Guselkumab
Guselkumab Uses, Dosage, Side Effects, Food Interaction and all others data.
Guselkumab is a human immunoglobulin G1 lambda (IgG1λ) monoclonal antibody that selectively blocks interleukin-23. IL-23 is an inflammatory cytokine that activates the CD4+ T-helper (Th17) cell pathway to mediate the inflammatory cascade that induces psoriatic plaque formation . In clinical trials, guselkumab demonstrated improved skin clearance and symptomatic improvements in dermatological manifestations of psoriasis.
Developed by Janssen, the subcutenous injection form of guselkumab was approved in July 2017 under the market name Tremfya for the treatment of adult patients with moderate-to-severe plaque psoriasis.
Guselkumab is shown to reduce serum levels of IL-17A, IL-17F and IL-22 .
| Trade Name | Guselkumab |
| Availability | Prescription only |
| Generic | Guselkumab |
| Guselkumab Other Names | Guselkumab |
| Related Drugs | Skyrizi, Tremfya, Humira, Otezla, Cosentyx, prednisone, methotrexate, Enbrel, Remicade, Stelara |
| Weight | 100mg/ml, |
| Type | Subcutaneous Solution, Subcutaneous |
| Formula | C6402H9864N1676O1994S42 |
| Weight | 143.6 Da (units in kg/mol) |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Guselkumab is a monoclonal antibody used to treat moderate to severe plaque psoriasis.
Indicated for the treatment of adults with moderate-to-severe plaque psoriasis who are candidates for systemic therapy or phototherapy.
Guselkumab is also used to associated treatment for these conditions: Severe Plaque psoriasis, Moderate Plaque psoriasis
How Guselkumab works
Guselkumab targets the p19 alpha subunit of IL-23. While IL-23 promotes the normal inflammatory and immune responses, the p19 and p40 subunits of IL-23 are found to be over-expressed in the condition of psoriasis and other autoimmune inflammatory skin diseases . Guselkumab selectively binds to the p19 subunit of IL-23 in dendritic cells and keratinocytes and blocks its interaction with IL-23 receptor, which further prevents the release of other pro-inflammatory cytokines and chemokines via stimulation of immune cells such as Th17 cells . Thus, guselkumab blocks the abnormally-heightened signalling of inflammatory cascades that promote epidermal abnormalities including keratinocyte hyperproliferation and psoriatic plaque formation .
Toxicity
Animal studies to assess the effect of guselkumab on carcinogenesis, mutagenesis and impairment on fertility have not been conducted. When subcutaneously injected into guinea pigs, the doses of guselkumab up to 100mg/kg twice-weekly demonstrated no effects on fertility parameters .
Food Interaction
No interactions found.Guselkumab Drug Interaction
Unknown: charcoal, epinephrine, ipratropium, sulfamethoxazole / trimethoprim, onabotulinumtoxinA, sulfamethoxazole / trimethoprim, ubiquinone, copper gluconate, duloxetine, testosterone, glucose, diltiazem, betamethasone topical, venlafaxine, pimecrolimus topical, epinephrine, glycerin, bioflavonoids, thiamine, cholecalciferol
Guselkumab Disease Interaction
Volume of Distribution
The apparent volume of distribution is 13.5 L .
Elimination Route
Following a 100mg subcutaneous administration, the peak plasma concentration (Cmax) of guselkumab is 8.09 ± 3.68 mcg/mL which is reached after approximately 5.5 days .
Half Life
Mean half-life of guselkumab is approximately 15 to 18 days in subjects with plaque psoriasis .
Clearance
Apparent clearance in subjects with plaque psoriasis is 0.516 L/day .
Elimination Route
Like other human IgG monoclonal antibodies, guselkumab is expected to be both renally and fecally excreted as smaller peptide units.
Innovators Monograph
You find simplified version here Guselkumab
