Miscellaneous Chemotherapy drugs Flashcards
Hydroxyurea
Class: N/A
Mechanism of Action: Inhibits the enzyme ribonucleotide diphosphate reductase which catalyzes the conversion of ribonucleotides to deoxyribonucleotides which is a rate limiting step in biosynthesis of DNA.
Therapeutic Uses: Myeloproliferative neoplasm (CML)
Polycythemia vera
Essential thrombocythemia
Sickle Cell Anemia
Retinoids
Class: N/A
Mechanism of Action: Induces differentiation in leukemic promyelocytes and produces remission in patients with APL
Therapeutic Uses: APL (type of AML)
Toxicity: Leukocyte Activation System (Fever, weight gain, respiratory distress, serosal effusion (pleural, pericardial), renal failure)
Other: Combined with Anthracyclins (to prevent relapse)
Used with corticosteroids to control the amount of WBCs (LAS)
Imatinib
Class: Tyrosine kinase inhibitor
Mechanism of Action: Inhibits abl by binding to ATP binding site and inhibiting fusion protein phosphorylation in CML. Also will bind and inhibit KIT and PDGFRA in GIST. Metabolized by cytochrome 450 in liver.
Therapeutic uses: CML, GIST
Toxicity: Nause, vomiting, myelosuppression, fluid retention, arthralgia, muscle cramps
Other: Dose once a day
Nilotinib
Class: Tyrosine kinase inhibitor
Mechanism of action: Inhibits abl protein in CML.
Therapeutic uses: Imatinib-resistant CML
Toxicity: QT prolongation, hepatotoxicity, electrolyte abnormalities.
Other: Dose 2/day
Dasatinib
Class: Tyrosine kinase inhibitor
Mechanism of action: Inhibits abl and src
Therapeutic uses: Imatinib resistant CML
Toxicity: Myelosuppression, fluid retention, bleeding, pulmonary artery hypertension, diarrhea, nausea, vomiting, infections
Other: Dose 1/day
Trastuzumab
Class: monoclonal antibody
Mechanism: Unknown mechanism of action but somehow inhibits HER2 (EGFR2) activity. May be downregulation (internalization of receptor), disruption of transduction pathway (prevention of dimerization), ADCC, etc
Therapeutic uses: HER2+ metastatic breast cancer
Toxicity: Hypersensitivity reaction, ventricular dysfunction
Other: Often combined with taxanes for best effect (Trastuzumab just inhibits proliferation and survival, taxanes actually cause cell death)
Can compound cardiotoxic effect of doxorubicin
Ceftuximab
Class: monoclonal antibody
Mechanism: competitively inhibits EGFR1 against EGF and or TGF
Therapeutic uses: colorectal cancer (combined with irinotecan), head and neck cancer (combined with radiation therapy)
Toxicities: Allergic reaction, cardiotoxicity, dermatologic toxicity, renal toxicity, electrolyte imbalances, interstitial pneumonia, pulmonary embolism
Other: Clinical trials with Cisplatin
Rituximab
Class: monoclonal antibody
Mechanism of action: Binds CD-20 protein on surface of B-cells and either induces apoptosis through intrinsic pathway, induces complement (lysis complex), or cell-mediated death.
Therapeutic uses: relapsed or recurrent follicular cell lymphomas (type of Non-Hodgkin’s)
Toxicity: Tumor lysis syndrome, severe mucocutaneous reactions, multifocal leukoencephalopathy
Other: patients need careful monitoring
Vemurafenib
Class: serine-threonine kinase inhibitor
Mechanism of action: Binds BRAF and inhibits oncogenic pathway that is constituatively active
Therapeutic uses: unresectable stage III or IV metastatic melanoma
Toxicity: QT prolongation, cutaneous squamous cell carcinoma, new primary melanoma, arthralgia, fatigue, photosensitivty alopecia, nausea, and diarrhea
Other: superior to decarbazine in Phase III trial
Dabrafenib
Class: serine-threonine kinase inhibitor
Mechanism of action: Binds BRAF and inhibits oncogenic pathway that is constitutively active.
Therapeutic uses: Unresectable stage III or IV metastatic melanoma.
Toxicity: Serious Febrile Drug Reactions (hypotension, rigors, chills, dehydration, kidney failure)
Increased risk of squamous cell carcinoma, melanoma
Uveitis, iritis, hyperglycemia
Other: May cause male infertility.
Trametinib
Class: N/A
Mechanism of action: Binds MEK and inhibits
Therapeutic uses: Unresectable stage III or IV metastatic melanoma.
Toxicity: Serious skin toxicity (rash, dermatitis, acneiform rash, palmar-plantar erythrodysesthesia syndrome, and erythema) Cardiomyopathy Retinal Pigment Epithelial Detachment Retinal vein occlusion Interstitial lung disease
Other: May cause female infertility.
Arsenic Trioxide
Therapeutic use: Relapsed APL
Gefitinib
Class: Tyrosine Kinase inhibitor
Mechanism of action: Inhibit epidermal growth factor receptor tyrosine kinase.
Therapeutic uses: Small cell lung cancer.
Toxicities: N/A
Erlotinib
Class: Tyrosine Kinase inhibitor
Mechanism of action: Inhibit epidermal growth factor receptor tyrosine kinase.
Therapeutic uses: Small cell lung cancer.
Toxicities: N/A
Ipilimumab
Class: Monoclonal antibody
Mechanism of action: Cytotoxic T cell antigen 4 inhibitor, stimulates the immune system.
Therapeutic uses: Melanoma.
