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Fall 2021: Therapeutics III > Additional Oncologic Agents (Wendt) > Flashcards

Additional Oncologic Agents (Wendt) Flashcards

1
Q

What are the two main problems associated with targeting RAS for direct inhibition?

A
  • RAS binds GTP at very low concentrations
  • allosteric sites on RAS have not been identified
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2
Q

Give an example of a KRAS G12C inhibitor.

A

Sotorasib (Lumakras)

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3
Q

Lumakras forms an irreversible, covalent bond with the ________ residue of KRAS G12C.

A

cysteine

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4
Q

What is absolutely required for indication of sotorasib?

A

identification of the G12C mutation via an FDA-approved test

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5
Q

Identify the drug based on its structure.

A

Sotorasib (Lumakras)

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6
Q

Beyond phosphorylation, what other posttranslational modifications (PTMs) can affect protein function?

A

acetylation and methylation

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7
Q

Acetylation of histones correlates with __________ activity.

A

transcriptional

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8
Q

Deacetylation of histones promotes the converesion of heterochromatin and prevents transcription of _______________.

A

tumor suppressor genes

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9
Q

Give an example of an HDAC inhibitor.

A

Romidepsin (Istodax)

*also vorinostat and belinostat*

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10
Q

What is romidepsin indicated for?

A

treatment of cutaneous and peripheral T-cell lymphoma in patients who have received at least one prior therapy

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11
Q

What is the most prevalent warning that should be given to patients taking Istodax?

A

infections (reactivation of DNA viruses)

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12
Q

True or false: romidepsin is a prodrug.

A

true

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13
Q

Give an example of an EZH2 inhibitor.

A

tazemetostat

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14
Q

What does EZH2 do?

A

methylates histones leading to the repression of tumor suppressor genes

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15
Q

What is tazemetostat currently approved for?

A

certain sarcomas and lymphoma

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16
Q

Identify the drug based on its structure.

A

tazemetostat

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17
Q

Give an example of a DNMT inhibitor.

A

Azacitidine (Onureg)

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18
Q

How are DNMT inhibitors and HDAC inhibitors similar?

A

they both result in the activation of tumor suppressor genes

19
Q

What is Onureg indicated for?

A

treatment of patients with myelodysplastic syndrome (MDS)

20
Q

Mechanistically, how does azacitidine inhibit DNMT?

A

it incorporates into DNA, covalent binds DNMT enzymes, and prevents their function to result in a DNA adduct

21
Q

Identify the drug based on its structure.

A

Azacitidine (Onureg)

22
Q

What do proteasomes do?

A

break down misfolded proteins

23
Q

Through what process are proteins targeted for degradation by proteasomes?

A

ubiquitination

24
Q

Why are multiple myelomas good targets for proteasome inhibition?

A

they make lots of proteins (i.e. antibodies)

25
Q

Give an example of a proteasome inhibitor.

A

Bortezomib (Velcade), Carfilzomib (Kyprolis), Ixazomib (Ninlaro)

26
Q

What is Velcade indicated for?

A

treatment of multiple myeloma

27
Q

Which proteasome inhibitor lacks the neuropathy side effects of Velcade?

A

Carfilzomib (Kyprolis)

28
Q

Which proteasome inhibitor is taken orally in a prodrug form?

A

Ixazomib (Ninlaro)

29
Q

Identify the drug based on its structure.

A

Bortezomib (Velcade)

30
Q

What protein does thalidomide bind to in order to increase protein degradation?

A

cereblon (CRBN)

31
Q

Thalidomide leads to the degradation of several proteins, including which developmental transcription factor?

A

SALL4

32
Q

Beyond being a potent teratogen, what other toxic element is important to note with thalidomide?

A

active component of proteolysis targeting chemeras (PROTACs)

33
Q

Pomalidomide is an analog of what drug?

A

thalidomide

34
Q

What indication is pomalidomide approved for?

A

multiple myeloma and Kaposi sarcoma

35
Q

How is pomalidomide regulated?

A

POMALYST risk evaluation and mitigation strategy (REMS)…must be prescribed/dispensed by certified providers

36
Q

Give an example of a BCL-2 inhibitor.

A

Venetoclax (Venclexta)

37
Q

What is BCL-2?

A

a protein overexpressed in many tumor cells that contributes to apoptotic resistance

38
Q

What indications has Venclexta been approved for?

A
  • chronic lymphocytic leukemia (CLL)
  • acute myeloid leukemia (in combination with azacytidine)
39
Q

Identify the drug based on its structure.

A

Venetoclax (Venclexta)

40
Q

What is the natural binder of RANKL?

A

osteoprotegrin (OPG)

41
Q

Give an example of a RANKL inhibitor.

A

denosumab

42
Q

What is denosumab indicated for?

A

multiple myeloma and advanced breast/prostate cancer

43
Q

What characteristic makes bisphosphonates effective in treating metastatic bone disease?

A

They are analogs of pyrophosphate, a constituent of the bone matrix

44
Q

Give three examples of bisphosphonates.

A

zoledronic acid, bisphosphonic acid, pyrophosphoric acid

Fall 2021: Therapeutics III (25 decks)

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