Antibodies
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Antibodies
Adalimumab
Adalimumab (Humira®) is a human monoclonal IgG1/kappa antibody indicated for the treatment of e.g. rheumatoid arthritis, psoriatic arthritis, or Crohn’s disease. Humira®was the third tumor necrosis factor (TNF) -α inhibitor on the market, but the first fully human antibody directed towards this target. Adalimumab consists of a tetramer of two heavy and two light chains with one N-glycosylation site per heavy chain. The patent of the originator owned by AbbVie expired in 2016 in the US and in the EU in 2018; however, in the last few years AbbVie has secured about 70 (US) patents covering Humira® formulations, manufacturing techniques and methods to treat multiple diseases. These additional patents expire between 2022 and 2034 and AbbVie pursued litigation to keep biosimilars off the US market until at least 2022. Learn more
Alemtuzumab
Alemtuzumab (Lemtrada®) depletes circulating T- and B-cells through antibody-dependent cellular cytolysis and complement-mediated lysis. Alemtuzumab was originally indicated for second-line treatment of chronic lymphocytic leukemia (CLL), cutaneous T-cell lymphoma (CTCL) and normal T-cell lymphoma under trade names Campath®, MabCampath® and Campath-1H®. Currently it is indicated for the treatment of multiple sclerosis as Lemtrada®. It is also applied for some conditioning regimens for bone marrow transplantation, kidney transplantation, and islet cell transplantation. Basic patents for Lemtrada® already expired in 2017. Learn more
Bevacizumab
Bevacizumab (Avastin®) is a humanized monoclonal IgG1/kappa antibody that inhibits vascular endothelial growth factor A (VEGF-A) and is used to treat various cancers including colorectal, lung, breast, kidney, and glioblastomas. Avastin® patents expired in 2019 in the US and will expire in the EU in 2022. Learn more
Cetuximab
Cetuximab (Erbitux®) is an epidermal growth factor receptor (EGFR) inhibitor indicated for the treatment of certain types of metastatic colorectal cancer, metastatic non-small cell lung cancer and head and neck cancer with or without radiotherapy or platinum-based chemotherapy. It is a chimeric mouse/human monoclonal antibody. The main patents for cetuximab expired in the EU in 2014 and in the US in 2016. Learn more
Denosumab
Denosumab (Prolia® Xgeva®) is a human monoclonal antibody indicated for the treatment of patients with osteoporosis at high risk for fracture, giant cell tumor of bone, hypercalcemia in malignancy and for the prevention of skeletal-related events in patients with bone metastases from solid tumors. It is the first FDA approved receptor activator of nuclear factor kappa-B ligand (RANKL) inhibitor. RANKL has been identified to affect the immune system and control bone regeneration and remodeling. Expiry dates of basic Prolia® patents related to the antibody and treatment of patients range from 2017 to 2023 in US and from 2017 to 2021 in EU. Learn more
Eculizumab
Eculizumab (Soliris®) is a humanized monoclonal antibody. It binds to the complement component 5 (C5), which is a terminal molecule in the complement cascade. Eculizumab inhibits the cleavage of C5 by C5 convertase into C5a and C5b and subsequent generation of the terminal complement attack complex C5b-9. Paroxysmal nocturnal hemoglobinuria (PNH) patients are deficient in terminal complement inhibitors. Eculizumab thus inhibits terminal complement mediated intravascular hemolysis and therefore the destruction of erythrocytes. Soliris® is indicated for treatment of patients with PNH to reduce hemolysis. It is also indicated for treatment of patients with atypical haemolytic uremic syndrome (aHUS) to inhibit complement mediated thrombotic micro-angiopathy. Patents on Soliris® will expire in USA in 2021 and in Europe in 2020. Learn more
Golimumab
Golimumab (Simponi®) is a fully human anti-tumor necrosis factor (TNF)-α IgG1қ monoclonal antibody. Simponi® is indicated in adults as an adjunct to methotrexate treatment for rheumatoid arthritis, alone or as an adjunct to methotrexate treatment for active psoriatic arthritis and as a single agent for active ankylosing spondylitis and ulcerative colitis. Patents for Simponi® will expire in 2024 in US as well as in EU. Learn more
Infliximab
Infliximab (Remicade®) is a chimeric (mouse/human) IgG1/kappa monoclonal antibody. Like etanercept and adalimumab, infliximab is a TNF-α blocker. Remicade® is indicated for treatment of Crohn’s disease, psoriatic arthritis, ulcerative colitis, psoriasis, ankylosing spondylitis, and rheumatoid arthritis used together with methotrexate. The main patent of Remicade® expired in 2015 (EU) and in US in 2018. J&J (Janssen Biotech), the owner of the originator molecule is trying to delay the market entry of biosimilars with additional patents, however, is struggling to defend their validity at court. Learn more
Ipilimumab
Ipilimumab (Yervoy®) is targeting the immune checkpoint T-lymphocyte-associated protein 4 (CTLA-4). It was the first immune checkpoint inhibitor to be approved for the treatment of cancer. Yervoy® is indicated for unresectable or metastatic melanoma, as an adjuvant in the treatment of cutaneous melanoma, to treat microsatellite-high or mismatch repair deficient metastatic colorectal cancer, hepatocellular carcinoma, and in combination with nivolumab (Opdivo®) for advanced renal cell carcinoma. Yervoy® patents will expire in the US in 2023 and in the EU in 2021. Learn more
Natalizumab
Natalizumab (Tysabri®) is a humanized monoclonal IgG4 antibody directed against α4 integrin, a cellular adhesion molecule. It is the first antibody in the class of selective adhesion molecule inhibitors. Tysabri® is indicated as monotherapy for treatment of relapsing forms of multiple sclerosis (MS) and in adult patients with moderately to severely active Crohn’s disease (CD) with evidence of inflammation, which have had an inadequate response or intolerance to conventional CD therapies. The Tysabri® patents expired in 2015 in the EU as well as in the US. Learn more
Nivolumab
Nivolumab (Opdivo®) is a fully human monoclonal IgG4 antibody. Nivolumab blocks programmed cell death ligand 1 or 2 (PD-L1 or PD-L2) from binding to PD-1, a protein on the surface of activated T cells. Opdivo® is indicated, among other cancer types, as a first- or second- line treatment for inoperable or metastatic melanoma. This includes advanced non-small cell lung cancer, metastatic melanoma, advanced renal cell carcinoma, squamous cell carcinoma of the head and neck. Several patent families are filed, with expiration dates of up to 2027 in US and 2026 in EU. Learn more
Omalizumab
Omalizumab (Xolair®) is a recombinant humanized IgG1 kappa monoclonal antibody, which binds to free human immunoglobulin E (IgE) and to membrane-bound form of IgE (mIgE) on the surface of mIgE-expressing B lymphocytes. Xolair® is indicated for moderate to severe persistent asthma and for chronic idiopathic urticaria in patients who remain symptomatic despite H1 antihistamine treatment. Key patents on Xolair® already expired in 2017. Learn more
Pembrolizumab
Pembrolizumab (Keytruda®) is a humanized monoclonal IgG4 antibody and is targeted to the cellular programmed cell death protein -1 (PD-1). Programmed cell death ligand 1 or ligand 2 (PD-L1 or PD-L2) is upregulated on 40–50 % of melanomas and has limited expression otherwise. Both ligands bind to PD-1, a protein on the surface of activated T-cells. If PD-L1 binds to PD-1, a T-cell becomes inactive and inhibited from attacking a tumor.The inhibitory effect results from promotion of apoptosis in antigen specific T cells while simultaneously blocking apoptosis in suppressor T-cells. Pembrolizumab binds to PD-1, thus blocks PD-L1 or PD-L2 from binding to PD-1, and T-cells can again attack tumor cells. Keytruda® is indicated for, among other cancer types (more than 30 indications), melanoma, non-small cell lung cancer, head and neck squamous cell cancer, classical Hodgkin lymphoma, gastric cancer, cervical cancer, hepatocellular carcinoma, and primary mediastinal large B-cell lymphoma. Patents for Keytruda® have expiry dates of up to 2036 in US and 2028 in EU. Learn more
Pertuzumab
Pertuzumab (Perjeta®) is a recombinant humanized monoclonal antibody that targets the dimerization domain II of human epidermal growth factor 2 (HER2) expressed on the cell surface. When HER2 is over-induced and dimerized with HER3, cell growth accelerates, which can lead to tumor formation. Whereas similar mAb trastuzumab binds to domain IV of the extracellular segment of HER2 receptor, pertuzumab binds to domain II located on the opposite side. Dimerization of HER2 / HER3 and activation of signaling pathways is thus prevented. Perjeta® is approved in combination with Herceptin® (trastuzumab) and docetaxel chemotherapy for the treatment of HER2-positive metastatic breast cancer not received prior anti-HER2 therapy or chemotherapy for metastatic disease. Patent expiry for Perjeta® will be in 2026 (US) and 2024 (EU). Learn more
Ramucirumab
Ramucirumab (Cyramza®) is a fully human monoclonal IgG1 / kappa antibody. Similar to bevacizumab, ramucirumab inhibits angiogenesis (formation of new blood vessels) by binding to a specific epitope on the extracellular domain of vascular endothelial growth factor receptor -2 (VEGFR-2) and blocking the interaction of VEGF-A, VEGF-C, or VEGF-D with its receptors. Cyramza® is indicated for gastric cancer, gastro -oesophageal junction adeno- carcinoma, metastatic colorectal cancer, non-small cell lung cancer that has spread to other parts of the body or in patients whose cancer involves mutations in EGFRs, and hepatocellular carcinoma in patients with a high blood level of alpha fetoprotein. Cyramza® patents will expire in the US in November 2025 and in the EU in May 2023. Learn more
Ranibizumab
Ranibizumab (Lucentis®) is a humanized monoclonal antibody fragment created from the same parent mouse antibody as bevacizumab. It is indicated for the treatment of neovascular (wet) age-related macular degeneration, macular edema following retinal vein occlusion, diabetic macular edema, diabetic retinopathy, and myopic choroidal neovascularization. Ranibizumab binds to the receptor binding site of active forms of vascular endothelial growth factor A (VEGF-A), including the biologically active, cleaved form of this molecule, VEGF110. The binding of ranibizumab to VEGF-A prevents the interaction of VEGF-A with its receptors (VEGFR1 and VEGFR2) on the surface of endothelial cells, reducing endothelial cell proliferation, vascular leakage, and new blood vessel formation. The patents on Lucentis® will expire in the US in 2020 and in the EU in 2022. Learn more
Rituximab
Rituximab (Rituxan®, MabThera®) is a chimeric IgG1/kappa monoclonal antibody targeting CD20, which is primarily found on the surface of B -cells. Rituximab destroys both normal and malignant B -cells that have CD20 on their surfaces, and is therefore used to treat diseases, which are characterized by having too many overactive or dysfunctional B -cells. Rituxan® is applied for treatment of many lymphomas and leukemias, transplant rejection and some autoimmune disorders. Rituxan® is also used off-label to treat difficult cases of multiple sclerosis, systemic lupus erythematosus and autoimmune anemias. Rituxan® patents expired in 2013 in the EU and in 2016 in the US. Learn more
Tocilizumab
Tocilizumab (Actemra®) is a recombinant humanized IgG1 monoclonal antibody targeting the interleukin-6 receptor (IL-6R). Tocilizumab recognizes both the membrane-bound and the soluble form of IL-6R and thus is able to block IL-6 functions. Actemra / RoActemra® is indicated for rheumatoid arthritis, active poly-articular, juvenile idiopathic arthritis, giant cell arteritis, cytokine release syndrome, and systemic sclerosis. In Japan, it is also approved for treatment of Castleman’s disease. The patents on Actemra/RoActemra® expired in US in 2015 and in Europe in 2017. Learn more
Trastuzumab
Trastuzumab (Herceptin®) is a humanized monoclonal antibody that interferes with the human epidermal growth factor 2 (HER2)/neu receptor. The HER2 pathway promotes cell growth and cell division via HER2 receptor. When HER2 is over-induced and dimerized, cell growth accelerates, which can lead to tumor formation. Trastuzumab binds to domain IV of the extracellular segment of HER2 receptor preventing it from dimerization and activation of its signaling pathways. Herceptin® is indicated for the treatment of HER2-positive metastatic breast cancer patients. It is also approved for adjuvant treatment of HER2 over-expressing breast cancer and metastatic gastric cancer. Primary patents for Herceptin® expired in 2014 in EU and in US in 2019. Learn more
Ustekinumab
Ustekinumab (Stelara®) is an IgG1 kappa human monoclonal antibody. Ustekinumab blocks interleukin IL-12 and IL-23, which activate T helper cells (Th cells). Specifically it is targeting the p40 shared subunit of IL-12 and IL-23, which subsequently cannot bind to their distinct receptors. Stelara® is indicated for treating patients with moderate to severe plaque psoriasis, and also to treat active psoriatic arthritis alone or with methotrexate. In 2016, it was also approved to treat Crohn’s disease. The patent protection for Stelara® will be until 2023 in US and 2024 in EU. Learn more