Tissue Necrosis Factor-alpha (TNF-alpha) inhibitors
Source
- Fully human
Mechanism of Action
- Fusion protein that Binds TNF alpha and beta and inactivate it.
- Contains 2 p75 TNF alpha receptors linked to FC IgG1
Dose
- Subcutaneous
- Initial 50 mg twice weekly x 3 months
- Subsequently, 50 mg once weekly
- In children, approved for 4 years and older if less than 63 kg: 0.8mg/kg weekly not to exceed 50 mg weekly
Half-Life
- 4.8 days
Indications
- FDA in Dermatology: Psoriasis and Psoriatic Arthritis
- Off Label: Neutrophilic dermatoses, Granulomatous skin diseases, Bullous dermatoses, AI-CTD (dermatomyositis and systemic lupus); Others: hidradenitis suppurativa, pityriasis rubra pilaris, GVHD, SJS/TEN.
Contraindications
- Hypersensitivity to Etanercept
- Concurrent administration of Anakinra (increased risk of serious infection)
- Active Infection
- Family History of Demyelinating diseases
- Congestive heart failure (moderate to severe NYC III-IV)
Side Effects
- General: Nausea. Pharyngitis, headache, abdominal pain
- Autoantibody against the targeted immune modulator
- Injection site reaction in 14% (most common side effect diminishes in frequency after first month)
- Malignancy: the most common is cutaneous squamous cell carcinoma
- Hematological: Leukopenia, thrombocytopenia, pancytopenia
- Infection
- Demyelinating disease
- Exacerbation of congestive heart failure
- Autoimmunity: ANA+ and Anti dsDNA+
Pregnancy Category
- Pregnancy Category B
Dermatological Side Effects
- New onset psoriasis
- Granulomatous eruption
- Cutaneous small vessel vasculitis
- Eczematous eruption
- Lichenoid dermatitis
- Lupus erythematosus
Source
- Fully human
Mechanism of Action
- IgG1 antibody against TNF alpha
Dose
- Subcutaneous
- Psoriasis: 80 mg on D1, then 40 mg on D8 then 40 mg on D22 then every 2 weeks (note: if not taken with methotrexate for psoriatic arthritis, then consider weekly dosing)
- Hidradenitis Suppurativa: 160mg on D1 or 80mg on D1 and D2, then 80 mg D15, then 40 mg D29 and weekly thereafter
Half-Life
- 14 days
Indications
- FDA in Dermatology: Psoriasis and Psoriatic arthritis, hidradenitis suppurativa
- Off Label: Neutrophilic Dermatoses, Granulomatous Skin diseases, AI-CTD, Others: pityriasis rubra pilaris, relapsing polychondritis and systemic vasculitis
Contraindications
- Hypersensitivity to Etanercept
- Concurrent administration of Anakinra (increased risk of serious infection)
- Active Infection
- Family History of Demyelinating diseases
- Congestive heart failure (moderate to severe NYC III-IV)
Side Effects
- General: Nausea. Pharyngitis, headache, abdominal pain
- Autoantibody against the targeted immune modulator
- Injection site reaction in 14% (most common side effect diminishes in frequency after first month)
- Malignancy: the most common is cutaneous squamous cell carcinoma
- Hematological: Leukopenia, thrombocytopenia, pancytopenia
- Infection
- Demyelinating disease
- Exacerbation of congestive heart failure
- Autoimmunity: ANA+ and Anti dsDNA+
Pregnancy Category
- Pregnancy Category B
Dermatological Side Effects
- New onset psoriasis
- Granulomatous eruption
- Cutaneous small vessel vasculitis
- Eczematous eruption
- Lichenoid dermatitis
- Lupus erythematosus
Notes
- Approved for children with Hidradenitis Suppurativa 12 years old and over.
Source
- Chimeric (25% mouse, 75% Human)
Mechanism of Action
- IgG1 monoclonal antibody against TNF alpha
Dose
- Intravenous
- 5mg/kg at weeks 0, 2, 6 then every 8 weeks
- (up to 10mg/kg have been used in Hidradenitis Suppurativa)
Half-Life
- 9 days
Indications
- FDA in Dermatology: Psoriasis and Psoriatic arthritis
- Off Label: Neutrophilic Dermatoses, Granulomatous Skin diseases, Bullous Dermatoses, AI-CTD, Others: hidradenitis suppurativa, pityriasis rubra pilaris, GVHD, Behcet, multicentric reticulohistiocytosis and systemic vasculitis and hidradenitis suppurativa
Contraindications
- Hypersensitivity to Etanercept
- Concurrent administration of Anakinra (increased risk of serious infection)
- Active Infection
- Family History of Demyelinating diseases
- Congestive heart failure (moderate to severe NYC III-IV)
Side Effects
- General: Nausea. Pharyngitis, headache, abdominal pain
- Autoantibody against the targeted immune modulator
- Injection site reaction in 14% (most common side effect diminishes in frequency after first month)
- Malignancy: the most common is cutaneous squamous cell carcinoma
- Hematological: Leukopenia, thrombocytopenia, pancytopenia
- Infection
- Demyelinating disease
- Exacerbation of congestive heart failure
- Autoimmunity: ANA+ and Anti dsDNA+
Pregnancy Category
- Pregnancy Category B
Dermatological Side Effects
- New onset psoriasis
- Granulomatous eruption
- Cutaneous small vessel vasculitis
- Eczematous eruption
- Lichenoid dermatitis
- Lupus erythematosus
Notes
- Infusion reaction (most commonly occur in 15%, linked to chimeric antibodies); during and up to 3 hours after (headache, flushing, nausea) and rarely anaphylaxis.
- Ways to reduce infusion reaction: premedication, slow infusion; if severe: epinephrine and corticosteroids; also infusion reaction is lessened with methotrexate
- Anti Drug Antibodies 38%: increase infusion reaction and reduce efficacy; methotrexate decreases the formation of antibodies, consider increases the dose or shorten the interval between doses if this occurs
- Hepatotoxicity
Source
- Recombinant Humanized
Mechanism of Action
- Pegylated antibody that binds TNF alpha
Dose
- Subcutaneous
- 400 mg at weeks 0, 2 and 4 followed by 200 mg every 2 weeks or 400 mg every month
Half-Life
- 11 days
Indications
- FDA approved for psoriatic arthritis but not psoriasis
Contraindications
- Hypersensitivity to Etanercept
- Concurrent administration of Anakinra (increased risk of serious infection)
- Active Infection
- Family History of Demyelinating diseases
- Congestive heart failure (moderate to severe NYC III-IV)
Side Effects
- General: Nausea. Pharyngitis, headache, abdominal pain
- Autoantibody against the targeted immune modulator
- Injection site reaction in 14% (most common side effect diminishes in frequency after first month)
- Malignancy: the most common is cutaneous squamous cell carcinoma
- Hematological: Leukopenia, thrombocytopenia, pancytopenia
- Infection
- Demyelinating disease
- Exacerbation of congestive heart failure
- Autoimmunity: ANA+ and Anti dsDNA+
Pregnancy Category
- Pregnancy Category B
Dermatological Side Effects
- New onset psoriasis
- Granulomatous eruption
- Cutaneous small vessel vasculitis
- Eczematous eruption
- Lichenoid dermatitis
- Lupus erythematosus
Notes
- Safest targeted immune modulator during pregnancy
Source:
- Fully Human
Mechanism of Action
- IgG1 kappa monoclonal antibody that binds TNF alpha
Dose
- Subcutaneous (or intravenously)
- 50 mg monthly
Half-Life:
- 11-14 days
Indications:
- FDA approved for psoriatic arthritis but not psoriasis
Contraindications
- Hypersensitivity to Etanercept
- Concurrent administration of Anakinra (increased risk of serious infection)
- Active Infection
- Family History of Demyelinating diseases
- Congestive heart failure (moderate to severe NYC III-IV)
Side Effects
- General: Nausea. Pharyngitis, headache, abdominal pain
- Autoantibody against the targeted immune modulator
- Injection site reaction in 14% (most common side effect diminishes in frequency after first month)
- Malignancy: the most common is cutaneous squamous cell carcinoma
- Hematological: Leukopenia, thrombocytopenia, pancytopenia
- Infection
- Demyelinating disease
- Exacerbation of congestive heart failure
- Autoimmunity: ANA+ and Anti dsDNA+
Pregnancy Category
- Pregnancy Category B
Dermatological Side Effects
- New onset psoriasis
- Granulomatous eruption
- Cutaneous small vessel vasculitis
- Eczematous eruption
- Lichenoid dermatitis
- Lupus erythematosus