-
DNA Alkylating or Methylating
- crosslinking btw DNA; modify base in DNA; cytotoxic to dividing/nondividng cells;
- myelosuppression/alopecia/amenorrhea/male sterility
-
Mechlorethamine
- DNA modifying; nitrogen mustards; crosslink DNA; MOPP for Hgk;
- toxicity-bone marrow/GI
-
Cyclophosphamide
- DNA modifying; nitrogen mustards; crosslink DNA;
- CMF, CVPP for Hgk/NHgk/breast/ovarian;
- Acrolein-hemorrhagic cystitis, treat with MESNA(acrolein inactivator)
-
Ifosfamide
- DNA modifying; nitrogen mustards;
- same as Cyclophophamide, less toxic,
- high doses=neurotoxicity
-
Melphalan
- DNA modifying; nitrogen mustards; crosslink DNA;
- multiple myeloma/ovarian cancer;
- toxicity-nausea/bonemarrow
-
Carmustine / Lomustine
- DNA modifying; nitrosoureas; alkylate DNA;
- brain tumors
- toxicity-myelosuppression/renal failure; highly lipophilic cross BBB
-
Busulfan
- DNA modifying; alkyl sulfonates; crosslinks; Leukemia;
- toxicity-pulmonary fibrosis, hyperpigmentation
-
Procarbazine
- DNA modifying; inhib DNA/RNA/pro syn;
- MOPP, CVPP for Hgk/NHgk/SCLC/melanoma/brain tumors;
- toxicity-BM/acetylaldehyde accumulation/monoamine oxidase P450 inhib;
- no milk/wine/drugs
-
Dacarbazine
- DNA modifing; triazens; form toxic methyl carbonium ions;
- Hgk
- toxicity-BM/GI/hepatotox
-
Cisplatin / Carboplatin
- DNA modifying; platinum complexes; crosslink;
- testicular (Vinblastine & Bleomycin) Ovarian (cyclophophamide) SC Lung (Etoposide) bladder;
- toxicity-ototox/nephtox;
- Carboplatin less toxic, for kidney pt
-
Methotrexate
- Antimetabolites; Folic acid analogs; S-phase specific, inhib DHFR-decr thymidylic acid;
- curative high dose- Choriocarcinoma, Osteogenic carcinoma;
- ALL/Burkitss/Breast/NHgk/head/neck/bladder; CMF;
- decree RA/psoriasis; tox-BM/GI/renal/hepatic fibrosis/nephrotox
- Leucovorin reduces toxicity; resistance-incr/altered DHFR
-
Leucovorin
- Antimetabolites; Folate antagonist rescue agent;
- reduces methotrexate toxicity
-
6-Mercaptopurine (6-MP)
- Antimetabolites; Purine analogs; S-phase specific HGPRT;
- ALL/ AML;
- tox-BM/hyperuricemia; allopurinal incr 6-MP toxicity
-
6-Thioguanine (6-TG)
- Antimetabolites; Purine analogs;
- AML (cytarabine and Daunorubicin);
- toxicity-BM/hyperuricemia
-
5-Fluorouracil (5-FU)
- Antimetabolites; Pyrimidine analogs; S-phase specific inhib tymidylate synthase;
- CMF-breast, FAM-colon;
- Toxicity-myelosuppression/GI; cimetidine-heartburn drug higher survival rate;
- Cisplatin/Leucovorin/Methotrexate modulate activity
-
Capecitabine
- Antimetabolites; Pyrimidine analogs; 5-FU prodrug;
- colon/breast
-
Cytarabine (AraC)
- Antimetabolites; Pyrimidine analogs; becomes Ara CTP which incorporates and terminates DNA elongation;
- AML (6-TG)
- tox-myelosuppression
-
Gemcitabine
- Antimetabolites; Pyrimidine analogs; Not S-phase specific,inhib DNA pol;
- pancreatic/NSCLC
- toxcity-myelosupppression/flu-like/incr liver enzyme
-
Vinblastine
- Natural products; Phase Specific; Vinca Alkaloids; bind tubulin;
- testicular (Bleomycin, Cisplatin)
- ABVD-Hgk/NHgk/Choriocarcinoma
- toxicity-BM
-
Vincristine
- Natural products; Phase Specific; Vinca Alkaloids; bind tubulin;
- ALL, MOPP-Hgk, NHgk, solid tumors;
- Toxicity-peripheral neuropathy
-
Paclitaxel / Docetaxel
- Natural products; Phase Specific; Taxanes; M-phase specific, promotes MT formation;
- metastatic ovarian/breast;
- toxicity-hypersensitivity (tx-dexamethasome, diphenhydramine) Neurtopenia (tx-GCS-F)
-
Etoposide
- Natural products; Phase Specific; Podophyllotoxins; inhib Topoisomerase II;
- testicular tumors (Bleomycin, Cisplatin) SC carcinoma lung (Cisplatin, Ifosfamide), NHgK/Leuk/Kaposi
- toxicity-myelosuppression
-
Topotecan
- Natural products; Phase Specific; Camptothecins; inhib Topoisomerase I;
- metastatic ovarian/SCLC;
- toxicity-diarrhea/BM/alopecia/naus/bronzing;
- UGT1A1, bilirubin detox enzyme->l low level WBC
-
Irinotecan
- Natural products; Phase Specific; Camptothecins; inhib Topoisomerase I;
- Colorectal Cancer;
- toxicity-diarrhea/BM/alopecia/naus/bronzing;
- UGT1A1, bilirubin detox enzyme->l low level WBC
-
Bleomycin
- Natural products; Phase Specific; G2-phase specific, binds DNA;
- testicular carcinomas (Cisplatin, Vinblastine, Etoposide) squamous cell carcinoma, lymphoma;
- toxicity-phneumonitis/pulmonary fibrosis/hyperpigmentation
-
Actinomycin D (Doxorubicin)
- Natural products; DNA-binding antibiotics;
- Wilm's Tumor, Rhabdomyosarcoma (vincristine, cyclosphosphamide);
- toxicity-myelosuppression/GI
-
Adriamycin
- Natural products; DNA-binding antibiotics; Anthracyclines; intercalate with DNA;
- ABVD, FAM for myelomas/sarcomas/lymphomas
- toxicity-cardiotoxicity
-
Daunorubicin
- Natural products; DNA-binding antibiotics; Anthracyclines; intercalate with DNA;
- AML, ALL;
- toxicity-cardiotoxicity
-
Epirubicin
- Natural products; DNA-binding antibiotics; Anthracyclines; intercalate with DNA;
- CEF for breast (more effective than CMF in premenopausal)
- toxicity-cardiotoxicity
-
Hydroxyurea
- Misc Antineoplastic Agent; S-phase specific, inhib ribonucleoside diphosphate reductase;
- leukemias
- toxicity-myelosuppression
-
L-asparaginase
- Misc Antineoplastic Agent; deprives cell of asparagine, effects protein syn;
- ALL (Vincristine, Prednisone)
- toxicity-hypersensitivity/hyperglycemia/coag defects/hypboalbuminemia
-
Thalidomide
- Misc Antineoplastic Agent; stimulates T and NK cells, inhib angiogenesis;
- multiple myelomas;
- toxicity-sedation/constipation
-
Vorinostat
- Misc Antineoplastic Agent; HDAC inhib, apop;
- Tcell lymphomas;
- toxicity-fatigue/diarrhea/ nausea/anorexia/thrombocytopenia/PE
-
Bortezomib
- Misc Antineoplastic Agent; proteasome inhibitor; 26Sproteosome inhib;
- multiple myeloma;
- toxicity-nausea/diarrhea/weak muscles/BM/fever/anorexia
-
Imatinib mesylate
- Misc Antineoplastic Agent; Protein Tyrosine Kinase Inhibitor; binds Bcr-Abl kinase;
- CML
- toxicity-nausea/muscle cramps/neutropenia/thrombocytopenia;
- competitive inhib of CYP3Y, 2C9, 2D6 so give Rx that aslo inhib->incr [imatinib]
-
Getfitinib / Erlotinib
- Misc Antineoplastic Agent; Protein Tyrosine Kinase Inhibitor; inhib EGFR;
- NSCLC
- toxicity-fatique, well-tolerated; polymorphs in EGFR correlate with drug efficacy;
- P450 inducers -> decr [Getfitinib]
-
Sunitinib
- Misc Antineoplastic Agent; Protein Tyrosine Kinase Inhibitor; inhib VEGFR, PDGFR;
- advanced renal cell carcinoma, Gi stromal tumors;
- toxicity-fatigue, well tolerated
- metab by CYP3A4
-
Sorafenib
Misc Antineoplastic Agent; Protein Tyrosine Kinase Inhibitor
-
Lapatinib
- Misc Antineoplastic Agent; Protein Tyrosine Kinase Inhibitor; EGFR, HER2 kinase blockers;
- ER+ breast cancer (letrozole/capecitabin);
- toxicity-fatigue, rash;
-
Trastuzumab
- Misc Antineoplastic Agent; Monocolonal Ab; blocks HER2/neu R;
- metastatic breast cancer w/ amplified HER2;
- toxicity-cardiotox with Adriamycin;
- doesn't cross BBB
-
Rituximab
- Misc Antineoplastic Agent; Monocolonal Ab; binds CD20 on Bcells, cause lysis;
- low-grade B cell NHgk;
- toxicity-fever/chills/nausea on first infusion
-
Cetuximab
- Misc Antineoplastic Agent; Monocolonal Ab; Binds EGFR;
- colon cancer;
- toxicity-acne like rash
-
Interferon-alfa
- Misc Antineoplastic Agent; Biological Response Modifiers; activate sin of 2'5'oligoadenylate synthase, proto-onc, decr c-myc, inhib port sin, activate nuclease;
- hairy cell leukemia/Kaposi/malignant melanoma;
- toxicity-fever/chills/myelosup/neurotox
-
Tamoxifen
- Hormonal Agents; Selective Estrogen Receptor Modulators; competitive inhib of estradiol, suppress growth, decree TGF IGF-1;
- advanced ER= breast cancer
- toxicity-hot flashes/vaginal bleeding/skin rashes/hypercalcemia/endometrial cancer risk
- resistance-decr affinity to receptor;
- Pro-estrogen on bone, lipids, uterus ->slow osteoporosis, decree cholesterol
-
Aminoglutethimide
- Hormonal Agents; Aromatase Inhibitors; reduces estradiol levels;
- metastatic breast cancer (glucocorticoid);
- toxicity-CNS depression/drowsiness/visual blurring/ataxia
-
Anastrozole
- Hormonal Agentst; Aromatase Inhibitors;
- advanced breast cancer in post-menop;
- toxicity-GI/myalgia/headache/bone/back reduced blood clots than tamoxifen
-
Leuprolide / Goserelin
- Hormonal Agentst; long-acting gonadotropin releasing, hormone analogs; continuously inhib FSH and LF;
- MOPP, CVPP,
- ALL/CLL/Hgk/NHgk/breast;
- toxicity-Cushing's/immunosuppression
-
Flutamide
- Hormonal Agents; Antiandrogens; blocks DHT binding to Androgen receptor;
- prostate cancer;
- toxicity-GI
-
MOPP
- Mechlorethamine, Oncovin, Prednisone, Procarbazine;
- Hgk
-
CVPP
- Cyclophosphamide, Vincristine, Prednisone, Procarbazine;
- NHgk
-
CMF
- Cyclophosphamide, Methotrexate, 5-fluorouracil;
- ER-Breast
-
ABVD
- Adriamycin, Bleomycin, Vinblastine, Dacarbazine;
- Lymphomas and Sarcomas
-
FAM
- 5-Fluorouracil, Adriamycin, Mitomysin;
- Colon
-
CMV
Cisplatin, Methotrexate, Vinblastine
-
FAC
5-Flurouracil, Adriamycin, Cyclophophamide
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