Cell Cycle Specific Drug Tables - Fitz Flashcards
5-Fluorouracil…active metabolites and their actions
FdUMP - inhibits thymidylate synthase (no dTMP)
FdUTP - insert and damage DNA
FUTP - insert and damage RNA
Cytarabine (Ara-C)…conversion and action
Kinases convert to Ara-CTP, which inhibits DNA synthesis
Gemcitabine…conversion and action
Kinases convert it to nucleotide analogs, which inhibit DNA synthesis
5-FU uses
- Solid tumors (colorectal, breast, ovarian)
- Topical - basal cell carcinoma
Capecitabine uses
Colorectal, metastatic/resistant breast
Gemcitabine use
Pancreatic cancer
Cytarabine use
AML (w/ 6-thioguanine, daunorubicin)
5-FU toxicities
GI intolerance, mucositis, myelosuppression
Capecitabine toxicities
Same as 5-FU, + hand-foot syndrome
Gemcitabine toxicity
Neutropenia
Cytarabine toxicity
Granulocytopenia (severe)
MTX function
MTX(glu)n function
MTX = blocks DHFR, blocking thymidine, methionine and serine synthesis MTX(glu)n = blocks GAR and AICAR transformylase, blocking purine synthesis
Pemetrexed function
Specialty vs. MTX?
Thymidylate synthase and GAR transformylase inhibitor
Does NOT inhibit DHFR, circumvents MTX resistance
Pemetrexed uses
Mesothelioma (w/ cisplatin), refractory NSCLC
High dose MTX uses
Requires what?
CNS prophylaxis for leukemia and high-risk lymphoma
Leucovorin rescue
Intermediate dose MTX use
Gestational trophoblastic disease (choriocarcinoma)
Low dose MTX uses
CNS prophylaxis (intrathecal), bladder and desmoid (IV), ALL and APL (oral)
MTX toxicities
BM suppression, mucositis, renal failure (high dose)
Pemetrexed toxicities
BM suppression, renal failure
6-Mercaptopurine function
Inhibits purine ring biosynthesis and nucleotide interconversion, disrupting DNA and RNA
6-Thioguanine function
Same as 6-Mercaptopurine
Inhibits purine ring biosynthesis and nucleotide interconversion, disrupting DNA and RNA
Fludarabine conversion and function
Tumor kinases convert it to nucleotide triphosphates, which insert and disrupt DNA and RNA
Cladribine conversion and functions
Tumor kinases convert it to nucleotide analogs, which inhibit DNA synthesis; also inhibits ribonucleotide reductase
6-Mercaptopurine use
ALL remission maintenance
6-Thioguanine use
AML (w/ daunorubicin and cytarabine)