Monoclonal Ab's Flashcards
Abatacept
CTLA4 fusion protein –> blocks CD80/CD86 –> prevents binding of T cell CD28 to APC CD80/CD86 –> prevents T cell activation RA
Anakinra
Recombinant form of human IL-1 Autoinflamm diseases, refractory RA
Nivolimab
PD-1 antibody –> binds PD-1 on T cells to prevent binding with PD-L1 from tumour cells –> reactivation of tumour T cells
Co-stimulatory pathway modulators
Abatcept, Ipilimumab CTLA4 pathway Nivoliumab, Pembrolizumab PD-1 antibody Atezolizumab, Tixolinumab PD-L1 antibody
Mepolizumab
IL-5 antibody Severe refractory eosinophilic asthma
Atezolizumab
PD-L1 antibody –> binds PD-L1 on tumour cells to prevent binding with PD-1 from T cells –> reactivation of tumour T cells
Rituximab
CD20 antibody Removes B cells from circulation for 6-9/12 Haematological malignancies, RA, SLE, immune thrombocytopaenia, autoimmune haemolysis, ANCA vasculitis, cryoglobulinaemia, MS, pemphigus
Ipilimumab
CTLA4 blcoker –> prevents binding of T cell CTLA4 to APC CD80/CD86, but maintains T cell stimulation Melanoma, prostate Ca, lung Ca
Golimumab
TNF-alpha
Tocilizumab
IL-6 antibody Refractory RA
Idarucizumab
Monoclonal antibody binds to Dabigatran & metabolites with very high affinity (300x affinity of dabigatran) Dabigatran reversal agent for life threatening bleeding or emergency surgery
Lorlatinib
EML4-ALK inhibitor (3rd generation) AML4/ALK = aberrant active fusion protein present in ~5% of lung adenoCa Non-curable EML4/ALK positive lung adenoCa This is now standard of care, superior to crizotinib
Sorafenib
Multi-kinase inhibitor: Raf signalling, VEGF, PDGF, C-kit HCC
Dasatanib
BCR-Abl inhibitor
BCR-Abl positive CML
GIST Disease progression on imatinib
Natalizumab
Alpha-4 integrin antibody –> blocks T cell entry into brain and gut (Brain homing T cells express alpha-4-beta-1 which binds VCAM-1 expressed on brain endothelium) Multiple sclerosis, Crohn’s
EML4-ALK inhibitors
Crizotinib (1st generation) Ceritinib (2nd generation) Alectinib (2nd generation) Lorlatinib (3rd generation)
Traztuzumab
HER2 Inhibits ligand independent HER2 signalling by preventing dimerization of HER2 R –> cell mediated cytotoxicity HER2+ breast Ca (Herceptin)
Benralizumab
IL-5 R antibody –> blocks Th2 pathway Asthma
Pembrolizumab
PD-1 antibody –> binds PD-1 on T cells to prevent binding with PD-L1 from tumour cells –> reactivation of tumour T cells
Crizotinib
EML4-ALK inhibitor (1st generation) AML4/ALK = aberrant active fusion protein present in ~5% of lung adenoCa Non-curable EML4/ALK positive lung adenoCa
Infliximab
TNF-alpha
Dabrafenib
BRAF V600E inhibitor Melanoma (BRAF V600E mutation seen in up to 80% of melanoma)
Certolizumab
TNF-alpha
Sunitinib
VEGF inhibitor
Metastatic renal cell Ca
Bevacizumab
VEGF antibody Metastatic CRC in combination with chemo
Basiliximab
IL-2 R antibody Renal transplant
TNF-alpha immunotherapies
Infliximab, Adalimumab, Certolizumab, Golimumab
Monoclonal Ab’s against TNF-alpha Etanercept Soluble TNF-alpha receptor
Nilotinib
BCR-Abl inhibitor BCR-Abl positive CML GIST Disease progression on imatinib
Etanercept
Soluble TNF-alpha receptor
Vemurafenib
BRAF V600E inhibitor Melanoma (BRAF V600E mutation seen in up to 80% of melanoma)
Adalimumab
TNF-alpha
Daclizumab
IL-2 R antibody Renal transplant
EGFR therapies
Erlotinib (1st generation, reversible) Gefitinib (1st generation, reversible) Afatinib (2nd generation, irreversible) Osimertinib (3rd generation)
Incurable EGFR positive lung adenoCa Cetuximab (antibody against EGFR) Metastatic CRC, KRAS, BRAF wild type only Head and neck Ca NSCLC
Eculizumab
Antibody to C5 of complement cascade Paroxysmal nocturnal haemoglobinuria
Tixolinumab
PD-L1 antibody –> binds PD-L1 on tumour cells to prevent binding with PD-1 from T cells –> reactivation of tumour T cells
Secukinumab
IL-17 antibody –> blocks Th17 activation Psoriasis, PA, AS Makes Crohn’s worse
Vedolizumab
Alpha-4-beta-7 ntegrin antibody –> blocks T cell entry into gut (Gut homing T cells express alpha-4-beta-7 which binds MadCAM expressed on gut endothelium) IBD - Crohn’s, UC
Omalizumab
IgE antibody –> blocks Th2 pathway Severe allergic asthma Chronic spontaneous urticaria
Ustekinumab
Binds p40 subunit of IL-12 & IL-23 –> blocks Th1 and Th17 activation Psoriasis, PA, AS, ?Crohn’s
Ceritinib
EML4-ALK inhibitor (2nd generation) AML4/ALK = aberrant active fusion protein present in ~5% of lung adenoCa Non-curable EML4/ALK positive lung adenoCa Brain mets on crizotinib (higher brain penetration)
Imatinib
BCR-Abl inhibitor BCR-Abl positive CML GIST