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Dad 4 test 5 > Cancer drugs > Flashcards

Cancer drugs Flashcards

1
Q

Tamoxifen

A
  • SERM (selective estrogen receptor modulator)
  • Antagonist at breast, agonist at other tissues
  • Prodrug (2D6, 3A4)
  • Keeps cells in G0 or G1 phases and prevents them from dividing
  • May also be anti-angiogenic
  • Used in hormone positive patients (men and women)
  • Used in early cancers alone, and in late stage with other agents
  • May be used for prophylaxtic used in those with high risk of cancer development
  • Increases the production of clotting factors→ thromboembolisms
  • Increases TG levels
  • Inc endometrial cancers
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2
Q

Raloxifene

A

• SERM
• Antagonist at breast and uterine tissues, agonists at other tissues
• Used for post-menopausal women and for osteoporosis
o Not as great for preventing invasive breast cancers from forming
• High first pass effect, and highly protein bound
• ADR: Hot flashes, leg cramps, less likely for thromboembolism to occur

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3
Q

Goserelin

A
  • Ovarian ablation drugs
  • May allow some hormonal therapies to work better
  • Produces symptoms of menopause since the ovaries can’t produce estrogen
  • Used in breast and prostate cancers
  • Given in injectable form either 1 month or 3 month intervals
  • Normal function should return after drug is stopped ~ 3 months
  • Initially causes an increase in estrogen or testosterone
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4
Q

Leuprolide

A
  • Ovarian ablation drugs
  • Not used for breast cancer, only for prostate cancer
  • Given 1/day SC
  • Normal function should return after drug is stopped ~ 3 months
  • Initially causes an increase in estrogen or testosterone
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5
Q

Anastrozole

A

• Aromatase inhibitor
o Used in hormone sensitive breast cancers for post menopausal women
• Reversible inhibitor
o Imidazole ring interacts with iron on the heme groups and prevents oxidation of normal substrates
• Nonsteroidal
• Used alone or after tamoxifen therapy
• Given orally
• Metabolized by CYP
• Inhibits CYP 3A4, 1A2, 2C9
• ADR: bone weakness, N/V, muscle weakness, hot flashes, vaginal dryness

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6
Q

Letrozole

A

• Aromatase inhibitor
o Used in hormone sensitive breast cancers for post menopausal women
• Reversible inhibitor
o Imidazole ring interacts with iron on the heme groups and prevents oxidation of normal substrates
• Nonsteroidal
• More potent than anastrozole
• Metabolized by CYP 2A6, 3A4
• Inhibits 2A6 and 2C19
• ADR: bone weakness, N/V, muscle weakness (less), hot flashes, vaginal dryness

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7
Q

Exmestane

A

• Aromatase inhibitor
o Used in hormone sensitive breast cancers for post menopausal women
• Suicide inhibitor (irreversible)
• Steroidal
• Poor absorption, but can be increased with high fat meal
• Metabolized by CYP 3A4
• ADR: hot flashes, N, Muscle pain

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8
Q

Trastuzumab

A

• Used in patients with metastatic breast cancer that have overexpression of HER2 receptors
• Given IV
• Its antibodies bind to the HER2 receptors on the breast cancer cells and are then recognized by phagocytic cells and are destroyed
• Can also bind to HER2 closer to cell membrane and prevent kinase pathways from occurring allowing apoptosis to occur more readily
o Would increase activity of other anticancer agents
• ADR: Cardiomyopathy, fever, chills, infections, increased cough, HA, rash, insomnia, D

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9
Q

Mertansine

A
  • Used for patients that are resistant to Transtuzumab and taxanes that are HER2 positive metastatic cancer
  • Tubulin inhibitor→ prevents cells from dividing→ death
  • ADR: muscle pain, thrombocytopenia, HA, fatigue, increased liver enzymes, constipation
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10
Q

Pertuzumab

A
  • Monoclonal antibody directed toward HER2 receptor binds distally and prevents dimerization
  • Can be used with trastuzamab and docetaxol since binding sites are different
  • Given IV
  • DC if LVEF drops below 40% (cardiotoxic)
  • ADR: D/N, hair loss, decreased WBC, fatigue, rash
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11
Q

Imatinib

A

• Used in CML (chronic mylogenous leukemia)
• Inhibits tyrosine Kinase by binding to the ATP binding site and prevents substrate from binding
o Useful for patients in chronic state, if they are in blast phase, will delay death by several months
• Metabolized by CYP 3A4, substrate for Pgp
• Resistance is due to tyrosine Kinases with altered amino acids which prevent the drug from binding
• ADR: ascites, neutropenia, thrombocytopenia, rash, pulmonary edema

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12
Q

Lapatinib

A
  • Tyroskine Kinase inhibitor
  • Used in breast cancers that overexpress HER2 for patients already recieveing capecitabine
  • Used in post menopausal women who are already receiving hormonal therapy
  • ADR: Skin rash, Diarrhea, decrease in LVEF (rare)
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13
Q

Bevacizumab

A

• Binds VEGF (angiogenic growth factors) and destroys them
• Monoclonal antibody
• Shuts of blood delivery to interior tumor → cell death (hopefully)
• Other agents should be used to kill exterior cells
• Used to treat colon and rectal cancers
• ADR: HTN, thrombosis, bleeding
o TONS of ADRS

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14
Q

Mechlorethamine

A

o Nitrogen Mustards
o Dialkylating agents (1 mustard- 2 nucleophiles)
o Can’t be given orally
o Given IV for leukemia/lymphomas
o Can be injected straight into solid mass tumor
o Effective from G0- M phase (not cell cycle specific agents)
o Less selective and more likely to mutate DNA
o Antidote= sodium thiosulfate

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15
Q

Cyclophosphamide

A 
o	Nitrogen Mustards
o	Used in breast cancer
o  Prodrug
o	Dose limiting myelosupression
o	Can be given orally and IV
o	Effective from G0- M phase (not cell cycle specific agents)
o	Less selective and more likely to mutate DNA
F
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16
Q

Ifosfamide

A

o Nitrogen Mustards
o Used in other cancers
o bladder and nephrotoxicities are seen
o Effective from G0- M phase (not cell cycle specific agents)
o Less selective and more likely to mutate DNA

17
Q

5-fluorouracil

A
  • Antimetabolites- Pyrimidine drug
  • Block the conversion of uridine to thymidine
  • Forms a covalent bond
  • Targeting thymidylate synthase inhibits the formation of DNA
  • Replication and cell division
  • Given IV or topically
  • Used in Breast cancer, colorectal cancer, stomach, pancreatic, and basal cell cancers
  • Can distribute to CNS
  • Triphosphate is encorporated into DNA and Ribose triphosphate in RNA
  • MOR: increased thymidylate synthase concentrations or decrease in folate substrate or increased concentrations of DPD
  • Myelosuppression is dose limiting
  • ADR: mucositis, D, hand food syndrome
18
Q

Floxuridine

A
  • Block the conversion of uridine to thymidine

* Antimetabolites- Pyrimidine drug

19
Q

Capecitabine

A
  • Antimetabolites- Pyrimidine drug
  • Prodrug
  • Block the conversion of uridine to thymidine
  • Some activation steps take place at a higher rate in tumor tissues leading to selective accumulation
  • Given orally
  • Used for breast cancer and colorectal cancer
  • Myelosuppression is dose limiting
  • ADR: mucositis, D, hand food syndrome:
20
Q

Methotrexate

A
  • Competitively inhibits the binding of substrate (folic acid) to DHFR
  • Reduces synthesis of nucleic acid bases
  • Purine synthesis is inhibited
  • Taken up by active transport
  • NH2 is electron donating and increases the basicity which allows for protonation at physiologic PH
  • Increase affinity
  • ~ irreversible inhibition
  • Given IV or orally
  • Used to treat acute lymphoblatic and myeloblastic leukemias and other lymphomas and sarcomas, Breast cancer, bladder cancer, colorectal and head and neck cancers
  • MOR: decreased carrier mediated transport into cells or increased concentrations of DHFR
  • ADR: bone marrow suppression, pulmonary fibrosis, GI ulceration, myelosupression, N/V HA, renal toxicity, acute cerebral dysfxn, rash, hyperpigmentation
21
Q

Pemetrexed

A
  • Inhibits DHFR, Thymidlate synthase and GARFT
  • Inhibits purine synthesis
  • Taken up into tumor cells by reduced folate carrier systems and converted into polyglutamate which stays within the cells
22
Q

Trimetrexate

A

Antifolate drug

23
Q

Doxorubicin

A

o Anthracyclines
o MOA:
• Intercalation
• inhibition of topoisomerase II→ strand breakage
o Specific for S phase of cell cycle
o MOR: decreased concentrations of topoisomerase II and mutations of that enzyme
o Cardiotoxicity is dose limiting→ CHF
o Can be used for a wide variety of cancers including breast cancer
o Substrate for PGP

24
Q

Epirubricin

A

o Anthracyclines
o Decreased cardiotoxicity
o Increased clearance, decreased toxicity
o MOA:
o Specific for S phase of cell cycle
o Given IV for breast cancer
• Can be used for other types of cancer—still has a limited use though
o Can be used in larger doses with LESS cardiotoxicity

25
Q

Dexrazoxane

A 
o	Anthracyclines
o	Chelate iron 
o	Weak inhibitor of topoisomerase II
•	Not associated with double strand breaks
o	Specific for S phase of cell cycle
26
Q

Daunorubicin

A

o Anthracyclines
o Given IV for nonlymphocytic and lymphocytic leukemia
o Use is more limited than doxorubicin
o Specific for S phase of cell cycle
o MOR: decreased concentrations of topoisomerase II and mutations of that enzyme
o Cardiotoxicity is dose limiting→ CHF

27
Q

Paclitaxel

A

o Taxane
o Administration of a antihistamines and corticosteroids prior to administration help reduce HSR
o MOA: bind to tubulin
o Work in the M phase
o Inhibit treadmilling and dynamic stability
o Can work to block BCL2
• Pro apoptotic proteins are stimulated (BAD and BAX)
o MOR:
• PGP efflux
• Alterations to structure of beta tubulin
o Used to treat breast, ovarian, non small cell lung cancer and AIDS related kaposi’s sarcoma
o Doesn’t penetrate the CNS
o Dose limiting myelosuppression which presents as neutropenia
o ADR: bradycardia→ heart block, alopecia, mucositis, Diarrhea, N/V
o Peripheral numbness
• Can be severe/long term/ irreversible
o Metabolized by CYP 3A4

28
Q

Docetaxel

A

o Taxne
o MOA: bind to tubulin
o Work in the M phase
o Inhibit treadmilling and dynamic stability
o MOR:
• PGP efflux
• Alterations to structure of beta tubulin
o Used to treat breast cancner, non small cell lung and prostate cancers
o Given IV
o Doesn’t cross the BBB
o Metabolized by CYP 3A4
o Myelosuppression is dose limiting
o ADR: reversible fluid retention that is dose related, peripheral neuropathy, fatigue, muscle pain, fever
Reduce sodium intake and pretreat with corticosteroid

Dad 4 test 5 (2 decks)

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