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Anticancer Therapeutics Part 1
Medical Oncology Board review
65
Medical
Professional
07/22/2019

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Cards

Term
Sequence of cell cycle
Definition
G1(G0)-S-G2-M
Term
Breakdown (%) of cell cycle
Definition
G1 40%
S 40%
G2 18%
M 2%
Term
Two classes of drugs that act only on specific phases of cell cycle
Definition
Plant alkaloids
DNA synthesis inhibitors
Term
Part of cell cycle where plant alkaloids work
Definition
G2-M
Term
Part of cell cycle where DNA synthesis inhibitors work
Definition
S phase
Term
Cell cycle specific drugs kill proliferating or nonproliferating cells?
Definition
Only proliferating
Term
Cell cycle non-specific drugs kill proliferating or nonproliferating cells?
Definition
Both
Term
Cell cycle specific drugs are schedule or dose dependent?
Definition
Schedule dependent
Term
Cell cycle non-specific drugs are schedule or dose dependent?
Definition
Dose dependent
Term
4 main categories of cell cycle specific agents
Definition
Plant alkaloids
Antibiotics
Alkylating agents
Antimetabolites
Term
List plant alkaloids and mechanism
Definition
Etoposide (topoisomerase II inhibitor)
Camptothecins (irinotecan, topotecan) topoisomerase I inhibitor
Taxanes (microtubule stabilizer)
Vinca alkaloids (microtubule destabilizer)
Term
List cell cycle specific antibiotics and mechanism
Definition
Bleomycin (DNA intercalation)
Epothilones (microtubule stabilizer)
Term
List the cell-cycle specific alkylating agent and mechanism
Definition
Procarbazine (DNA alkylation, mostly on newly synthesized DNA
Term
Where do antimetabolites work and general mechanism
Definition
S-phase
Interfere with cell's ability to process new DNA)
Term
List antimetabolites
Definition
5-FU
Capecitabine
6-MP
6-TG
Cladribine
Ara-C
Fludarabine
Gemcitabine
Leucovorin
Methotrexate
Pemetrexed
Hydroxyurea
Term
Pemetrexed mechanism
Definition
DHFR inhibitor
Term
Hydroxyurea mechanism
Definition
Ribonucleotide reductase inhibitor
Term
List categories of non-cell cycle specific alkylating agents
Definition
Nitrogen mustard
Nitrosureas
Miscellaneous (busulfan, dacarbazine, procarbazine, temozolomide)
Term
List non-cell cycle specific nitrogen mustards
Definition
Clorambucil
Cyclophosphamide
Ifosfamide
Mechlorethamine
Melphalan
Term
List non-cell cycle specific nitrosureas
Definition
CCNU (lomustine)
BCNU (carmustine)
Term
List the non-cell cycle specific antibiotic
Definition
Mitomycin
Term
What part of cell cycle do steroids work?
Definition
G0-G1
Term
Virtually all drugs induce myelosuppression except ______
Definition
Vinca alkaloids
Term
List drugs that are vesicants (7)
Definition
Alkylating agents
Mitomycin
Vinca alkaloids
Anthracyclines
Mechlorethamine
Carmustine
Dactinomycin
Term
Treatment for vinca alkaloid extravasation
Definition
Topical heat
SQ hyaluronidase
Term
Treatment for taxane extravasation
Definition
Topical cold
SQ hyaluronidase
Term
Treatment for anthracycline extravasation
Definition
Topical cold
IV dextazoxane
Term
Treatment for mechlorethamine extravasation
Definition
Topical cold
SQ sodium thiosulfate
Term
Treatment for platinum extravasation
Definition
Topical cold
Term
Drugs most likely to cause CNS toxicity
Definition
Most alkylators (except cyclophosphamide)
Antimetabolites (gemcitabine, Ara-C, methotrexate)
Erlotinib, lapatinib
Term
Chemotherapy-induced neuropathy is primarily sensory/motor?
Definition
Sensory
Term
Drugs most likely to cause neuropathy (5)
Definition
Taxanes
Epothilones
Platinums
Vincristine
Bortezomib
Term
Drugs that cause complete alopecia (7)
Definition
Taxanes
Epothilones
Topoisomerase I inhibitors (irinotecan, topotecan)
Anthracyclines (all)
Alkylators (esp. cyclophosphamide)
Dactinomycin
Bleomycin
Term
Drugs that cause permanent infertility (4)
Definition
Vinblastine
Alkylators (virtually all)
Cisplatin
Melphalan
Term
Risk of secondary malignancies with etoposide, teniposide (topoisomerase II inhibitors)
Definition
Mixed lineage leukemia, 11q23 rearrangement
Mean latency 2-3 years after stopping treatment
Term
Risk of secondary malignancy with alkylators
Definition
AML M1/M2
MDS 5q- 7q-
5-7 year latency
Term
Risk of secondary malignancy with anthracyclines
Definition
AML M1/M2
MDS 5q- 7q-
5-7 latency
Term
Toxicity reversal for methotrexate
Definition
Leucovorin
Glucarpidase (Carboxypeptidase G)
Term
5-FU toxicity reversal (non DPD deficient patient)
Definition
Leucovorin
Term
5-FU toxicity reversal (DPD deficient patient)
Definition
Uridine triacetate
Term
Irinotecan treatment reversal UGT1A1 polymorphism
Definition
Azathioprine (thiopurine methyltransferase)
Dose reduction with subsequent cycles
Term
Tamoxifen toxicity reversal
Definition
CY2D6 (controversial)
Term
Drug categories requiring renal monitoring and/or adjustment of dose (4)
Definition
All platinums
All antimetabolites
Alkylators
Other (etoposide, topotecan, bleomycin, mitomycin)
Term
Major metabolism enzyme cyclophosphamide
Definition
Cytochrome p450 CY286
Term
Major metabolism enzyme paclitaxel
Definition
Cytochrome p450 CY2C8
Term
Major metabolism enzyme warfarin
Definition
Cytochrome p450 CYP2C9
Term
Major metabolism enzyme tamoxifen
Definition
Cytochrome p450 CYP2D6
Term
Major metabolism enzyme codeine
Definition
Cytochrome p450 CYP2D6
Term
Major metabolism enzyme irinotecan
Definition
Carboxylesterases
UGT1A
Term
Major metabolism enzyme 5-FU
Definition
DPD
Term
Major metabolism enzyme gemcitabine
Definition
Cytidine deaminase
Term
Major metabolism enzyme Ara-C
Definition
Cytidine deaminase
Term
Likely alkylator increasing INR
Definition
Cyclophosphamide
Term
Antimetabolites increasing INR
Definition
Capecitabine
5-FU
Gemcitabine
Methotrexate
Term
Likely anthracycline increasing INR
Definition
Doxorubicin
Term
Targeted agents increasing INR
Definition
TKIs (imatinib, sorafenib, nilotinib)
EGFR inhibitors (erlotinib, gefitinib)
Term
Do vinca alkaloids increase INR?
Definition
Yes
Term
Taxane likely increasing INR
Definition
Paclitaxel
Term
HDAC inhibitor likely increasing INR
Definition
Vorinostat
Term
Strategy if antacids required with erlotinib
Definition
Change to sucralfate
Administer 8 hours later
Term
Agents affected by food, AUC increases
Toxicity increase/decrease?
Definition
Erlotinib
Gefitinib
Nilotinib
Lapatinib

Toxicity increases
Term
Agents affected by food, AUC decreases
Efficacy increase/decrease?
Definition
Afatinib

Efficacy decreases
Term
Common CYP3A4 inducers/inhibitors
Definition
Antifungals, especially ketoconazole
Grapefruit juice
Herbals (St. Johns wort)
Antibiotics (Rifampicin)
Term
What happens with NSAIDs and methotrexate (renal function)
Definition
Impairs clearance of methotrexate, concentration of methotrexate increases
Term
What happens with renal failure/third spacing and methotrexate?
Definition
Volume of distribution increases
Concentration of methotrexate increases
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