Hamann Cancer
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