Table 1.
Therapeutic monoclonal antibodies for non-cancer therapy currently marketed with regulatory approval from the U.S. FDA or EMA or both (as at December 2021).
| Monoclonal Antibody INN and Trade Names | Antibody Type | Target | Approved Indications |
|---|---|---|---|
|
Human–Mouse Chimeric
(-ximab) |
|||
| Abciximab (ReoPro®) | Chimeric IgG Fab | Glycoprotein IIb/IIIa | Adjunct therapy for prevention of cardiac ischemic complications |
| Basiliximab (Simulect®) | Chimeric IgG1 | α-chain IL-2 receptor (CD25) | Prevent organ transplant rejection |
| Infliximab (Remicade®) | Chimeric IgG1 | TNF | Crohn’s disease; ulcerative colitis; RA; ankylosing spondylitis; psoriatic arthritis; plaque psoriasis |
| Obiltoxaximab (Anthim®) | Chimeric IgG1 | Bacillus anthracis PA | Inhalational anthrax Bacillus
anthracis PA |
| Humanized (-zumab) | |||
| Alemtuzumab (Lemtrada®) | Humanized IgG1 | CD52 | Lemtrada®: multiple sclerosis |
| Benralizumab (Fasenra®) | Humanized IgG1 (afucosylated) |
IL-5Rα | Asthma |
| Bimekizumab (Bimzelx®) | Humanized IgG1 | IL-17A, IL-17F, IL-17AF | Plaque psoriasis |
| Brolucizumab (Beovu®) | Humanized single-chain (scFv) fragment |
VEGF-A | Neovascular (wet) age-related macular degeneration |
| Caplacizumab-yhdp (Caplivi®) | Humanized bivalent single-domain nanobody | von Willebrand factor (vWF) | Acquired thrombotic thrombocytopenic purpura |
| Certolizumab pegol (Cimzia®) | Humanized IgG1 Fab, pegylated |
TNF | Crohn’s disease; RA |
| Crizanlizumab-tmca (Adakveo®) |
Humanized IgG2 | P-selectin | Sickle cell disease |
| Daclizumab (Zinbryta®) | Humanized IgG2 | α-chain IL-2 receptor (CD25) | Multiple sclerosis |
| Eculizumab (Soliris®) | Humanized IgG2/4 | Complement C5 | Paroxysmal nocturnal hemoglobinuria; atypical hemolytic uremic syndrome; neuromyelitis optica spectrum disorder (NMOSD) in adult patients who are anti-aquaporin-4 (AQP4) antibody-positive |
| Emicizumab-kxwh (Hemlibra®) | Humanized IgG4 bispecific | Factors IXa and X | Hemophilia A |
| Eptinezumab-jjmr (Vyepti®) | Humanized IgG1 | CGRP | Migraine |
| Fremanezumab-vfrm (Ajovy®) | Humanized IgG4 | CGRP | Migraine |
| Galcanezumab-gnlm (Emgality®) |
Humanized IgG4 | CGRP | Migraine |
| Ibalizumab-uiyk (Trogarzo®) | Humanized IgG4 | CD4 | HIV-1 infection |
| Idarucizumab (Praxbind®) | Humanized IgG1 antibody fragment Fab |
Dabigatran | Reversal of anticoagulant effects of dabigatran; life-threatening or uncontrolled bleeding |
| Inebilizumab-cdon (Uplizna®) | Humanized afucosylated IgG1 |
CD19 | Neuromyelitis optica spectrum disorder (NMOSD) in adult patients who are anti-aquaporin-4 (AQP4) antibody positive |
| Ixekizumab (Taltz®) | Humanized IgG4 | IL-17A | Plaque psoriasis; psoriatic arthritis |
| Mepolizumab (Nucala®) | Humanized IgG1 | IL-5 | Asthma; eosinophilic granulomatosis with polyangiitis |
| Natalizumab (Tysabri®) | Humanized IgG4 | α4 integrin (binds to α4β1 and α4β7 integrins) | Multiple sclerosis; Crohn’s disease |
| Ocrelizumab (Ocrevus®) | Humanized IgG1 | CD20 | Multiple sclerosis |
| Omalizumab (Xolair®) | Humanized IgG1 | IgE | Persistent asthma; chronic idiopathic urticaria |
| Palivizumab (Synagis®) | Humanized IgG1 | RSVF | Prevention of lower respiratory tract disease RSV in children |
| Ranibizumab (Lucentis®) | Humanized IgG1 Fab | VEGF-A | Neovascular (wet) age-related macular degeneration; macular edema following retinal vein occlusion; diabetic macular edema |
| Ravulizumab-cwvz (Ultomiris®) | Humanized IgG2/4 | Complement C5 | Paroxysmal nocturnal hemoglobinuria |
| Reslizumab (Cinqair®) | Humanized IgG4 | IL-5 | Asthma |
| Risankizumab-rzaa (Skyrizi®) | Humanized IgG1 | IL-23 p19 | Plaque psoriasis |
| Romosozumab-aqqg (Evenity®) | Humanized IgG2 | Sclerostin | Osteoporosis |
| Satralizumab-mwge (Enspryng®) |
Humanized IgG2 | IL-6R | Neuromyelitis optica spectrum disorder (NMOSD) in adult patients who are anti-aquaporin-4 (AQP4) antibody-positive |
| Tildrakizumab-asmn (Ilumetri®; Ilumya®) |
Humanized IgG1 | IL-23 p19 | Plaque psoriasis |
| Tocilizumab (Actemra®; RoActemra®) |
Humanized IgG1 | IL-6R | RA; polyarticular juvenile idiopathic arthritis; systemic juvenile idiopathic arthritis |
| Vedolizumab (Entyvio®) | Humanized IgG1 | α4β7 integrin | Adult ulcerative colitis; adult Crohn’s disease |
| Fully human (-umab) | |||
| Adalimumab (Humira®) | Human IgG1 | TNF | RA; psoriatic arthritis; ankylosing spondylitis; plaque psoriasis; Crohn’s disease |
| Aducanumab-avwa (Aduhelm®) |
Human IgG1 | Amyloid beta | Alzheimer’s disease |
| Alirocumab (Praluent®) | Human IgG1 | PCSK9 | Heterozygous FH; atherosclerotic CV disease requiring additional ↓ of LDL-C |
| Anifrolumab-fnia (Saphnelo®) | Human IgG1 | Subunit I type I interferon receptor (IFNAR) |
Systemic lupus erythematosis |
| Ansuvimab-zykl (Ebanga®) | Human IgG1 |
Zaire ebolavirus (EBOV) glycoprotein 1 (GP1) |
Zaire ebolavirus infection |
| Atoltivimab, Maftivimab and Odesivimab-ebgn (Inmazeb®) |
Human IgG1 |
Zaire ebolavirus (EBOV) glycoprotein 1 (GP1) |
Zaire ebolavirus infection |
| Belimumab (Benlysta®) | Human IgG1 | BlyS | Systemic lupus erythematosus |
| Bezlotoxumab (Zinplava®) | Human IgG1 | Clostridium difficile toxin B | Recurrence of Clostridium difficile toxin B infection |
| Brodalumab (Siliq®; Kyntheum®; Lumicef®) |
Human IgG2 | IL-17RA | Plaque psoriasis |
| Burosumab-twza (Crysvita®) | Human IgG1 | FGF23 | X-linked hypophosphatemia |
| Canakinumab (Ilaris®) | Human IgG1 | IL-1β | Cryopyrin-associated periodic syndromes (CAPS) including familial cold autoinflammatory and Muckle–Wells syndromes; SJIA with body weight ≥7.5 kg; NOMID/CINCA; FCAS/FCU; gouty arthritis |
| Casirivimab + Imdevimab (REGEN-COV®; Ronapreve®) |
Human IgG1 | The 2 mAbs bind to separate epitopes of the spike protein RBD of SARS-CoV-2, thus preventing its binding to the human ACE2 receptor and subsequent cell entry |
COVID-19 disease |
| Denosumab (Prolia®) | Human IgG2 | RANKL | Bone loss—for osteoporosis and to increase bone mass in menopausal women at high risk of fracture |
| Dupilumab (Dupixent®) | Human IgG4 | IL-4Rα subunit | Atopic dermatitis |
| Efgartigimod-alfa-fcab (Vyvgart®) |
Human IgG1 Fc fragment | Neonatal Fc receptor FcRn | Generalized myasthenia gravis |
| Emapalumab-lzsg (Gamifant®) | Human IgG1 | IFNγ | HLH |
| Erenumab-zooe (Aimovig®) | Human IgG2 | CGRP receptor | Migraine |
| Evinacumab-dgnb (Evkeeza®) | Human IgG4 | ANGPTL3 (angiopoietin-like 3) | Homozygous familial hypercholesterolemia (HoFH) |
| Evolocumab (Repatha®) | Human IgG2 | PCSK9 | Primary hyperlipidemia and mixed dyslipidemia; homozygous FH to reduce LDL-C and other lipids |
| Golimumab (Simponi®) | Human IgG1 | TNF | RA; psoriatic arthritis (both in combination with methotrexate); ankylosing spondylitis |
| Guselkumab (Tremfya®) | Human IgG1 | IL-23 | Plaque psoriasis |
| Lanadelumab-flyo (Takhzyro®) | Human IgG1 | Plasma kallikrein | HAE prevention |
| Raxibacumab (ABthrax®) | Human IgG1 | Bacillus anthracis PA | Inhalational anthrax to Bacillus anthracis and prophylaxis in absence of alternative therapies |
| Regdanvirimab (Regkirona®) | Human IgG1 | mAb binds to the spike protein RBD of SARS-CoV-2 preventing its binding to the human ACE2 receptor and subsequent cell entry |
COVID-19 disease |
| Sarilumab (Kevzara®) | Human IgG1 | IL-6R | RA |
| Secukinumab (Cosentyx®) | Human IgG1 | IL-17A | Moderate to severe plaque psoriasis |
| Sotrovimab (Xevudy®) 1 |
Human IgG1 | Spike protein RBD of SARS-CoV-2 | COVID-19 disease |
| Teprotumumab-trbw (Tepezza®) |
Human IgG1 | IGF-1R | Thyroid eye disease |
| Tezepelumab-ekko (Tezspire®) | Human IgG2 | Thymic stromal lymphopoietin | Severe asthma |
| Tralokinumab (Adtralza®) | Human IgG4 | IL-13 | Atopic dermatitis |
| Ustekinumab (Stelara®) | Human IgG1 | IL-12, IL-23 | Plaque psoriasis |
ACE2—angiotensin-converting enzyme 2; ADCC—antibody-dependent cell-mediated cytotoxicity; BlyS—B lymphocyte stimulator, also known as B cell-activating factor, BAFF; C5—complement component 5; CDC—complement-dependent cytotoxicity; CGRP—calcitonin gene-related peptide; CHO—Chinese hamster ovary cells; CINCA—chronic infantile neurological, cutaneous, articular syndrome; COVID—coronavirus disease; CV—cardiovascular; EMA—European Medicines Agency; FCAS—familial cold autoinflammatory syndrome; FCU—familial cold urticaria; FDA—U.S. Food and Drug Administration; FH—familial hypercholesterolemia; FGF23—fibroblast growth factor 23; GI—gastrointestinal; HAE—hereditary angioedema; HIV—human immunodeficiency virus; HLH—primary hemophagocytic lymphohistiocytosis; IGF-1R—insulin-like growth factor-1 receptor; IPP—International Nonproprietary Name; LDL—low-density lipoprotein; LDL-C—LDL-cholesterol; LDLR—LDL receptor; NLRP-3—gene cryopyrin or nucleotide-binding domain, leucine rich family, pyrin domain-containing 3 gene; NOMID—neonatal-onset multisystem inflammatory disease; NSCLC—non-small cell lung cancer; NSO—non-Ig-secreting, non-L chain-synthesizing, 8-azaguanine-resistant and HAT-sensitive mouse myeloma cell line; PA—protective antigen of B. anthracis toxin; PCSK9—proprotein convertase subtilisin/kexin type 9; RA—rheumatoid arthritis; RANKL—receptor activator of nuclear factor kappa-B ligand (CD254), a member of the TNF cytokine family; RBD—receptor-binding domain; RSV—human respiratory syncytial virus (F viral protein coat antigen); SARS-CoV-2—severe acute respiratory syndrome coronavirus 2; SJIA—active systemic juvenile idiopathic arthritis; Sp2/0—BALB/c mouse spleen cells fused with P3 myeloma. Cells do not secrete Ig, are resistant to 8-azaguanine, and are HAT-sensitive; TNF— tumor necrosis factor; VEGF—vascular endothelial growth factor (a subfamily of growth factors; includes VEGF-A); VEGFR2—vascular endothelial growth factor receptor 2, also known as KDR (kinase insert domain-containing receptor), FLK1 (fetal liver kinase 1), or CD309. 1 Note added in press: Approved by the FDA 17 December 2021. ↓ decrease.