Anti-Neoplastics

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Filgrastim

Back 1

Ameliorate cytopenia in high dose chemo

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Bischlorethylamines (nitrogen mustards)

Back 2

Alkylation. Mechlorethamine and cyclophosphamide

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Mechlorethamine

Back 3

Highly reactive IV bischloroethyl amine

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Cyclophosphamide

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Oral, less reactive bischloroethyl amine. Requires liver biotransformation

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Cyclophosphamide

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Oral, less reactive bischloroethyl amine. Requires liver biotransformation

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Nitrosureas

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Alkylation. Little cross resistance with other alkylating agents

Cross BBB

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Cyclophosphamide

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Oral, less reactive bischloroethyl amine. Requires liver biotransformation

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Nitrosureas

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Alkylation. Little cross resistance with other alkylating agents

Cross BBB

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Procarbazine

Back 9

Monofunctional alkylating--> mutagen

MOPP

Little cross resistance

Leukomogenic with MOPP

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Alkylating agents

Back 10

Bischloroethyl amines, nitrosureas, and procarbazine

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Alkylating agents

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Bischloroethyl amines, nitrosureas, and procarbazine

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Anti-tumor antimetabolites

Back 12

Inhibit metabolic processes in S cycle

Methotrexate, purine/pyrimidine antagonists

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Alkylating agents

Back 13

Bischloroethyl amines, nitrosureas, and procarbazine

Front 14

Anti-tumor antimetabolites

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Inhibit metabolic processes in S cycle

Methotrexate, purine/pyrimidine antagonists

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Methotrexate

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Anti-tumor antimetabolite

Folic acid derivative

Inhibit DHFR, deplete THF, no cofactor for thimidylate synthetase

Accumulates in cells as polyglutamate derivative

Front 16

Alkylating agents

Back 16

Bischloroethyl amines, nitrosureas, and procarbazine

Front 17

Anti-tumor antimetabolites

Back 17

Inhibit metabolic processes in S cycle

Methotrexate, purine/pyrimidine antagonists

Front 18

Methotrexate

Back 18

Anti-tumor antimetabolite

Folic acid derivative

Inhibit DHFR, deplete THF, no cofactor for thimidylate synthetase

Accumulates in cells as polyglutamate derivative

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Pyrimidine antagonists

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5-fluorouracil

Capecitabine

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Alkylating agents

Back 20

Bischloroethyl amines, nitrosureas, and procarbazine

Front 21

Anti-tumor antimetabolites

Back 21

Inhibit metabolic processes in S cycle

Methotrexate, purine/pyrimidine antagonists

Front 22

Methotrexate

Back 22

Anti-tumor antimetabolite

Folic acid derivative

Inhibit DHFR, deplete THF, no cofactor for thimidylate synthetase

Accumulates in cells as polyglutamate derivative

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Pyrimidine antagonists

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5-fluorouracil

Capecitabine

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Purine antagonists

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6-MP

6-TG

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Alkylating agents

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Bischloroethyl amines, nitrosureas, and procarbazine

Front 26

Anti-tumor antimetabolites

Back 26

Inhibit metabolic processes in S cycle

Methotrexate, purine/pyrimidine antagonists

Front 27

Methotrexate

Back 27

Anti-tumor antimetabolite

Folic acid derivative

Inhibit DHFR, deplete THF, no cofactor for thimidylate synthetase

Accumulates in cells as polyglutamate derivative

Front 28

Pyrimidine antagonists

Back 28

5-fluorouracil

Capecitabine

Front 29

Purine antagonists

Back 29

6-MP

6-TG

Front 30

Alkylating agents

Back 30

Bischloroethyl amines, nitrosureas, and procarbazine

Front 31

Anti-tumor antimetabolites

Back 31

Inhibit metabolic processes in S cycle

Methotrexate, purine/pyrimidine antagonists

Front 32

Methotrexate

Back 32

Anti-tumor antimetabolite

Folic acid derivative

Inhibit DHFR, deplete THF, no cofactor for thimidylate synthetase

Accumulates in cells as polyglutamate derivative

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Pyrimidine antagonists

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5-fluorouracil

Capecitabine

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Purine antagonists

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6-MP

6-TG

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Hypoxanthine-guanine phosphoribosyl transferase

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Activates purines to NMP form

Downregulated as mechanism of resistance to purine antagonists

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6-MP

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Metabolically inactivated by xanthine oxidase

Low F when given with cow milk (high in xanthine oxidase)

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Allopurinol

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Xanthine oxidase inhibitor used with chemo to reduce uric acid levels/kidney toxicity

Increases cytotoxicity of 6-MP

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Fraudulent base incorporation

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Purine and pyrimidine antagonists incorporated into DNA (effective modification/damage)

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5-FU

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Pyrimidine antagonist

Also inhibits thymidylate synthetase through metabolite FdUMP

Thymineless death

Colorectal cancer

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Leucovorin

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Formyl tetrahydrofolate/folinic acid

Enhances 5-FU toxicity

Treat myelosuppression caused by methotrexate (folinic acid rescue)

Variable oral absorption, generally IV

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Dihydropyrimidine dehydrogenase

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Metabolizes 80-85% 5-FU

Genetic mutation decreases 5-FU clearance and increases toxicity (myelosuppression, NVD, neuro)

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Capecitabine

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Pyrimidine antagonist, prodrug of 5-FU. Tumor cells with thymidine phosphorylase to activate preferentially

Colon cancer, refractory breadth cancer

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Anti-tumor abx

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Anthracyclines (doxorubicin and daunorubicin)

Bleomycin

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Anthracyclines

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Doxorubicin and daunorubicin

DNA intercalating agents, topoisomerase II inhibitors

Cardiac toxicity

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Bleomycin

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Free radical generation

Broad spectrum of tumors

Pulmonary fibrosis (avoid 100% O2 to those taking this drug, could lead to recall pulmonary fibrosis

Possible anaphylaxis-start with small doses

ABVD for Hodgkin lymphoma

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MOPP

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Hodgkin lymphoma

Mechlorethamine, vincristine, procarbazine, prednisone

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ABVD

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Hodgkin lymphoma

Doxorubicin, bleomycin, vinblastine, dacarbazine

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Mitotic spindle poisons

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Vinca alkaloids (vincristine and vinblastine)

Taxanes (paclitaxel)

Bind tubulin

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Vinca alkaloids

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Vincristine and vinblastine

Interfere with tubulin polymerization

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Vinblastine

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Dose limiting myelosuppression, NV

ABVD

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Vincristine

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Non dose limiting mild myelosuppression

Dose limiting neurotoxicity

Treat acute childhood leukemia

MOPP

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Taxanes

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Paclitaxel (Taxol)

Inhibit depolymerization

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Paclitaxel

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Plant alkaloid (western Yew)

Ovarian and advanced breast cancer

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DNA topoisomerase I inhibitors

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Topetecan, irinotecan

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Irinotecan

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Cholinergic syndrome, ameliorated by prophylactic atropine

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DNA topoisomerase II inhibitors

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Etoposide, anthracyclines

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Cisplatin

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Platinum coordination complex, similar to alkylating. DNA crosslink

Myelosuppression, nephrotoxic (avoid through proper hydration), neurotoxic, acoustic dysfunction

Ovarian/testicular cancer

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SERMs benefits and risks

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Risk of endometrial cancer and PE

cardio protective

Increase bone density

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STAR and main result

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Study of Tamoxifen and Raloxifene: breast cancer preventive. Raloxifene with lower risk of endometrial cancer

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Tamoxifen

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Female and male breast, uterine endometrium

Prophylactic but may not significantly increase life span

Low toxicity

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Aromatase inhibitors

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Letrozole, anastrozole, exemestane

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Why are aromatase inhibitors not used in premenopausal

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Compensatory gonadotropin production and harmful ovarian effects (ovarian estrogen production)

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Exemestane

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Greatly reduces breast cancer (75%)

No increase risk for VTE or uterine cancer

Side effects: joint pain, decreased bone density (bisphosphonates)

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Leuprolide (2)

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Gonadotroin releasing hormone agonist

Treats prostrate cancer

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Flutamide

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Androgen receptor antagonist.

Used only in conjunction with leuprolide to block flare of prostate cancer at start of leuprolide therapy

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Degarelix

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GnRH antagonist

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Enzalutamide

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Androgen receptor antagonist

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Abiraterone

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CYP17A1 inhibitor for prostate cancer

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Adrenocorticosteroids

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Prednisone and dexamethasone

Used in multi drug regimens for leukemia, lymphoma, and myeloma (induces apoptosis of leukemia cells)

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Adrenocorticosteroids in other cancers

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Palliative agents in other cancers to reduce inflammation and nausea

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Oncogene addiction

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Tumor proliferation/survival becomes dependent upon oncogenically activated proteins

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Secondary mutations

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Mutations of tumors for genes encoding for kinase inhibitor, reducing affinity

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Erlotinib

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EGFR kinase inhibitor used in NSCLC (non small cell lung cancer) . Clinical trials for head and neck cancer

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Lapatinib

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EGFR and HER2 kinase inhibitor, approved for breast cancer

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Imatinib (3)

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ABL protein kinase inhibitor for CML

PDGFR kinase inhibitor for chronic myelomonocytic leukemia

Kit kinase inhibitor for GI stromal tumors

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Vemurafenib

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B-RAF inhibitor for late stage melanoma

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Pertuzumab

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Immunotherapeutic: Blocks HER2/EGFR dimerization and activation

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Cetuximab and cancers it treats

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EGFR antibody

Colon and head/neck cancer

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Trastuzumab and specific cancer

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HER2 antibody for breast cancer

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Rituximab and specific cancer

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IgG antibody against CD20.

Non-Hodgkin lymphoma (also kills B cells)

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Brentuximab vedotin

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Anti-CD30 IgG conjugated to vedotin (mitotic spindle poison) with a cleavable linker

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CD30

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Expressed on some Hodgkin and non Hodgkin lymphoma cells

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Mechanism and FDA approval of brentuximab-vedotin

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Bind CD30 positive cells, vedotin internalized, proteolytically cleaved to release toxin

Accelerated FDA approval for Hodgkin lymphoma and anaplastic large cell lymphoma