Biologic Overview

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)

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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