SIMPONI

Clinical safety rating: caution

Comprehensive clinical and safety monograph for SIMPONI (SIMPONI).

How it works

Golimumab is a human monoclonal antibody that binds to and neutralizes tumor necrosis factor alpha (TNF-α), inhibiting its interaction with TNF receptors and thereby reducing inflammatory responses.

What the body does with it

Metabolism	Metabolism is not typical for monoclonal antibodies; it is degraded into small peptides and amino acids via general protein catabolism. No CYP450 involvement.
Excretion	Primarily degraded into small peptides and amino acids via reticuloendothelial system; no significant renal or biliary elimination. Less than 0.1% excreted unchanged in urine.
Half-life	Terminal elimination half-life approximately 12-14 days (mean 12.3 days in rheumatoid arthritis patients). Supports subcutaneous dosing every 2 weeks.
Protein binding	Binding to serum proteins is not specified; as a monoclonal antibody, minimal non-specific binding; primarily distributed in plasma and interstitial fluid.
Volume of Distribution	Volume of distribution is approximately 100-130 mL/kg (0.1-0.13 L/kg), indicating distribution largely confined to the vascular and interstitial spaces.
Bioavailability	Subcutaneous: Absolute bioavailability is approximately 51% (range 39-72%) after a single SC injection.
Onset of Action	Subcutaneous: Clinical improvement may be observed as early as 2-4 weeks after initiation; maximal effect may take up to 12-16 weeks.
Duration of Action	Duration of therapeutic effect is maintained with every 2-week dosing. Steady-state concentrations achieved by 12 weeks. After stopping, drug concentrations decline gradually over 2-3 months.

Classification & Brands

Dosing & administration

Simponi (golimumab) is administered subcutaneously. For adult rheumatoid arthritis, psoriatic arthritis, and ankylosing spondylitis: 50 mg once monthly. For ulcerative colitis: 200 mg subcutaneously at week 0, then 100 mg at week 2, then 100 mg every 4 weeks.

Dosage form	INJECTABLE
Renal impairment	No specific dose adjustment is recommended for renal impairment. Simponi has not been studied in patients with severe renal impairment; use with caution.
Liver impairment	No specific dose adjustment is recommended for hepatic impairment. Simponi has not been studied in patients with severe hepatic impairment (Child-Pugh C); use with caution.
Pediatric use	Simponi is not approved for pediatric use; safety and efficacy have not been established in patients under 18 years of age.
Geriatric use	No specific dose adjustment is required in elderly patients. However, due to a higher incidence of infections in the elderly, caution is advised. The pharmacokinetics of golimumab are not significantly affected by age.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for SIMPONI (SIMPONI).

Breastfeeding	Unknown if excreted in human milk; endogenous IgG is present in breast milk. M/P ratio not established. Weigh benefits of breastfeeding against potential for drug transfer causing immunosuppression in infant.
Teratogenic Risk	Pregnancy Category B. No evidence of teratogenicity in animal studies. Limited human data; monoclonal antibodies cross placenta minimally in first trimester and increasingly in second and third trimesters. Theoretical risk of immune suppression in neonate if exposed in utero during third trimester.

Warnings & precautions

■ FDA Black Box Warning

Increased risk of serious infections leading to hospitalization or death, including tuberculosis, bacterial sepsis, invasive fungal infections, and opportunistic infections. Malignancy, including lymphoma, has been reported in children and adolescents treated with TNF blockers.

Side Effect Profile

Serious Effects

Absolute Contraindications

["Known hypersensitivity to golimumab or any product component","Active serious infections","Concurrent use with other TNF blockers or abatacept or anakinra (due to increased infection risk)"]

Clinical Precautions

Precautions

["Serious infections (including TB, invasive fungal, and other opportunistic infections)","Hepatitis B reactivation","Malignancies (including lymphoma and leukemia)","Demyelinating disorders","Heart failure exacerbation","Hematologic cytopenias","Hypersensitivity reactions","Live vaccines should not be administered during therapy"]

Clinical Tips & Counseling

Drug interactions

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SIMPONI

Clinical safety rating: caution

Comprehensive clinical and safety monograph for SIMPONI (SIMPONI).

How it works

Golimumab is a human monoclonal antibody that binds to and neutralizes tumor necrosis factor alpha (TNF-α), inhibiting its interaction with TNF receptors and thereby reducing inflammatory responses.

What the body does with it

Metabolism	Metabolism is not typical for monoclonal antibodies; it is degraded into small peptides and amino acids via general protein catabolism. No CYP450 involvement.
Excretion	Primarily degraded into small peptides and amino acids via reticuloendothelial system; no significant renal or biliary elimination. Less than 0.1% excreted unchanged in urine.
Half-life	Terminal elimination half-life approximately 12-14 days (mean 12.3 days in rheumatoid arthritis patients). Supports subcutaneous dosing every 2 weeks.
Protein binding	Binding to serum proteins is not specified; as a monoclonal antibody, minimal non-specific binding; primarily distributed in plasma and interstitial fluid.
Volume of Distribution	Volume of distribution is approximately 100-130 mL/kg (0.1-0.13 L/kg), indicating distribution largely confined to the vascular and interstitial spaces.
Bioavailability	Subcutaneous: Absolute bioavailability is approximately 51% (range 39-72%) after a single SC injection.
Onset of Action	Subcutaneous: Clinical improvement may be observed as early as 2-4 weeks after initiation; maximal effect may take up to 12-16 weeks.
Duration of Action	Duration of therapeutic effect is maintained with every 2-week dosing. Steady-state concentrations achieved by 12 weeks. After stopping, drug concentrations decline gradually over 2-3 months.

Classification & Brands

Dosing & administration

Dosage form	INJECTABLE
Renal impairment	No specific dose adjustment is recommended for renal impairment. Simponi has not been studied in patients with severe renal impairment; use with caution.
Liver impairment	No specific dose adjustment is recommended for hepatic impairment. Simponi has not been studied in patients with severe hepatic impairment (Child-Pugh C); use with caution.
Pediatric use	Simponi is not approved for pediatric use; safety and efficacy have not been established in patients under 18 years of age.
Geriatric use	No specific dose adjustment is required in elderly patients. However, due to a higher incidence of infections in the elderly, caution is advised. The pharmacokinetics of golimumab are not significantly affected by age.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for SIMPONI (SIMPONI).

Breastfeeding	Unknown if excreted in human milk; endogenous IgG is present in breast milk. M/P ratio not established. Weigh benefits of breastfeeding against potential for drug transfer causing immunosuppression in infant.
Teratogenic Risk	Pregnancy Category B. No evidence of teratogenicity in animal studies. Limited human data; monoclonal antibodies cross placenta minimally in first trimester and increasingly in second and third trimesters. Theoretical risk of immune suppression in neonate if exposed in utero during third trimester.

Warnings & precautions

■ FDA Black Box Warning

Side Effect Profile

Serious Effects

Absolute Contraindications

["Known hypersensitivity to golimumab or any product component","Active serious infections","Concurrent use with other TNF blockers or abatacept or anakinra (due to increased infection risk)"]