Drugs Profiles

Cyclophosphamide:
* class & MOA
* indications
* side effects
* Nitrogen mustard crosslinks DNA
* Widely used
* Hemorrhagic cystitis! with high high doses, CYP450 makes acrolein which binds bladder -->
hematuria --> prevent with H20 & MESNA, which binds acrolein
* Delayed N/V
* SIADH

Ifosfamide:
* class & MOA
* indications
* side effects
* Nitrogen mustard crosslinks DNA
* Solid tumors, especially sarcoma
* Hemorrhagic cystitis --> greater risk, therefore giveMESNA for prevention (at ALL doses)
* Neurotoxicity

Cisplatin:
* class & MOA
* indications
* side effects
* platinum alklylating agent crosslinks DNA
* Solid tumors
* Nephrotoxicity!! particularly dangerous b/c it's renally cleared AND nephrotoxic
* Ototoxic!!
* hypersensitivity
* A/D- N-V

Carboplatin:
* class & MOA
* indications
* side effects
* platinum alkylating agent crosslinks DNA
* Solid tumors

* Hypersensitivity
* Myelosuppression --> decreased PLTs

Oxaliplatin:
* class & MOA
* indications
* side effects
* platinum alkylating agent crosslinks DNA
* Solid tumors
* Cold-Neuropathy
* Hypersensitivity

Busulfan:
* class & MOA
* indications
* side effects
* Alkylating agent that crosslinks DNA
* Bone Marrow Transplant ablation; CML
* Seizures**, pulmonary fibrosis, hyperpigmentation

Ironotecan:
* class & MOA
* indications
* side effects
* camptothecin, inhibit topo I
* Solid tumor
* Severe diarrhea (treat acutely w/ atropine, chronically w/ loperamide)

Topotecan:
* class & MOA
* indications
* side effects
* Camptothecin inhibits Topo I
* Solid tumor
* Myelosuppression (WCC, PLT)

Mitaxantrone:
* class & MOA
* indications
* side effects
* Topo II inhibitor
* Leukemia
* does NOT form free radicals, therefore lower risk of cardiotoxicity, extravasation, N/V
* turns urine blue/green

Etoposide:
* class & MOA
* indications
* side effects
* Epipodophyllotoxin, topo II inhibitor
* Wide usage: solid tumors, leukemias, lymphomas
* Myelosuppression
* Mucositis
* Hypotension (caused by diluent, not drug)

Methotrexate:
* class & MOA
* indications
* side effects
* Folate antagonist: inhibits DHFR, decreasing THF, purines, DNA and protein synthesis
* Widely used
* Myelosuppression
* Nephrotoxicity
* GI toxicity, Dermatitis
* High dose is lethal: need to check for third spacing --> also, give leucovorin 24 hrs after MTX
dose (goes directly to THF), can also use glucarpidase as final rescue (cleaves MTX)

Pemetrexed:
* class & MOA
* indications
* side effects
* Multitarget antifolate
* Lung cancer
* Cutaneous reaction --> give folate/B12 supplement to reduce side effects

Pralatrexate:
* class & MOA
* indications
* side effects
* folate analog that doesn't compete with folate --> hence can give Folate/B12
* T-Cell lymphoma
* Mucositis
* Myelosuppression (WCC, PLT)
* Folate/B12 supplement required!!

Fluorouracil:
* class & MOA
* indications
* side effects
* Pyrimidine analog: activated to F-dUMP whichinhibits thymidylate synthase, decreasing T/U,
decreasing DNA and protein synthesis -->
**LEUCOVORIN** given to increase efficacy, by locking FdUMP into TS
* Solid tumors
* Continuous Infusion: bloody diarrhea, mucositis, hand/foot syndrome
* Bolus infusion: myelosuppression

Capecitabine:
* class & MOA
* indications
* side effects
* Folate analogue: oral prodrug of FU, activated in tumor cells (then inhibits TS)
* Solid Tumors: colorectal, breast
* Same toxicities as continuous infusion of FU:bloody diarrhea, mucositis, hand/foot syndrome

Cytarabine:
* class & MOA
* indications
* side effects
* Pyrimidine analog: phosphorylated to active form in cancer, has large group on it, helping
to inhibit DNA-Pol
* Leukemia: AML/ALL (NOT SOLID**)
* Low dose (induction): myelosuppresion
* High dose (consolidation): CNS toxicity (monitor signature), and Conjunctivitis (give
dexamethasone eye drops)

Gemcitabine:
* class & MOA
* indications
* side effects
* Pyrimidine analog, functioning like cytarabine (Inhibit DNA-Pol), but intracellular conc. 20x greater
* Solid tumors
* Myelosuppression
* NOT neurotoxic (different from cytarabine)

Vincristine:
* class & MOA
* indications
* side effects
* Vinca alkaloid: "spaghetti microtubule"
* Childhood leukemia, solid tumors
* CNS toxicity & peripheral neuropathy
* MARROW SPARING

Vinblastine:
* class & MOA
* indications
* side effects
* Vinca alkaloid: "spaghetti microtubules"
* Breast cancer, HL, testicular
* Bone marrow suppression

Vinorelbine:
* class & MOA
* indications
* side effects
* Vinca alkaloid: "spaghetti microtubules"
* Breast cancer, NSCLC, lymphoma, ovarian
* Bone marrow suppression
Eculixumab:
* MOA
* indication
* MAB targeting C5
* PNH**

Hydroxyurea:
* MOA
* indications
* side effects
* Inhibits Ribonucleotide Reductase, decreasing DNA synthesis (S-phase)
* CML blast crisis, Sickle Cell
* Myelosuppression

Omacetaxine Mepasuccinate:
* MOA
* indications
* side effects
* decrease BCR-ABL protein synthesis
* CML
* Myelosuppression
* Hemorrhage
* Hyperglycemia

Vismodegib:
* MOA
* indications
* side effects
* inhibit hedgehog signaling via binding PTCH1, which decreases SMOH signals, and decreases
transcription
* BCC

Asparaginase:
*MOA
* indications
* side effects
* Degrades serum asparagine, which cancer cells use as fuel
* Leukemia / Lymphoma
* Pancreatitis (monitor amylase)
* decreased fibrinogen

Bleomycin:
* class & MOA

* indications
* side effects
* Antibiotic: induces free radicals causing DNA breaks
* Testicular cancer, HL
* Pulmonary fibrosis**

Dactinomycin:
* class & MOA
* indications
* side effects
* Antibiotics, intercalates in DNA
* Childhood tumors ("children act out"): Wilms' tumor, Ewings sarcoma, etc.
* Myelosuppressoin

Mitomycin:
* class
* indications
* antibiotic
* Bladder, GI

Tamoxifen, Raloxifene:
* class & MOA
* indications
* side effects
* SERMs- estrogen receptor antagonists in breast
* Breast cancer
* DVT, osteoporosis, mood, hot flashes, endometrial cancer

Azacitidine:
* class & MOA
* indications
* side effects
* Hypomethylating agent: incorporates into DNA and inhibits methyl transfer
* MDS
* Myelosuppression

Decitabine:
* class & MOA

* indications
* side effects
* Hypomethylating agent: incorporates into DNA and inhibits methyl transfer
* MDS, AML
* Myelosuppression

Thalidomide:
* class & MOA
* indications
* side effects
* immunomodulator
* Multiple Myeloma
* Teratogenic, thromboembolism
* Drowsy/somnolence

Lenalidomide:
* class & MOA
* indications
* side effects
* Immunomodulator
* Multiple Myeloma, MDS (5q-)
* Teratogenic, thromboembolism
* Secondary malignancy

Bortezomib:
* class & MOA
* indications
* side effects
* Reversibly binds proteasome, decreasing NF-kB signaling
* Multiple Myeloma
* Peripheral neuropathy
* decreased PLT

Carfilzomib:
* class & MOA
* indications
* side effects
* Irreversibly binds proteasome, inhibits NF-kB signaling
* Multiple Myeloma
* More severe toxicities than Bortezomib:

- cardio, pulmonary, low PLT

Imatinib:
* class & MOA
* indications
* side effects
* TKI against BCR-ABL, c-KIT
* CML
* drug interactions
* GI tox, Hepatotox

Nilotinib:
* class & MOA
* indications
* side effects
* TKI against BCR-ABL, c-KIT
* CML
* Pancreatitis
* GI-tox, hepatotox

Dasatinib:
* class & MOA
* indications
* side effects
* TKI against BCR-ABL, c-KIT
* CML
* GI-Tox, Hepatotox

Erlotinib:
* class & MOA
* side effect
* TKI that targets EGFR1/HER1
* skin rash

Lapatinib:
* class & MOA
* indications
* side effects

* TKI against EGFR2/HER2

* Breast cancer
* Cardiac --> low EF

Sorafenib:
* class & MOA
* indications
* side effects
* TKI against RAF-K
* RCC
* GI toxicity

Ruxolitinib:
* class & MOA
* indications
* side effects
* JAK inhibitor (JAK1 & JAK2)
* Myelofibrosis
* Myelosuppression

Rituximab:
* class & MOA
* indications
* side effects
* MAB against CD20
* CLL, NHL
* Infusion reaction** (release of cytokines) --> get fever, chills, rigors, hypotension, hypoxia -->
premedicate to prevent

Ofatumumab:
* class & MOA
* indications
* side effects
* MAB against CD20
* CLL
* Infusion reaction **

Trastuzumab:
* class & MOA

* indications
* side effects
* MAB against HER2
* Breast cancer
* Infusion reaction
* Cardiac toxicity**

Pertuzumab:
* class & MOA
* indications
* side effects
* MAB against HER2
* Breast cancer
* Infusion reaction
* Cardiac toxicity**

Bevacizumab:
* class & MOA
* indications
* side effects
* MAB against VEGF-receptor
* Solid tumors
* Bleeding** (VTE, etc)

Ziv-aflibercept
* class & MOA
* indications
* side effects
* MAB against VEGF-ligand
* CRC
* Bleeding ***

ATRA:
* class & MOA
* indications
* side effects
* Differentiating agent that releases PML-RARa allowing promyelocytes to differentiate
* APL
* Retinoid acid syndrome --> treat with dexamethasone

ATO:
* class & MOA
* indications
* side effects
* differentiating agent that breaks the PML-RARa translocation (given w/ ATRA)
* APL
* Retinoid acid syndrome --> treated with dexamethasone

Eculixumab:
* MOA
* indication
* MAB targeting C5
* PNH**