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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
Q

Eriotinib: target and disease

A

EGFR inhibitor
NSCLC

AE: acne, diarrhoea, pneumonitis, hepatitis

26
Q

Evolocumab: target and disease

A

PCSK9 inhibitor
Increases hepatic cholesterol uptake
Hypercholesterolaemia

27
Q

Etanercept: target and disease

A

TNF blockade

RA, psoriasis, ank spond

28
Q

Everolimus: target and disease

A

mTOR blockade
Prevents cell cycle progression and cytokine-induced T and B cell proliferation
Breast cancer, neuroendocrine tumors

29
Q

Golimumab: target and disease

A 
Anti TNF
RA (use with methotrexate)
Psoriatic arthritis
Non radiologic Ank Spond
Ulcerative Colitis
30
Q

Gefitinib: target and disease

A

EGFR inhibitor

NSCLC

31
Q

Ibritumomab: target and disease

A

Anti-CD20 bound to radioisotope

Non Hodgkin’s

32
Q

Ibrutinib: target and disease

A

BTK (Burton’s tyrosine kinase) inhibitor inhibitor-B cell
CLL, Waldenstrom’s, Mantle Cell, chronic GVHD

AE: AF, diarrhoea, platelet dysfunction, fluid retention

33
Q

Imatinib: target and disease

A

Target: TKI
Bar-Abl Fusion Protein (CML, ALL)
C-kit mutations

34
Q

Infliximab: target and disease

A

Anti TNF alpha

Crohn’s disease, Ulcerative Colitis

35
Q

Ipilimumab: target and disease

A

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
Q

Ixekizumab: target and disease

A

Inhibits activity IL-17a

Plaque psoriasis, psoriatic arthritis

37
Q

Ocrelizumab: target and disease

A

Anti-CD20
Primary Multiple Sclerosis
Relapsing Multiple Sclerosis

38
Q

Idarucizumab

A

Dabigatran reversal

39
Q

Mepolizumab: target and disease

A

Anti IL-5 - reducing production and survival of eosinophils

Severe refractory eosinophilic asthma

40
Q

Natalizumab: target and disease

A

Anti Alpha-4 beta-7 integrin
Thought to inhibit leukocyte migration from blood into CNS, reducing inflammation demyelination
MS

41
Q

Omalizumab: target and disease

A

IgE
Maintenance treatment of mod-severe allergic asthma
Chronic idiopathic urticaria

42
Q

Pembrolizumab: target and disease

A

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
Q

Rituximab: target and disease

A

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
Q

Secukinumab: target and disease

A

Anti IL-17A
Chronic plaque psoriasis
Active psoriatic arthritis

45
Q

Sorafenib: target and disease

A 
TKI
Targets c-raf, VEGFR
Renal cell cancer
Hepatocellular cancer
Differentiated thyroid cancer
46
Q

Sunitnib: target and disease

A

TKI
Targets VEGFR
Renal Cell Carcinoma, pancreatic neuroendocrine tumor, GI stromal tumor

47
Q

Trastuzumab: target and disease

A

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
Q

Ustekinumab: target and disease

A

Anti IL-12 and IL-23

Psoriasis, psoriatic arthritis, Crohn’s

49
Q

Levantinib: target and disease

A

Multikinase inhibitor
Inhibits VEGFR, Platelet Derived Growth Factor Receptor (PDGFR), c-kit and RET proto-oncogene
Thyroid cancer

AE: hypertension

50
Q

Abatacept: target and disease

A

CTLA4 bound to fc end of Ig
= B7 blocker (CD80 / CD86)
Prevents T cell activation

51
Q

Nivolumab: target and disease

A

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
Q

Tofacitinib: mechanism and disease

A

Jack 3 > 1 > 2

RA, IBD, psoriasis, transplant rejection

53
Q

Ruxolitinib: target and disease

A

Jak1 and Jak2

Myeloproliferative diseases

54
Q

Erenumab: target and disease

A

CGRP: calcitonin gene-related peptide
Mediated trigemino-vascular pain transmission and vasodilatory component of neurological inflammation
Indication: prevention of migraine

55
Q

Tocilizumab: target and disease

A

Anti IL-6
RA, Giant Cell Arteritis

AE: neutropenia, thrombocytopenia, increased risk of GI perforation (e.g diverticulitis)

56
Q

Venetoclax: target and disease

A

Inhibits BCL-2 protein
CLL

BCL2 = anti apoptotic protein over expressed in CLL cells

57
Q

Ocrelizumab: target and disease

A

Selectively depletes CD20 positive B lymphocytes

MS

58
Q

Daratumumab

A

CD38

Myeloma

59
Q

Emicizumab

A

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
Q

Durvalumab

A

PD-L1 inhibitor

Advanced urothelial carcinoma

61
Q

Osimertinib

A

T790M mutation in NSCLC

62
Q

Ribociclib

A

Inhibits cyclin dependent kinase 4 and 6

Advanced breast ca

BPT Written (16 decks)

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