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GOBBLERS 2023 > SGO Chemo/Targeted cards > Flashcards

SGO Chemo/Targeted cards Flashcards

1
Q

Anti-metabolites (5)

A

5-FU
capecitabine
MTX
Gemcitabine
Pemetrexed

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2
Q

Methotrexate:
1. Specific to which phase of the cell cycle
2. MOA

A
  1. S phase
  2. Inhibition of dihydrofolate reductase blocks DHFR from reducing dihydrofolate to tetrafolic acid > blocks thymidylate synthase and purine synthesis > arrests DNA/RNA/protein synthesis
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3
Q

Methotrexate:
1. Drug clearance
2. Dose reduction for___
3. Drug synergy

A
  1. Mostly renal, small amount in bile
  2. Renal insufficiency. Contraindicated for Crcl <40, Cr>2
  3. Hepatic insufficiency Bili 3.1-5. Avoid if Bili >5
  4. MTX and 5-FU are maximally synergistic when MTX is given 24 h before 5-FU, inhibiting the production of nl purine (remember purines are PUR As Gold = Adenine & Guanine) precursors
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4
Q

Methotrexate:
1. Dose-limiting toxicity for high dose regimens
2. Other SE/Tox
3. Tox related to intrathecal

A
  1. Nausea/vomiting - per B&H(!) (vs in general Stomatitis / mucositis & myelosuppression )
  2. Myelosuppression, mucositis (stomatitis*), elevated LFTs, pneumonitis, oliguric renal failure
  3. Acute aseptic meningitis (self-limited usually)
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5
Q

Medication to reverse the immediate cytotoxic effects of MTX

A

Leucovorin

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6
Q

5-Fluorouracil:
1. Specific to which phase of the cell cycle
2. MOA

A
  1. S phase
  2. Inhibits the formation of the DNA base thymidine by 3 mechanisms:
    (1) Active metabolite 5-FdUMP inhibits thymidylate synthase (–> formation of an inactive ternary complex, enhanced by co-administration of folinic acid > depletes thymidine pools > inhibits DNA synthesis)
    (2) Metabolite 5-FdUTP incorporation into DNA as a fraudulent thymidine precursor > induce single-strand breaks > cytotoxic effects
    (3) Metabolite FUTP incorporation into RNA > impaired RNA function/ impaired protein synthesis
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7
Q

5 FU:
1. Activated in __
2. Drug Clearance
3. Contraindication
4. Drug synergy

A
  1. PRODRUG, activated in liver but also by target tissues
  2. Metabolized by liver
  3. Pregnancy
  4. MTX and 5-FU are maximally synergistic when MTX is given 24h before 5-FU, inhibiting the production of nl purine precursors
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8
Q

5 FU side effects/tox
1. Dose limiting tox
2. other common
3. Rare

A
  1. Myelosuppression
  2. Mucositis, diarrhea
  3. PPE, Dermatitis, cerebellar syndrome (PPD - headache, ataxia, nystagmus, confusion)
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9
Q

Adavosertib

A

Small molecule tyrosine kinase inhibitor of WEE1

MOA: inhibits WEE1 (nuclear protein, a tyrosine kinase involved in cell cycle regulation)

Not FDA approved, ovarian and UPSC clinical trials

SE: bone marrow toxicity, GI upset

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10
Q

Anastrozole

A

Aromatase inhibitor

MOA: non steroid competitive inhibitor of aromatase enzyme (blocks conversion of androgens to estrogens). Decrease estrogen

FDA: breast cancer

SE: loss bone density, bone/muscle pain, hot flashes, raises LDL

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11
Q

Atezolizumab

A

Anti-PDL1

MOA: binds to PD-L1 to stop interaction btw PD-1 on T cell and PDL1 on cancer cell.

FDA: none in gyn

SE: fatigue, immune related toxicities (MC irSAE is rash 20-30%)

Atezo, avelu, durva - all PD-L1

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12
Q

Avelumab

A

anti PD-L1

MOA: Anti PD-L1 with wild type Fc-1 region, binds to PD-L1

FDA: none in gyn cancers

SE: fatigue, immune related toxicities

Atezo, avelu, durva - all PD-L1

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13
Q

Balstilimab

A

Anti PD-1

MOA: routine anti PD-1

SE: fatigue, immune related toxicities

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14
Q

Bevacizumab

A

VEGF inhibitor

MOA: binds to and neutralizes the ligand VEGF (specifically VEGF-A) thus preventing association with FLT-1 (same thing as VEGFR1) and KDR (same thing as VEGFR2) — it is anti-angiogenic

FDA: ovarian and cervix

common side effects: HTN (give ACEI, ARB, CCB), Proteinuria, Joint pains (give NSAID), Rhinorrhea + bloody noses

less common side effects: VTE (ok to resume once anti coagulated), GI perforation, fistulas, hemorrhage, PRES

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15
Q

Cediranib

A

Tyrosine kinase inhibitor

MOA: small molecule vascular endothelial growth factor receptor tyrosine kinase inhibitor. It inhibits all 3 VEGF receptors which prevents activation of MAPK kinase signal transduction pathway and inhibits cellular replication

FDA: no approvals

Side effects: fatigue, HTN, diarrhea, nausea

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16
Q

Cemiplimab

A

Anti PD-1

MOA: routine anti PD-1

FDA: none

SE: in bold - IrAEs can occur up to 1 year after completion of therapy

17
Q

Dostarlimab

A

anti PD-1

MOA: routine anti PD-1

FDA approval - MMR deficient endometrial cancers

SE: in bold - IrAEs can occur up to 1 year after completion of therapy (rash/hypothyroidism/diarrhea most reported in RUBY)

18
Q

Durvalumab
-Class, MOA, FDA approval?, SE

A

Anti-PDL1

MOA: binds to PD-L1 to stop interaction btw PD-L1 and PD-1

FDA: NEW 6/2024 approved in dMMR advanced EMCa in combo with C/T

SE: fatigue, immune related toxicities

Atezo, avelu, durva - all PD-L1

19
Q

Everolimus
-Class, MOA, FDA approval?, administration, SE

A

mTOR inhibitor

MOA: Binds intracellularly to FK binding protein 12–>creates a complex that binds to mTOR (a regulatory kinase part of the PI3K/Akt signal transduction pathway. Binding of mTOR results in inhibition of protein production.

FDA: metastatic breast, renal, NETs

Off label use: in combination w/ letrozole for recurrent/advanced endometrial cancer

PO daily dosing

SE: fatigue, stomatitis, metabolic: hyper triglyceridemia, hypercholesterolemia, and hyperglycemia, nausea. Rare but serious noninfectious pneumonitis

20
Q

Erlotinib
-Class, MOA, FDA approval?, administration, SE, contraindications

A

Epidermal growth factor (EGFR) tyrosine kinase inhibitor

MOA: inhibits EGFR tyrosine kinase to prevent dimerization of EGFR and subsequent transduction of proliferative signals (MAPK, Atk, JNK pathways) –>uncontrolled cell division

FDA: non small cell lung cancer, pancreatic

Off label: advanced or recurrent/metastatic vulvar cancer

PO daily dosing

SE: Diarrhea can be severe, rash (49-85%!), fatigue, electrolyte abnl (due to diarrhea), dry eyes, elevated LFTs. Less common: renal failure, GI bleed/perf.

Contra: interstitial lung disease, severe renal impairment, hepatic impairment, GI bleed

Think Erlot like merlot. Some get rash (splotchy wine rash), others get diarrhea. Too much wine —> increased LFTs

21
Q

Exemestane
-class, MOA, FDA approval/off label uses, dose adjustment reason, side effects

A

Aromatase inhibitor

MOA: blocking conversion of androgens into estrogen in peripheral tissue, lowers circulating estrogen (irreversible binding; steroidal)

FDA: Breast
Off label: recurrent ovary and endometrial

Dose adjustment: increase dose if also taking a CYP3A4 inducer (rifampin, phenytoin, dabrafenib, st john’s wort)

SE: hot flashes, fatigues, arthralgias, bone pain

22
Q

Fulvestrant
-class, MOA, FDA approval/off label uses, route, dose adjustment reason, side effects, contraindications

A

Estrogen receptor antagonist

MOA: estrogen receptor antagonist, competitively binds to estrogen receptor on tumor tissue and other tissues. accelerates degradation of the estrogen receptor, resulting in pure antiestrogenic effects.

FDA: breast
Off label: recurrent ovary, recurrent endometrial

Route: IM injection

Dose adjustment: for mild liver impairment reduce the dose.

Common SE: hot flashes, fatigue, headache, injection site pain, *not associated with significant bone turnover

CI: pregnancy, renal failure

23
Q

Ipilimumab
-Class, MOA, FDA/off label uses, side effects

A

Anti-CTLA-4 monoclonal Ab, immune checkpoint inhibitor

MOA: binds to CTLA-4 [cTla-4 on T cells], allows CTLs to destroy cancer cells. The antibody works by allowing the patients’ T cells to target a greater variety of antigens rather than by increasing the number of attacking a single antigen.

FDA: not GYN tumors, but in active investigation in multiple trials. Approved for melanoma, lung

SE:
-most common: dermatitis, enterocolitis, endocrinopathies
-less common but concerning: hepatitis, nephritis, stevens johnson, pancreatitis, myocarditis, diabetes

24
Q

Ixabepilone
-Class, MOA, FDA/off label uses, side effects

A

Antimicrotubular epothilone B analog

MOA: Epothilone B analog that binds to beta-tubulin subunit of the microtubule to stabilize microtubular function resulting in the arrest of cell cycle in the G2/M phase leading to apoptosis. [similar to Taxol]

Of particular note is its activity in taxane- resistant cells.

FDA: breast cancer

Off label: plat resistant ovarian cancer in combo with bev or monotherapy; recurrent ovarian cancer as monotherapy

SE: Neuropathy - dose limiting and may require dose reduction; neutropenia, alopecia, n/v

25
Q

Letrozole
-class, MOA, FDA/off label, side effects

A

Aromatase inhibitor

MOA: inhibits conversion of androgens to estrogens

FDA: breast cancer
Off label: ovarian, endometrial

SE: loss of bone density, elevation in cholesterol profile, arthralgias, weight gain, hot flushes, insomnia, nausea, edema, headache

Clinical pearl: Arthralgias are a class effect of the aromatase inhibitors (AI). While some patients may tolerate alternative other AI agent, there is usually similar crossover toxicity

26
Q

Vinblastine
-Class
-MOA
-Cell cycle:
-Metabolism
-Excretion
-DLT
-Other SE

A

Plant alkaloid

MOA: binds to the tubulin dimer, inhibits assembly of microtubles during M phase. Also inhibits RNA synthesis, affecting DNA dependent RNA polymerase.
M phase

Metabolized in the liver
Excreted in the Bile

DLT: Neutropenia (VBB)

Other se: constipation, n/v, mucositis, interstitial pneumonitis

27
Q

Vincristine
-MOA
-Cell cycle
-Metabolism
-Excretion
-DLT

A

Plant alkaloid

MOA: binds to the tubulin dimer, inhibits assembly of microtubles during M phase. Also inhibits RNA synthesis, affecting DNA dependent RNA polymerase.
M phase

Metabolized in the liver
Excreted in the Bile

DLT: peripheral neuropathy (think like Christ on a cross with pain in hands and feet. Binds tubulin DIE-mer)
Other se: alopecia (20-50%)

28
Q

Vinorelbine MOA DLT Metabolism

A

Semi synthetic alkaloid derived from vinblastine

MOA: binds to the tubulin dimer, inhibits assembly of microtubles during M phase. Also inhibits RNA synthesis, affecting DNA dependent RNA polymerase.
M phase

Metabolized in the liver
Excreted in the Bile

DLT: Myelosuppresion (logical since, vinblastine DLT is neutropenia). (VBB very bad for bones)

29
Q

Mirena - dosage of levonorgestrel released daily

Liletta - dosage of levonorgestrel released daily

A

20mcg/day for both!

30
Q

Mirvetuximab
-Class
-MOA
-FDA

A

ADC: Folate receptor alpha-binding MAB (Payload is Maytansinoid DM4)

MOA: Antibody drug conjugate that targets the folate receptor alpha (FRα) and is then internalized by and degraded to DM4 and S-methyl-DM4. These catabolic molecules promote antimitotic activity, via inhibition of tubulin polymerization and microtubule assembly resulting in cell death and they are able to diffuse from antigen-positive tumor cells into neighboring cells and kill them in an antigen-independent manner, an effect known as ‘bystander’ killing

FDA: approved for plat resistant recurrent folic acid receptor positive ovarian/FT/PP cancer [FOLR1 75% 2+ IHC staining]

31
Q

Mirvetuximab
-SE
-Contraindications
-dosage adjustments for renal/hepatic impairment

A

-SE: nausea (54%), diarrhea (44%), reversable ocular AEs (blurred vision, corneal ketatopathy), LFTs, peripheral neuropathy

-CI: avoid treatment in patients with preexisting occular conditions like glaucoma

-No dosage adjustment needed for renal disease
-avoid use in mod-severe hepatic impairment

32
Q

Nivolumab
Class
MOA
FDA approval
off label uses
SE

A

Anti PD-1

MOA: routine anti PD-1

FDA: not in gyn

Off label: Recurrent cervical, vulvar or vaginal cancer, ovarian cancer, MSI-Hi/MMRd endometrial cancer

SE: fatigue, immune related toxicities

33
Q

Oxaliplatin

Class
MOA
FDA
Off label
Dosing adjustments for…
SE

A

Platinum derivative

MOA: functions as an alkylating agent by binds to DNA forming cross-links which inhibit DNA replication and transcription, resulting in cell death

FDA-APPROVED: Advanced colorectal cancer OFF-LABEL: Mucinous ovarian cancer

Renal dose adjustments

SE: Grade 3/4 neutropenia (common when in combo with capecitabine); diarrhea; hand food syndrome

34
Q

Box warning for use of capecitabine with which anti-coagulant?

A

Warfarin. The combo can increase anticoagulant effects of warfarin, bleeding events

35
Q

Palbociclib

A

Cyclin-dependent kinase 4/6 inhibitor

MOA: Palbociclib is a reversible cyclin-dependent kinase inhibitor. It is specific to CDK4 and CDK6 which are responsible for cell cycle progression particularly at the G1/S phase of mitosis.

Normally, Phosphorylation of the retinoblastoma protein by CDK4 and 6 leads to passage through the G1-S phase

CDK4 and CDK6 inhibitors inhibit the phosphorylation of the retinoblastoma protein and prevent progression from G1 to S.

FDA approved: breast cancer

Off label: recurrent ovarian, ER+ recurrent endometrial (in combo with an AI)

SE: neutropenia, nausea, increased LFTs, ocular, fatigue

GOBBLERS 2023 (32 decks)

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