Common agents
Agent | Mechanism |
Nitrosoureas: BCNU (carmustine), CCNU (AKA lomustine), ACNU (nimustine) | DNA crosslinks, carbamoylation of amino groups |
Alkylating (methylating) agents: procarbazine, temozolomide (Temodar®) | DNA alkylation, interferes with protein synthesis |
Carboplatin, cisplatin | Chelation via intrastrand crosslinks |
Nitrogen mustards: cyclophosphamide, isofamide, cytoxan | DNA alkylation, carbonium ion formation |
Vinca alkaloids: vincristine, vinblastine, paclitaxel | Microtubule function inhibitors |
Epidophyllotoxins (ETOP-oside, VP16, teniposide, VM26) | Topoisomerase II inhibitors |
Topotecan, irinotecan (CPT-11) | Topoisomerase I inhibitors |
Tamoxifen | Protein kinase C inhibitor at high doses |
Bevacizumab (Avastin®) | Anti-VEGF antibody, may be useful in vestibular neuromas |
Hydroxyurea | |
Bleomycin | |
Taxol (paclitaxel) | |
Methotrexate | |
Cytosine, arabinoside | |
Corticosteroids: dexamethasone, prednisone | |
Fluorouracil (FU) |
Chemotherapy agent (example) | Mechanism | Key comments / uses and toxicities* |
Bevacizumab (Avastin) | VEGF inhibitor | GBM; hypertension, delayed wound healing, bowel perforation, intracranial hemorrhage, thrombosis |
Erlotinib | EGFR tyrosine kinase inhibitor | Metastatic non‑small‑cell lung cancer |
Carmustine (BNCU) | Alkylating agent | GBM, astrocytoma, medulloblastoma; wafer form may cause seizures, cerebral infarction; IV can cause nausea/vomiting, fatigue, respiratory complications, pulmonary fibrosis, bone‑marrow suppression |
Cisplatin | Platinum alkylating agent | Glioma, medulloblastoma, others; minor pancytopenia, ototoxicity, peripheral neuropathy, nephrotoxicity, nausea/vomiting (carboplatin variant may cause alopecia) |
Everolimus | mTOR inhibitor | GBM, subependymal giant‑cell astrocytoma (SEGA) |
Tamoxifen | Estrogen receptor antagonist | Breast cancer |
Methotrexate | Dihydrofolate reductase inhibitor | Lymphoma; myelosuppression, mucositis, nausea/vomiting, nephrotoxicity, hepatic fibrosis, pulmonary toxicity, neurotoxicity if intrathecal |
Lomustine (CCNU) | Alkylating agent | PCV regimen for oligodendroglioma/mixed oligoastrocytoma |
Procarbazine | Alkylating agent | PCV regimen for oligodendroglioma/mixed oligoastrocytoma; risk of malignant hypertension with tyramine‑containing foods |
Temozolomide | Alkylating agent | GBM; constipation, nausea/vomiting, fatigue, headache |
Vincristine | Microtubule inhibitor | PCV regimen for oligodendroglioma/mixed oligoastrocytoma; pancytopenia, neuropathy, nausea/vomiting, mouth ulcers, fatigue |
Antineoplastic
Drug stem | Drug class / description | Example drug |
‑case | Recombinant uricase | Rasburicase |
‑mustine | Nitrosourea | Carmustine |
‑platin | Platinum compound | Cisplatin |
‑poside | Topoisomerase II inhibitor | Etoposide |
‑rubicin | Anthracycline | Doxorubicin |
‑taxel | Taxane | Paclitaxel |
‑tecan | Topoisomerase I inhibitor | Irinotecan |
Mechanism of action of some anticancer drugs
- Doxorubicin
- Mechanism of action
- Doxorubicin intercalate within DNA base pairs, causing breakage of DNA strands and inhibition of both DNA and RNA synthesis.
- Doxorubicin inhibits the enzyme topoisomerase II, causing DNA damage and induction of apoptosis.
- When combined with iron, doxorubicin also causes free radical-mediated oxidative damage to DNA, further limiting DNA synthesis.
- Iron chelators, such as dexrazoxane, may prevent free radical formation by limiting the binding of doxorubicin with iron
- Platinum-based chemotherapy
- Causes high frequency hearing loss
- Alkylating agents increase risk of leukemia
- Temozolomide
- Alkylating agent
- Dose
- Strupp protocol
- During radiotherapy: 75 mg per square metre of body-surface area per day, 7 days per week
- Post-radiotherapy (adjuvant): six cycles consisting of 150-200 mg per square metre for 5 days during each 28-day cycle
- Side effects
- Constipation
- N/V
- Fatigue
- Headache
- Amenorrhoea
- Loss of apetite
- Pneumonia
- Low platelets
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