golimumab (go-li-mu-mab) Simponi, Simponi Aria, Simponi IV

 Indications

Simponi and Simponi Aria: Treatment of moderately

to severely active rheumatoid arthritis (with methotrexate).

Simponi: Treatment of active psoriatic arthritis

(alone or with methotrexate). Simponi: Treatment of

active ankylosing spondylitis. Simponi: Moderately to

severely active ulcerative colitis in patients who have

demonstrated corticosteroid dependence or have responded

inadequately to immunosuppressants such as

aminosalicylates, corticosteroids, azathioprine, or 6–

mercaptopurine.

Action

Inhibits binding of TNF to receptors inhibiting activity

and resulting in anti-inflammatory and antiproliferative

activity. Therapeutic Effects: Decreased pain and

swelling with decreased joint destruction in patients

with rheumatoid arthritis, psoriatic arthritis, and ankylosing

spondylitis. Induction and maintenance of clinical

remission of ulcerative colitis.

Pharmacokinetics

Absorption: Well absorbed following subcutaneous

administration. IV administration results in complete

bioavailability.

Distribution: Distributed primarily in the circulatory

system with limited extravascular distribution.

Metabolism and Excretion: Unknown.

Half-life: 2 wk.

TIME/ACTION PROFILE (improvement)

ROUTE ONSET PEAK DURATION

Subcut within 3 mo 2–7 days† unknown

IV within 3 mo unknown unknown

† Blood levels. 

Contraindications/Precautions

Contraindicated in: Active infection (including localized);

Concurrent use of abatacept or anakinra (q

risk of infections); Lactation: Avoid during breast feeding.

Use Cautiously in: History of chronic or recurrent

infection or underlying illness/treatment predisposing

to infection; History of exposure to tuberculosis; History

of opportunistic infection; Patients residing, or

who have resided, where tuberculosis, histoplasmosis,

coccidioidomycoses, or blastomycosis is endemic; History

of HF (may worsen); Pre-existing or recent-onset

CNS demyelinating disorders; History of cytopenias

(may worsen); History of psoriasis (may exacerbate);

Hepatitis B virus carriers (risk of reactivation); Geri:

Use cautiously in elderly patients due toqrisk of infection;

OB: Use during pregnancy only if clearly needed;

Pedi: Safety not established;qrisk of lymphoma (including

HSTCL), leukemia, and other malignancies.

Adverse Reactions/Side Effects

CNS: CENTRAL NERVOUS SYSTEM DEMYELINATING DISORDERS,

Guillain-Barre syndrome, multiple sclerosis.

EENT: nasopharyngitis, optic neuritis. Resp: upper

respiratory tract infection. CV: HF, hypertension. GI:

qliver enzymes. Derm: psoriasis. Hemat: aplastic

anemia, leukopenia, neutropenia, pancytopenia,

thrombocytopenia. Local: injection site reactions.

Neuro: paresthesia. Misc: ANAPHYLAXIS, HYPERSENSITIVITY

REACTIONS, INFECTIONS (including reactivation tuberculosis

and other opportunistic infections due to

bacterial, invasive fungal, viral, mycobacterial, and

parasitic pathogens), MALIGNANCY (including lymphoma,

HSTCL, leukemia, and skin cancer), fever, lupus-

like syndrome.

Interactions

Drug-Drug: Abatacept, anakinra, corticosteroids,

or methotrexateqrisk of serious infections;

concurrent use with anakinra or abatacept is not recommended.

Use of live virus vaccines or therapeutic

infectious agents mayqrisk of infection; avoid concurrent

use. Concurrent use with azathioprine and/or

6–mercaptopurine mayqrisk of HSTCL. May normalize

previously suppressed levels of CYP450 enzymes,

following initiation or discontinuation of golimumab,

effects of substrates of this system may be

altered and should be monitored, including warfarin,

theophylline, and cyclosporine.

Route/Dosage

Rheumatoid Arthritis

Subcut (Adults): 50 mg once monthly.

IV (Adults): 2 mg/kg initially and 4 wk later, then 2

mg/kg every 8 wk.

Psoriatic Arthritis and Ankylosing Spondylitis

Subcut (Adults): 50 mg once monthly.

Ulcerative Colitis

Subcut (Adults): 200 mg initially, then 100 mg 2 wk

later, then 100 mg every 4 wk.

Availability

Solution for subcutaneous injection: 50 mg/0.5

mL in single-dose prefilled syringes and Smartject autoinjectors,

100 mg/mL in single-dose prefilled syringes

and Smartject autoinjectors. Solution for intravenous

injection (Simponi Aria): 12.5 mg/mL.