Biologic Overview – Hannah Lomzenski
Background
- "-cept" refers to fusion of a receptor to the Fc part of human immunoglobulin G1 (IgG1)
- "-mab" indicates a monoclonal antibody (mAb)
- "-ximab" indicates a chimeric mAb
- "-zumab" indicates a humanized mAb
- "-umab" indicates a fully human mAb
- “-tinib” indicates a tyrosine kinase inhibitor (TKIs are small molecule inhibitors rather than true biologics)
Kinase inhibition
|
Generic Name |
Brand Name |
Mechanism of Action |
Common Uses |
Common Side Effects |
|
Tofacitinib |
Xeljanz |
JAK-1 and JAK-3 inhibitors |
RA, UC, JIA, psoriatic arthritis |
infections, nasopharyngitis, skin rash, GI sx, GU sx; <1% lymphoma |
|
Baracitinib |
Olumiant |
JAK-1 and JAK-2 inhibitor |
RA; off-label: COVID-19 |
infections, URI, nausea, ÝAST/ALT; <1% lymphoma |
|
Upadacitinib |
Rinvoq |
non-specific JAK inhibitor |
RA |
URI, nausea, neutropenia, ÝAST, ÝCPK |
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, neonatal multi-system inflammatory Dz, RA; off-label: gout flares, FMF, recurrent pericarditis, 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 |
|
Rilonacept |
Arcalyst |
binds to IL-1β (some binding of IL-1α and IL-1 receptor antagonist) |
CAPS, deficiency of IL-1 receptor antagonist |
URI, infections, hypoesthesia, Ab development |
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, infections, Ý 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, infections |
|
Etanercept |
Enbrel |
tumor necrosis factor receptor linked to Fc portion of IgG1; binds TNF |
RA, AS, psoriasis, JIA |
skin rash, diarrhea, infections, +ANA titer (11%) |
|
Infliximab |
Remicade |
chimeric mAb against TNFα |
RA, IBD, AS, psoriasis |
abd pain, URI sx, anemia, Ý ALT, Ab development (10-50%), infections |
|
Golimumab |
Simponi |
mAb against TNFα |
RA, UC, AS, psoriasis, JIA |
URI, infections, Ab development (16-38%), +ANA titer (4-17%) |
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 |
infections, nasopharyngitis, GI, IBD (<1%) |
|
Ixekizumab |
Taltz |
human IgG4 mAb against IL-17A |
AS, psoriasis |
neutropenia, Ab development, infections, URI, Crohn’s (<1%) |
Costimulation blockade
|
Generic Name |
Brand Name |
Mechanism of Action |
Common Uses |
Common Side Effects |
|
Abatacept |
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, infections, 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, Ý ALT, infections, 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 sx, hypersensitivity rxn, infections, psychiatric disturbances |
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 |
Ý serum cholesterol, Ý AST/ALT, infusion rxn, HSV infection (<2%) |
|
Sarilumab |
Kevzara |
IL-6 receptor antagonist (soluble + membrane-bound) |
RA |
Ý 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 |
infections, nasopharyngitis, Ab development, acne vulgaris, GI sx, GU sx |
|
Guselkumab |
Tremfya |
human IgG1 mAb against IL-23 |
psoriasis |
infections, URI, tinea, GI sx |