Anti cancer Flashcards by bailey craig

agents that donate an alkyl group - DNA crosslinks @ position N-7 guanine

alkylating agents

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is activated by hepatic cytochrome P450

Cyclophosphamide

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treats hematologic and solid malignancies (leukemia’s, lymphomas, breast cancer, ovarian cancer)

Cyclophosphamide

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ADR: BM depression, hemorrhagic cystitis, increases risk of bladder cancer, hyponatremia due to SIADH, infertility and premature menopause

Cyclophosphamide

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MOA: increase DNA repair, decrease drug permeability, production of trapping agents (thiols)

Alkylating agents

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causes cystitis

acrolein

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binds and inactivates acrolein and hydration

MESNA

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active form of Cyclophosphamide

phosphoramide mustard

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nitrosoureas

temozolomide - most used
carmustine
lomustine
streptozotocin

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cross BBB and treat brain tumors and cause ADR of neurotoxicity

nitrosoureas

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treats insulinoma and induces type 1 diabetes

streptozotocin

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MOA: same as Cyclophosphamide, but also forms hydrogen peroxide, which generates free radicals that cause DNA damage

procarbazine

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Treats Hodgkins lymphoma

ADR: disulfiram like reaction after drinking alcohol & secondary cancers (acute leukemia - years after)

procarbazine

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analogs that bind DNA and form intra strand and inter strand cross links

Platinum analogs

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treats solid malignancies - specifically testicular cancer;
Is marrow sparing;
same MOA as Cyclophosphamide

cisplatin

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ADR: ototoxicity, neurotoxicity and nephrotoxicity

cisplatin

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what drug can prevent nephrotoxicity

amifostine

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similar to cisplatin but ADR less renal toxicity, but increase BM depression

carboplatin

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inhibit microtubule production and mitotic spindle assembly; acts on M phase

vincristine

vinblastine

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resistance: increase efflux of drug from tumor cells (p glycoprotein)

plant alkaloids

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Treats: Hodgkins, breast cancer, testicular cancer

vinblastine

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toxicity: BM suppression, anorexia, nausea, vomiting, diarrhea, alopecia

vinblastine

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treats: childhood leukemias, childhood wilms tumor, neuroblastoma, Hodgkins

vincristine

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toxicity: peripheral neuritis with paresthesia, SIADH, muscle weakness
muscle sparing effect!

vincristine

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enhance microtubule production and prevent their degradation - improper mitotic spindle function

paclitaxel | docetaxel

ADR: neutropenia, peripheral neuropathy, hypersensitivity reactions, alopecia

paclitaxel | docetaxel

topoisomerase 2 inhibitors | active in late S and early G2 phase

etoposide | teniposide

treats testicular and prostate cancer and small cell lung cancer

etoposide | teniposide

topoisomerase 1 inhibitors

topotecan | irinotecan

treats ovarian cancer and small cell lung cancer

topotecan | irinotecan

pyrimidine analog and is only active against hematologic malignancies (AML, Non-Hodgkins)

cytarabine

acts in S phase | converted to 5' (ara-CMP) then converted to dCMP kinase converted to ara CTP (active)

cytarabine

inhibits DNA poly | incorporates into DNA and RNA

cytarabine

ADR: neurotoxicity, hand - foot syndrome, BM depression, corneal toxicity, keratoconjunctivitis

cytarabine

need HGPRT to activate blocks synthesis of IMP inhibits DNA synthesis blocks S phase

6-MP | 6-TG

inhibits IMP to AMP and guanine

6-MP

inhibits guanine synthesis from IMP

6-TG

XO inhibitor

allopurinol

inhibition of XO increases level of purine analogs (6-MP) and cause toxicity/effects

allopurinol

Resistance: cancer cells having decrease activity of HGPRT; also increases alkaline phosphatase that inactivates toxic nucleotides

6-MP | 6-TG

cytotoxic folate analog, preventing conversion of DHF to THF; inhibits dihydrofolate reducatase

methotrexate

causes build up of DHF stop DNA and RNA synthesis in rapidly dividing cells affects S phase does not cross BBB

methotrexate

Treats 1) antineoplastic cancers 2) w/ misoprostol used as abortifacient and ectopic pregnancy 3) invasive molar pregnancy, trophoblastic tumors 4) choriocarcinoma 5) psoriasis 6) first line in RA

methotrexate

mech. of resistance 1) decrease drug transport 2) decrease polyglutamate 3) altered DHFR 4) increase levels of DHFR

methotrexate

ADR: 1) folate def 2) megaloblastic anemia 3) myelosuppression 4) pancytopenia 5) renal toxicity 6) lung fibrosis 7) mucositis 8) baldness 9) hepatotoxicity 10) immunosuppressed have increased risk of infection

methotrexate

antidote for methotrexate give after methotrexate only works in normal cells

leucovorin (folonic acid)

complexes with THF and inhibits thymidylate synthase to block thymidine production; increase dUMP; interferes with mRNA translation and inhibits DNA synthesis

5-FU

ADR: diarrhea, photosensitivity, rash, myelosuppression , infection, hyperpigmentation, hand foot syndrome, neurologic deficits

5-FU

resistance due to decrease activation of 5-FU, decrease thymidylate synthesis activity

5-FU

uses: carcinomas - breast, GIT, hepatoma, ovary, cervix, urinary, bladder, prostate, pancreas, colon, oropharyngeal

5-FU

antidote for overdose of 5-FU

uridine triacetate

ribonucleotide reductase inhibitor | blocks thymidine synthesis

hydroxyurea

treats sickle cell and CML; increases HbF - protection against HbS ADR: myelosupression and increased infection side effect

hydroxyurea

binds DNA and produces free radicals; free radicals produced cause single and double strand breaks in DNA

bleomycin

blocks the G2 phase of cell cycle

bleomycin

treats hematologic and solid malignancies and acts as sclerosing agent - (tx varicose veins)

bleomycin

cures pulmonary toxicity - pulmonary fibrosis

bleomycin

CCNS drugs produce free radicals intercalate in DNA - block DNA and RNA synthesis inhibit topoisomerase 2

doxorubicin | daunorubicin

treats a broad range of solid and hematologic malignancies and lymphomas

doxorubicin | daunorubicin

causes cardio toxicity - dilated cardiomyopathy myelosupression alopecia

doxorubicin | daunorubicin

prevents anthracycline induced cardiomyopathy

dexrazoxane

erythema and desquamation of skin observed at sites of prior radiation therapy

radiation recall reaction

intercalates in DNA - block DNA and RNA synthesis

actinomycin D

treats choriocarcinoma if no response to MTX

actinomycin D

used in childhood acute lymphoblastic leukemia ADR: hypersensitivity and pancreatitis Note: increase S amylase/ S lipase levels clue

asparaginase

Immunosuppressant; breaks down lymphocytes | ADR: compromised immune system

prednisone

resistance; MDR 1 coded efflux pump

anticancer antibiotics

small molecule kinase inhibitors

``` imatinib erlotinib sorafenib sunitinib vemurafenib gefitinib pazopanib ```

treats CML - 1st line blocks tyrosine kinase domain of the BCR/ABL fusion protein blocks the c kit tyrosine kinase (GIST) can cause fluid retention - ankle and periorbital edema

imatinib

translocation between chromosomes 9 and 22 - BCR/ABL oncogene on chromosome 22

Philadelphia chromosome - imatinib

blocks the epidermal growth factor receptor (EGFR) tyrosine kinase tumors with EGFR over expression (non small cell lung and pancreatic cancer)

erlotinib | gefitinib

inhibits the vascular endothelial growth factor receptor (VEGFR) tyrosine kinase treat renal cell carcinoma

sorafenib sunitinib pazopanib

treat hairy cell leukemia, CML, AIDS related capos sarcoma

interferon alpha 2a

treats hairy cell leukemia, melanoma, follicular lymphoma, AIDS related capos sarcoma

interferon alpha 2b

cyclin dependent kinase inhibitor | used: CDK 4/6 inhibitor for postmenopausal women with ER +, but HER 2 - breast cancer

palbociclib

- depletes B cells - binds CD20 on B cells - treats chronic lymphocytic leukemia, RA and non Hodgkin lymph - immunosuppression and increased risk infection

rituximab

SE: headache, fever, skin rash, pruritus, dyspnea, hypotension, can cause serum sickness (arthralgia within 7-10 days)

rituximab

- binds the epidermal growth factor receptor (EGFR) - treat colorectal cancer - SE: can cause papulopustular acneiformrash

cetuximab | panitumab

- binds VEGF - inhibits growth of blood vessels in tumors - treats metastatic tumors (colorectal cancer, ovarian), retinopathy, RCC, NSCLC and wet macular degeneration

bevacizumab

- against HER 2 receptor - binds epidermal growth factor receptor 2 (HER2, c-erbB2) - treats HER2 + breast cancer - can cause cardiotoxicity

trastuzumab