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Class: Antineoplastic (Cell Cycle-Nonspecific) (Alkylating Agent) (Mustard) Class: Antineoplastic (Cell Cycle-Nonspecific) (Alkylating Agent) (Mustard)
Mech.: Alkylates DNA → crosslinkages. Mech.: Alkylates DNA → crosslinkages.
Absorption: Absorption:
Dist.: Dist.:
Metab.: Metab.:
Excretion, t_: Excretion, t_:
Toxicity/S.E.s: N/V. DLT = bone marrow suppression, esp. leukocytosis. Max. Toxicity/S.E.s: Seizures DLT = bone marrow suppression, pulmonary fibrosis.
suppression at 10-12 days, recovery around 42 days. Utility: CLL
Utility: Hodgkin’s disease (in combination therapy—MOPP). Special Features: Slow-acting. Good activity against some chronic cancers.
Special Features: Fast-acting. Active against a wide variety of cancers. Not
widely used due to toxicity.
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Name: BCNU (Carmustine) Name: CCNU (Lomustine)
Class: Antineoplastic (Cell Cycle-Nonspecific) (Alkylating Agent) (Nitrosourea) Class: Antineoplastic (Cell Cycle-Nonspecific) (Alkylating Agent) (Nitrosourea)
Mech.: Alkylates DNA → crosslinkages. Mech.: Alkylates DNA → crosslinkages.
Absorption: Absorption: Crosses BBB.
Dist.: Crosses BBB. Dist.:
Metab.: Metab.:
Excretion, t_: Excretion, t_:
Toxicity/S.E.s: N/V. DLT = bone marrow suppression. Max. suppression at 28 Toxicity/S.E.s: N/V. DLT = bone marrow suppression. Max. suppression at 28
days, recovery around 42 days. Pulmonary fibrosis, renal days, recovery around 42 days. Pulmonary fibrosis, renal
toxicity. toxicity.
Utility: Hodgkin’s and non-Hodgkin’s lymphomas, primary glioblastoma, brain Utility: Hodgkin’s and non-Hodgkin’s lymphomas, primary glioblastoma, brain
tumors. tumors.
Special Features: Fast-acting. Active against a wide variety of cancers. Not Special Features: Fast-acting. Active against a wide variety of cancers. Not
widely used due to toxicity. widely used due to toxicity.
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Name: Procarbazine (Mutalane) Name: Dacarbazine (DTIC)
Class: Antineoplastic (Cell Cycle-Nonspecific) (Alkylating Agent) Class: Antineoplastic (Cell Cycle-Nonspecific) (Alkylating Agent)
Mech.: Alkylates DNA. Mech.: Alkylates DNA.
Absorption: Absorption:
Dist.: Dist.:
Metab.: Metab.:
Excretion, t_: Excretion, t_:
Toxicity/S.E.s: N/V. Leukopenia and thrombocytopenia. Inhib. MAO (danger Toxicity/S.E.s: N/V. Leukopenia and thrombocytopenia.
w/tyramine-containing foods). Disulfiram-type rxn w/alcohol. Utility: Melanoma.
Utility: Hodgkin’s disease. Special Features:
Special Features:
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Name: Doxorubicin (Adriamycin) Name: Mitoxantrone (Novantrone)
Class: Antineoplastic (Cell Cycle-Nonspecific) (Antibiotic) (Anthracycline) Class: Antineoplastic (Cell Cycle-Nonspecific) (Antibiotic) (Anthracycline)
Mech.: Intercalation into DNA → stabilization of topoisomerase II-DNA Mech.: Intercalation into DNA → interference w/topoisomerase II-catalyzed
cleavable complexes → DNA breaks. Quinone structure reduced by cyt. breakage-reunion reaction of DNA strands to cause unreparable breaks.
P-450 → oxygen radical production → DNA strand breaks. Quinone structure reduced by cyt. P-450 → oxygen radical production
Absorption: → DNA strand breaks.
Dist.: Absorption:
Metab.: Dist.:
Excretion, t_: Metab.:
Toxicity/S.E.s: Myelosuppression—max. in week 2, recovery in week 4. Excretion, t_:
Radiation recall (hypersensitivity and necrosis in prev. or Toxicity/S.E.s: Myelosuppression—max. in week 2, recovery in week 4.
subseq. irradiated tissue). DLT = cardiomyopathy in 1/3 of pts if Radiation recall. DLT = cardiomyopathy.
total dose exceeds 550 mg/m2. Utility: One of the most useful cancer drugs. Soft-tissue, osteogenic and
Utility: One of the most useful cancer drugs. Soft-tissue tumors, osteogenic other sarcomas, small cell CA of lung, Hodgkin’s and non-Hodgkin’s
and other sarcomas, small cell CA of lung, Hodgkin’s and non-Hodgkin’s lymphomas, acute leukemias, others.
lymphomas, acute leukemias, others. Special Features: Synthetic doxorubicin with reduced cardiotoxicity.
Special Features:
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Name: Mitomycin C (Mutamycin) Name: Bleomycin (Blenoxane)
Class: Antineoplastic (Cell Cycle-Nonspecific) (Antibiotic) (Quinone) Class: Antineoplastic (Cell Cycle-Specific) (Antibiotic)
Mech.: DNA alkylation/adduction, formation of oxygen radicals. Mech.: Binds DNA and copper or iron. The metals generate reactive oxygen
Absorption: species → double strand breaks in DNA.
Dist.: Absorption:
Metab.: Dist.:
Excretion, t_: Metab.:
Toxicity/S.E.s: N/V. DLT = bone marrow suppression (cumulative). Very toxic. Excretion, t_:
Utility: Bladder cancer, some GI cancers. Toxicity/S.E.s: N/V, skin toxicity. DLT = pulmonary fibrosis at total dose of
Special Features: 400 units (can be fatal).
Utility: Testicular tumors (curative), head and neck tumors, cervical tumors,
squamous cell CA, lymphomas.
Special Features: Myelosuppression is rare.
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Name: 6-Mercocaptopurine/6-MP (Purinethol) Name: Methotrexate (Amethopterine)
Class: Antineoplastic (Cell Cycle-Specific) (Antimetabolite) (Guanine Analog) Class: Antineoplastic (Cell Cycle-Specific) (Antimetabolite) (Folic Acid Analog)
Mech.: Inhibits DNA and protein synthesis. Mech.: Inhib. dihydrofolate reductase and thymidylate synthase → ↓ DNA
Absorption: synth.
Dist.: Absorption:
Metab.: Dist.:
Excretion, t_: Metab.:
Toxicity/S.E.s: N/V. DLT = bone marrow suppression. Excretion, t_:
Utility: Maintenance of remission of ALL. Toxicity/S.E.s: GI toxicity, N/V. DLT = bone marrow suppression. Renal
Special Features: tubular damage w/↑ doses
Utility: Curative for choriocarcinoma and osteogenic sarcoma. ALL
maintenance. Breast cancer.
Special Features: Follow treatment w/leucovorin admin. to rescue the bone
marrow.
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Name: Vincristine (Oncovin) Name: Vinblastine (Velban)
Class: Antineoplastic (Cell Cycle-Specific) (Vinca Alkaloid) Class: Antineoplastic (Cell Cycle-Specific) (Vinca Alkaloid)
Mech.: Binds tubulin → prevention of microtubule formation → block of mitosis Mech.: Binds tubulin → prevention of microtubule formation → block of mitosis
in metaphase. in metaphase.
Absorption: Absorption:
Dist.: Dist.:
Metab.: Metab.:
Excretion, t_: Excretion, t_:
Toxicity/S.E.s: N/V. Bone marrow suppression. DLT = neurotoxicity. Toxicity/S.E.s: N/V. DLT = Bone marrow suppression.
Utility: Hodgkin’s disease and other lymphomas. ALL in kids, Wilm’s tumor, Utility: Hodgkin’s disease and other lymphomas, testicular tumors + bleomycin
Ewing’s soft-tissue sarcomas. and cisplatin.
Special Features: Special Features:
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Name: Tamoxifen (Nolvadex) Name: Leuprolide (Lupron)
Class: Antineoplastic (Hormone) (Estrogen Analog) Class: Antineoplastic (Hormone) (GnRH Analog)
Mech.: Antiestrogen → depletion of estrogen receptors. Mech.: Occupies GnRH receptor in pituitary → desensitization → inhib. of
Absorption: release of FSH and LH.
Dist.: Absorption:
Metab.: Dist.:
Excretion, t_: Metab.:
Toxicity/S.E.s: Rarely severe. N/V, hot flashes. Excretion, t_:
Utility: Estrogen receptor positive breast cancer. Has potential to cause Toxicity/S.E.s: Less toxic than DES. N/V, hot flashes, impotence.
endometrial cancer. Utility: Prostatic cancer.
Special Features: Special Features:
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Name: Interferon α Name: Bacillus Calumet-Guerin (BCG)
Class: Immunostimulant Class: Immunostimulant
Mech.: Binds to cell-surface receptors → inhib. of viral replication, inhib. of cell Mech.: Viable strain of Mycobaterium bovis. Enhances Mφ activity, promotes Mφ
proliferation. tumoricidal activity.
Absorption: Absorption:
Dist.: Dist.:
Metab.: Metab.:
Excretion, t_: Excretion, t_:
Toxicity/S.E.s: Fever w/chills; dose-related leukopenia, thrombocytopenia;
Toxicity/S.E.s:
fatigue, malaise, anorexia, weight loss, alopecia, transient elevation of
liver enzymes. High doses may → transient & reversible nephrotoxicity. Utility: Treat bladder carcinoma and melanomas.
Special Features:
Utility: IFN α2A is approved for mgt. of hairy cell leukemia. Also useful for
chronic hepatitis B, virally induced tumors, recurrent varicella zoster,
HSV keratitis, Kaposi’s sarcoma, cutaneous T cell lymphoma.
Special Features: Produced by mononuclear leukocytes. Interferon production
is induced by dsRNA (poly I:C), ampligen (mismatched
nucleotides), LPS.
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