Biweekly 2 Flashcards
Bevacizumab
VEGF inhibitor
Anti-angiogenesis
MOA: IgG that binds against VEGF
Side Effects: Hypertension, impaired wound healing, bowel perforation, proteinuria, pulmonary hemorrhage, CHF, deep venous and arterial thrombosis, pulmonary embolism, other thrombo-embolic events, reversible posterior leukoencephalopathy syndrome (RLS) .
Bleomycin
Antibiotic
Natural Product
MOA: Mixture of fungal glycopeptides. Strandcision. It binds to DNA and binds to iron atom, and oxidizes it, and these nip up DNA.
Inhibits S/G2 phase of cell cycle.
Side Effects: Main one is pulmonary, there is dose dependent toxicity and idiosyncratic.
Carboplatin
Alkylating Agent
Platinum Coordination
MOA: Gets hydroxylated to get activated, and they are alkylating, and they cause kinks, breaks, etc in DNA
Side Effects: Less nephrotoxicity, N/V, neuropathy than cisplatin. More myelosupression than cisplatin.
Carmustine
Alkylating Agent
Nitrosurea
It is hydrophobic and is injected with alcohol, resulting in burning at site of injection.
SIDE EFFECT: There is myelosupression on days 21-28
Administer every 6-8 weeks
Available in wafers for direct brain implantation
Cetuximab
EGFR inhibitor
Monoclonal Antibody
MOA: IgG against extracellular domain of EGFR
Side Effects: Severe anaphylaxis, skin rash, acne, folliculitis, diarrhea, abdominal pain, lung inflammation, hypomagnesemia.
Cisplatin
Alkylating Agent
Platinum Coordination
ERCC1 increase leads to cisplatin resistance in lung cancer
MOA: Gets hydroxylated to get activated, and they are alkylating, and they cause kinks, breaks, etc in DNA
Side Effects: More nephrotoxicity, N/V, neuropathy than carboplatin. Less myelosupression than carboplatin.
Cyclophosphamide
Alkylating Agent( microsomal P450 activates it)
Nitrogen Mustard
Acrolein, a byproduct, can cause severe hemorrhagic cystitis. MESNA is used as a cryoprotectant
Toxicity: Bone marrow supression days 8-14, cystitis, cardiac toxicity(high doses), immunosupression
Cytarabine (AraC)
Antimetabolite
Pyrimidine Antagonist
MOA: Mimic of cytosine. Inhibits at S phase of Cell cycle.
Side effects: Myelosupression, fevers, arthralgias, irreversible cerebellar toxicity, and ocular toxicity
Docetaxel
Microtubule inhibitor
Antimitotic Agent
MOA: Stabilizes microtubules, leading to apoptosis( same as paclitaxel). Can be used in cancers resisitant to paclitaxel. Inhibits at M phase of Cell cycle
Side Effects: hypersensitivity, myelosupression, edema)
Doxorubicin
Anthracycline
Antibiotic
MOA: Intercalating agent between DNA base pairs and results in free oxygen radicals.
Side Effects: Cardiotoxic( maximal lifetime dose of 550mg/m2), as well as the other normal myelosupressive, N/v etc.
Erlotinib
EGFR inhibitor Targeted Molecule T790M mutation in EGFR leads to increase resistance to erlotinib MOA: Tyrosine kinase inhibitor Side Effects: Acneiform Rash
Fludarabine
Antimetabolite
Purine Antagonist
MOA: Inhibits at S Phase of Cell cycle
5-Fluorouracil
Antimetabolite
Pyrimidine Antagonist
Used in combination with leucovorin to increase its activity
MOA: Inhibits both DNA and RNA synthesis. It inhibits thymidylate synthase, and the leucovorin stabilizes the enzyme so it has a greater effect, but also a greater toxicity.
Inhibits at S phase of Cell Cycle
Side Effects: Mucositis, myelosupression, hand-foot syndrome
Imatinib
TKI
Targeted Molecule
GLEEVAC USED FOR CML
MOA: Inhibits BCR-ABL tyrosine kinase by binding to ATPase site and inhibiting ATP cleavage and transphosphorylation
Irinotecan
Topoisomerase I Inhibitor
Natural Product
MOA: Topoisomerase I inhibitor. Inhibits at S Phase of cell cycle
Side effects: Myelosupression, transaminitis, fever, and the big one is diarrhea; acute and delayed.
Methotrexate
Antimetabolite
Folic Acid Antagonist
DHFR increase leads to methotrexate resistance
MOA: Inhibits DHFR, leading to an inability to synthesize DNA. Inhibits at S phase of Cell Cycle
High Dose Methotrexase requires leucovorin rescue
Side Effects: Myelosupression, N/V, mucositis, hepatotoxicity, neurotoxicity, nephrotoxicity.
Paclitaxel
Microtubule Inhibitor
Semi-natural Product( dissolved in Cremaphor AL, which can lead to anaphylaxis)
MOA: Stabilize microtubules in cell so that the cells cannot dissemble and divide, and they undergo apoptosis. Inhibits at M phse of cell cycle
Side Effects: Hypersensitivity, cardiotoxic, myelosupressive, N/V, alopecia.
Rituximab
Immunological Agent
Monoclonal Antibody
MOA: IgG against CD20 on B cells
Side Effects:
Cytokine-release syndrome/tumor lysis syndrome
Prolonged and severe lymphopenia, immunosuppression, opportunistic infections, reactivation of viral hepatitis.
Severe mucocutaneous reactions (Rituxan®)
Pancytopenia/bone marrow failure (CAMPATH®)
Thalidomide
Antiangiogenic Agent
Small Molecule
Side Effects: teratogenic, neurotoxic
Trastuzumab
Immunological Agent
Monoclonal Antibody
MOA: IgG that targets HER-2/neu, a member of the EGFR family
Side Effects: Congestive heart failure (CHF)/dysfunction, diarrhea
Vinblastine
Microtubule Inhibitor
Natural Product
MOA: Probably similar to vincristine, mitotic spindle poison, leading to fragmentation of microtubules. Inhibits M phase of cell cycle.
Vincristine
Microtubule Inhibitor
Natural Product
MOA: Mitotic Spindle Poison, leading to fragmentation of microtubules.
Inhibits M phase of cell cycle
Side Effect: Neuropathy, including constipation
mechlorethamine
Alkylating Agent
Nitrogen Mustard
Leucovorin
Used for methotrexate rescue therapy and in combination with 5-FU for modulation
Alkylating agents MOA
Inactive until metabolized by the P450 system, leads to cross linking of DNA and eventually apoptosis of cell
