Hamann Cancer

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Irinotecan

-Camptosar -colon/small cell lung cancer -IV -prodrug -SE: diarrhea, vomiting, bone marrow suppression, hair loss, shortness of breath, and fever

Certolizumab pegol

-Crohn's disease and arthritis -TNF inhibitor preventing resultant immune responses

Ifosfamide

-DNA cross-linking agent -Testicular cancer, soft tissue sarcoma, osteosarcoma, bladder cancer, small cell lung cancer, cervical cancer, and ovarian cancer -MoA: requires biotransformation in liver

Dacarbazine

-Hodgkin disease and malignant melanoma with vinblastine, bleomycin, and doxorubicin -Metabolism: prodrug -SE: loss of appetite, vomiting, low white blood cell count, and low platelets -MoA: alkylates cross-linking DNA during all phases of the cell cycle

Lomustine

-Hodgkin disease, lymphoma, and brain cancer -MoA: DNA cross-linking agent -highly lipophilic → hydrolyzed into reactive metabolites that cause alkylation and cross-linking

Procarbazine

-Hodgkin's lymphoma and brain cancers. -Used with vincristine, lomustine, prednisone, chlormethine. BEACOPP regimen Bleomycin, Etoposide, Adriamycin, Cyclophosphamide, Vincristine (tradename Oncovin), Prednisone, and Procarbazine -DNA cross-linking agents -inhibit trans-methylation of methionine into tRNA

Idursulfase

-Hunter's syndrome is an X-linked recessive disease caused by insufficient levels of lysosomal enzyme iduronate-2-sulfatase. Idursulfase serves as an endogenous source

Aldoxorubicin

-IV -SE: cardiac tox -MoA: binds selectively to the cysteine-34 position position of albumin -links HYDRAZONE LINKER to induce apoptosis

Interferon Beta

-IV -antiviral, antiproliferative, and immunomodulating -recombinant form used to slow disease progression of multiple sclerosis and reduce clinical symptoms

Oxaliplatin

-IV platinum containing alkylating agent -advanced colorectal cancer -MoA: DNA cross-linking agents

Doxorubicin

-Leukemias, Hodgkin lymphoma, bladder, breast, stomach, lung, thyroid, ovarian, multiple Myeloma -IV -forms complexed with DNA by intercalation between base pairs and inhibits topoisomerase II -HEAVY-LIFTER IN ANTICANCER DRUG COMBOS

Mylotarg

-Metabolism: removed by opsonization -MoA: binding of the anti-CD33 antibody

Denileukin diftitox

-SE: vision loss -MoA: selectively directs the diphtheria toxin to cells expressing IL-2 receptor

Mitoxantrone

-acute leukemia, lymphoma, and prostate and breast cancer -SE: nausea, vomiting, hair loss, heart damage and immunosuppression, possibly with delayed onset, Cardiomyopathy -regular monitoring with echocardiograms or MUGA scans recommended -MoA: intercalation and topoisomerase II inhibitor

Tretinoin

-acute promyelocytic leukemia -SE: when used PO, SOB, headache, numbness, depression, skin dryness, itchiness, hair loss, vomiting, muscle pains, an dvision changes -MoA: binds to and activates retinoic acid receptors

Epirubicin

-adjuvant therapy in patients with axillary node tumor and primary breast cancer -IV -MoA: forms complex by intercalation with base pairs & inhibits topoisomerase II

Carmustine

-alone and in combo -leukemias, lymphomas, and breast, testicular, ovarian, gastric and pancreatic cancer -causes cross-links in DNA and RNA → DNA synthesis inhibition

Gemtuzumab ozogamicin (Mylotarg)

-antibody conjugate with calicheamicin class of cytotoxic agent used to treat acute myeloid leukemia -MoA: CD33, calicheamicins target DNA and cause strand to mess up in the minor groove

Brentuximab vedotin

-antibody-drug conjugate for relapsed or refractory Hodgkin lymphoma and anaplastic large cell lymphoma -Target: CD30 antigen expression

Nitrogen mustards

-bad smell, used as potential warfare -HN-2 used in cancer treatment (not anymore)

Ado-trastuzumab emtansine

-binds HER receptors and internalized into cell -IV-adds 5.8 months of life over combo drugs -MoA: after internalization, conjugate catabolized in the lysosome and DM1 binds to tubulin to cause mitotic arrest and cell death

Valrubicin

-bladder cancer -direct infusion to the bladder -readily penetrates cells -MoA: inhibits incorporation of nucleosides into nucleic acids, causes extensive chromosomal damage, and arrests cell cycle in G2

Temozolomide

-brain cancer -second-line treatment for astrocytoma an first-line treatment for glioblastoma multiforme -MoA: methylation of DNA → DNA replication inhibited

Idarubicin

-breast cancer, lymphomas and leukemias, together with the potential for reduced cardiac toxicity -SE: nausea. vomiting. diarrhea. sores in the mouth and throat. stomach pain. headache. joint pain. hair loss -MoA: intercalation with DNA and topoisomerase II

Thiotepa

-breast, ovarian, and bladder cancer for Hodgkin disease -organophosphorus compound -MoA: converted and induces cross-linking

Docetaxel

-breast, ovarian, prostate, and non-small cell lung cancer -IV infusion -different half lives depending on which phase -SE: hair loss, low blood cell counts, numbness, SOB, vomiting, muscle pains -MoA: binds to beta-tubulin subunit of microtubules

Trabectedin

-caribbean sea squirt -soft tissue sarcoma -MoA: binds in minor groove of DNA

Bevacizumab

-chemo combo -MoA: blocks angiogenesis by inhibiting VEG-F

Chlorambucil

-chronic lymphocytic leukemia (CLL), Hodgkin lymphoma, and non-Hodgkin lymphoma. For CLL it is a preferred treatment -SE: bone marrow suppression, risk of developing cancer, allergic reactions, and infertility -MoA: 3 mechanisms, -DNA cross-linking agent

Alemtuzumab

-chronic lymphocytic leukemia and MS -binds CD52 -SE: rare stroke and bv wall tears -MoA: binding → antibody dependent lysis of leukemic cells

Alglucosidase alpha

-consists of GAA (needed to degrade glycogen to glucose in lysosomes) -Pompe disease in infants and peds -MoA: Acts as an exogenous source of GAA

Bexarotene

-cutaneous T cell lymphoma -off label for lung and breast cancer and Kapodi's sarcoma -inducing changes in gene expression

Bleomycin

-cytotoxic antibiotic for testicular and germ cell cancer, Hodgkin disease, lymphomas and head/neck tumors -MoA: inhibition of DNA synthesis with some evidence of lesser inhibition of RNA and protein synthesis

Letrozole

-did not demonstrate significantly superior efficacy or safety compared with anastrozole

Topotecan

-from an asian tree -ovarian cancer, cervical lung cancer, and others -IV and aerosol -lactone form active -neutropenia, leukopenia, anemia, thrombocytopenia

Interferon alpha

-from human leukocytes with Sendai virus -great inflammatory action which skews immune response towards a Th1 profile -MoA: induce a broad spectrum of anti-viral and immunoregulatory responses -enhances proliferation of human B cells and activate NK cells

Belinostat

-histone deacetylase inhibitor -antineoplastic -refactory/relapsed peripheral T cell lymphoma -IV -SE: nausea, fatigue, pyrexia, anemia, vomiting

Alteplase

-human tissue plasminogen activator, purified, glycosylated, 527 residues purified from CHO cells -for acute MI & ischemic stroke and lysis of acute pulmonary emboli -controls arterial blood clots

Basiliximab

-immunosuppressive for IL-2R alpha or CD25 -for kidney transplant rejection

Arsenic trioxide

-inorganic compound for APL -MoA: causes damage/degradation of promyelocytic leukemia protein/retinoic acid receptor-aplha fusion protein

Daunorubicin

-leukemia and AIDS related Kaposi sarcoma -IV -SE: hair loss, vomiting, bone marrow suppression, inflammation in mouth -inhibits topoisomerase II

Degarelix

-long-acting antagonist for advanced prostate cancer -Half-life 41.5-70.2 days -MoA: competitively inhibits GnHR receptors in pituitary gland, stopping release of LH and FSH → testosterone suppressed → slow growth of cancer

Cyclophosphamide

-lymphoma, multiple myeloma, leukemia, ovarian cancer, breast cancer, small cell lung cancer, neuroblastoma, and sarcoma -immune suppressor for nephrotic syndrome, granulomatosis with polyangiitis, and following an organ transplant, among other conditions -oral and IV administration -low white blood cell counts, loss of appetite, vomiting, hair loss, and bleeding from the bladder -MoA: DNA cross-linking of tumor cell

Etoposide

-mandrake root -oral and IV -inhibits DNA topoisomerase II

Mitotane

-metastatic, unresectable adrenocorticical carcinoma -Half-life: 18-159 days -MoA: modifies peripheral metabolism of steroids and directly supressing the adrenal cortex

Imiglucerase

-modified oligosaccharide chains of human B-glucocerebrosidase -Gaucher's disease -MoA: Catalyzes the hydrolysis of glycolipid glucocerebroside to glucose and ceramide

Pomalidomide

-multiple myeloma (for previous therapy failure) -MoA: enhances T cell and NK cells & inhibit production of pro-inflammatory cytokines -primary target: protein cereblon

Romidepsin

-natural product -IV -SE: nausea, vomiting, anorexia -MoA: binds and inhibits HDAC

Tamoxifen

-non-steroidal antiestrogen for estrogen receptor + BC -2 week half-life -major metabolite: N-desmethyl tamoxifen -SE: narrow therapeutic index, breathing difficulty, or convulsions, increased incidence of uterine malignancies -MoA: competitively inhibits estrogen binding to its receptor, which is critical for it's activity in breast cancer cells

Enzalutamide

-nonsteroidal antiandrogen is used to treat metastatic castration-resistant prostate cancer -oral -half-life 5.8 days -CYP2C8 metabolism -unusual functional groups: Sulphonamide, Nitrile, Trifluoromethyl as well as fluorine and an amide -competitive androgen receptor inhibitor (nuclear translocation → interaction with DNA → decreases proliferation of prostate cells → apoptosis → decreased tumor volume)

Thalidomide

-oral -excreted as a glycine conjugate -MoA: Cul4-Rbx1-DDB1-Cereblon E3 ubiquitin ligase complex is the target

Vorinostat

-oral HDACI/antineoplastic -refractory/relapsed cutaneous T cell lymphoma -2nd gen polar-planar compound, binds to HDAC

Melphalan

-oral and parental -multiple myeloma an ovarian cancer -SE: nausea and bone marrow suppression -MoA: alkylates DNA inducing DNA interstrand cross-linkages

Panobinostat

-oral histone deacetylase inhibitor and neoplastic for refractory or relapsed multiple myeloma -extensively metabolized to 77 metabolites -MoA: DAC inhibitor

Carboplatin

-ovarian, head, neck, and lung cancer -MoA: activated IC to form to induce cross-linking

Bendamustine

-parenterally administered alkylating agent used alone and in combo with other meds for CLL and non-Hodgkin lymphoma and multiple myeloma -SE: Common side effects include low blood cell counts, fever, nausea, diarrhea, loss of appetite, cough, and rash -MoA: causes intra- and interstrand crosslinking

Cisplatin

-platinum-based chemotherapy drug -cancer, sarcoma, carcinoma, lymphomas, and germ cell tumors -MoA: binds to DNA and interfere with the repair mechanism

Cabazitaxel

-prostate cancer that has progressed despite treatment with docetaxel and hormones -MoA binds and stabilizes tubulin resulting in cell cycle arrest

Catumaxomab

-rat-mouse hybrid for metastasizing cancer -binds antigens CD3 and EpCAM -binds to CD3 on killer T cells

Anakinra

-recombinant non glycosylated human IL-1 antagonists -has extra methionine residue at amino terminus -for adult RA and NOMID and MAS (cytokine storm) -SE: not use in people with active infections, latent TB, low WBC counts, or taking TNF inhibitors -MoA: block IL-1 to reduce inflammatory responses and mitigating cartilage degradation and bone resorption

Inotuzumab

-relapsed or refractory B-cell precursor acute lymphoblastic leukemia -IV -MoA: against CD22+

Inotuzumab ozogamicin

-relapsed or refractory B-cell precursor acute lymphoblastic leukemia with CD22 mAB and calicheamicin class -MoA: after cleavage from the MAB in lysosome, it travels to nucleus causing DNA strand breakage

Dactinomycin

-solid tumors in children and choriocarcinoma in adult women -Metabolism: only slightly -MoA: binds strongly and reversibly to DNA

Teniposide

-solid tumors, leukemia, lymphoma -inhibits DNA synthesis by forming complex with toposiomerase II and DNA

Leuprolide

-synthetic analog of GnRH -treat advanced prostate cancer, uterine fibroids, and endometriosis -IM or IV -MoA: binds to the gonadotropin releasing hormone receptor and potently inhibits gonadotropin secretion

Belimumab

-systemic lupus erythematosis -fully human recombinant mab -MoA: Inhibits BLyS from binding on B lymphocytes which is essential to cell survival

Canakinumab

-targeted at Il-1B used to treat CAPS, FCAS, MWS, and lung cancer -neutralizes its inflammatory activity bl blocking its interaction with IL1 receptors

Lenalidomide

-thalidomide derivative -multiple myeloma, hematological disorders (MDS) -MoA: inhibits COX-2 in vivo → induces tumor cell apoptosis

Nusinersen

-there's only one of these so it might be a question -for spinal muscular atrophy associated with a mutation in the SMN1 gene -goes directly to the CNS via intrathecal injection -only for young babies bc pricey -Half life: 63-135 days -SE: Acute neurological impairment observed in adult monkeys -MoA: antisense, splice-altering oligonucleotide that increases exon 7 inclusion in SMN2 and mRNA transcripts to produce full-length SMN protein

IL-2 fusion protein

-this one was in all red -produced by T-cells in response to antigenic or mitogenic stimulation -regulates immune response -stimulate all the fighter cells -Il2/antibody complexes called SUPERKINES -MoA; kinase activity activator

Tenecteplase

-thrombolytic agent for MI and PE -binds to fibrin rich clots

Mechlorethamine

-topical for cutaneous T-cell lymphomas and mycosis fungoides -DNA-cross linking agent (nitrogen mustard) -Hodgkins, chronic leukemia, lung cancer and polycythemia vera -interferes with DNA replication and transcription of RNA

Streptozocin

-unique to treat metastatic pancreatic islet cell carcinome -IV -SE: N&V -MoA: DNA cross linking agent, interfere with biochem reactions of NAD and NADH and enzyme inhibition

Clofarabine

2nd gen prine nucleoside antimetabolite FOR CHILDREN (lymphoma if other treatments fail) MoA: depletion of IC dNTP to block DNA synthesis

Nelarabine

Acute T-cell lymphoblastic leukemia Purine nucleoside analog

Cytarabine

Acute non-lymphoblastic leukemia Used with daunorubicin MoA: incorporates into DNA and inhibit DNA polymerase

Ixabepilone

Binds to tubulin and promotes tubulin polymerization and microtubule stabilization causing cell cycle arrest

Hydroxyurea

Cancer and Stimulate fetal hemoglobin production in sickle cell disease MoA: converted into free radical NO in vivo → repair of DNA inhibited

Trifluridine/tipiracil

Combo drug 3rd or 4th line for metastatic colorectal cancer MoA: DNA poly inhibitor by incorporating into DNA

Pemetrexed

Combo with cisplatin for malignant pleural mesothelioma MoA: antifolate

Pralatrexate

First drug approved for relapsed or refractory peripheral T-cell lymphoma or PTCL MoA: antifolate, competitively inhibits DHFR, cell unable to synthesize DNA and RNA

Methotrexate

GAntimetabolite Leukemia, lymphoma, solid tumors, psoriasis, and rheumatoid arthritis Immunosuppressive Half life: 3-10 hours in adults HEPATOTOXIC SE: neuro damage and memory loss MoA: inhibits enzymes responsible for nucleotide synthesis

Cladribine

Immmunosuppresive effects Lymphoproliferative diseases including hairy-cell leukemia MoA: adds to dNTP causing DNA strand breaks

Fludarabine

Leukemia and lymphoma Inhibit DNA polymerase alpha, ribonucleotide reductase, and DNA primase

Azacitidine

MDS MoA: DNA methyltransferase inhibitor at low doses and cytotoxicity thru incorporation into RNA and DNA at high disease

Pentostatin

Nonlymphocytic leukemia and hairy cell leukemia MoA: IC activation results in incorporation into DNA as a false purine base

**Gemcitabine**

This one was in red so must be important Nucleoside analog NSCLC, pancreatic, bladder, and breast cancer IV Half life: 42-94 min (short infusion) or 245-638 min (long infusion) Metabolism: can undergo deamination to an inactive uracil metabolite PRODRUG MoA: DNA polymerase inhibitor and inhibits ribonucleotide reductase

Thioguanine

acute leukemia SE: bone marrow suppression, liver problems, mouth inflammation MoA: incorporates into DNA and resulting in inhibition of DNA and RNA synthesis and cell death

Capecitabine

advanced breast and colon cancer Used in combo Off label: gastric and esophageal cancer PRO DRUG metabolized by tumor and normal cells and inhibits DNA synthesis and cell division Pyrimidine antagonist

Anastrozole

aromatase inhibitor -a nonsteroidal inhibitor of estrogen synthesis -selectively binds to and reversibly inhibits aromatase -nonsteroidal benefits include an absence of weight gain and acne -contains two nitrile groups and a triazole

Anastrozole (Arimidex)

aromatase inhibitor -endocrine drugs of choice in the treatment/prevention of postmenopausal breast cancer due to more favorable efficacy and adverse effect profile as compared to earlier estrogen receptor modulators such as tamoxifen -oral Half-life: 50 hours -SE: hot flashes, increased risk of heart disease and osteoporosis

Paclitaxel

breast, lung, ovarian, cervical, pancreatic, Kaposi's sarcoma Messes with microtubules

Vinorelbine

breast, non-small cell lung cancer 3rd gen in platinum combo with advanced NSCLC metabolism: metabolites in blood, plasma, and urine MoA: mitotic spindle poison that interferes with chromosomal segregation during mitosis/cell division

Fluorouracil

colon, esophageal, stomach, pancreatic, breast, skin, and cervical cancer SE: mouth and skin inflammation, loss of appetite, low blood cell counts, hair loss MoA: converted into active metabolite, replaces uracil in RNA, inhibiting cell growth

Consensus interferon (CIFN)

hep c

Mercaptopurine

immunosuppressant properties Leukemia and Crohn's disease SE: bone marrow suppression, liver tox, vomiting, loss of appetite Harmful in pregnancy

Vincristine

leukemia, lymphoma, myeloma, breast cancer, head and neck cancer SE: change in sensation, hair loss, constipation, difficulty walking, headaches, infection NOT for pregnant patients MoA: binds irreversibly to microtubules in the S phase

Floxuridine

liver metastases if GI adenocarcinima IV infusion MoA: pyrimidine antagonist antimetabolite Incorporates into RNA and disrupts DNA

Eribulin (Halaven)

metastatic breast cancer with two treatments before From marine sponge lol Inhibits the growth phase of microtubules

Vinblastine

used in combo for Hodgkin's lymphoma, NSC lung, brain, bladder, Milano a, testicular cancers Metabolism: metabolite more active


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