MABs Flashcards

1
Q

Adalimumab: target and disease

A

TNF alpha antagonist
RA, Psoriatic Arthritis, Ank Spondylitis
Crohn’s Disease, Ulcerative Colitis

Contraindicated in MS; CCF NYH class III-IV; LVEF <50%

AE: exacerbation / change in psoriasis; development of autoantibodies (i.e. SLE), malignancy

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2
Q

Afatinib: Target and disease

A

EGFR inhibitor

NSCLC with EGFR mutations

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3
Q

Alemtuzumab: Target and disease

A

Anti CD52
MS, CML, cutaneous T cell lymphoma, transplant induction

AE: profound lymphopenia >12months, Autoimmune Thrombocytopenia, Infusion related reactions

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4
Q

Anakinra:target and disease

A

IL-1 blockade
RA, Still’s Disease
Cryopyrin-associated periodic syndromes e.g. familial cold auto-inflammatory syndrome

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5
Q

Axitinib: target and disease

A

VEGF mainly

2nd line RCC

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6
Q

Basiliximab: target and disease

A

Anti-IL2R — AntiCD25
antibody against IL-2 receptors expressed on activated T lymphocytes; blocks binding of IL-2, inhibiting T cell activation
Renal transplant

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7
Q

Belatacept: target and disease

A

CTLA4 fused with Fc, blocks T cell co-stimulation

Renal transplant

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8
Q

Abciximab: target and disease

A

Platelet gpIIb/IIIa
IgG antibody directed against glycoprotein receptors on the surface of platelets. Prevents fibrinogen from binding to activated platelets
High risk patients for developing re-stenosis post coronary angioplasty

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9
Q

Belimumab: target and disease

A

Anti-BlyS / BAFF on B cells
BlyS = B lymphocyte stimulator protein
Reduces B cell survival and differentiation into immunoglobulin producing plasma cells

Indication: Active auto antibody positive SLE

AE: depression / mood disorders

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10
Q

Benralizumab: target and disease

A

Anti-IL5R (CD125)
Blocks IL-5 receptor (expressed on eosinophils and basophils), reducing the production and survival of eosinophils. Also induces eosinophil apoptosis
Severe refractory eosinophilic asthma

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11
Q

Bevacizumab: Target and disease

A

Anti-VEGF
Inhibits formation of new blood vessels, reducing vascularisation and growth of tumours
Solid organ cancer (colorectal, ovarian CNS), proliferative diabetic retinopathy

AE: HTN, GN, poor wound healing, thrombosis

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12
Q

Beziotoxumab: target and disease

A

Anti-C. Diff Toxin B

C. Diff

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13
Q

Blinatumomab: target and disease

A

Bi-specific T cell engaging antibody
Engages CD3 on T-cell to CD19 on B cell
ALL relapse

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14
Q

Bortezomib: target and disease

A

Proteasome inhibitor
Multiple myeloma

AE: neuropathy, thrombocytopenia

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15
Q

Brentuximab: target and disease

A

Anti-CD30

Hodgkin’s

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16
Q

Brodalumab: target and disease

A

Anti-IL17R

Psoriasis

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17
Q

Canakinumab: target and disease

A

Anti-IL1 beta
Cryopyrin associated periodic syndromes
RA
Gout

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18
Q

Certolizumab: target and disease

A

Anti-TNF
RA, Psoriatic arthritis, Ank spondylitis, plaque psoriasis
Crohn’s
Does NOT cross the placenta

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19
Q

Cetuximab: target and disease

A
Endothelial Growth Factor Receptor (EGFR) inhibitor 
Metastatic CRC (KRAS or NRAS wild type)
Head and neck SCC

AE: acneiform rash, diarrhoea, ILD, conjunctivitis

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20
Q

Denosumab: target and disease

A

RANK-L inhibitor
Prevents RANKL binding to its receptor (RANK) on the osteoclast surface. Osteoclast formation, function and survival is disrupted = decreased bone resorption and increased bone mass
Osteoporosis

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21
Q

Eculizumab: target and disease

A

Anti-C5 ( blocks cleavage of C5 into C5a)
Atypical HUS, PNH, membroproliferative GN, neuromyelitis optica

MUST be meningococcus vaccinated
AE: meningitis

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22
Q

Icatibant: target and disease

A

Bradykinin-2 receptor antagonist
Anticipated emergency treatment of an acute attack of hereditary angioedema

PBS: patient must have confirmed diagnosis of C1-esterase inhibitor deficiency

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23
Q

Infliximab: target and disease

A

Anti TNF alpha

First line treatment in Crohn’s; Ulcerative Colitis

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24
Q

Eltrombopag: target and disease

A

TPO receptor agonist

ITP

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25
Eriotinib: target and disease
EGFR inhibitor NSCLC AE: acne, diarrhoea, pneumonitis, hepatitis
26
Evolocumab: target and disease
PCSK9 inhibitor Increases hepatic cholesterol uptake Hypercholesterolaemia
27
Etanercept: target and disease
TNF blockade | RA, psoriasis, ank spond
28
Everolimus: target and disease
mTOR blockade Prevents cell cycle progression and cytokine-induced T and B cell proliferation Breast cancer, neuroendocrine tumors
29
Golimumab: target and disease
``` Anti TNF RA (use with methotrexate) Psoriatic arthritis Non radiologic Ank Spond Ulcerative Colitis ```
30
Gefitinib: target and disease
EGFR inhibitor | NSCLC
31
Ibritumomab: target and disease
Anti-CD20 bound to radioisotope | Non Hodgkin’s
32
Ibrutinib: target and disease
BTK (Burton’s tyrosine kinase) inhibitor inhibitor-B cell CLL, Waldenstrom’s, Mantle Cell, chronic GVHD AE: AF, diarrhoea, platelet dysfunction, fluid retention
33
Imatinib: target and disease
Target: TKI Bar-Abl Fusion Protein (CML, ALL) C-kit mutations
34
Infliximab: target and disease
Anti TNF alpha | Crohn’s disease, Ulcerative Colitis
35
Ipilimumab: target and disease
CTLA-4 Binds to CTLA-4 resulting in an enhanced T cell mediated immune response which leads to tumor cell death Melanoma, Renal Cell Carcinoma
36
Ixekizumab: target and disease
Inhibits activity IL-17a | Plaque psoriasis, psoriatic arthritis
37
Ocrelizumab: target and disease
Anti-CD20 Primary Multiple Sclerosis Relapsing Multiple Sclerosis
38
Idarucizumab
Dabigatran reversal
39
Mepolizumab: target and disease
Anti IL-5 - reducing production and survival of eosinophils | Severe refractory eosinophilic asthma
40
Natalizumab: target and disease
Anti Alpha-4 beta-7 integrin Thought to inhibit leukocyte migration from blood into CNS, reducing inflammation demyelination MS
41
Omalizumab: target and disease
IgE Maintenance treatment of mod-severe allergic asthma Chronic idiopathic urticaria
42
Pembrolizumab: target and disease
PD1 Inhibits programmed death 1 (PD-1) receptor from binding to its ligands (PD-L1 and PD-L2) on tumor cells, reactivating cytotoxic T lymphocytes and anti-tumor immunity Melanoma NSCLC AE: immune related reactions - skin (itch, rash, vitiligo), endocrine (hypothyroid, T1DM), pneumonitis, colitis, autoimmune hepatitis, nephritis, uveitis
43
Rituximab: target and disease
Anti-CD20 Binds to CD20 on B lymphocytes In cancer starts an immune response that loses normal and malignant B cells In chronic inflammatory diseases (e.g. RA) suppresses immune response and inflammation by reducing T cell activation and resulting cytokine production AE: Hep B reactivation, hypergammaglobulinemia, PML
44
Secukinumab: target and disease
Anti IL-17A Chronic plaque psoriasis Active psoriatic arthritis
45
Sorafenib: target and disease
``` TKI Targets c-raf, VEGFR Renal cell cancer Hepatocellular cancer Differentiated thyroid cancer ```
46
Sunitnib: target and disease
TKI Targets VEGFR Renal Cell Carcinoma, pancreatic neuroendocrine tumor, GI stromal tumor
47
Trastuzumab: target and disease
HER2 Binds to human epidermal growth factor receptor 2 and inhibits the proliferation of tumor cells that over-express HER2. Also activates an immune response that loses tumour cells HER-2 positive cancers e.g. breast, gastric AE: cardiac failure
48
Ustekinumab: target and disease
Anti IL-12 and IL-23 | Psoriasis, psoriatic arthritis, Crohn’s
49
Levantinib: target and disease
Multikinase inhibitor Inhibits VEGFR, Platelet Derived Growth Factor Receptor (PDGFR), c-kit and RET proto-oncogene Thyroid cancer AE: hypertension
50
Abatacept: target and disease
CTLA4 bound to fc end of Ig = B7 blocker (CD80 / CD86) Prevents T cell activation
51
Nivolumab: target and disease
Anti-PD-1 Reactivates cytotoxic T cells and anti tumor immunity Metastatic Melanoma, NSCLC, SCC head and neck cancer, Hodgkin Lymphoma, HCC, RCC, bladder cancer
52
Tofacitinib: mechanism and disease
Jack 3 > 1 > 2 | RA, IBD, psoriasis, transplant rejection
53
Ruxolitinib: target and disease
Jak1 and Jak2 | Myeloproliferative diseases
54
Erenumab: target and disease
CGRP: calcitonin gene-related peptide Mediated trigemino-vascular pain transmission and vasodilatory component of neurological inflammation Indication: prevention of migraine
55
Tocilizumab: target and disease
Anti IL-6 RA, Giant Cell Arteritis AE: neutropenia, thrombocytopenia, increased risk of GI perforation (e.g diverticulitis)
56
Venetoclax: target and disease
Inhibits BCL-2 protein CLL BCL2 = anti apoptotic protein over expressed in CLL cells
57
Ocrelizumab: target and disease
Selectively depletes CD20 positive B lymphocytes | MS
58
Daratumumab
CD38 | Myeloma
59
Emicizumab
Binds to factors IXa and X simultaneously Brings these 2 molecules together- substitutes for the scaffold role of factor VIIIa as a cofactor for factor IXa in activating factor X. Prophylaxis for patients with Haemophilia A
60
Durvalumab
PD-L1 inhibitor | Advanced urothelial carcinoma
61
Osimertinib
T790M mutation in NSCLC
62
Ribociclib
Inhibits cyclin dependent kinase 4 and 6 | Advanced breast ca