Block 3 materials (Anticancers) Flashcards by isabelle courtney

Bleomycin

MOA:

Clinical uses:

Adverse effects:

MOA:
Forms free radicals to cause DNA strand breaks in G2 & Mitosis

Clinical uses:
Testicular cancer
Hodgkin Lymphoma

Adverse effects:
1) Pulmonary fibrosis
2) Skin hyperpigmentation

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MOA:
Forms free radicals to cause DNA strand breaks in G2 & Mitosis

Clinical uses:
Testicular cancer
Hodgkin Lymphoma

Adverse effects:
1) Pulmonary fibrosis
2) Skin hyperpigmentation

Bleomycin

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What drugs are used to treat Hodgkin Lymphoma?

Adriamycin
Bleomycin
Vinblastine
Dacarbazine

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Dactinomycin (Actinomycin D)

MOA:

Clinical uses:

Adverse effects:

MOA:
Intercalates into DNA to prevent RNA synthesis (blocks RNA polymerase) in G2 & Mitosis

Clinical uses:
Childhood tumors
- Wilms
- Ewing sarcoma
- Rhabdomyosarcoma

Adverse effects:
Myelosuppression

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MOA:
Intercalates into DNA to prevent RNA synthesis (blocks RNA polymerase) in G2 & Mitosis

Clinical uses:
Childhood tumors
- Wilms
- Ewing sarcoma
- Rhabdomyosarcoma

Adverse effects:
Myelosuppression

Dactinomycin (Actinomycin D)

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Anthracyclines

MOA:

Clinical uses:

Adverse effects:

Doxorubicin & Daunorubicin

MOA:
Makes free radicals that intercalate into DNA & cause strand breaks to reduce replication & inhibit topoisomerase II (DNA gyrase)

Clinical uses:
Solid tumors
Leukemia
Lymphoma

Adverse effects:
1) Dilated cardiomyopathy (avoid with dexrazoxane)
2) Alopecia
3) Myelosuppression

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Doxorubicin & Daunorubicin

MOA:
Makes free radicals that intercalate into DNA & cause strand breaks to reduce replication & inhibit topoisomerase II (DNA gyrase)

Clinical uses:
Solid tumors
Leukemia
Lymphoma

Adverse effects:
1) Dilated cardiomyopathy (avoid with dexrazoxane)
2) Alopecia
3) Myelosuppression

Anthracyclines

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Thiopurines

MOA

Clinical uses

Adverse effects

Azathioprine & 6-Mercaptopurine

MOA: Antimetabolites
Purine (thiol) analogs that reduce de novo purine synthesis.
AZA is converted to 6-MP & then activated by HGPRT to form purine analogs that insert into DNA/RNA to halt synthesis

Clinical uses:
Prevent organ transplant rejection
Weaning off steroids
Rheumatoid arthritis
IBD
SLE
ALL
Steroid factory disease

Adverse effects:
1) 6-MP toxicity when given with Allopurinol or Febuxostat (antigout)
2) Pancreatitis
3) Myelosuppression
4) Liver & Gi toxicity

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Azathioprine & 6-Mercaptopurine

MOA: Antimetabolites
Purine (thiol) analogs that reduce de novo purine synthesis.
AZA is converted to 6-MP & then activated by HGPRT to form purine analogs that insert into DNA/RNA to halt synthesis

Clinical uses:
Prevent organ transplant rejection
Weaning off steroids
Rheumatoid arthritis
IBD
SLE
ALL
Steroid factory disease

Adverse effects:
1) 6-MP toxicity when given with Allopurinol or Febuxostat (antigout)
2) Pancreatitis
3) Myelosuppression
4) Liver & Gi toxicity

Thiopurines

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Cladribine & Pentostatin

MOA:

Clinical uses:

Adverse effects:

MOA: Antimetabolites
Purine analogs that cause premature DNA breaks

Clinical uses Antimetabolites:
Hairy cell leukemia

Adverse effects:
1) Nephrotoxicity
2) Neurotoxicity
3) Myelosuppression

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MOA: Antimetabolites
Purine analogs that cause premature DNA breaks

Clinical uses:
Hairy cell leukemia

Adverse effects:
1) Nephrotoxicity
2) Neurotoxicity
3) Myelosuppression

“Purine analogs break hairy Cell leukemia”

Cladribine & Pentostatin

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Cytarabine (arabinofuranosylcytosine)

MOA:

Clinical uses:

Adverse effects:

MOA: Antimetabolites
Pyrimidine analog that causes DNA chain termination & DNA polymerase inhibition during S phase

Clinical uses:
Leukemias (ALL & AML)
Lymphomas

Adverse effects:
1) Myelosuppression
2) Megaloblastic anemia

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MOA: Antimetabolites
Pyrimidine analog that causes DNA chain termination & DNA polymerase inhibition during S phase

Clinical uses:
Leukemias (ALL & AML)
Lymphomas

Adverse effects:
1) Myelosuppression
2) Megaloblastic anemia

Cytarabine (arabinofuranosylcytosine)

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5-Fluorouracil

MOA:

Clinical uses:

Adverse effects:

MOA: Antimetabolites
Pyrimidine analog that is bioactivated by 5-FdUMP to inhibit thymidylate synthase to reduce DNA synthesis

Clinical uses:
Colon & Pancreatic cancers
Actinic keratosis
Basal cell carcinoma

Adverse effects:
1) Myelosuppression
2) Palmar-Plantar erythrodysesthesia (hand/foots syndrome)

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MOA: Antimetabolites
Pyrimidine analog that is bioactivated by 5-FdUMP to inhibit thymidylate synthase to reduce DNA synthesis

Clinical uses:
Colon & Pancreatic cancers
Actinic keratosis
Basal cell carcinoma

Adverse effects:
1) Myelosuppression
2) Palmar-Plantar erythrodysesthesia (hand/foots syndrome)

5-Fluorouracil

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Hydroxyurea

MOA:

Clinical uses:

Adverse effects:

MOA: Antimetabolites
Inhibits RNR (ribonucleotide reductase) to reduce DNA synthesis in S phase

Clinicals:
1) Myeloproliferative disorders (CML, & Polycythemia vera)
2) Megaloblastic anemia

Adverse effects:
1) Severe myelosuppression
2) Megaloblastic anemia

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MOA: Antimetabolites
Inhibits RNR (ribonucleotide reductase) to reduce DNA synthesis in S phase

Clinicals:
1) Myeloproliferative disorders (CML, & Polycythemia vera)
2) Megaloblastic anemia

Adverse effects:
1) Severe myelosuppression
2) Megaloblastic anemia

Hydroxyurea

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Methotrexate

MOA:

Clinical uses:

Adverse effects:

MOA: Antimetabolites
Folic acid analog that competitively inhibits dihydrofolate reductase to reduce DNA synthesis

Clinicals:
- Cancers
(leukemias (ALL), lymphomas, choriocarcinoma, & sarcomas)
- Ectopic pregnancy
- Medical abortion (with misoprostol)
- Rheumatoid arthritis
- Psoriasis
- IBD
- Vasculitis

Adverse:
1) Myelosuppression (give leucovorin)
2) Hepatotoxicity
3) Mucositis (Mouth ulcers)
4) Pulmonary fibrosis
5) Folate deficiency
6) Nephrotoxicity

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MOA: Antimetabolites
Folic acid analog that competitively inhibits dihydrofolate reductase to reduce DNA synthesis

Clinicals:
- Cancers
(leukemias (ALL), lymphomas, choriocarcinoma, & sarcomas)
- Ectopic pregnancy
- Medical abortion (with misoprostol)
- Rheumatoid arthritis
- Psoriasis
- IBD
- Vasculitis

Adverse:
1) Myelosuppression (give leucovorin)
2) Hepatotoxicity
3) Mucositis (Mouth ulcers)
4) Pulmonary fibrosis
5) Folate deficiency
6) Nephrotoxicity

Methotrexate

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Busulfan

MOA:

Clinical uses:

Adverse effects:

MOA: Alkylating agent
Cross-links DNA via guanosine (N7) that affects a cell’s ability to multiply

Clinicals:
Ablate bone marrow (transplant)

Adverse effects:
1) Severe myelosuppression
2) Pulmonary fibrosis
3) Hyperpigmentation

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MOA: Alkylating agent
Cross-links DNA via guanosine (N7) that affects a cell’s ability to multiply

Clinicals:
Ablate bone marrow (transplant)

Adverse effects:
1) Severe myelosuppression
2) Pulmonary fibrosis
3) Hyperpigmentation

Busulfan

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Nitrogen Mustards

MOA:

Clinical uses:

Adverse effects:

MOA: Alkylating agents
Cross-links DNA via guanosine (N7) that is bioactivated by the liver & interferes with replication & transcription

Clinical uses:
1) Solid tumors (breast & ovary)
2) Leukemia
3) Non-Hodgkin lymphoma
4) Rheumatic disease (SLE & Wegners)

Adverse effects:
1) Hemorrhagic cystitis (avoid with MESNA)
2) Myelosuppression
3) Fanconi syndrome (Ifosfamide)

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Cyclophosphamide,
ifosfamide

MOA: Alkylating agents
Cross-links DNA via guanosine (N7) that is bioactivated by the liver & interferes with replication & transcription

Clinical uses:
1) Solid tumors (breast & ovary)
2) Leukemia
3) Non-Hodgkin lymphoma
4) Rheumatic disease (SLE & Wegners)

Adverse effects:
1) Hemorrhagic cystitis (avoid with MESNA)
2) Myelosuppression
3) Fanconi syndrome (Ifosfamide)

Nitrogen Mustards

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Nitrogen Mustards

MOA:

Clinical uses:

Adverse effects:

Cyclophosphamide & Ifosfamide

MOA:
Cross-links DNA via guanosine (N7) that is bioactivated by the liver & interferes with replication & transcription

Clinicals:
Solid tumors (breast & ovary)
Leukemia
Non-Hodgkin lymphoma
Rheumatic disease (SLE & Wegners)

Adverse effects:
1) Hemorrhagic cystitis (avoid with MESNA)
2) Myelosuppression
3) Fanconi syndrome (Ifosfamide)

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Cyclophosphamide & Ifosfamide MOA: Cross-links DNA via guanosine (N7) that is bioactivated by the liver & interferes with replication & transcription Clinicals: Solid tumors (breast & ovary) Leukemia Non-Hodgkin lymphoma Rheumatic disease (SLE & Wegners) Adverse effects: 1) Hemorrhagic cystitis (avoid with MESNA) 2) Myelosuppression 3) Fanconi syndrome (Ifosfamide)

Nitrogen Mustards

Procarbazine MOA: Clinical uses: Adverse effects:

MOA: Alkylating agent Weak MAO inhibitor Clinicals: Hodgkin lymphoma Brain tumors - Primary CNS lymphoma - Glioblastoma multiforme - Anaplastic oligodendroglioma Adverse effects: 1) Bone marrow suppression 2) Pulmonary toxicity (pneumocystis) 3) Leukemia 4) Disulfiram-like reaction

Procarbazine

Platinum-containing drugs MOA: Clinical uses: Adverse effects:

Cisplatin, Carboplatin, & Oxaliplatin MOA: Platinum ions cross-links DNA Clinical uses: 1) Solid tumors (Testicular, Bladder, Ovarian, Gi, & Lungs) 2) Lymphoma Adverse effects: 1) Nephrotoxicity (ATN & Fanconi syndrome avoid with Amifostine & Chloride diuresis) 2) Peripheral neuropathy 3) Ototoxicity (hearing loss)

Platinum-containing drugs

Taxanes MOA: Clinical uses: Adverse effects:

Paclitaxel & Docetaxel MOA: Microtubule inhibitors Inhibits microtubule formation & prevents mitotic spindle breakdown (hyper stabilize) in M phase Clinicals: Ovarian & Breast cancers Adverse effects: 1) Myelosuppression 2) Neuropathy 3) Hypersensitivity

Taxanes

Vinca alkaloids MOA: Clinical uses: Adverse effects:

Vincristine & Vinblastine MOA: Microtubule inhibitors Binds B-tubulin & inhibits it's polymerization to prevent mitotic spindle formation in M phase Clinical uses: Solid tumors Leukemia Hodgkin/Non-Hodgkin lymphoma Adverse effects: 1) Neurotoxicity (Vincristine) - peripheral neurotoxicity - areflexia - Paralytic ileus 2) Bone marrow suppression (Vinblastine)

Vinca alkaloids

Etoposide & Teniposide MOA: Clinical uses: Adverse effects:

MOA: Topoisomerase II inhibitors (DNA gyrase) in S & G2 phase, causing double strand breaks Clinicals: Testicular & SCLC Leukemia Lymphoma ALL cancer Adverse effects: 1) Myelosuppression 2) Alopecia 3) Gi upset

Etoposide & Teniposide

Irinotecan & Topotecan MOA: Clinical uses: Adverse effects:

MOA: Topoisomerase I inhibitor that causes single stranded breaks in G2 & S phases Clinical uses: Colon cancer (Irinotecan) Ovarian & SCLC (Topotecan) Adverse effects: 1) Severe myelosuppression 2) Diarrhea

Irinotecan & Topotecan

Tamoxifen & Raloxifene MOA: Clinical uses: Adverse effects:

MOA: SERM Antagonists in breast tissue & partial agonist in endometrial & bone tissue Clinical uses: ER/PR +ve breast cancers Adverse effects: 1) Higher risk of endometrial cancer (Tamoxifen) 2) Higher risk of thromboembolic events (DVT & PE) 3) Hot flashes

Tamoxifen & Raloxifene

Alemtuzumab MOA: Clinical uses: Adverse effects:

MOA: Anticancer monoclonal antibodies against CD52 Clinical uses: 1) Chronic lymphocytic leukemia (CLL) 2) Multiple sclerosis Adverse effects: 1) Higher risk of infections & autoimmunity (ITP)

Alemtuzumab

Bevacizumab MOA: Clinical uses: Adverse effects:

MOA: Anticancer monoclonal antibodies against VEGF to inhibit blood vessel formation Clinical uses: 1) Solid tumors (Colorectal cancer, Renal cell carcinoma & Non-small cell carcinoma 2) Angio-proliferative retinopathy (wet-age related macular degeneration) Adverse effects: 1) Hemorrhaging 2) Blood clots 3) Impaired wound healing

Bevacizumab

Cetuximab & Panitumumab MOA: Clinical uses: Adverse effects:

MOA: Anticancer monoclonal antibodies targeted against EGFR Clinical uses: Metastatic (stage IV) Colorectal cancer Head & Neck cancers Adverse effects: 1) Elevated LFT's 2) Rash 3) Diarrhea

Cetuximab & Panitumumab

Rituximab MOA: Clinical uses: Adverse effects:

MOA: Anticancer monoclonal antibodies against CD20 on the surface of B cells Clinical uses: 1) Non-Hodgkin lymphoma 2) CLL 3) Immune Thrombocytopenic Purpura 4) Rheumatoid arthritis Adverse effects: 1) increased risk of subsequent progressive multifocal leukoencephalopathy caused by JC virus reactivation

Rituximab

Trastuzumab MOA: Clinical uses: Adverse effects:

MOA: Anticancer monoclonal antibodies against HER2/neu tyrosine kinase receptor Clinicals: 1) HER2/neu +ve Breast cancer 2) Gastric cancer Adverse effects: Dilated cardiomyopathy

Trastuzumab

Alectinib MOA: Clinical uses: Adverse effects:

MOA: Targets ALK genes Clinical uses: Non-Small cell carcinoma Adverse effects: 1) Edema 2) Rash 3) Diarrhea

Alectinib

Erlotinib, Gefitinib, & Afatinib MOA: Clinical uses: Adverse effects:

MOA: Targets EGFR tyrosine kinase inhibitor Clinical uses: Non-small cell carcinoma Adverse effects: Rash (face/back)

Erlotinib, Gefitinib, & Afatinib

Imatinib, Dasatinib, & Nilotinib MOA: Clinical uses: Adverse effects:

MOA: Targets BCR-ABL (cKIT) Clinical uses: CML, ALL, GIST Adverse effects: 1) Myelosuppression 2) Elevated LFT's 3) Edema 4) Myalgias

Imatinib, Dasatinib, & Nilotinib

Ruxolitinib MOA Clinical uses: Adverse effects:

MOA: Targets jak 1/2 Clinical uses: Polycythemia vera Adverse effects: 1) Bruises 2) LFT's

Ruxolitinib

Bortezomib, Carfizomib, & Ixazomib MOA Clinical uses: Adverse effects:

MOA: Targets proteasomes to induce cell cycle arrest at G2 & M phase to cause apoptosis Clinicals: Multiple myeloma Mantle cell lympoma Adverse effects: 1) Rash/fatigue/diarrhea

Bortezomib, Carfizomib, & Ixazomib

Vemurafenib, Dabrafenib, & Encorafenib MOA Clinical uses: Adverse effects:

MOA: BRAK Kinase mutase inhibitor used for BRAF mutations like V600E Clinical uses: Metastatic melanoma Adverse effects: 1) Peripheral neuropathy (HSV reactivation)

Vemurafenib, Dabrafenib, & Encorafenib