08 - Chemotherapy

Question 1

enfuvirtide

Answer 1

fusion inhibitor
gp41 blocker
target step: attachment to host

Question 2

AZT (zidovudine)

Answer 2

NRTI (nucleotide reverse transcription inhibitor)
thymidine analog
target step: reverse transcription

Question 3

lamivudine

Answer 3

NRTI (nucleotide reverse transcription inhibitor)
cytidine analog
target step: reverse transcription

Question 4

nevirapine

Answer 4

NNRTI (non-nucleotide reverse transcription inhibitor)
allosteric modulation
targets step: reverse transcription

Question 5

indinavir

Answer 5

protease inhibitor
competitive inhibitor for active site
target step: maturation of virons

Question 6

penicillin

Answer 6

cell wall synthesis inhibitor (bactericidal)
beta-lactams
block transpeptidase

Question 7

vancomycin

Answer 7

cell wall synthesis inhibitor (bactericidal)
non-beta-lactams
block peptidoglycan synthesis

Question 8

tetracycline

Answer 8

protein synthesis inhibitor (bacteriostatic)

inhibit 30S ribosome subunit

Question 9

chloramphenicol

Answer 9

protein synthesis inhibitor (bacteriostatic)

inhibit 50S ribosome subunit

Question 10

sulfonamides

Answer 10

folate synthesis inhibitor (bacteriostatic)

competes with PABA

Question 11

metronidazole

Answer 11

nucleic acid synthesis inhibitor (bacteriocidal)

Question 12

quinolones

Answer 12

nucleic acid synthesis inhibitor (bacteriocidal)

Question 13

polymyxins

Answer 13

increases cell permeability (bacteriocidal)

Question 14

cisplatin

Answer 14

alkylating agents
DNA intercalators
inhibit DNA replication

Question 15

5-FU (5-fluorouracil)

Answer 15

anti-metabolites
pyrimidine analog (also folate, purine)

Question 16

tamoxifen

Answer 16

hormone-related therapy
inhibit estradiol binding to estrogen receptor (ER)
treat ER-positive breast cancer

Question 17

degarelix

Answer 17

hormone-related therapy
LHRH (luteinizing hormone-releasing hormone) antagonist
treat prostate cancer

Question 18

flutamide

Answer 18

hormone-related therapy
anti-androgen
treat prostate cancer

Question 19

cetuximab

Answer 19

Targeted therapy
molecular target: EGFR (proto-oncoprotien)

blocker (monoclonal antibody)
inhibit function of proliferation; survival; anti-apoptosis; metastasis

treat recurrent head and neck cancer

Question 20

avastin

Answer 20

Targeted therapy
molecular target: VEGF (activator of angiogenesis pathway)

neutralizes VEGF

treat colorectal cancer

Question 21

Sutent

Answer 21

Targeted therapy
molecular target: VEGF (activator of angiogenesis pathway)

VEGF receptor blocker

treat renal cell carcinoma; pancreatic cancer; GI stromal tumour

Question 22

lapatinib

Answer 22

Targeted therapy / Precision medicine
molecular target: HER2/Neu

competitive blocker at ATP-binding site of the over-expressed HER2 receptor kinase kinase
inhibit function of proliferation and survival

treat breast cancer

Question 23

gefitinib (Iressa)

Answer 23

Precision medicine
molecular target: EGFR (proto-oncoprotien)

blocker at ATP-binding site of EGFR
inhibit phosphorylation (activation)
inhibit function of proliferation; survival; anti-apoptosis; metastasis
induce senescence

resistance

1) mutation in EGFR
2) other genomic events activate EGFR signalling

treat NSCLC (with EGFR activation)

Question 24

vemurafenib

Answer 24

Precision medicine
molecular target: B-raf
BRAF V600E (proto-oncogene)

B-raf inhibitor
inhibit function of growth; metastasis

treat (BRAF-mutated) metastatic melanoma

Question 25

olaparib

Answer 25

Precision medicine
target pathway: BRCA1/2 (anti-oncogene)

resistance in short time

treat (BRCA-mutated) ovarian cancer

Question 26

ATRA

combination therapy with ATO (arsenic trioxide)

Answer 26

Differentiation therapy

induces differentiation and proliferation of myeloblasts,
which is blocked at promyelocyte stage

treat acute promyelocytic leukaemia (APL)