Drugs Flashcards

1
Q

Introduced in 2012 for melanoma, 85,000 eur for treatment,not a life-saving, curative drug

A

Ipilimumab

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2
Q

Monoclonal antibody, first in-class drug, acts on Il-4 and Il-13 signalling, modulating Thelper 2-type responses. Approved for dermatitis, asthma, COPD, various inflammatory and allergic diseases

A

Dupiliumab

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3
Q

Newer version of Rituximab, andti-CD20 mAb, fully humanised, for relapsing and primary progressive MS

A

Ocrelizumab

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4
Q

Body produces anti-mAbs in response to foreign mAbs

A

HAMA response

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5
Q

Components of a chimeric Ab

A

Fab: foreign species, Fc: human, overall 2/3 human

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6
Q

Components of a humanised Ab

A

Only CDR is foreign, results in 95% human

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7
Q

Components of a human Ab

A

Entirely Human

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8
Q

Group I Biotherapeutics

A

Assoc with metabolic and endocrine disease e.g. insulin, clotting factors viii and ix

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9
Q

Group III Biotherapeutics

A

Protein vaccines e.g. HPV vaccine

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10
Q

Group IV Biotherapeutics

A

Protein Diagnostics e.g. GHRH to diagnose defective GH secretion, anti-PSA antibody for prostate cancer

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11
Q

Group IIa Biotherapeutics

A

Interfere with a molecule/protein

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12
Q

Group IIb Biotherapeutics

A

Delivering other compounds/proteins

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13
Q

chimeric IgG1 mAb that binds to and neutralises TNF-a, used in treatment of RA and Crohn’s Disease

A

Infliximab

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14
Q

mAb, binds to integrins blocking VCAM-1 interaction, used in MS

A

Natalizumab

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15
Q

Humanized mAb that binds VEGF, used in CRC

A

Bevacizumab

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16
Q

Chimeric mAb against CD20, used in Non-Hodgkin’s Lymphoma and RA, depletes B cell populations

A

Rituximab

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17
Q

Type IIB Biotherapeutic, Humanized anti-CD33 antibody, conjugated to calicheamicin, used to treat acute myeloid leukaemia, very serious liver disease as a result, withdrawn by FDA

A

Gemtuzumab ozogamicin (Mylotarg)

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18
Q

Type IIB Biotherapeutic, Antibody-Drug Conjugate. Employs very cytotoxic agent. Ant-CD30 Ab. Used in Hodgkin’s lymphoma and anaplastic large cell lymphoma. Antibody conjugated to Auristatin drug MMAE

A

Brentuximab verdotin

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19
Q

Human mAb, , anti-TNF-a, used in RA

A

Adalimumab/ golimumab

20
Q

TNF receptor and Fc fusion protein (IgG1), Anti-TNF, used in RA

A

Etanercept

21
Q

Anti-TNF, Pegylated, humanized antibody Fab fragment, used in RA

A

Certolizumab Pegol

22
Q

Anti-IL1 R, used in RA

A

Anakinra

23
Q

CTLA-4 -Fc Fusion protein, used in RA, modulates T cell co-stimulatory pathway

A

Abatacept

24
Q

Anti-IL6 R, used in RA

A

Tocilizumab

25
Q

Used in treatment of melanoma, small molecule kinase inhibitor, targets BRAF mutation (V600E)

A

Vemurafenib

26
Q

Used in treatment of Basal cell carcinoma, small molecule kinase inhibitor, binds to extracellular domain of SMO to inactivate, in cancer where there is a PTCH1 deficiency (dysregulation of Hedgehog pathway)

A

Vismodegib

27
Q

Small molecule kinase inhibitor that is approved for ErbB2 positive breast cancer, works intracellularly to inhibit the downstream MAP3K and PI3K pathways

A

Lapatinib

28
Q

Monoclonal antibody that binds to extracellular domain of ErbB2, used in HER2 positive breast cancer, recruits NK cells and induces ADCC

A

Transtuzumab

29
Q

Humanised mAb that binds to domain II of HER2 receptor inhibiting receptor dimerisation and thus preventing downstream signalling. Used in HER2 positive breast cancer

A

Pertuzumab

30
Q

p95HER2

A

A truncated and very active form of HER2, targeted by Trastuzumab Emtansine

31
Q

Maytansine Derivative

A

DM1 is a maytansinoid, antimitotic, inhibits microtubule assembly leading to apoptosis

32
Q

Example of an Antibody Drug Conjugate (ADC) used in HER2-positive breast cancer.

A

Trastuzumab Emtansine (T-DM1)

33
Q

Chemotherapeutic agents that once chlorine group leaves, forms highly reactive product that binds to N-7 of guanine and forms cross-links, interrupting DNA replication

A

Alkylating Agents: Busulfan, Cyclophosphamide

34
Q

Chemotherapeutic: Folic Acid analogue, inhibits dihydrofolate reductase, used in RA in smaller doses.

A

Methotrexate

35
Q

Minimises toxicity of Methotrexate

A

Folinic Acid

36
Q

Purine analogue. important for childhood leukaemia

A

6-Mercaptopurine

37
Q

Drug that interrupts xanthine oxidase, patients on this drug need to be given a lower dose of xanthine oxidase

A

Allopurinol (Gout)

38
Q

Pyrimidine Analogue, ‘thymineless death’, short half-life

A

5-fluorouracil

39
Q

Topoisomerase I inhibitor, Topo I relieves torisonal strain in DNA, these drugs stop re-ligation happening, increases sensitivity to radiotherapy

A

Irinotecan, Topotecan

40
Q

Binds to Topoisomerase II, involved in coiling/uncoiling DNA

A

Etoposide

41
Q

Platinum analog, acts similarly to alkylating agent. Used in lung, ovarian, testicular cancer. Most toxic of Platinum analouges (Emetic, nephrotoxicity, ototoxicity)

A

Cisplatin

42
Q

Platinum analog used in lung, ovarian, testicular cancer

A

Carboplatin

43
Q

Platinum analog used in colorectal cancer

A

Oxilaoplatin

44
Q

Bind to tubulin, inhibit microtubule formation, cell undergoes apoptosis

A

Vinca alkaloids (Vincristine. Vinblastine)

45
Q

Anti-tumour Abx, particualr axample can work as Topoisomerase I inhibitor, can intercalate DNA

A

Anthracyclines e.g .Doxorubicin (also Daunorubicin, Bleomycin)

46
Q

Prevent microtubules from dissembling, cell become clogged up with microtubules

A

Taxanes: Paclitaxel, Doxetaxel (Semi-synthetic derivative)