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Golimumab

Class: Disease-modifying Antirheumatic Drugs
VA Class: MS190
Chemical Name: Disulfide with human monoclonal CNTO 148 k-chain anti-(human tumor necrosis factor a) (human monoclonal CNTO 148 g1-chain) immunoglobulin G1 dimer.
Molecular Formula: C6530H10068N1752O2026S44
CAS Number: 476187-74-5
Brands: Simponi

Warning(s)

  • Serious Infections
  • Increased risk of serious infections involving various organ systems and sites that may require hospitalization or result in death; tuberculosis (frequently disseminated or extrapulmonary), invasive fungal infections (may be disseminated), bacterial (e.g., legionellosis, listeriosis) and viral infections, and other opportunistic infections reported.1 9 19 24 (See Infectious Complications under Cautions.)

  • Carefully consider risks and benefits prior to initiating golimumab therapy in patients with chronic or recurring infections.1 19 24

  • Evaluate patients for latent tuberculosis infection prior to and periodically during golimumab therapy; if indicated, initiate appropriate antimycobacterial regimen prior to initiating golimumab therapy.1 19 24

  • Closely monitor patients for infection, including active tuberculosis in those with a negative tuberculin skin test, during and after treatment.1 9 19 24 Discontinue golimumab if serious infection occurs.1 9 24 Consider empiric antifungal therapy if serious systemic illness occurs in a patient at risk for invasive fungal infections.1 9 19 24

  • Malignancy
  • Lymphoma and other malignancies (some fatal) reported in children and adolescents receiving TNF blocking agents.1 8 20 24 (See Malignancies and Lymphoproliferative Disorders under Cautions.)

Introduction

Biologic response modifier and disease-modifying antirheumatic drug (DMARD); a human immunoglobulin G1 kappa (IgG1) monoclonal antibody specific for human tumor necrosis factor (TNF; TNF-α).1 2 3 4 5 6 13 14 15 24

Uses for Golimumab

Rheumatoid Arthritis in Adults

Used in conjunction with methotrexate for the management of moderately to severely active rheumatoid arthritis in adults.1 2 3 4 17 24 27 28 29 37 38 39 40 41 42

Psoriatic Arthritis

Used alone or in conjunction with methotrexate for the management of active psoriatic arthritis in adults.1 5 34 35 36

Ankylosing Spondylitis

Used for the management of ankylosing spondylitis in adults with active disease.1 6 32 33

Ulcerative Colitis

Used in adults with moderately to severely active ulcerative colitis who require continuous corticosteroid therapy or who had inadequate response to or were intolerant to conventional therapies (oral aminosalicylates, oral corticosteroids, azathioprine, or mercaptopurine) to induce and maintain clinical response, to improve endoscopic appearance of the mucosa during induction therapy, to induce clinical remission, and to achieve and sustain clinical remission in those who responded to induction therapy.1 26 30

Golimumab Dosage and Administration

General

Concomitant Therapy

  • Used in conjunction with methotrexate for the management of moderately to severely active rheumatoid arthritis in adults;1 24 may be used with or without methotrexate for management of psoriatic arthritis or ankylosing spondylitis in adults.1

  • Corticosteroids, other nonbiologic DMARDs, and NSAIAs or analgesics may be continued in adults receiving golimumab for the management of rheumatoid arthritis, psoriatic arthritis, or ankylosing spondylitis.1 24 43

  • Aminosalicylates, corticosteroids, azathioprine, mercaptopurine, and/or methotrexate could be continued during pivotal trials of golimumab in patients with ulcerative colitis.1 26 30 Carefully consider possibility of an increased risk of hepatosplenic T-cell lymphoma with combination immunosuppressive therapy.1 (See Malignancies and Lymphoproliferative Disorders under Cautions.)

Administration

Administer by sub-Q injection.1 Also may administer by IV infusion in the management of rheumatoid arthritis in adults.24 Efficacy and safety of switching between IV and sub-Q formulations and routes of administration not established.24

Sub-Q Administration

Administer by sub-Q injection into the thigh, lower abdomen, or upper arm; do not make abdominal injections within 2 inches of the umbilicus.1 Use thigh (the preferred site) or abdomen for self-administration; may use upper arm if not self-administered.1 Rotate injection sites.1 Do not make injections into areas where the skin is tender, bruised, red, or hard or into scars or stretch marks.1

Allow golimumab prefilled syringe or auto-injector to sit at room temperature outside of the carton for 30 minutes prior to injection; do not warm the drug in any other way (e.g., microwave, hot water).1 Do not remove the syringe needle cover or auto-injector cap while the drug is warming to room temperature.1

Intended for use under the guidance and supervision of a clinician, but may be self-administered if the clinician determines that the patient and/or their caregiver is competent to safely administer the drug after appropriate training.1

IV Administration

For solution compatibility information, see Compatibility under Stability.

Administer by IV infusion.24

Golimumab injection concentrate must be diluted prior to IV administration.24

Do not infuse golimumab simultaneously through the same IV line with other drugs.24

Use an inline, nonpyrogenic, low-protein-binding filter with pore size ≤0.22 µm.24

Dilution

Dilute the required volume of golimumab injection concentrate in 0.45 or 0.9% sodium chloride injection to provide a total volume of 100 mL (i.e., remove a volume of diluent equal to the total required volume of the injection concentrate from a 100-mL bag or bottle of 0.45 or 0.9% sodium chloride injection prior to adding the injection concentrate).24 Slowly add golimumab injection concentrate to the infusion container and mix gently.24

Do not use the injection concentrate if it is discolored (should appear colorless to light yellow) or contains particulates other than a few fine translucent particles.24

Discard any unused portion remaining in the vial since the injection concentrate contains no preservative.24

Rate of Administration

Administer by IV infusion over 30 minutes.24

Dosage

Adults

Rheumatoid Arthritis
Sub-Q

50 mg once monthly.1

IV

2 mg/kg at weeks 0 and 4, then every 8 weeks thereafter.24

Psoriatic Arthritis
Sub-Q

50 mg once monthly.1

Ankylosing Spondylitis
Sub-Q

50 mg once monthly.1

Ulcerative Colitis
Sub-Q

200 mg at week 0 and 100 mg at week 2 (induction regimen), then 100 mg every 4 weeks thereafter (maintenance regimen).1

Special Populations

Dosage adjustment of sub-Q golimumab based on weight or gender not necessary.1 15 (See Elimination: Special Populations, under Pharmacokinetics.)

Hepatic Impairment

Manufacturer makes no specific dosage recommendations.1 15 24 (See Elimination: Special Populations, under Pharmacokinetics.)

Renal Impairment

Manufacturer makes no specific dosage recommendations.1 15 24 (See Elimination: Special Populations, under Pharmacokinetics.)

Geriatric Patients

Manufacturer makes no specific dosage recommendations.1 15 24 (See Elimination: Special Populations, under Pharmacokinetics.)

Cautions for Golimumab

Contraindications

  • Manufacturer states none known.1 24

Warnings/Precautions

Warnings

Infectious Complications

Increased risk of serious infections involving various organ systems and sites that may require hospitalization or result in death.1 19 24 Opportunistic infections caused by bacterial, mycobacterial, invasive fungal, viral, or parasitic organisms (e.g., aspergillosis, blastomycosis, candidiasis, coccidioidomycosis, histoplasmosis, legionellosis, listeriosis, pneumocystosis, tuberculosis) reported, particularly in patients receiving concomitant therapy with immunosuppressive agents (e.g., methotrexate, corticosteroids).1 9 19 24 Infections frequently are disseminated.1 24 (See Boxed Warning.)

Increased incidence of serious infections observed with concomitant use of a TNF blocking agent and anakinra or abatacept.1 10 11 24 (See Specific Drugs under Interactions.)

Patients >65 years of age, with comorbid conditions, and/or receiving concomitant therapy with immunosuppressive agents (e.g., corticosteroids, methotrexate) may be at increased risk of infection.1 19 24

Do not initiate golimumab in patients with active infections, including clinically important localized infections.1 24 Consider potential risks and benefits of the drug prior to initiating therapy in patients with a history of chronic, recurring, or opportunistic infections; patients with underlying conditions that may predispose them to infections; and patients who have been exposed to tuberculosis or who have resided or traveled in regions where tuberculosis or mycoses such as histoplasmosis, coccidioidomycosis, and blastomycosis are endemic.1 19 24

Closely monitor patients during and after golimumab therapy for signs or symptoms of infection (e.g., fever, malaise, weight loss, sweats, cough, dyspnea, pulmonary infiltrates, serious systemic illness including shock).1 9 19 24

If new infection occurs during therapy, perform thorough diagnostic evaluation (appropriate for immunocompromised patient), initiate appropriate anti-infective therapy, and closely monitor patient.1 9 24 Discontinue golimumab if serious infection, opportunistic infection, or sepsis develops.1 9 24

Evaluate all patients for active or latent tuberculosis and for risk factors for tuberculosis prior to and periodically during therapy.1 19 24 When indicated, initiate appropriate antimycobacterial regimen for treatment of latent tuberculosis infection prior to golimumab therapy.1 24 Also consider antimycobacterial therapy prior to golimumab therapy for individuals with a history of latent or active tuberculosis in whom an adequate course of antimycobacterial treatment cannot be confirmed and for individuals with a negative tuberculin skin test who have risk factors for tuberculosis.1 24 Consultation with a tuberculosis specialist is recommended when deciding whether to initiate antimycobacterial therapy.1 24

Monitor all patients, including those with negative tuberculin skin tests, those receiving treatment for latent tuberculosis, and those previously treated for tuberculosis infection, for active tuberculosis.1 24 Consider tuberculosis in patients who develop new infections while receiving golimumab, especially if they previously have traveled to countries where tuberculosis is highly prevalent or have been in close contact with an individual with active tuberculosis.1 24

Failure to recognize invasive fungal infections has led to delays in appropriate treatment.9 Consider empiric antifungal therapy in patients at risk for invasive fungal infections who develop severe systemic illness; consider the risk for severe fungal infection as well as risks associated with antifungal therapy.1 9 19 24 Whenever feasible, consult specialist in fungal infections when making decisions regarding initiation and duration of antifungal therapy.1 9 24

When deciding whether to reinitiate TNF blocking agent therapy following resolution of an invasive fungal infection, reevaluate risks and benefits, particularly in patients who reside in regions where mycoses are endemic.9 Whenever feasible, consult specialist in fungal infections.1 9 24

Malignancies and Lymphoproliferative Disorders

Lymphoma and other malignancies (some fatal) reported during postmarketing surveillance in children and adolescents receiving TNF blocking agents, particularly in those receiving other immunosuppressive agents (e.g., azathioprine, methotrexate) concomitantly.1 8 24 Malignancies included lymphomas (about 50% of the cases) (e.g., Hodgkin’s disease, non-Hodgkin’s lymphoma) and various other malignancies (e.g., leukemia, melanoma, solid organ cancers), including rare malignancies usually associated with immunosuppression and malignancies not usually observed in children and adolescents (e.g., leiomyosarcoma, hepatic malignancies, renal cell carcinoma).1 8 24 Median time to occurrence was 30 months (range: 1–84 months) after the initial TNF blocking agent dose.1 24 FDA has concluded that there is an increased risk of malignancy with TNF blocking agents in children and adolescents; however, the strength of the association is not fully characterized.8

Hepatosplenic T-cell lymphoma (a rare, aggressive, usually fatal T-cell lymphoma) reported mainly in adolescent and young adult males with Crohn’s disease or ulcerative colitis receiving TNF blocking agents and/or thiopurine analogs (mercaptopurine or azathioprine).1 20 24 Most of the patients received a combination of immunosuppressive agents, including TNF blocking agents and thiopurine analogs, at or before diagnosis.1 20 24

In controlled studies, lymphoma was reported more frequently in patients receiving golimumab or other TNF blocking agents than in control patients.1 24 Patients with rheumatoid arthritis, Crohn’s disease, ankylosing spondylitis, psoriatic arthritis, and other chronic inflammatory diseases, especially those with highly active disease and/or chronic exposure to immunosuppressive therapies, may be at increased risk of lymphoma;1 20 24 may be difficult to measure added risk of TNF blocking agents, azathioprine, and/or mercaptopurine.20

Acute and chronic leukemias (some fatal) reported in adults and pediatric patients receiving TNF blocking agents, including golimumab, particularly in those receiving other immunosuppressive agents concomitantly.1 8 24 Leukemia (most commonly acute myeloid leukemia, chronic lymphocytic leukemia, and chronic myeloid leukemia) generally occurred during first 2 years of therapy.8 FDA has concluded that there is a possible association between TNF blocking agents and development of leukemia; interpretation of findings is complicated because patients with rheumatoid arthritis may be at increased risk for leukemia independent of any treatment with TNF blocking agents.1 8 24

Melanoma and Merkel cell carcinoma reported in patients receiving golimumab or other TNF blocking agents.1 24 Periodic skin examination recommended for all patients, especially those with risk factors for skin cancer.1 24

In controlled studies of other TNF blocking agents in patients at increased risk for malignancies (e.g., patients with COPD, patients with Wegener’s granulomatosis receiving concomitant cyclophosphamide), a greater proportion of malignancies occurred in patients receiving the TNF blocking agent compared with control patients.1 24

Malignancies also reported in a limited number of patients with uncontrolled, severe persistent asthma who received golimumab; not reported in control patients.1 16 24

Consider possibility of and monitor for occurrence of malignancies during and following treatment with TNF blocking agents.8 20

Consider risks and benefits of TNF blocking agents, including golimumab, before initiating therapy in patients with a known malignancy (other than successfully treated nonmelanoma skin cancer) or when considering whether to continue therapy in patients who develop a malignancy.1 24 Carefully consider risks and benefits of these agents, especially in adolescents and young adults and especially in the treatment of Crohn’s disease or ulcerative colitis.20

Not known whether golimumab influences risk of developing dysplasia or colon cancer.1 Screen all patients with ulcerative colitis who have a history of dysplasia or colon carcinoma, or are at increased risk for these conditions (e.g, those with long-standing ulcerative colitis or primary sclerosing cholangitis), for dysplasia at regular intervals in accordance with current standard of care.1 Carefully consider risks and benefits of continued therapy in those with newly diagnosed dysplasia.1

Other Warnings/Precautions

HBV Reactivation

Increased risk of reactivation of HBV infection in patients who are chronic carriers of this virus (i.e., hepatitis B surface antigen-positive [HBsAg-positive]).1 24 Death reported in a few individuals.1 24 Use of multiple immunosuppressive agents may contribute to HBV reactivation.1 24

Screen all patients for HBV infection prior to initiation of therapy.1 24 Consultation with an HBV infection specialist is recommended prior to initiation of therapy in patients who test positive for HBsAg.1 24

Evaluate and monitor HBV carriers before, during, and for up to several months after therapy.1 24 Safety and efficacy of antiviral therapy for prevention of HBV reactivation not established.1 24 Discontinue golimumab and initiate appropriate treatment (e.g., antiviral therapy) if HBV reactivation occurs.1 24 Not known whether golimumab can be readministered once control of a reactivated HBV infection is achieved; caution advised in this situation.1 24

Cardiovascular Effects

New-onset or worsening CHF, sometimes fatal, reported in patients receiving TNF blocking agents, including golimumab; golimumab not studied in patients with history of CHF.1 24 If used in patients with CHF, caution and careful monitoring recommended.1 24 Discontinue therapy if new or worsening symptoms of heart failure occur.1 24

Nervous System Effects

New onset or exacerbation of central or peripheral nervous system demyelinating disorders (e.g., multiple sclerosis, Guillain-Barré syndrome) reported rarely in patients receiving TNF blocking agents.1 24 Central demyelination, multiple sclerosis, optic neuritis, and peripheral demyelinating polyneuropathy reported rarely with golimumab.1 24

Exercise caution when considering golimumab therapy in patients with central or peripheral nervous system demyelinating disorders.1 24 Consider discontinuing golimumab if these disorders develop.1 24

Hematologic Effects

Pancytopenia, leukopenia, neutropenia, aplastic anemia, and thrombocytopenia reported in patients receiving golimumab or other TNF blocking agents.1 24 Use with caution in patients who have or have had substantial cytopenias.1 24

Immunization and Use of Therapeutic Infectious Agents

Patients may receive inactivated vaccines.1 24 Avoid live vaccines and therapeutic infectious agents.1 24 (See Vaccines and Therapeutic Infectious Agents under Interactions.)

Infants exposed to golimumab in utero should not receive live vaccines for 6 months following the last golimumab dose given to the infant’s mother during pregnancy.1 24 (See Pregnancy under Cautions.)

Immunologic Reactions and Antibody Formation

Formation of autoimmune antibodies and, rarely, development of a lupus-like syndrome reported with TNF blocking agents, including golimumab; discontinue golimumab if symptoms suggestive of a lupus-like syndrome develop.1 24 Antibodies to double-stranded DNA (anti-dsDNA) also reported.1 24

Antibodies to golimumab may develop.1 24 However, the relationship between antibodies to the drug and efficacy or safety is not fully elucidated.1 24

Psoriasis

New-onset psoriasis, including pustular and palmoplantar psoriasis, and exacerbation of existing psoriasis reported with TNF blocking agents, including golimumab.1 8 Most patients experienced improvement following discontinuance of the TNF blocking agent.8

Consider possibility of and monitor for manifestations (e.g., new rash) of new or worsening psoriasis, particularly pustular and palmoplantar psoriasis.8 May consider discontinuance of golimumab if new-onset or worsening psoriasis occurs.1

Hepatic Effects

Severe hepatic reactions, including acute liver failure, reported in patients receiving TNF blocking agents.1 24

Increased serum ALT and AST concentrations reported in patients receiving golimumab.1 24 Relationship between golimumab and increased liver enzyme concentrations not clear because many patients received concomitant therapy with drugs that increase liver enzyme concentrations (e.g., methotrexate, NSAIAs).1 24

Sensitivity Reactions

Serious systemic hypersensitivity reactions (e.g., anaphylactic reactions) reported in patients receiving golimumab, sometimes after the first dose.1 24 Immediately discontinue golimumab and initiate appropriate therapy if an anaphylactic or other serious allergic reaction occurs.1 24

The needle cover of the prefilled syringe and the syringe in the auto-injector contain dry natural rubber and should not be handled by individuals sensitive to latex.1

Specific Populations

Pregnancy

Category B.1 24

Infants born to women who received golimumab during their pregnancy may be at increased risk of infection for up to 6 months.1 24 Infants exposed to golimumab in utero should not receive live vaccines for 6 months following the last golimumab dose given to the infant’s mother during pregnancy.1 24 (See Vaccines and Therapeutic Infectious Agents under Interactions.)

Lactation

Distributed into milk in cynomolgus monkeys.1 24 Not known whether golimumab is distributed into human milk or absorbed systemically following ingestion.1 24 Discontinue nursing or drug.1 24

Pediatric Use

Safety and efficacy not established in children <18 years of age.1 24

Malignancies, some fatal, reported in children and adolescents who received TNF blocking agents.1 8 24 (See Malignancies and Lymphoproliferative Disorders under Cautions.)

Geriatric Use

In studies of sub-Q golimumab in patients with rheumatoid arthritis, psoriatic arthritis, or ankylosing spondylitis, no overall differences in serious adverse events, serious infections, and adverse events in those ≥65 years of age compared with younger adults.1

In studies of sub-Q golimumab in patients with ulcerative colitis or IV golimumab in those with rheumatoid arthritis, insufficient numbers of patients ≥65 years of age to determine whether they respond differently than younger adults.1 24 (See Elimination: Special Populations, under Pharmacokinetics.)

Overall incidence of infection is higher in the geriatric population than in younger adults; use with caution.1 24

Common Adverse Effects

Sub-Q golimumab: Upper respiratory infection (nasopharyngitis, pharyngitis, laryngitis, rhinitis),1 injection site reactions (injection site erythema, urticaria, induration, pain, bruising, pruritus, irritation, paresthesia),1 viral infections (e.g., herpes, influenza),1 increased AST/ALT concentrations,1 hypertension.1

IV golimumab: Upper respiratory infection (e.g., nasopharyngitis, pharyngitis, laryngitis, rhinitis),24 27 28 29 viral infections (e.g., influenza, herpes),24 27 bronchitis,24 28 29 hypertension,24 27 28 29 rash.24

Interactions for Golimumab

Administered concomitantly with methotrexate, hydroxychloroquine, sulfasalazine, corticosteroids, and/or NSAIAs/analgesics in clinical studies.1 24

Drugs Metabolized by Hepatic Microsomal Enzymes

Because increased levels of TNF-α during chronic inflammation may suppress formation of CYP isoenzymes, antagonism of TNF-α activity by golimumab may normalize formation of CYP enzymes.1 15 24

Drugs metabolized by CYP isoenzymes that have a low therapeutic index: Monitor therapeutic effect and serum concentrations following initiation or discontinuance of golimumab; adjust dosage as needed.1 15 24

Biologic Antirheumatic Agents

Possible increased risk of infection.1 24 Concomitant use with other biologic agents used in the management of rheumatoid arthritis, psoriatic arthritis, or ankylosing spondylitis is not recommended.1 24

Use caution when switching from one biologic DMARD to another, since overlapping biologic activity may further increase the risk of infection.1 24

Vaccines and Therapeutic Infectious Agents

Inactivated vaccines: May be administered concomitantly.1 24

Live vaccines: Avoid concomitant use.1 15 24 Risk of infections, including disseminated infections.1 24 Limited data regarding response to live vaccines or secondary transmission of infection by live vaccines in golimumab-treated patients.1 24 Infants exposed to golimumab in utero should not receive live vaccines for 6 months following the last golimumab dose given to the infant’s mother during pregnancy.1 24 (See Pregnancy under Cautions.)

Therapeutic infectious agents: Avoid concomitant use.1 24 Risk of infections, including disseminated infections.1 24

Specific Drugs

Drug

Interaction

Comments

Abatacept

Increased incidence of infection and serious infection, without additional clinical benefit, reported with abatacept and TNF blocking agents in rheumatoid arthritis1 11 24

Concomitant use not recommended1 11 15 24

Use caution when switching from one biologic DMARD to another, since overlapping biologic activity may further increase risk of infection1 24

Anakinra

Increased incidence of serious infections and neutropenia, without additional clinical benefit, reported with anakinra and etanercept (another TNF blocking agent) in rheumatoid arthritis1 10 24

Concomitant use not recommended1 15 24

Use caution when switching from one biologic DMARD to another, since overlapping biologic activity may further increase risk of infection1 24

BCG for intravesical instillation

Risk of infections, including disseminated infections1 24

Avoid concomitant use1 24

Corticosteroids, oral

Concomitant use does not appear to alter golimumab clearance1 24

Cyclosporine

Possible effect on cyclosporine metabolism; because increased levels of TNF-α during chronic inflammation may suppress formation of CYP isoenzymes, antagonism of TNF-α activity by golimumab may normalize formation of CYP enzymes1 15 24

Monitor therapeutic effect and serum concentrations of cyclosporine following initiation or discontinuance of golimumab; adjust dosage as needed1 15 24

Methotrexate

Concomitant use or nonuse of methotrexate does not appear to influence efficacy or safety of sub-Q golimumab for management of psoriatic arthritis or ankylosing spondylitis1

Decreased incidence of antibodies to golimumab reported with concomitant use1 24

Increased mean steady-state trough concentrations of sub-Q golimumab and decreased clearance of IV golimumab reported with concomitant use1 24

Use golimumab in conjunction with methotrexate for management of rheumatoid arthritis1 24

Golimumab may be used with or without methotrexate for management of psoriatic arthritis or ankylosing spondylitis1

NSAIAs

Concomitant use does not appear to alter golimumab clearance1 24

Pneumococcal polysaccharide vaccine

Study data suggest that golimumab does not suppress the humoral immune response to pneumococcal vaccine1

Rituximab

Increased risk of serious infection reported in patients who received rituximab and subsequently received a TNF blocking agent1 24

Concomitant use not recommended1 24

Use caution when switching from one biologic DMARD to another, since overlapping biologic activity may further increase risk of infection1 24

Sulfasalazine

Concomitant use does not appear to alter golimumab clearance1 24

Theophylline

Possible effect on theophylline metabolism; because increased levels of TNF-α during chronic inflammation may suppress formation of CYP isoenzymes, antagonism of TNF-α activity by golimumab may normalize formation of CYP enzymes1 15 24

Monitor therapeutic effect and serum concentrations of theophylline following initiation or discontinuance of golimumab; adjust dosage as needed1 15 24

Warfarin

Possible effect on warfarin metabolism; because increased levels of TNF-α during chronic inflammation may suppress formation of CYP isoenzymes, antagonism of TNF-α activity by golimumab may normalize formation of CYP enzymes1 15 24

Monitor therapeutic effect of warfarin following initiation or discontinuance of golimumab; adjust dosage as needed1 15 24

Golimumab Pharmacokinetics

Absorption

Bioavailability

Absolute bioavailability is approximately 53% following sub-Q administration.1

Peak serum concentrations achieved in a median of 2–6 days following sub-Q administration.1

Steady-state concentrations achieved within 12 weeks following sub-Q administration of golimumab 50 mg once monthly in patients with rheumatoid arthritis, psoriatic arthritis, or ankylosing spondylitis; within 12 weeks following IV administration of golimumab 2 mg/kg at weeks 0 and 4 and every 8 weeks thereafter in patients with rheumatoid arthritis; or within 8 weeks after first maintenance dose in patients with ulcerative colitis receiving sub-Q administration of golimumab 200 mg at week 0 and 100 mg at week 2 (induction) and every 4 weeks thereafter (maintenance).1 18 24

Patients who developed antibodies to golimumab generally had lower steady-state trough serum concentrations of golimumab.1 24

Special Populations

Following weight-based IV dosing, patients with higher body weight tended to have higher serum golimumab concentrations; however, population pharmacokinetic analysis indicated no clinically important differences in exposure to 2-mg/kg IV dose in patients across various body weights.24

Distribution

Extent

Distributed mainly into the circulatory system with limited extravascular distribution.1 24

Distributed into milk in cynomolgus monkeys; not known whether golimumab is distributed into human milk.1 24

Elimination

Elimination Route

Elimination pathways not characterized.1 24

Half-life

Approximately 2 weeks in healthy individuals and patients with active rheumatoid arthritis, psoriatic arthritis, or ankylosing spondylitis.1 24

Special Populations

Pharmacokinetics not formally studied in renal or hepatic impairment.1 24

Among adults, age does not appear to influence pharmacokinetics of sub-Q golimumab.1 Clearance appears to be similar in patients ≥65 years of age and younger adults.1 (See Geriatric Use under Cautions.)

With increasing body weight, there is a trend toward higher clearance of sub-Q golimumab; however, no clinically important weight-related differences in efficacy observed in psoriatic arthritis, ankylosing spondylitis, or ulcerative colitis populations.1 18 Reduction in clinical efficacy with increasing body weight observed with both 50- and 100-mg sub-Q doses in 1 study in rheumatoid arthritis.1 (See Special Populations under Dosage and Administration and see Absorption: Special Populations, under Pharmacokinetics.)

No gender-related pharmacokinetic differences with sub-Q golimumab apparent in patients with rheumatoid arthritis, psoriatic arthritis, or ulcerative colitis; in patients with ankylosing spondylitis, apparent clearance was approximately 13% higher in females than in males.1 However, both genders achieved clinically important responses at the recommended sub-Q dose.1 (See Special Populations under Dosage and Administration.)

Ethnicity-related pharmacokinetic differences between Caucasian and Asian patients not observed with sub-Q golimumab; limited number of patients of other races available to assess for pharmacokinetic differences.1

Stability

Storage

Parenteral

Injection

2–8°C.1 Protect from light; store in original carton until administration.1 Do not freeze or shake.1 Discard unused portions.1

Concentrate for IV Infusion

2–8°C.24 Protect from light; store in original carton until administration.24 Do not freeze or shake.24 Discard unused portions.24

Diluted solution: Store up to 4 hours at room temperature.24

Compatibility

For information on systemic interactions resulting from concomitant use, see Interactions.

Parenteral

Solution Compatibility24

Compatible

Sodium chloride 0.45 or 0.9%

Actions

  • Potent antagonist of TNF biologic activity.1 2 3 4 5 6 14 15 18 24

  • Has high specificity and affinity for soluble and transmembrane TNF (TNF-α); does not bind to or neutralize human lymphotoxin.1 3 4 5 6 14 15 18 24 Prevents the binding of TNF to its receptors, thereby blocking the biologic activity of TNF.1 15 18 24

  • TNF-α is an important mediator of articular inflammation in rheumatoid arthritis, psoriatic arthritis, and ankylosing spondylitis.1 24 Exact mechanism of action of golimumab in the treatment of ulcerative colitis is unknown.1

  • Does not appear to bind to other TNF superfamily ligands.1 24

  • Does not lyse human monocytes expressing transmembrane TNF in the presence of complement or effector cells.1 24

  • An IgG1 kappa monoclonal antibody created using genetically engineered mice immunized with human TNF, resulting in an antibody with human-derived antibody variable and constant regions.1 24

  • Produced by a recombinant cell line cultured by continuous perfusion; purified by a process that includes specific viral inactivation and removal steps.1 24

Advice to Patients

  • A copy of the manufacturer’s patient information (medication guide) for golimumab should be provided to all patients with each prescription of the drug.1 8 24 Importance of advising patients about potential benefits and risks of golimumab.1 8 19 20 24 Importance of patients reading the medication guide prior to initiation of therapy and each time the prescription is refilled.1 19 20 24

  • Importance of instructing patient and/or caregiver regarding proper dosage and administration of golimumab, including the use of aseptic technique, and proper disposal of needles and syringes if it is determined that the patient and/or caregiver is competent to safely administer the drug.1

  • Increased susceptibility to infection.1 24 Importance of promptly informing clinicians if any signs or symptoms of infection (e.g., persistent fever, sweating, cough, dyspnea, fatigue, diarrhea, burning upon urination, warm, red, or painful skin) develop.1 9 24

  • Risk of lymphoma, including hepatosplenic T-cell lymphoma, leukemia, and other malignancies with use of TNF blocking agents.1 8 20 24 Importance of informing patients and caregivers about the increased risk of cancer development in children, adolescents, and young adults, taking into account the clinical utility of TNF blocking agents, the relative risks and benefits of these and other immunosuppressive drugs, and the risks associated with untreated disease.8 20 Importance of promptly informing clinicians if signs and symptoms of malignancies (e.g., unexplained weight loss; fatigue; abdominal pain; persistent fever; night sweats; swollen lymph nodes in the neck, underarm, or groin; easy bruising or bleeding; hepatomegaly or splenomegaly; changes in skin appearance or skin growths) occur.1 8 20 24

  • Importance of alerting clinician if allergy to latex exists.1

  • Importance of informing clinician of any new or worsening medical conditions (e.g., heart failure, neurologic disease [e.g., demyelinating disorders], autoimmune disorders [e.g., lupus-like syndrome], liver disease, cytopenias, psoriasis).1 18 24

  • Importance of taking the drug as prescribed and of not altering or discontinuing therapy without first consulting with a clinician.8 20

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses or any history of cancer, tuberculosis, HBV infection, or other chronic or recurring infections.1 19 24

  • Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.1 24

  • Importance of informing patients of other important precautionary information.1 24 (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

Golimumab

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Parenteral

Injection, for subcutaneous use

50 mg/0.5 mL

Simponi (available as disposable prefilled syringes and prefilled auto-injectors [SmartJect])

Janssen Biotech

100 mg/mL

Simponi (available as disposable prefilled syringes and prefilled auto-injectors [SmartJect])

Janssen Biotech

Concentrate, for Injection, for IV use

12.5 mg/mL (50 mg)

Simponi Aria

Janssen Biotech

AHFS DI Essentials. © Copyright 2017, Selected Revisions June 19, 2017. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

† Use is not currently included in the labeling approved by the US Food and Drug Administration.

References

1. Janssen Biotech Inc. Simponi (golimumab) injection prescribing information. Horsham, PA; 201-6 Jan.

2. Smolen JS, Kay J, Doyle MK et al. Golimumab in patients with active rheumatoid arthritis after treatment with tumour necrosis factor alpha inhibitors (GO-AFTER study): a multicentre, randomised, double-blind, placebo-controlled, phase III trial. Lancet. 2009; 374:210-21. [PubMed 19560810]

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