Miscellaneous Agents Flashcards by Sam Lucrezia

What class of drug is Imatinib (Gleevac)?

Tyrosine Kinase Inhibitor

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What is the mechanism of action of Imatinib?

It inhibits Abl kinase by binding where ATP should go

It also inhibits PDGFR and c-kit

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How is Imatinib metabolized?

Cytochrome P450

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What is Imatinib used to treat?

CML (first line therapy)

Gastrointestinal tumor

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What are the major side effects of Imatinib?

Nausea and vomiting

Fluid Retention

Muscle Cramps

Arthraligia

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What are the minor side effects Imatinib?

Myelosuppression

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How is imatinib administered?

Orally`

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What class of drug is Gefitinib (Iressa)?

Tyrosine kinase inhibitor

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What is the mechanism of action of Gefitinib?

Inhibits the epidermal growth factor recepto tyrosine kinase

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What is gefitinib used to treat?

Non- small lung cancer

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What calass of drug is Erlotinib (Tarceva)?

Tyrosine kinase inhibitor

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What is the mechanism of action of Erlotinib?

Inhibits epidermal growth factor receptor tyrosine kinase

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What is erlotinib used to treat?

Non-small lung cancer

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What class of drug is Nilotinib (Tasigna)?

Tyrosine kinase inhibitor

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What is the mechanism of action of nilotinib?

Inhibits Abl kinase

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What is nilotinib used to treat?

Imatinib-resistant CML

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What are the major and minor side effects of nilotinib?

Major: Myelosupression

Minor: QT prolongation, hepatotoxicity, electrolyte abnormalitis

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What class of drug is dasatinib (Sprycel)?

Tyrosine kinase inhibitor

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What is the mechanism of action of dasatinib?

Inhibits Abl and Src kinases

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What is dasatinib used to treat?

Imatinib-resistant CML

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Major and minor side effects of dasatinib?

Major: Myelosupresion, bleeding, fluid retention, pulmonary arterial hypertension

Minor: Diarrhea, nausea and vomiting, weakness and infections

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How are dasatinib and nilotinib administered?

Orally

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What class of drug is rituximab?

Monoclonal antibody

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What is the mechanism of action of rituximab?

CD20 B-cell antibody that can directly activate apoptosis, compliment or cell mediated cytotoxicity

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What is rituximab used to treat?

Non-hodgkin's lymphoma

Major side effects of rituximab?

Infusion reactions, tumor lysis syndrome, severe mucocutaneous reactions, PML

What are the minor side effects of rituximab?

Skin reactions, irregular heartbeat, muscle or joint pain

What class of drug is trastuzumab?

Monoclonal antibody

What is the mechanism of action of trasuzumab?

mechanism is not completely known. But it is known that it interacts somehow with the HER2/neu receptor. Theories include: enhanced receptor endocytosis or blocking homo- or heterodimerization

What is trastuzumab used to treat?

HER2/ neu overexpressing metastatic breast cancer

Side effects of trastuzumab?

Hypersensitivity reaction; ventricular dysfunction

What is trastuzumab usually administered with?

Usually combined with taxanes ( )

What happens when trastuzumab is given with doxorubicin?

It enhances the cardiotoxicity of doxorubicin

What type of agent is cetuximab (Erbiux)?

Monoclonal Antobody

What is the mechanism of action of cetuximab?

Binds the EGFR1 (Erb1) receptor

What is cetuximab used to treat?

EGFR- positive metastatic colorectal cancer

What are the major ride effects associated with cetuximab?

Allergic reaction, sudden cardiac death, dermatologic problems, infections, renal failure, electrolyte abnormalities

What are the minor side effects of cetuximab?

Asthenia/ malaise, fever, nausea, constipation, interstitial pneumonitis

Is cetuxmab used as a single agent or in combination?

There are current clinical trials to see efficacy as a combination therapy regimen...it will probably be used with cisplatin

What type of agent is vemurafenib (zelboraf)?

Serine/ theonine kinase inhibitor

What is the mechanism of action of vemurafenib?

It inhibits the oncogenic BRAF kinase

What is vemurafenib used to treat?

Unresectable stage III or IV or Metastatic melanomas with BRAF mutations

Major side effects of vemurafenib?

Arthralgia, fatigue, photosensitivity, nausea, alopecia, diarrhea, QT prolongation

What are the minor side effects of vemurafenib?

cutaneous squamous cell carcinoma, keratoacanthoma, new primary cutaneous melanoma

T/F: Clinical trails show that dacarbazine is better in treating unresectable stage III or IV or metastatic melanoma than vemurafenib?

False....vemurafenib has been shown to be the superior drug

What type of drug is Ipilimumab ( Yervoy)?

Human monoclinal antibody

What is the mechanism of action of Ipilimumab?

Cytotoxic T- lymphocyte antigen 4 inhibitor It has the ability to stimulate the immune system

What is Ipilimumab used to treat?

Melanoma

What type of drug us dabrafenib (Tafinlar)? What is its mechanism of action?

Class: Serine/ Tyrosine kinase inhibitor Mechanism: Inhibits oncogenic BRAF kinase

What is dabrafenib used to treat?

Unresectable stage III or IV or metastatic melanomas with BRAF mutations

What are the major side effects of dabrafenib?

Serious febrile drug reactions, uveitis and iritis, hyperglycemia, hyperkeratsis

What are the less common side effects of dabrafenib?

Cutaneous squamous cell carcinoma, keratocanthoma, new primary cutaneous melanoma ** Has a greater risk of developing these side effects than Vemurafenib does.

What is the mechanism of action of Trametinib (Mekinist)?

Inhibits MEK

What is Trametinib used to treat?

unresectable stage II or IV or metastati melanomas w/ BRAF mutations

Major side effects of Trametinib?

Cardiomyopathy, retinal disorders, interstitial lung disease, serious skin toxicities

Minor side effects of Trametinib?

Rash, diarrhea, stomatitis, hypertension, pruritis

Which of the following can cause male infertility: Trametinib Dabrafenib Vemurafenib

Trametinib | Dabrafenib

What is the mechanism of action of hydroxyurea?

inhibits ribonucleoside diphosphate reductase

What is hydroxyurea used to treat?

CML (but was replaced by imatinib) Polycythemia vera Essential thrombocythemia Sickle cell disease (increases fetal Hb)

What is the mechanism of action of retinoids?

all trans- retinoic acid induces terminal differentiation in malignant immature promyelocytes...which then apoptose

What are retinoids used to treat?

APL

What are the major side effects of retinoids?

"Leukocyte activation syndrome": increase in WBCs, fever, weight gain, respirator distress, serosal effusion, renal failure

What is the combination therapy that retinoids is used in and why?

Combined with anthracyclines, and also corticosteroids to block the leukocyte activation syndrome (LAS)

What is arsenic trioxide (trisenox) used to treat?

relapsed APL

What is Thalidomide used to treat?

Multiple myeloma and myelodysplastic syndromes

What are interferons used to treat?

Hairy-cell leukemia, CML and AIDS related Kaposi Sarcoma