Therapeutic antibodies (Abs) are used in the treatment of numerous diseases, including infection, cancer, and autoimmune disorders, in which they have already demonstrated their efficacy. The success of Abs is due to (I) a high level of specificity and affinity to their target antigen, (II) a favorable safety profile, and (III) a unique pharmacokinetic profile, supporting a longer half-life as compared to other drugs. While the majority of Abs are delivered through IV injection, evidence in the literature showed that beyond the reduction of invasiveness, a better efficacy could be achieved with a local delivery of Abs. Among those routes, one has been in full development these last few years, with already good clinical results and still promising developments: The Subcutaneous route.
International Non-Proprietary Name | Trade Name | Target | Indication | Format | Sponsoring Company | Year of Approval (FDA) | Year of Approval (EMA) | ||||||||||||
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Adalimumab | Humira | TNF-α | Rheumatoid Arthritis, Psoriatic Arthritis, and Ankylosing Spondylitis, Crohn disease | ||||||||||||||||
Casirivimab + Imdevimab | Spike protein | Human full-length IgG1 | AbbVie Inc. | 2002 | 2003 | ||||||||||||||
SARS-CoV2 | Human full-length IgG1 cocktail | Regeneron Pharmaceuticals | URR (EMA + FDA) | NCT05074433 | Efalizumab | Raptiva | CD11a | ||||||||||||
Ofatumumab | Psoriasis | 1 | Humanized full-length IgG1 | Merck Biopharma/Serono Europe | 2003 | 1 | 2004 1 | ||||||||||||
CD20 | Relapsing multiple sclerosis | Human full-length IgG1 | Novartis Pharmaceuticals | Phase 3 (Recruiting) | NCT04486716 | NCT04510220 NCT04353492 |
Omalizumab | Xolair | IgE | Severe Asthma | Humanized full-length IgG1 | Genentech/Novartis | 2003 | 2005 | |||||
CSL312 (Garadacimab) | Factor XIIa | Hereditary Angioedema | Human full-length IgG4 | CSL Behring | Phase 3 (Active, not recruiting) | NCT04656418 | Certolizumab Pegol | Cimzia | TNF-α | Crohn Disease | Humanized PEGylated Fab’ IgG1 fragment | UCB Pharma | 2008 | 2009 | |||||
SAR440340 /REGN3500 (Itepekimab) | IL-33 | COPD | Human full-length IgG4 | Sanofi | Phase 3 (Recruiting) | NCT04701983 NCT04751487 | Canakinumab | Ilaris | IL-1β | Cryopirin-Associated Periodic Syndromes | Human full-length IgG1 | Novartis | 2009 | 2009 | |||||
JS002 (Ongericimab) | PCSK9 | Heterozygous Familial Hypercholesterolemia; Hyperlipidemia | Human full-length IgG4 | Shanghai Junshi Bioscience Co., Ltd. | Phase 3 (Recruiting) | NCT05325203 NCT04781114 | Golimumab | Simponi | TNF-α | Rheumatoid Arthritis, Psoriatic Arthritis, and Ankylosing Spondylitis | Human full-length IgG1 | Centocor Ortho Biotech/Janssen Biologics | 2009 | 2009 | |||||
BCD-085 (Netakimab) | IL-17 | Psioratic Arthritis | Humanized genetically modified IgG1 | Biocad | Phase 3 (Active, not recruiting) | NCT03598751 | Ustekinumab | Stelara | IL-12 and IL-23 | Psoriasis | Human full-length IgG1 | Centocor Ortho Biotech/Janssen Cilag International | 2009 | ||||||
AK002 (Lirentelimab) | 2009 | ||||||||||||||||||
Siglec-8 | Eosinophilic Gastritis and/or Eosinophilic Duodenitis | Humanized non fucosylated IgG1 | Allakos, Inc. | Phase 3 (Recruiting) | NCT05152563 | Denosumab | Prolia | RANK-L | Postmenopausal Osteoporosis | Human full-length IgG2 | Amgen | 2010 | 2010 | ||||||
MW032 | RANK-L | Bone Metastases from solid tumors | Human full-length IgG2 | Abwell (Shanghai) Bioscience Co., Ltd. | Phase 3 (Active, not recruiting) | NCT04812509 | Tocilizumab | Actemra/RoActemra | IL-6R | ||||||||||
Tralokinumab | Rheumatoid Arthritis, Polyarticular Juvenile Idiopathic Arthritis, Systemic Juvenile Idiopathic Arthritis | 1 | IL-13 | Humanized full-length IgG1 | Genentech/Roche | 2013 | 2014 | ||||||||||||
Atopic Dermatitis | Human full-length IgG4 | LEO Pharma | Phase 3 (Recruiting) | NCT05194540 NCT03587805 | Alirocumab | Praluent | PCSK9 | LDL-C Lowering | Human full-length IgG1 | Sanofi-Aventis | 2015 | 2015 | |||||||
Golimumab 1 | TNF-a | Moderately to Severely Active Ulcerative Colitis | Human full-length IgG1 | Janssen Research & Development, LLC | Phase 3 (Recruiting) | NCT03596645 | Evolocumab | Repatha | PCSK9 | LDL-C Lowering | Human full-length IgG2 | Amgen | 2015 | 2015 | |||||
LY01011 | RANK-L | Bone Metastases from solid tumors | Human full-length IgG2 | Luye Pharma Group Ltd. | Phase 3 (Recruiting) | NCT04859569 | Mepolizumab | Nucala | IL-5 | Severe Asthma | Humanized full-length IgG1 | GlaxoSmithKline | 2015 | 2015 | |||||
Secukinumab | |||||||||||||||||||
QL1206 | RANK-L | Bone Metastases from solid tumors | Human full-length IgG2 | Qilu Pharmaceutical Co., Ltd. | Phase 3 (Recruiting) | NCT04550949 | Cosentyx | IL-17a | Psoriasis | Human full-length IgG1 | Novartis | 2015 | 2015 | ||||||
Daclizumab | Zinbryta | IL-2 receptor-α | Multiple Sclerosis | Humanized full-length IgG1 | Biogen | 2016 2 | 2016 2 | ||||||||||||
Ixekizumab | Taltz | IL-17a | Psoriasis | Humanized full-length IgG4 | Eli Lilly | 2016 | 2016 | ||||||||||||
Dupilumab | Dupixent | IL4 receptor-α | Atopic Dermatitis | Human full-length IgG4 | |||||||||||||||
Adalimumab 1 | TNF-a | Ulcerative Colitis | Human full-length IgG1 | AbbVie | Regeneron Pharmaceuticals/Sanofi-Aventis | 2017 | 2017 | ||||||||||||
Phase 3 (Active, not recruiting) | Sarilumab | Kevzara | IL-6 receptor | Rheumatoid Arthritis | Human full-length IgG1 | Regeneron Pharmaceuticals/Sanofi-Aventis | 2017 | 2017 | |||||||||||
Elranatamab + Daratumumab | BCMA-CD3 + CD38 | Multiple Myeloma | Humanized) bispecific IgG2 + Human full-length IgG1 | Pfizer | Phase 3 (Recruiting) | NCT05020236 | |||||||||||||
Teclistamab | BCMA-CD3+ | Hematological Malignancies | Human bispecific IgG4 | Janssen Research & Development, LLC | Phase 3 (Recruiting) | NCT03145181 | |||||||||||||
PRO 140 (Leronlimab) | CCR5 | HIV | Humanized full-length IgG4 | CytoDyn, Inc. | Phase 3 (Active, not recruiting) | 2018 | 2018 | ||||||||||||
NCT02632175 | |||||||||||||||||||
IBI306 | PCSK9 | Homozygous and Heterozygous Familial Hypercholesterolemia | Human full-length IgG2 | Innovent Biologics (Suzhou) Co., Ltd. | Phase 3 (Recruiting) | Guselkumab | Tremfya | IL-23 p19 | Psoriasis | Human full-length IgG1 | Janssen Biotech/Johnson & Johnson | 2017 | 2017 | ||||||
NCT04031742 | NCT04709536 | NCT04179669 | |||||||||||||||||
Alirocumab 1 | PCSK9 | Postprandial Hyperlipemia in Type 2 Diabetes | Human full-length IgG1 | Regeneron Pharmaceuticals | Phase 3 (Recruiting) | NCT03344692 | |||||||||||||
SYN023 (CTB-011 and CTB-012) | Proteins of human Rabies | Human Rabies | Humanized full-length IgG cocktail | Synermore Biologics (Suzhou) Co., Ltd. | Phase 3 (Active, not recruiting) | NCT04644484 | |||||||||||||
Adalimumab 1 | TNF-a | Uveitis | Human full-length IgG1 | JHSPH Center for Clinical Trials | Phase 3 (Recruiting) | NCT03828019 | Brodalumab | Siliq/Kyntheum | |||||||||||
CM310 | IL-4Ra | Atopic Dermatitis | Humanized full-length IgG | Keymed Biosciences Co., Ltd. | Phase 3 (Not yet Recruiting) | NCT05265923 | |||||||||||||
Benralizumab | IL-17 receptor-α | Psoriasis | Human full-length IgG2 | Valeant Pharmaceuticals/Leo Pharma | 2017 | 2017 | |||||||||||||
1 | IL-5Ra | Eosinophilic Gastritis and/or Gastroenteritis | Humanized full-length IgG1 | AstraZeneca | Benralizumab | Fasenra | IL-5 receptor-α | Severe Asthma | Humanized full-length IgG1 | AstraZeneca | 2017 | 2018 | |||||||
Phase 3 (Recruiting) | Emicizumab | Hemlibra | Factor IX and X | Hemophilia A | Humanized full-length bispecific IgG4 | Genentech/Roche | 2017 | 2018 | |||||||||||
Rituximab and hyaluronidase | Rituxan Hycela/MabThera SC | CD20 | Follicular Lymphoma, Diffuse large B cell Lymphoma, and Chronic Lymphocytic Leukemia | Chimeric full-length IgG1 | Genentech/Roche | 2017 | NCT03902522 NCT052713702014 |
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NCT02859961 | NCT02990858 | Belimumab | Benlysta | BAFF | Systemic Lupus Erythematosus | Human full-length IgG1 | GlaxoSmithKline | 2017 | 2017 | ||||||||||
Olokizumab | IL-6 | COVID-19 | Humanized full-length IgG4 | R-Pharm | Phase 3 (Recruiting) | NCT05187793 | Tildrakizumab | Ilumya/Ilumetri | IL-23 p19 | Psoriasis | Humanized full-length IgG1 | Merck Sharp & Dohme Corp/Almirall | 2018 | 2018 | |||||
Etrolizumab | α4-β7/αE-β7 integrin receptor | Crohn’s disease | Humanized full-length IgG1 | Hoffmann-La Roche | Phase 3 (Recruiting) | NCT02403323 | Burosumab | Crysvita | FGF23 | X-linked Hypophosphatemia | Human full-length IgG1 | Ultragenyx Pharmaceutical/Kyowa Kirin Holdings | 2018 | 2018 | |||||
Erenumab | |||||||||||||||||||
Gantenerumab | β-amyloid | Alzheimer’s disease | Human full-length IgG1 | Hoffmann-La Roche | Phase 3 (Recruiting) | NCT03444870 NCT05256134 NCT04374253 NCT01760005 |
Aimovig | CGRP | Migraine | Human full-length IgG2 | Amgen/Novartis | 2018 | 2018 | ||||||
Emicizumab 1 | FIX, FX | Hemophilia A Without Inhibitor | Humanized bispecific IgG4 | Margaret Ragni, University of Pittsburgh | Phase 3 (Recruiting) | NCT04303559 | Lanadelumab | Takhzyro | pKal | Hereditary Angioedema | Human full-length IgG1 | Galcanezumab | Emgality | CGRP | Migraine | Humanized full-length IgG4 | Eli Lilly | 2019 | 2018 |
Caplacizumab 3 | Cablivi | A1 from factor Willebrand | Acquired Thrombocytopenic Thrombotic Purpura | Humanized bivalent nanobody | Sanofi-Aventis | 2019 | 2018 | ||||||||||||
NCT05251909 | Takeda Pharmaceuticals | Romosozumab | Evenity | RANK-L | Postmenopausal Osteoporosis | Humanized full-length IgG2 | Amgen/UCB Pharma | 2019 | 2019 | ||||||||||
Trastuzumab and hyaluronidase | Herceptin Hylecta | HER2 | HER2+ Breast Cancer | Humanized full-length IgG1 | Genentech, inc./Roche | 2019 | 2013 | ||||||||||||
Risankizumab | Skyrizi | IL-23 p19 | Psoriasis | Humanized full-length IgG1 | AbbVie Inc. | 2019 | 2019 | ||||||||||||
Fremanezumab | Ajovy | CGRP | Migraine | Humanized full-length IgG2 | Teva Branded Pharmaceutical Products R&D | 2020 | 2019 | ||||||||||||
Daratumumab and hyaluronidase | Darzalex Faspro | CD38 | Light-chain Amyloidosis, Multiple Myeloma | Human full-length IgG1 | Janssen Biotech | 2020 | 2020 | ||||||||||||
Satralizumab | Enspryng | IL-6 receptor | Neuromyelitis Optical Spectrum Disorder | Humanized full-length IgG2 | Genentech/Roche | 2020 | 2021 | ||||||||||||
Ofatumumab | Kesimpta | CD20 | Multiple Sclerosis | Human full-length IgG1 | Novartis Pharmaceuticals Corporation | 2020 | 2021 | ||||||||||||
Pertuzumab, Trastuzumab, and hyaluronidase | Phesgo | HER2 | Early Breast Cancer | Humanized full-length IgG1 | Genentech/Roche | 2020 | 2020 | ||||||||||||
Tralokinumab | Adtralza | IL-13 | Eczema | Human full-length IgG4 | Leo Pharma A/S | 2021 | - | ||||||||||||
Tezepelumab | Tezspire | TSLP | Asthma | Human full-length IgG2 | AstraZeneca | 2021 | - |
International Non- Proprietary Name or Code Name | Target | Indication | Format | Primary Sponsor | Clinical Study Phase | ClinicalTrials.gov—Identifiers |
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