Miscellaneous Agents Flashcards by Justin Faulkner

Name the 7 tyrosine kinase inhibitors…

Imatinib
Gefitinib
Erlotinib
Afatinib
Nilotinib
Dasatinib
Lapatinib

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Which tyrosine kinase inhibitor inhibits Abl kinase by binding where ATP should and also inhibits PDGFR and c-kit

Imatinib

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What are the three things inhibited by Imatinib?

Abl kinase
PDGFAR
c-kit

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What tyrosine kinase inhibitor is considered the first line of therapy for CML?

Imatinib

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What three tyrosine kinase inhibitors inhibit epidermal growth factor receptor (EGFR) tyrosine kinase?

Gefitinib
Erlotinib
Afatinib

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Which tyrosine kinase inhibitor inhibits Abl kinase?

Nilotinib

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Which tyrosine kinase inhibitor inhibits both Abl kinase and Src kinase?

Dasatinib

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Which tyrosine kinase inhibitor inhibits both EGFR (epidermal growth factor receptor) and ErbB2 (HER2) tyrosine kinase?

Lapatinib

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What three tyrosine kinase inhibitors are used to treat non-small lung cancer?

Gefitinib
Erlotinib
Afarinib

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Erlotinib is used to treat non-small lung cancer and _______.

Pancreatic cancer

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If a patient is found to have imatinib-resistant CML what are the other two tyrosine kinase inhibitors that are used?

Nilotinib

Dasatinib

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Lapatinib, a tyrosine kinase inhibitor, is used for the treatment of what?

Advanced or metastatic breast cancer over expressing HER2 and hormone + metastatic breast cancer over expressing HER2 receptor in postmenopausal women

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What are the side effects of Imatinib?

N/V
Fluid retention
Muscle cramps
Arthralgia
Myelosuppression

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What are the side effects of Gefitinib?

Interstitial lung disease
Liver damage
GI perforation
Severe diarrhea
Ocular disorders
Skin reactions--rash, acne, pruritis, dry skin

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What are the side effects of Erlotinib?

Rash
Diarrhea
Appetite loss
N/V
stomach pain
Fatigue
SOB
mouth sores
Dry skin
itching
cough
Liver/renal failure
interstitial lung dz
increased bleeding or clot formation
GI perforation
Corneal ulceration/perforation

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What are the side effects of Afatinib?

Diarrhea
Vomiting
rash/dermatitis
Acneiform
Stomatitis
Paronichia
Dry skin
Pruritis
Decreased appetite
Dyspnea
Fatigue
Pulmonary toxicity
Pneumonia
Sepsis

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What are the side effects of Nilotinib?

Myelosuppression
QT prolongation
Hepatotoxicity
Electrolyte abnormalities

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What are the side effects of Dasatinib?

Myelocuppression
Bleeding
Fluid retention
Pulmonary arterial HTN
Diarrhea 
N/V
Weakness
infections

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What are the side effects of Lapatinib?

Hepatotoxicity
Nausea
Diarrhea
Fatigue
Rashes
QT-prolongation
Decreased LV function when combined with capecitabine
Hypokalemia
Hypomagnesemia

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All the tyrosine kinase inhibitors are PO QD except ______, which is PO BID.

Nilotinib

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Name the three monoclonal antibody drugs…

Rituximab
Trastuzumab
Cetuximab

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Name the antibody-drug conjugate…

Ado-trastuzumab emtansine

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Name the human monoclonal antibody drugs…

Ipilimumab

Nivolumab

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Name the fully human monoclonal antibody…

Panitumumab

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What monoclonal antibody is a CD20 B-cell antibody that can directly activate apoptosis, activate complement, or activate cell-mediated cytotoxicity?

Rituximab

Which monoclonal antibody works through a HER2/neu receptor antibody mechanism?

Trastuzumab

What mechanism does Ado-trastuzumab emtansine an antibody-drug conjugate work through?

Conjugate undergoes receptor-dependent internalization and drug released inside cell

What two monoclonal antibodies work through epidermal growth factor receptor--EGFR (ErbB1)?

Cetuximab | Panitumumab

what mechanism of action does ipilimumab, a human monoclonal antibody, use?

Cytotoxic T-Lymphocyte antigen 4 inhibitor--stimulates immune system

Which monoclonal antibody inhibits programmed cell death protein 1 (PD-1)?

Nivolumab

Which monoclonal antibody is used in the treatment of non-hodgkin's lymphoma?

Rituximab

Which monoclonal antibody is used in the treatment of HER/neu-overexpressing metastatic breast cancer?

Trastuzumab

Ado-Trastuzumab emtansine is an antibody-drug conjugate used in the treatment of what?

ErbB2 (HER2) + metastatic breast cancer patients with prior treatment hx of trestuzumab and/or taxane

EGFR-+ metastatic colorectal cancer is treated with ______ in combination with irinotecan, 5-FU, and Leu ovarian.

Cetuximab

What monoclonal antibody is used for the treatment of squamous cell carcinoma of the head and neck combined with radiation therapy?

Cetuximab

EGFR-expressing metastatic colorectal cancers that are resistant to fluoropyrimidine, oxaliplatin, and irinotecan regimens is treated with what?

Panitumumab

Which monoclonal antibody is used in the treatment of melanoma?

Ipilimumab

After a patient with melanoma have been unsuccessfully treated with ipilimumab, the next monoclonal antibody used is?

Nivolumab

Melanoma patient with the BRAF V600 mutation previously treated with ipilimumab is treated with?

Nivolumab

Metastatic squamous NSCLC that has progressed after platinum-based chemo is treated with?

Nivolumab

What are the side effects of Rituximab?

``` Infusion reactions tumor lysis syndrome (TLS) Severe mucocutaneous reactions progressive multifocal leukoencephalopathy (PML) Skin reactions Irregular heartbeat Muscle or joint pain ```

What are the side effects of Trastuzumab?

Hypersensitivity reaction | LV dysfunction

What are the side effects of Ado-trastuzumab emtansine?

``` Fatigue Nausea MSK pain Thrombocytopenia Headache Hypokalemia Peripheral neuropathy Ventricular dysfunction Interstitial lung disease Intersitial lung dz Infusion associated reactions Hepatotoxicity Birth defects ```

What are the side effects of Cetuximab?

``` Allergic reactions sudden cardiac death dermatologic problems infections renal failure electrolyte abnormalities Asthenia/malaise Fever Nausea Constipation interstitial pneumonitis ```

What are the side effects of Panitumumab?

``` Skin toxicities paronychia hypomagnesemia fatigue abdominal pain nausea diarrhea constipation ```

What are the side effects of Nivolumab?

``` Rash Itching Cough Upper respiratory tract infections Edema fatigue SOB MSK pain Decreased appetite Nausea Constipation Severe immune-mediated side effects on healthy organs ```

Which monoclonal antibody is usually combined with taxanes and enhances doxorubicin cardiotoxicity?

Trastuzumab

Name the two serine/threonine kinase inhibitors...

Vemurafenib | Dabrafenib

Name the dual specificity kinase...

Trametinib

What two drugs are used to inhibit oncogenic BRAF kinase?

Vemurafenib | Dabrafenib

Tramentinib inhibits____.

MEK

What three drugs are used to treat unresectable Stage III and IV or metastatic melanomas with BRAF mutations?

Vemurafenib Dabrafenib Trametinib

What are the side effects of Vemurafenib, a serine/threonine kinase inhibitor?

``` Arthralgia Fatigue Photosensitivity Nausea Alopecia Diarrhea QT prolongation Cutaneous squamous cell carcinoma Keratoacanthoma new primary cutaneous melanoma ```

What are the side effects of Dabrafenib, a serine/threonine kinase inhibitor?

Serious febrile drug reactions Uveitis and iritis hyperglycemia hyperkeratosis Higher risk of developing: Cutaneous squamous cell carcinoma Keratoacanthoma new primary cutaneous melanoma

What are the side effects of Trametinib, a dual specificity kinase?

``` Cardiomyopathy Retinal disorders Interstitial lung dz Serious skin toxicities Rash Diarrhea Stomatitis HTN Pruritis ```

What serine/threonine kinase inhibitor is superior to dacarbazine in Phase III trials?

Vemurafenib

Dabrafenib may cause what to occur in males?

Infertility

Trametinib may cause what to occur in females?

Infertility

What mechanism of action is used by hydroxyurea?

Inhibits ribonucleoside diphosphate reductase

Hydroxyurea is used in the treatment of what?

CML--replaced by Imatinib Polucythemia vera Essential thrombocythemia Treatment of sickle cell dz (increases Hb-F)

What is the mechanism of Retinoids?

ATRA induces terminal differentiation in malignant immature promyelocytes, which subsequently apoptose

Retinoids are used for the treatment of what?

APL

What are the side effects of Retinoids used for the treatment of APL?

``` Leukocyte activation syndrome (LAS) increase in WBCs -Fever -Weight gain -respiratory distress -serosal effusion -renal failure ```

What are retinoids combined with to block the side effect of leukocyte activation syndrome (LAS)?

anthracyclines--corticosteroid

Arsenic trioxide is used to treat what?

Relapsed APL

Thalidomide is used to treat what?

Multiple myeloma and myelodysplastic syndromes

Interferons are used to treat what?

Hairy cell leukemia CML AIDS related to Kapok's sarcoma

What does ABVD (combination therapy) stand for?

Doxorubicin Bleomycin Vinblastine Dacarbazine

What does CHOP (combination therapy) stand for?

Cyclophosphamide Hydroxydoxubicin Vincristine Prednisone

What does MOPP (combination therapy) stand for?

Mechlorethamine Vincristine Procarbazine Prednisone

What does CMF (combination therapy) stand for?

Cyclophosphamide Methotrexate 5-fluorouracil

What does FEC (combination therapy) stand for?

5-Fluorouracil Epirubicin cyclophosphamide