Millikan IHO Week 3 Flashcards
(26 cards)
anti-tubulin, small, epithelial malignancies, especially breast and ovarian
Paclitaxel
topisomerase inhibitor, small, breast cancer, lymphoma
Doxorubicin
topoisomerase inhibitor, small, germ cell tumors, lymphoma
Etoposide
proteosome inhibitor, small, multiple myeloma, mantle cell lymphoma, Waldenstroms (a type of non-hodgkin lymphoma)
Bortexomib
active metabolite (SN-38) can be liberated by ubiquitous hydrolytic enzymes in/outside of cells; in the liver oxidized by several different P-450 members and conjugated to sugars to bile to excreted; gut flora can convert back to SN-38
Irinotecan (in the family of Camptothecins)
4 Pharmacologic Points for Irinotecan
- inhibits the re-ligation step of Topo1 activity 2. prodrug of SN-38 and relies on intact lactone 3. effort to make analogs with improved TI 4. now formulated in 2 ways
3 Clinical Points for Irinotecan
- GI cancers including the pancreas 2. DLT is diarrhea 3. neutropenia is not cumulative and the drug can be given for extended time (>1yr)
What causes intercalation into DNA (pi stacking)
Doxorubicin
What causes most of the toxicity in use of Doxorubicin
generation of ROS and blocking of Topo 2
What do you give to help prevent Doxorubicin toxicity
Iron Chelators
4 Clinical Points for Doxorubicin
- broad spectrum anti-cancer activity 2. DLTs are stomatitis and myelosuppression 3. cardiac damage 4. nasty vesicant
broad spectrum anti-cancer drug essential for small cell carcinoma of lung and germ cell tumors and (aggressive lymphomas)
Etoposide
Causes acute leukemia at 1-2 per thousand at 2-3 yr latency, rapidly fatal, DLT is myelosuppression
Etoposide
Work by inhibiting tubulin polymerization and thereby causing mitotic arrest
Vinca alkaloids
Dose limiting toxicity of Vinca Alkaloids
neuropathy
What is not very myelosuppressive and is added to many regimens
Vincristine
What is extremely constipating
Vinblastine
What works by binding to inner surface of microtubules where GDP binds the beta-subunit and stabilizes the structure, preventing depolymerization
Taxanes
Dose limiting toxicity of the Taxanes
Neuropathy
Most common chemotherapy for solid tumors combination?
carboplatin and paclitaxel
What binds to the positive end of microtubule preventing elongation (doesn’t seem to work)?
Eribulin
Drug that causes myelosuppression and is dose-limiting and neuropathy
Eribulin
If can’t feel feet think what category of cancer med?
Anti-microtubule agent (Paclitaxel)
What blocks the 26S proteasome proteolytic activity (a threonine protease) given IV or subq
Bortezomib
