Cancer Chemotherapy and Ant-Neoplastic Drugs Flashcards
What are the 4 Pyrimidine anti-metabolite drugs that inhibit DNA synthesis?
- 5-fluorouracil
- Capecitabine
- Cytarabine (Ara-C)
- Gemcitabine
What is adjust chemotherapy?
Drug given after tumor has been removed
What is Neoadjuvant chemotherapy?
Drug given prior to surgery to remove a tumor
What is the MOA of 5-fluorouracil?
FdUMP inhibits thymidylate synthase.
What is unique about Capecitabine?
Prodrug of 5FU
What is the MOA of Gemcitabine?
Kinases convert gemcitabine to nucleotide analogs-> inhibit DNA synthesis.
What is the MOA of Cytarabine (Ara C)?
Kinases convert Ara-C to AraCTP-> inhibits DNA synthesis.
What are some therapeutic uses for 5FU?
Solid tumors: colorectal and other GI; breast, ovarian carcinomas.
Topical use: basal cell carcinoma
What are some therapeutic uses for 5FU?
Colorectal cancer; metastatic breast cancer
What are some therapeutic uses for Gemcitabine?
Pancreatic cancer
What are some therapeutic uses for Cytarabine?
Acute Myelogenous leukemia
What is the toxicity associated with use of 5FU?
Severe GI intolerance, mucositis, myelosuppression.
What is the toxicity associated with use of Capecitabine?
GI intolerance, mucositis, myelosuppression, hand and foot syndrome.
What is the toxicity associated with use of Gemcitabine?
Myelosuppression-neutropenia
What is the toxicity associated with use of Cytarabine (Ara C)?
Severe myelosuppression- granulocytopenia
Where is the cell cycle does 5FU exert its effects?
S phase
What two medications are given with 5FU to enhance its anticancer activity?
Methotrexate and Leucovorin
Where is 5FU cleared and what enzyme does this?
Mainly in the liver by Dihydropyrimidine dehydrogenase (DPD).
Where is Capecitabine activated in the body?
Activated by the liver via carboxyesterase and Cytidine deaminase, delivered to the tumor, and then converted into 5FU by T/U phosphorylase.
What is a use for Capecitabine?
Advanced breast cancer
What is the MOA for resistance with Ara C?
Liver and spleen contain cytidine deaminase (CDA) that has the ability to inactive Ara-C to Ara-U.
Besides chain termination, what else does Gemcitabine inhibit?
inhibits ribonucleotide reductase thus depleting cellular dNTPs.
