Biologic Overview¶
Hannah Lomzenski
Background¶
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"-cept" refers to fusion of a receptor to the Fc part of human immunoglobulin G1 (IgG1)
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"-mab" indicates a monoclonal antibody (mAb)
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"-ximab" indicates a chimeric mAb
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"-zumab" indicates a humanized mAb
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"-umab" indicates a fully human mAb
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“-tinib” indicates a tyrosine kinase inhibitor (small molecule inhibitors, not true biologics)
Selected biologics¶
Kinase inhibition¶
Generic Name (Brand Name) |
Mechanism of Action | Common Uses | Common Side Effects |
|---|---|---|---|
Tofacitinib (Xeljanz) |
JAK-1 and JAK-3 inhibitor | RA, UC, JIA, psoriatic arthritis | nasopharyngitis, skin rash, GI sx, GU sx; <1% lymphoma |
Baracitinib (Olumiant) |
JAK-1 and JAK-2 inhibitor | RA; off-label: COVID-19 | URI, nausea, ⇑AST/ALT; <1% lymphoma |
Upadacitinib (Rinvoq) |
non-specific JAK inhibitor | RA | URI, nausea, neutropenia, ⇑AST, ⇑CPK |
IL-1 inhibition¶
Generic Name (Brand Name) |
Mechanism of Action | Common Uses | Common Side Effects |
|---|---|---|---|
Anakinra (Kineret) |
IL-1 receptor antagonist | IL-1 receptor antagonist deficiency, gout flares, FMF, HLH | HA, vomiting, infections, nasopharyngitis, Ab development; in RA: eosinophilia, decreased WBC |
Canakinumab (Ilaris) |
mAb against IL-1β | Cryoporin-associated periodic syndromes (CAPS), FMF, hyperimmunoglobin D syndrome, TRAPS; off-label: gout flare | Weight gain, GI sx, HA, vertigo, serious infections |
IL-17 inhibition¶
Generic Name (Brand Name) |
Mechanism of Action | Common Uses | Common Side Effects |
|---|---|---|---|
Secukinumab (Cosentyx) |
human IgG1 mAb against IL-17A | AS, psoriasis | nasopharyngitis, GI, IBD (<1%) |
Ixekizumab (Taltz) |
human IgG4 mAb against IL-17A | AS, psoriasis | neutropenia, Ab development, URI, Crohn’s (<1%) |
IL-6 inhibition¶
Generic Name (Brand Name) |
Mechanism of Action | Common Uses | Common Side Effects |
|---|---|---|---|
Tocilizumab (Actemra) |
IL-6 receptor antagonist | cytokine release syndrome, giant cell arteritis, RA, JIA | ⇑ serum cholesterol, ⇑ AST/ALT, infusion rxn, HSV infection (<2%) |
Sarilumab (Kevzara) |
IL-6 receptor antagonist (soluble + membrane-bound) | RA | ⇑ AST/ALT, HSV infection (<2%) |
IL-12/23 inhibition¶
Generic Name (Brand Name) |
Mechanism of Action | Common Uses | Common Side Effects |
|---|---|---|---|
Ustekinumab (Stelara) |
mAb against IL-12 + IL-23 | IBD, psoriasis | nasopharyngitis, Ab development, acne vulgaris, GI sx, GU sx |
Guselkumab (Tremfya) |
human IgG1 mAb against IL-23 | psoriasis | URI, tinea, GI sx |
Costimulation blockade¶
Generic Name (Brand Name) |
Mechanism of Action | Common Uses | Common Side Effects |
|---|---|---|---|
Abatacep (Orencia) |
inhibits T-cell activation by binding CD80 and CD86 on APCs, thus blocking the required CD28 ixn between APCs and T cells. | RA, psoriasis, JIA | nausea, UTI, HA, URI, Ab development |
B-cell depletion and inhibition¶
Generic Name (Brand Name) |
Mechanism of Action | Common Uses | Common Side Effects |
|---|---|---|---|
Rituximab (Rituxan) |
mAb against the CD20 antigen on surface of B-lymphocytes | CLL, Non-Hodgkin lymphomas, GPA, microscopic polyangiitis, pemphigus vulgaris, RA; many off-label uses (GvHD, lupus nephritis, MG, neuromyelitis optica) | HTN, peripheral edema, night sweats, fever, weight gain, angioedema, arthralgias, ⇑ ALT, hypophosphatemia, hematologic abnormalities |
Belimumab (Benlysta) |
IgG1-lambda mAb that prevents survival of B-lymphocytes by blocking the binding of soluble human B lymphocyte stimulator protein (BLyS) to receptors on B lymphocytes | lupus nephritis, SLE | GI symptoms, hypersensitivity reaction, infections, psychiatric disturbances |
TNF-inhibition¶
Generic Name (Brand Name) |
Mechanism of Action | Common Uses | Common Side Effects |
|---|---|---|---|
Adalilumab (Humira) |
mAb against TNFα | RA, IBD, AS, psoriasis, uveitis, hidradenitis suppurativa | skin rash, HA, URI, ⇑ CPK, +ANA titer (12%), Ab development (3-26%) |
Certolizumab (Cimzia) |
humanized mAb Fab fragment against TNFα | RA, Crohn’s, AS, psoriasis; \*approved for use during pregnancy | skin rash, nausea, URI |
Etanercept (Enbrel) |
tumor necrosis factor receptor linked to Fc portion of IgG1; binds TNF | RA, AS, psoriasis, JIA | skin rash, diarrhea, +ANA titer (11%) |
Infliximab (Remicade) |
chimeric mAb against TNFα | RA, IBD, AS, psoriasis | abd pain, URI sx, anemia, ⇑ ALT, Ab development (10-50%) |
Golimumab (Simponi) |
mAb against TNFα | RA, UC, AS, psoriasis, JIA | URI, Ab development (16-38%), +ANA titer (4-17%) |