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Pharmacy > Oncology Med Chem Pharmacology > Flashcards

Oncology Med Chem Pharmacology Flashcards

0
Q

-tinib

A

Small molecule
Enzyme kinase inhibitor
Modifies cellular signaling

Chemical synthesis
100% pure defined structure
Can take orally

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1
Q

Targeted (signal based) therapies

HAG SINS TTZ

A 
Herceptin
Avastin
Gleevec
Sutent 
Iressa 
Nexavar 
Sprycel 
Tarceva 
Tykerb 
Zactima
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2
Q

-mab

A

Monoclonal antibody
Biologic

Works on receptor to modulate cell signaling

Living cells and cell lines
Heterogenous complex structure
Injected
Less stable and sensitive to denaturation

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3
Q

Purines

A

Two rings fused

Guanine
Adenine purines

2GAPurines

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4
Q

Pyrimidines

A

One ring

1CT pyramid

Cytosine
Thymine

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5
Q

Guanine

GC3

A

Double bond O purine
3 Hbonds
ONN

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6
Q

Adenine

A

3 nitrogen purine

2 Hbonds

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7
Q

Cytosine

A

Double bond O Pyrimidine
3 Hbond
ONN

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8
Q

Thymine

A

Two double bond O pyrimidine

2 Hbonds

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9
Q

Go

A

Growth factors - EGF, VEGF

Oncogenes - ras

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10
Q

Stop

A

Tumor suppressor genes

P53

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11
Q

Purine biosynthesis

GGACT

A 
Glycine
Glutamine
Aspartic acid
Cofactor THF
CO2
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12
Q

6-MPRP

Mercapto-purine-ribose-phosphate

A

From 6-MP prodrug

Deplete PRPP stores
InosineMP mimic

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13
Q

Methotrexate

A

Works and interferes wherever THF cofactors is active

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14
Q

Purine antagonists

A

Fake nucleoside mimic

Competitively inhibit DNA polymerase

Vidarabine
Fludrabine
Cladribine

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15
Q

Pentostatin

A

Adenosine Deaminase (ADA) inhibitor

Transition state analog mimic

Prevent breakdown of vidarabine and other nucleoside mimics

Adjunct therapy

16
Q

Xanthine oxidase inhibitor

A

Inhibit xanthine (from guanine and adenine) from oxidizing to Uric acid and causing gout

17
Q

Tumors with high EGFR expression

A

NSCLC - non-small cell lung cancer
Prostate
Gastric

Breast - HER2 human EGFR

18
Q

HER2

A

Human EGFR,

Active as homodimer

Herceptin (trastuzumab) flags for immune cell destruction and blocks downstream HER2 signaling by preventing dimerization of HER receptors

19
Q

Iressa and tarceva

A

EGFR kinase antagonists with common anikinoquinazoline skeleton

Affinity and compete for ATP-binding site

Tarceva has key water molecule interaction

20
Q

Gleevec

A

Bind and stabilize an inactive form

21
Q

Gleevec resistance mutation

A

Threonine 315 to isoleucine 315

ATP can displace gleevec easier

22
Q

Iressa resistance mutation

A

Threonine to methionine

23
Q

Nilotinib

A

Designed against amino acid resistance

Backup for gleevec resistant tumors

24
Q

Zolinza

A

HDAC inhibitor: Epigenetic target

Acetyl makes lysine neutral and loosens histone grip on DNA: more transcription of p53

Lysine is normally positive without Acetyl and binds tightly to DNA

25
Q

Interchangeable biosimilar

A

FDA determined safe for substitution

26
Q

Glycine

A

Only amino acid with no chirality

27
Q

Mizoribine

A

IMP dehydrogenase inhibitor

Blocks XMP/guanine nucleotide synthesis

28
Q

Mycophenolate

A

IMP dehydrogenase inhibitor and

GMP synthetase inhibitor

29
Q

ADA

A

Amine to double bond O

Deactivated purine antagonists

SCID = ADA deficiency & lymphocyte destruction

30
Q

Gout

A

Excess (AMP/GMP) purine catabolism

Or deficient HGPRT salvage pathway (inosine gets deaminated and later forms Uric acid)

31
Q

Von gierks disease

A

Increase G6phosphatase
Increase PRPP for purine biosynthesis
Excess Uric acid production

32
Q

Purine metabolism disorders

A

Increases PRPP synthetase
PRPP amido transferase
Defective HGPRT
Increase G6phosohatase

33
Q

Leech-Nyhan Syndrome

A

HGPRT deficiency

34
Q

Febuxostat

A

Selective XO inhibitor
Non purine

Less interactions and side effects than allopurinol

35
Q

Allopurinol

A

Nonselective XO inhibitor

Purine analog

36
Q

Rate limiting step of purine biosynthesis

A

PRPP to PRA

Inhibited by 6MPRP

Pharmacy (63 decks)

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