on animal data, maternal use of a CTLA-4 inhibitor may also result in immune-mediated disorders in the newborn.
The European Society for Medical Oncology has published guidelines for diagnosis, treatment, and follow-up of cancer during pregnancy. The guidelines recommend referral to a facility with expertise in cancer during pregnancy and encourage a multidisciplinary team (obstetrician, neonatologist, oncology team) approach (ESMO [Peccatori 2013]; Swetter 2019). Until additional data are available, use of ipilimumab for the treatment of melanoma during pregnancy is not recommended (ESMO [Peccatori 2013]).
Data collection to monitor pregnancy and infant outcomes following exposure to ipilimumab is ongoing. Ipilimumab exposures during pregnancy should be reported to the manufacturer (1-844-593-7869).
A long-term observational research study is collecting information about the diagnosis and treatment of cancer during pregnancy. For additional information about the pregnancy and cancer registry or to become a participant, contact Cooper Health (877-635-4499).
Monitor liver function and evaluate for signs of hepatotoxicity prior to each dose; if hepatotoxicity develops, liver function should be monitored more frequently until resolution. If LFTs are >8 times ULN, monitor every other day until they begin to fall, then weekly until normal (Weber 2012). Monitor serum chemistries and ACTH prior to each dose. Monitor SCr (baseline and periodic). Monitor for signs of hypophysitis, adrenal insufficiency, and thyroid disorders (eg, abdominal pain, fatigue, headache, hypotension, mental status changes, unusual bowel habits). Monitor thyroid-stimulating hormone, free T4, and cortisol levels (morning) at baseline, prior to dose, and as clinically indicated. Monitor for signs and symptoms of enterocolitis (abdominal pain, blood or mucus in stool or diarrhea) and intestinal perforation (peritoneal signs, ileus). Monitor for rash and pruritus. Monitor for signs of motor or sensory neuropathy (unilateral or bilateral weakness, sensory changes, or paresthesia). Monitor for ocular toxicity at baseline, then at 4 to 8 weeks with further evaluations as clinically indicated (Renouf 2012). Monitor for signs/symptoms of pneumonitis, encephalitis, and infusion-related reactions. In adult patients, additional cancer-specific monitoring parameters may be necessary (refer to specific protocols or manufacturer labeling).
Ipilimumab is a recombinant human IgG1 immunoglobulin monoclonal antibody that binds to the cytotoxic T-lymphocyte associated antigen 4 (CTLA-4). CTLA-4 is a down-regulator of T-cell activation pathways. Blocking CTLA-4 allows for enhanced T-cell activation and proliferation. In melanoma, ipilimumab may indirectly mediate T-cell immune responses against tumors. Combining ipilimumab (anti-CTLA-4) with nivolumab (anti-PD-1) results in enhanced T-cell function that is greater than that of either antibody alone, resulting in improved antitumor responses in metastatic melanoma and advanced renal cell carcinoma.
Half-life elimination: Terminal: 15.4 days.
Excretion: Clearance: Ipilimumab monotherapy: 16.8 mL/hour; compared to ipilimumab monotherapy, ipilimumab clearance is unchanged when administered every 3 weeks in combination with nivolumab, increased 30% when administered every 6 weeks in combination with nivolumab, and increased 22% when administered every 6 weeks in combination with nivolumab and platinum-based doublet chemotherapy.
Body weight: Clearance is increased with increasing body weight.
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