Pharm - Oncology

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cyclophosphamide/ifosfamide

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aka Cytoxan/Ifex
alkylating agents
prodrugs activated by P450
metabolite acrolein accumulates in bladder - bound by mesna

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melphalan

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alkylating agent with phenylalanine
for multiple myeloma
no alopecia

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estramustine

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alkylating agent with estradiol
inhibits microtubule formation
prostate cancer

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chlorambucil

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alkylating agent with aromatic ring
decreased reactivity
for CLL

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carmustine / lomustine

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nitrosourea - alkylating agent
lipophilic - cross BBB
brain tumors

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thiotepa

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alkylating agent
very lipophilic
carcinomatous meningitis and bladder cancer

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mitomycin c

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alkylating agent
natural product
2nd line for colon cancer

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busulfan

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alkylating agent
oral administration
for CML
associated w/ pulmonary fibrosis

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procarbazine

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alkylating agent
Hodkin and non-Hodkin lymphoma

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decarbazine

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alkylating agent
malignant melanoma, Hodgkin lymphoma, brain tumor

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temozomoide

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alkylating agent
excellent brain penetration
glioma

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cisplatin

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cross link DNA
for testicular and solid tumors
most emetogenic, ototoxicity and renal toxicity

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carboplatin and oxaliplatin

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cross link DNA
less renal toxicity than cisplatin

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methotrexate

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folic acid analogue that inhibits dihydrofolate reductase (DHFR)
ALL, non-Hodgkin, breast, osteosarcoma, bladder
abortifacient
immunosupressant

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trimetrexate

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antifolate
does not need RFC (reduced folate carrier) and does not depend on polyglutamation
for penumocystic carnii and osteosarcoma

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leucovorin

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folinic acid
needed for therapy with antifolates

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raltitrexed

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selective inhibitor of thymidine synthetase

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lemotrexol

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polyglutamated inhibitor of purine synthesis

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fluorouracil

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inhibits thymidylate synthase and decreases theymine
incorporates into DNA and RNA
needs reduced folate (leucovorin)
for colorectal ca

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capecitabine

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oral 5FU precursor
thymidine phosphorylase in tumors converts it to 5FU
for refractory breast and colon ca

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cytosine arabinoside

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cytidine analogue
misincorporated into DNA and inhibits DNA elongation
poisons topoiromerases
for myelogenous leukemia and lymphoma

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gemcitabine

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cytidine analogue
inhibits DNA synthesis and repair
great affinity for deoxycytidine kinase, long cell retention
for pancreatic, bladder, mesothelioma, NSCL and HL

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6-mercaptopurine (6MP)

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analog of hypoxanthine, inhibits purine synthesis
for ALL
hepatotoxicity

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6-thioguaning (6TG)

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analog of hypoxanthine and guanine for HGPT
inhibits purine synthesis
for ALL and AML
hepatotoxicity

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fludarabine

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adenosine analog
CLL, hairy cell leukemia, HL

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pentostatin/ deoxycoformycin

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inhibitor of adenoside deaminase (ADA)
accumulation of deoxyadenoside and dADP
negative feedback on ribonucleotide reductase
for hairy cell, CLL, Tcell leukemia, macroglobulinemia

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cladribine

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adenosine analog
potent against lymphocytes
CLL, NHL, cutaneous T cell lymphoma

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hydorxyurea

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ribonucleotide reductase inhibitor
myelosuppression, sicle cell, CML

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l-asparaginase

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enzyme that degrades asparagine
forALL
bacterial protein - immunogenic

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doxorubicin

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anthracycline
intercalates DNA and induces topoII dependent DNA breaks
wide use: acute leukemia and lymphoma, Wilms, neuroblastoma

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idarubicin

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anthracycline
AML
oral availability

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tamoxifen

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SERM
antagonist in breast and agonist in endometrium

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raloxifene

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SERM
antagonist in both breast and endometrium

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fulvesterant

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pure estrogen receptor antagonist

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flutamide

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androgen receptor inhibitor
for prostate cancer

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bicalutamide

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anti-androgen

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nilutamide

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anti-androgen

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aminoglutethimide

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aromatase inhibitor
no glucocorticoid synthesis

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anastrozole and letrozole

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aromatase inhibitors
competitive
no DVTs
osteoporosis

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exemestane

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aromatase inhibitor
non-competitive

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leuprolide and goserelin

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GnRH agonists
initially stimulate FSH and LH
later downregulate LH-R in pituitary
for prostate and breast CA

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all trans retinoic acid

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interacts with fusion protein PML-RARa
differentiation of APML cells into neutrophils
for acute promyelocytic leukemia

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glucocorticoids

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high doses incude apoptosis in B cell malignancies
for ALL, MM, B cell lymphomas

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imantinib

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inhibitor of Abl kinase fusion protein, PD-GFR and cKIT
for CML and gastrointestinal stromal tumor

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dasatinib and nilotinib

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2nd gen tyrosine kinase inhibitors (TKI)

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trastuzumab

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monoclonal antibody to HER2
interferes with signaling andcauses immune mediated destruction
HER2 is an oncogene - transmembrane receptor tyrosine kinase
cardiac toxicity - dilated cardiomyopathy

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Lapatanib

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competitive inhibitor of HER2 and HER1

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gefitinib and erlotonib

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inhibitors of EGFR/ HER1
for NSCLC
resistance with 2nd mutations in EGFR

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cetuximab

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monoclonal antibody to EGFR
for breast and colon CA

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sunitinib

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small molecule tyrosine kinase inhibitor targeting VEGFR and PDGF-R
for renal cell cancer

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sorafenib

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small molecule tyrosine kinase inhibitor targeting VEGFR2, 3, cKIT, RAF
for renal cell cancer

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bevacizumab

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aka Avastin
monoclonal antibody to VEGF
improves survival with chemo
for colon, lung, breast and neovascular eye disease
side effects: HTN, pulm hemmorrhage, proteinuria

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temsirolimus

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MTOR inhibitor
for advanced renal cell cancer

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rituximab

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chimeric monoclonal antibody binds CD20
for non-Hodkin lymphoma and autoimmune disorders

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gemtuzumab ozogomicin

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monoclonal antibody against CD33
for AML

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tositumomab and ibritumomab

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anti CD20 antibodies
for low grade follicular NHL resistant to rituximab

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bortezomib

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inhibits 26S proteosome activity
for multiple myeloma

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decitabine

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cytosine analogue
inhibits DNA methyltransferase - de-repress tumor suppressor genes
for myelodysplastic syndrome

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voranistat

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DNA methyltransferase inhibitor
second line treatment for cutaneous T cell lymphoma, glioblastoma multiforme

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PARP inhibitor

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poly(ADP-ribose) polymerase inhibitor
causes single strand nicks in DNA
in BRCA mutations where DNA can't be repaired it kills the cells

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l-asparaginase

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degrades serum asparagine
for ALL because these cells can't make asparagine

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interferons

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bind to receptors to activate JAK tyrosine kinases
antiproliferative activity and immune functions

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IL-2

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activation of immune system
for renal cell cancer and melanoma

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thalidomide

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inhibits angiogenesis and inflammation
for multiple myeloma

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dexrazoxane

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prevents ROS damage to myocardium and prevents acute cardiac toxicity from anthracyclines

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mesna

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binds to toxis metabolites and prevents renal toxicity

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irinotecan

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topoisomerase inhibitor
converted to active metabolite carboxylesterase
myelosuppression and diarrhea

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MTX resistance

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reduced MTX influx into cell - reduced folate carrier RFC
reduced metabolism to active metabolite
increased expression or mutation of DHFR

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cyclophosphamide resistance

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reduced metabolism to active metabolite

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5FU resistance

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reduced metabolism to active metabolite

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gemcitabine resistance

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reduced metabolism to active metabolite

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6-mercaptopurine resistance

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reduced metabolism to active metabolite

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cyclophosphamide resistance

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increased metabolism to Inactive metabolite

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ara-c resistance

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increased metabolism to Inactive metabolite

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anthracycline resistance

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increased GSH expression: detox of ROS

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what is MDR?

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multidrug resistance phenotype
resistance to vinca alkyloids, anthracyclines, actinomycin D, epipodophyllotoxins, steroids
peds tumor overexpression of P-gp (plasma membrane glycoprotein) - ABC family - mdr1 gene
reversed by Ca channel blockers, amiodarone, cyclosporine A, quinidine

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platinum compounds notorious for

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nausea and vomiting

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vinca alkyloids notorious for

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peripheral neuropathy with pain and constipation and SIADH
tissue injury

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antimetabolites notorious for

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mucositis

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anthracyclines notorious for

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cardiac toxicity, nausea and vomiting, myelosuppression, radiation recall, mucositis, secondary malignancy

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gemcitabine notorious for

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non-cardiogenic pulmonary edema

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bleomycin notorious for

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pulmonary fibrosis

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alkylating agents notorious for

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infertility and secondary malignancy

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cyclophosphamide notorious for

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SIADH or renal toxicity

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antiemetics

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serotonin antagonists, ondansetron, granisetron, benzos, antihistamines, phenothiazines, corticosteroids, cannabinoids

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trastuzumab notorious for

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cardiac toxicity