PDR MEMBER LOGIN:
  • PDR Search

    Required field
  • Advertisement
  • CLASSES

    Antineoplastic Monoclonal Antibodies Targeting Programmed Death-1 (PD-1) and Programmed Death-Ligand 1 (PD-L1) Pathways

    DEA CLASS

    Rx

    DESCRIPTION

    Programmed death ligand-1 (PD-L1) blocking monoclonal antibody
    Used for certain types of Merkel cell carcinoma, renal cell, and urothelial carcinoma
    Immune-mediated reactions have been reported; treatment may need to be withheld or permanently discontinued

    COMMON BRAND NAMES

    BAVENCIO

    HOW SUPPLIED

    BAVENCIO Intravenous Inj Sol: 1mL, 20mg

    DOSAGE & INDICATIONS

    For the treatment of metastatic Merkel cell carcinoma.
    NOTE: The FDA has designated avelumab as an orphan drug for the treatment of Merkel cell carcinoma.
    Intravenous dosage
    Adults, Adolescents, and Children 12 years of age

    800 mg IV over 60 minutes every 2 weeks until disease progression. All patients should receive premedication with an antihistamine and acetaminophen 30 to 60 minutes prior to the first 4 avelumab infusions; premedication may be administered prior to subsequent doses based upon clinical judgment and presence/severity of prior infusion reactions. Therapy may need to be temporarily withheld or permanently discontinued in patients who develop immune-related reactions. Permanently discontinue therapy for severe or life-threatening infusion-related reactions.[61826] The confirmed objective response rate (ORR) was 31.8% in patients with metastatic, chemotherapy-refractory Merkel cell carcinoma who received avelumab (median of 7 doses; median duration of therapy, 17 weeks) in a multinational, phase 2 study (n = 88); the complete response rate was 9%. The response duration ranged from 2.8 months to at least 17.5 months. The ORR was 26.1% in 46 patients with Merkel-cell polyomavirus (MCPyV)-positive tumors and 35.5% in 31 patients with MCPyV-negative tumors. The ORR was 34.5% in 58 patients with PD-L1-positive tumors and 18.8% in 16 patients with PD-L1-negative tumors. At a median follow-up time of 10.4 months, the median progression-free survival (PFS) time was 2.7 months and the 6-month PFS rate was 40%. Additionally, the median overall survival (OS) time was 11.3 months and the 6-month OS rate was 69%. Adult patients (median age, 72.5 years) with stage IV Merkel cell carcinoma that progressed after at least 1 prior line of chemotherapy for metastatic disease were eligible for study treatment.[61829] Efficacy for pediatric patients has been extrapolated from results from clinical trials in adult patients and from pharmacokinetic data suggesting that drug exposure is comparable between adults and pediatric patients age 12 years and older.[61826]

    For the treatment of urothelial carcinoma.
    For the treatment of locally advanced or metastatic urothelial carcinoma, in patients with disease progression on or following platinum-containing chemotherapy, or within 12 months of neoadjuvant or adjuvant platinum-containing chemotherapy.
    Intravenous dosage
    Adults

    800 mg IV over 60 minutes every 2 weeks until disease progression or unacceptable toxicity. All patients should receive premedication with an antihistamine and acetaminophen 30 to 60 minutes prior to the first 4 avelumab infusions; premedication may be administered prior to subsequent doses based upon clinical judgment and presence/severity of prior infusion reactions. Therapy may need to be temporarily withheld or permanently discontinued in patients who develop immune-related reactions. Permanently discontinue therapy for severe or life-threatening infusion-related reactions. In a multicenter, open-label, single arm clinical trial, a cohort of patients from the Javelin Solid Tumor trial who had platinum-resistant, locally advanced or metastatic urothelial cancer were treated with avelumab. In this cohort, the objective response rate was 13.3% (complete response (CR), 4%; partial response (PR), 9.3%) after at least 13 weeks of follow-up (n = 226), and 16.1% (CR, 5.6%; PR, 10.6%) after at least 6 months of follow-up (n = 161). The median duration of response was not estimable but ranged from 1.4 to 17.4+ months.[61826]

    For maintenance treatment of locally advanced or metastatic urothelial carcinoma that has not progressed with first-line platinum-containing chemotherapy.
    Intravenous dosage
    Adults

    800 mg IV over 60 minutes every 2 weeks until disease progression or unacceptable toxicity. All patients should receive premedication with an antihistamine and acetaminophen 30 to 60 minutes prior to the first 4 avelumab infusions; premedication may be administered prior to subsequent doses based upon clinical judgment and presence/severity of prior infusion reactions. Therapy may need to be temporarily withheld or permanently discontinued in patients who develop immune-related reactions. Permanently discontinue therapy for severe or life-threatening infusion-related reactions. Maintenance therapy with avelumab significantly improved the median overall survival (OS) compared with best supportive care in patients with unresectable, locally advanced or metastatic urothelial cancer that did not progress with first-line platinum-based chemotherapy in a multicenter, open-label clinical trial (23.8 months vs. 15 months). In a prespecified endpoint of OS based on PD-L1 status, the effect of avelumab maintenance therapy remained statistically significant for patients with PD-L1 positive tumors. The effect was not significant in patients with PD-L1 negative tumors in an exploratory analysis.[61826]

    For the treatment of renal cell cancer.
    For the first-line treatment of advanced renal cell cancer, in combination with axitinib.
    Intravenous dosage
    Adults

    800 mg IV over 1 hour every 2 weeks, in combination with axitinib (initial dose, 5 mg PO twice daily) until disease progression or unacceptable toxicity. The axitinib dosage may be increased to 7 mg twice daily and then to 10 mg twice daily in normotensive patients (not receiving antihypertensive medications) who tolerate the lower dosage for at least 2 consecutive weeks with no greater than grade 2 adverse reactions. All patients should receive premedication with an antihistamine and acetaminophen 30 to 60 minutes prior to the first 4 avelumab infusions; premedication may be administered prior to subsequent doses based upon clinical judgment and presence/severity of prior infusion reactions. Avelumab therapy may need to be temporarily withheld or permanently discontinued in patients who develop immune-related reactions. Permanently discontinue therapy for severe or life-threatening infusion-related reactions. Coadministration of certain drugs may need to be avoided or dosage adjustments may be necessary; review drug interactions. In the first interim analysis of an open-label phase 3 clinical trial (JAVELIN Renal 101), first-line combination therapy with avelumab and axitinib significantly improved PFS in patients with advanced renal cell carcinoma and PD-L1 expression of 1% or more compared with sunitinib monotherapy; the confirmed objective response rate almost doubled with combination therapy. Overall survival was not reached in either group and continues to be monitored.

    MAXIMUM DOSAGE

    Adults

    800 mg IV every 2 weeks.

    Geriatric

    800 mg IV every 2 weeks.

    Adolescents

    800 mg IV every 2 weeks.

    Children

    Children 12 years of age: 800 mg IV every 2 weeks.
    Children less than 12 years: safety and effectiveness not established.

    DOSING CONSIDERATIONS

    Hepatic Impairment

    Treatment-Related Immune-Mediated Hepatitis
    Monotherapy
    No Tumor Involvement of the LiverAST or ALT level of more than 3 to 8 times the ULN or a total bilirubin level of more than 1.5 to 3 times the ULN: Hold avelumab and administer corticosteroids (i.e., prednisone 1 to 2 mg/kg per day or equivalent, followed by a 1-month taper). Resume therapy when the adverse event recovers to grade 1 or less after the corticosteroid taper. Permanently discontinue avelumab in patients who do not have a complete or partial resolution of toxicity or who cannot reduce their daily prednisone dose to less than 10 mg (or equivalent) within 12 weeks of initiating steroids. AST or ALT level more than 8 times the ULN or a total bilirubin level more than 3 times the ULN: Permanently discontinue avelumab and administer corticosteroids (i.e., prednisone 1 to 2 mg/kg per day or equivalent, followed by a 1-month taper starting when the toxicity resolves to grade 1 or less).Tumor Involvement of the LiverBaseline AST or ALT level at the ULN or less: Hold or permanently discontinue avelumab based on recommendations for hepatitis with no tumor involvement of the liver.Baseline AST or ALT level of more than 1 to 3 times the ULNAST or ALT level of more than 5 to 10 times the ULN: Hold avelumab and administer corticosteroids (i.e., prednisone 1 to 2 mg/kg per day or equivalent, followed by a 1-month taper). Resume therapy when the adverse event recovers to grade 1 or less after the corticosteroid taper. Permanently discontinue avelumab in patients who do not have a complete or partial resolution of toxicity or who cannot reduce their daily prednisone dose to less than 10 mg (or equivalent) within 12 weeks of initiating steroids. Baseline AST or ALT level of more than 3 to 5 times the ULNAST or ALT level of more than 8 to 10 times the ULN: Hold avelumab and administer corticosteroids (i.e., prednisone 1 to 2 mg/kg per day or equivalent, followed by a 1-month taper). Resume therapy when the adverse event recovers to grade 1 or less after the corticosteroid taper. Permanently discontinue avelumab in patients who do not have a complete or partial resolution of toxicity or who cannot reduce their daily prednisone dose to less than 10 mg (or equivalent) within 12 weeks of initiating steroids. Any Baseline AST or ALT levelAST or ALT level more than 10 times the ULN or a total bilirubin level to more than 3-times the ULN: Permanently discontinue avelumab and administer corticosteroids (i.e., prednisone 1 to 2 mg/kg per day or equivalent, followed by a 1-month taper starting when the toxicity resolves to grade 1 or less).
    Combination Therapy with Axitinib
    AST or ALT level of 3 to less than 10 times the ULN and a total bilirubin level of less than 2 times the ULN: Hold both avelumab and axitinib and consider corticosteroid therapy. Consider rechallenge with avelumab or axitinib (or sequential rechallenge with both) when hepatic enzymes recover to grade 1 or less. Per axitinib manufacturer guidance, consider a dose reduction if rechallenging with axitinib.AST or ALT level of 10 times the ULN or more OR an AST or ALT level more than 3 times the ULN and a total bilirubin level 2 times the ULN or more: Permanently discontinue avelumab and axitinib and consider corticosteroid therapy.

    Renal Impairment

    Treatment-Related Immune-Mediated Nephritis with Renal Dysfunction Grade 2 or 3 increased serum creatinine (SCr) level: Hold avelumab and administer corticosteroids (i.e., prednisone 1 to 2 mg/kg per day or equivalent, followed by a 1-month taper). Resume therapy when the adverse event recovers to grade 1 or less after the corticosteroid taper. Permanently discontinue avelumab in patients who do not have a complete or partial resolution of toxicity or who cannot reduce their daily prednisone dose to less than 10 mg (or equivalent) within 12 weeks of initiating steroids. Grade 4 increased SCr level: Permanently discontinue avelumab and administer corticosteroids (i.e., prednisone 1 to 2 mg/kg per day or equivalent, followed by a 1-month taper starting when the toxicity resolves to grade 1 or less).

    ADMINISTRATION

    Emetic Risk
    Minimal

    Injectable Administration

    Visually inspect parenteral products for particulate matter and discoloration prior to administration whenever solution and container permit.

    Intravenous Administration

    Dilution
    Add the required amount/volume of drug to a 250 mL bag of 0.9% Sodium Chloride Injection or 0.45% Sodium Chloride Injection.
    Mix by gentle inversion; avoid foaming or excessive shearing.
    Discard any unused drug left in the vial.
    Storage following dilution: Store at room temperature (up to 25 degrees C or 77 degrees F) for up to 4 hours from the time of dilution, or refrigerated (2 to 8 degrees C; 36 to 46 degrees F) for up to 24 hours from the time of dilution. If refrigerated, allow the diluted solution to warm to room temperature prior to administration. Do not freeze or shake; protect from light.[61826]
    Administration
    Administer the diluted solution IV over 60 minutes.
    Use a sterile, non-pyrogenic, low-protein-binding 0.2-micron in-line filter.
    Do not administer other drugs through the same infusion line.[61826]

    STORAGE

    BAVENCIO:
    - Discard product if it contains particulate matter, is cloudy, or discolored
    - Discard unused portion. Do not store for later use.
    - Do not freeze
    - Protect from light
    - Refrigerate (between 36 and 46 degrees F)
    - See package insert for detailed storage information
    - Store in original package until time of use

    CONTRAINDICATIONS / PRECAUTIONS

    Immune-mediated reactions

    Immune-mediated reactions, which may be severe or fatal, can occur in patients treated with drugs that bind to either the programmed death-receptor 1 (PD-1) or the PD-ligand 1 (PD-L1), thus removing inhibition of the immune response, such as avelumab. These immune-mediated reactions can occur in any organ system or tissue and can also affect more than one body system simultaneously. Although usually occurring during treatment with PD-1/PD-L1 inhibitors, immune-mediated reactions can occur at any time after starting therapy including after discontinuation of therapy. Because early identification and management is critical to safe usage of PD-1/PD-L1 inhibitors, closely monitor patients for signs and symptoms that may be clinical manifestations of underlying immune-mediated reactions. Initiate an appropriate workup to exclude alternative etiologies including infection in cases of suspected immune-mediated reaction. Begin medical management promptly, including specialty consultation as appropriate. An interruption or discontinuation of avelumab therapy may be necessary, depending on the severity of the reaction. In general, if an interruption or discontinuation of therapy is necessary, administer systemic corticosteroids (1 to 2 mg/kg per day of prednisone or equivalent); upon improvement to grade 1 or less, begin a steroid taper over at least 1 month. Consider additional systemic immunosuppression in patients whose symptoms are not controlled with corticosteroid therapy.

    Pneumonitis, radiation therapy

    Immune-mediated pneumonitis has been reported with avelumab therapy; some cases were fatal. The incidence of pneumonitis with other PD-1/PD-L1 inhibitors is higher in patients who have received prior thoracic radiation therapy. Monitor patients for signs and symptoms of pneumonitis (e.g., new or worsening cough, chest pain, shortness of breath). If confirmed, avelumab therapy may need to be interrupted or discontinued; treatment with systemic corticosteroids may be necessary.

    Hepatitis, hepatotoxicity

    Immune-mediated hepatitis has been reported with avelumab therapy. The incidence of hepatotoxicity was higher in patients treated with avelumab in combination with axitinib compared with avelumab alone. Monitor hepatic function at baseline and periodically during treatment; consider more frequent monitoring in patients receiving avelumab with axitinib. Avelumab therapy may need to be interrupted or discontinued depending on the severity of hepatitis and if there is tumor involvement of the liver; treatment with systemic corticosteroids may also be necessary.

    Colitis, Crohn's disease, inflammatory bowel disease, ulcerative colitis, viral infection

    Immune-mediated colitis has been reported with avelumab therapy. Additionally, cytomegalovirus (CMV) viral infection/reactivation has been reported in patients with steroid-refractory immune-mediated colitis. Use avelumab with caution in patients with pre-existing inflammatory bowel disease such as ulcerative colitis or Crohn's disease. Monitor patients for symptoms of colitis (e.g., diarrhea, severe abdominal pain). Avelumab therapy may need to be interrupted or discontinued depending on severity; treatment with systemic corticosteroids may be necessary. In patients with steroid-refractory colitis, consider repeating infectious workup to exclude alternative etiologies.

    Adrenal insufficiency, hypophysitis, hypopituitarism

    Primary or secondary adrenal insufficiency and immune-mediated hypophysitis can occur in patients treated with avelumab. Hypophysitis can present with acute symptoms associated with mass effect such as headache, photophobia, or visual field defects; hypophysitis can cause hypopituitarism. Initiate symptomatic treatment including hormone replacement therapy for grade 2 or higher adrenal insufficiency and for hypophysitis as clinically indicated. Avelumab therapy may need to be interrupted or discontinued depending on severity; treatment with systemic corticosteroids may also be necessary.

    Hyperthyroidism, hypothyroidism

    Avelumab can cause immune-mediated thyroid disorders. Thyroiditis can present with or without endocrinopathy; hypothyroidism can follow hyperthyroidism. Evaluate thyroid function at baseline and monitor periodically during treatment. Begin hormone replacement for hypothyroidism or medical management of hyperthyroidism as clinically indicated. Avelumab therapy may need to be interrupted or discontinued depending on severity; treatment with systemic corticosteroids may also be necessary.

    Diabetes mellitus, diabetic ketoacidosis, hyperglycemia, type 1 diabetes mellitus

    Type 1 diabetes mellitus, which can present with diabetic ketoacidosis, has been reported with avelumab therapy. If avelumab and axitinib are used together, optimize the management of pre-existing diabetes mellitus, a cardiac risk factor with this combination. Monitor patients for hyperglycemia and other signs and symptoms of diabetes. Withhold avelumab therapy for cases of severe hyperglycemia until blood sugar control is achieved; administer insulin as clinically indicated.[61826]

    Renal failure, renal impairment

    Immune-mediated nephritis and renal failure have been reported with avelumab therapy. Monitor renal function at baseline and periodically during treatment. Avelumab therapy may need to be interrupted or discontinued depending on the severity of renal impairment; treatment with systemic corticosteroids may also be necessary.

    Infusion-related reactions

    Severe or life-threatening infusion-related reactions have occurred with avelumab. All patients should receive premedication with an antihistamine and acetaminophen 30 to 60 minutes prior to the first 4 avelumab infusions; premedication may be administered prior to subsequent doses based upon clinical judgment and presence/severity of prior infusion reactions. Monitor patients for signs and symptoms of infusion reactions including fever, chills, flushing, hypotension, dyspnea, wheezing, back pain, abdominal pain, and urticaria. Interrupt or slow the rate of infusion for mild or moderate infusion related reactions (grade 1 or 2); stop the infusion and permanently discontinue avelumab for severe or life-threatening infusion-related reactions (grade 3 or 4).

    Autoimmune disease, organ transplant, systemic lupus erythematosus (SLE)

    Use avelumab with caution in patients who have previously had an organ transplant or who have autoimmune disease such as systemic lupus erythematosus (SLE). Immune-mediated organ transplant rejection has been reported with PD-1/PD-L1 inhibitor therapy.

    Cardiac disease, heart failure, hyperlipidemia, hypertension, myocardial infarction

    Use avelumab in combination with axitinib with caution in patients with a history of cardiac disease; this combination can cause severe and fatal cardiovascular events including myocardial infarction and congestive heart failure. If avelumab and axitinib are used together, optimize the management of cardiovascular risk factors such as hypertension or hyperlipidemia; consider baseline and periodic evaluations of left ventricular ejection fraction; and monitor for signs and symptoms of cardiovascular events. Discontinue avelumab and axitinib for grade 3 or 4 cardiovascular events.

    Allogeneic stem cell transplant

    Fatal and other serious complications including hyperacute, acute, and chronic graft-versus-host-disease, sinusoidal obstruction syndrome (SOS) previously termed veno-occlusive disease (VOD) after reduced intensity conditioning, and a steroid-requiring febrile syndrome (without an identified infectious cause) have been reported in patients who receive an allogeneic stem cell transplant (SCT) before or after being treated with a PD-1/PD-L1 blocking antibody. Therefore, perform a risk/benefit analysis prior to starting treatment with a PD-1/PD-L1 blocking antibody, such as avelumab, in patients who may receive or who have a history of undergoing an allogeneic SCT. Monitor patients closely for evidence of transplant-related complications and intervene promptly. Complications may occur despite intervening therapy between PD-1/PD-L1 blockade and allogeneic SCT.

    Serious rash

    Immune mediated serious rash, including exfoliative dermatitis, Stevens-Johnson Syndrome (SJS), toxic epidermal necrolysis (TEN), and drug reaction with eosinophilia and systemic symptoms (DRESS) has occurred in patients treated with PD-1/PD-L1 inhibitors. Monitor patients for suspected severe skin reactions and exclude other causes. Topical emollients and/or topical corticosteroids may be adequate to treat mild-to-moderate non-exfoliative rashes. Avelumab therapy may need to be interrupted or discontinued depending on the severity of rash; treatment with systemic corticosteroids may also be necessary.

    Guillain-Barre syndrome, myasthenia gravis, neurological disease

    Immune-mediated neurotoxicity has been reported with avelumab or other PD-1/PD-L1 inhibitors. Use avelumab with caution in patients who have a history of neurological disease such as myasthenia gravis or Guillain-Barre syndrome. Avelumab may need to be interrupted or discontinued depending on the severity of the neurotoxicity; treatment with systemic corticosteroids may also be necessary.

    Pregnancy

    Based on its mechanism of action, avelumab may cause fetal harm if used during pregnancy. Avelumab is an immunoglobulin G1 antibody and may cross the placental barrier. Fetal exposure to avelumab may increase the risk of developing immune-mediated disorders or altering the normal immune response. Advise pregnant women of the risk to a fetus. The PD-1 pathway is associated with decidual CD8-positive T-cell function and the PD1/PD-L1 interaction may be important in maintaining fetal tolerance during pregnancy. PD1/PDL1 inhibitors, such as avelumab, may impair maternal immune tolerance resulting in spontaneous abortion, intrauterine growth restriction, or early-onset preeclampsia.    

    Contraception requirements, reproductive risk

    Counsel patients about the reproductive risk and contraception requirements during avelumab therapy. Females of reproductive potential should avoid pregnancy and use effective contraception during and for at least 1 month after the last avelumab dose. Women who become pregnant while receiving avelumab should be apprised of the potential hazard to the fetus. Fertility studies have not been conducted with avelumab; however, weekly administration of avelumab did not result in any notable effects in the male and female reproductive organs of Cynomolgus monkeys.

    Breast-feeding

    Due to the potential for serious adverse reactions in breastfed children, the manufacturer recommends that patients avoid breast-feeding during avelumab therapy and for at least 1 month after the final dose. It is not known if avelumab is present in human milk or if it has effects on the breastfed child or on milk production. Use avelumab with caution during breastfeeding, especially while nursing a newborn or preterm infant. Because avelumab is a large protein molecule (molecular weight of 147,000 Daltons), the amount of drug in milk is likely to be very low. It may also be partially destroyed in the gastrointestinal tract resulting in minimal absorption.

    ADVERSE REACTIONS

    Severe

    lymphopenia / Delayed / 0-19.0
    hepatotoxicity / Delayed / 0-9.0
    anemia / Delayed / 3.0-9.0
    hyperglycemia / Delayed / 0-7.0
    hypertension / Early / 3.0-6.0
    infection / Delayed / 3.0-6.0
    elevated hepatic enzymes / Delayed / 1.0-5.0
    hyperamylasemia / Delayed / 1.0-5.0
    musculoskeletal pain / Early / 1.2-3.2
    dyspnea / Early / 0-3.0
    hyponatremia / Delayed / 0-3.0
    anorexia / Delayed / 0.3-2.0
    rash / Early / 0-1.2
    vomiting / Early / 0-1.2
    hyperbilirubinemia / Delayed / 0-1.0
    constipation / Delayed / 0.6-1.0
    Guillain-Barre syndrome / Delayed / 0-1.0
    myelitis / Delayed / 0-1.0
    arthralgia / Delayed / 0.6-1.0
    myocarditis / Delayed / 0-1.0
    pericarditis / Delayed / 0-1.0
    pancreatitis / Delayed / 0-1.0
    neutropenia / Delayed / 0-1.0
    uveitis / Delayed / 0-1.0
    vasculitis / Delayed / 0-1.0
    aplastic anemia / Delayed / 0-1.0
    hemolytic anemia / Delayed / 0-1.0
    thrombocytopenia / Delayed / 0-1.0
    organ transplant rejection / Delayed / 0-1.0
    infusion-related reactions / Rapid / 0-0.9
    hepatitis / Delayed / 0.7-0.7
    diarrhea / Early / 0-0.6
    pneumonitis / Delayed / 0.5-0.5
    dysphonia / Delayed / 0-0.5
    colitis / Delayed / 0.4-0.4
    peripheral edema / Delayed / 0-0.4
    cough / Delayed / 0-0.3
    hypothyroidism / Delayed / 0-0.3
    fever / Early / 0-0.3
    pruritus / Rapid / 0-0.3
    nausea / Early / 0-0.3
    adrenocortical insufficiency / Delayed / 0.1-0.1
    abdominal pain / Early / 1.4
    renal failure (unspecified) / Delayed / 2.0
    fatigue / Early / 1.7
    ileus / Delayed / Incidence not known
    GI obstruction / Delayed / Incidence not known
    diabetic ketoacidosis / Delayed / Incidence not known
    myocardial infarction / Delayed / Incidence not known
    heart failure / Delayed / Incidence not known
    pericardial effusion / Delayed / Incidence not known
    Stevens-Johnson syndrome / Delayed / Incidence not known
    exfoliative dermatitis / Delayed / Incidence not known
    Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS) / Delayed / Incidence not known
    erythema multiforme / Delayed / Incidence not known
    toxic epidermal necrolysis / Delayed / Incidence not known
    visual impairment / Early / Incidence not known
    retinal detachment / Delayed / Incidence not known
    Vogt-Koyanagi-Harada syndrome / Delayed / Incidence not known
    thromboembolism / Delayed / Incidence not known
    sinusoidal obstruction syndrome (SOS) / Delayed / Incidence not known
    graft-versus-host disease (GVHD) / Delayed / Incidence not known
    veno-occlusive disease (VOD) / Delayed / Incidence not known

    Moderate

    antibody formation / Delayed / 4.1-15.0
    gastritis / Delayed / 0-1.0
    paresis / Delayed / 0-1.0
    hyperthyroidism / Delayed / 0.4-0.4
    diabetes mellitus / Delayed / 0.1-0.1
    dehydration / Delayed / 2.0
    hematuria / Delayed / 1.5
    hypophysitis / Delayed / Incidence not known
    hypopituitarism / Delayed / Incidence not known
    bone pain / Delayed / Incidence not known
    hypercholesterolemia / Delayed / Incidence not known
    hypertriglyceridemia / Delayed / Incidence not known
    hypophosphatemia / Delayed / Incidence not known
    cystitis / Delayed / Incidence not known
    pyuria / Delayed / Incidence not known
    hypotension / Rapid / Incidence not known
    palmar-plantar erythrodysesthesia (hand and foot syndrome) / Delayed / Incidence not known
    erythema / Early / Incidence not known
    bullous rash / Early / Incidence not known
    iritis / Delayed / Incidence not known
    stomatitis / Delayed / Incidence not known

    Mild

    weight loss / Delayed / 0-20.0
    dizziness / Early / 0-14.0
    headache / Early / 0-10.0
    malaise / Early / Incidence not known
    asthenia / Delayed / Incidence not known
    back pain / Delayed / Incidence not known
    myalgia / Early / Incidence not known
    chills / Rapid / Incidence not known
    flushing / Rapid / Incidence not known
    maculopapular rash / Early / Incidence not known
    lichen planus-like eruption / Delayed / Incidence not known
    acneiform rash / Delayed / Incidence not known

    DRUG INTERACTIONS

    Palifermin: (Moderate) Palifermin should not be administered within 24 hours before, during infusion of, or within 24 hours after administration of antineoplastic agents.
    Penicillamine: (Major) Do not use penicillamine with antineoplastic agents due to the increased risk of developing severe hematologic and renal toxicity.
    Tuberculin Purified Protein Derivative, PPD: (Moderate) Immunosuppressives may decrease the immunological response to tuberculin purified protein derivative, PPD. This suppressed reactivity can persist for up to 6 weeks after treatment discontinuation. Consider deferring the skin test until completion of the immunosuppressive therapy.

    PREGNANCY AND LACTATION

    Pregnancy

    Based on its mechanism of action, avelumab may cause fetal harm if used during pregnancy. Avelumab is an immunoglobulin G1 antibody and may cross the placental barrier. Fetal exposure to avelumab may increase the risk of developing immune-mediated disorders or altering the normal immune response. Advise pregnant women of the risk to a fetus. The PD-1 pathway is associated with decidual CD8-positive T-cell function and the PD1/PD-L1 interaction may be important in maintaining fetal tolerance during pregnancy. PD1/PDL1 inhibitors, such as avelumab, may impair maternal immune tolerance resulting in spontaneous abortion, intrauterine growth restriction, or early-onset preeclampsia.    

    Due to the potential for serious adverse reactions in breastfed children, the manufacturer recommends that patients avoid breast-feeding during avelumab therapy and for at least 1 month after the final dose. It is not known if avelumab is present in human milk or if it has effects on the breastfed child or on milk production. Use avelumab with caution during breastfeeding, especially while nursing a newborn or preterm infant. Because avelumab is a large protein molecule (molecular weight of 147,000 Daltons), the amount of drug in milk is likely to be very low. It may also be partially destroyed in the gastrointestinal tract resulting in minimal absorption.

    MECHANISM OF ACTION

    Avelumab is a human IgG1 lambda monoclonal antibody that binds to the programmed death ligand-1 (PD-L1). PD-L1 may be expressed on tumor cells and tumor-infiltrating immune cells and can contribute to inhibition of the anti-tumor immune response in the tumor microenvironment. Binding of PD-L1 to the PD-1 and B7.1 receptors found on T cells and antigen-presenting cells suppresses cytotoxic T-cell activity, T-cell proliferation, and cytokine production. Avelumab binds PD-L1 and blocks the interaction of PD-L1 with PD-1 and B7.1 receptors. Blocking the PD-1/PD-L1 pathway improves the anti-tumor immune response by reducing immunosuppressive signals between immune cells and tumor cells. Additionally, avelumab induced antibody-dependent cell-mediated cytotoxicity (ADCC) in vitro. In mice models, inhibiting PD-1 activity deceased tumor growth.

    PHARMACOKINETICS

    Avelumab is administered intravenously. In a population pharmacokinetic analysis in patients with solid tumors who received avelumab 10 mg/kg IV, the total systemic clearance was 0.59 L/day and the terminal half-life was 6.1 days. Clearance decreased from baseline by 32.1% (coefficient of variation, 36.2%) over time in a subpopulation of patients with Merkel cell carcinoma, which is not considered clinically important; there was no evidence to suggest a change of avelumab clearance over time in patients with urothelial or renal cell carcinoma. The geometric mean steady-state volume of distribution (Vd) was 4.72 L. Avelumab is eliminated primarily by proteolytic degradation.

    Intravenous Route

    In a population pharmacokinetic analysis (n = 1,629), steady-state avelumab concentrations were reached at approximately 4 to 6 weeks following an every 2-week dosing regimen; the systemic accumulation was approximately 1.25-fold after 4 to 6 weeks. Avelumab exposure increased proportionally in the dose range of 10 to 20 mg/kg IV every 2 weeks. Based on exposure efficacy and exposure safety relationships, there are no expected clinically meaningful differences in the safety, efficacy, or exposure of avelumab administered every 2 weeks at a dose of either 800 mg or 10 mg/kg.[61826]