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Lecture one
Anticancer drug
| Term | Definition |
|---|---|
| Curative cancer by chemotherapy | choriocarcinoma (advance stage); Hodgkin's disease, carcinoma of tests; acute leukemia (some case) |
| Biologic therapy | immunotherapy (involves stimulating the host's immune system to fight the cancer) |
| Agent of Biologic therapy | cytokines (Produce by DNA tech). tumor vaccines; interferons (IFNs); interleukins (ILs); monoclonal antibodies (mAbs) |
| Adjuvant therapy | the use of systemic agents to eradicate micrometastatic disease following localized modalities such as surgery and radiation or both. |
| Palliative therapy | relieving and preventing the suffering of patients |
| Alkylating agents | Nitrogen mustards; ethylenimine & methylmelamines; alkyl sufonates; nitrosourea; triazenes and platinum complexes |
| Antimetabolites | folic acid analogs; pyrimidine analogs and purine analogs |
| Natural products | anti mitotic drugs; epipodophyllotoxins; camptothecin analogs; antibiotics |
| Hormones and antagonists | estrogens; androgens and their antagonists (tamoxifen, flutamide) |
| Miscellaneous agents | substituted urea (hydroxyurea); enzymes; tyrosine kinase inhibitors; monoclonal Abs |
| Factor affect chemotherapy | drug resistance; tumor cell heterogeneity; does intensity; patient-specific factors |
| Drug resistance | 1) decrease activation of drug; 2) decrease drug uptake or incase efflux; 3) change in target enzymes; 4) increase repair ability of cell damage; 5) increase drug inactivation |
| Drug resistance protein | MRP (ABCC); BCRP (ABCG2/MXRABCP) |
| General inhibitors of organic anion transport | Probeanecid; sulfinpyrazone; indomethacin |
| Inhibitors or P-glycoprotein and MRPs | PAK104P; Verapamil; cyclosporinA; genistein; MK571; ONO1078; TKI |
| GSH-dependent inhibitors of MRP1 | AgosteolA; LY475776; LY402913 |
| Inhibitors of ABCG2/BCRP | Fumitremorgin C(FTC); GF120918; TKIs |
| Taxanes, Paclitaxel (Taxol) | Ovarian carcinoma MOA: Promotes microtubule formation, inhibits the replication and also enhance the radiation therapy. |
| Docetaxel (Doc, Taxotere, TXT) | It is analog of Taxol. Breat, ovarian cancer; NSCLC |
| Camptothecin's analog, topotecan | Advance ovarian carcinoma, some efficacy on lung cancer. MOA: inhibits topoisomerase I |
| Irinotecan (CPT-11) | metastatic colorectal cancer. |
| Small molecule compounds (TK inhibitors) | Imatinib mesylate (Gleevec, ST1571); Gefitinib (Iressa, ZD1839); Erlotinib (Taceva); Sutent (sunitinib malate, formerly SU-11248); Trastuzumab (Herceptin); Lapatinib or lapatinib ditosylate (GW572016); Dasatinib (Sprycel); Nilotinib (Tasigna) |
| Imatinib mesylate (Gleevec, STI571) | Chronic myelogenous leukemia (CML); Gastrointestinal stromal tumor (GIST) |
| Gefitinib (Iressa, ZD1839) | NSCLS |
| Erlotinib (Tarceva) | NSCLS |
| Sunitinib malate (SU11248) suttent | MOA: TKis, also inhibiting blood vessel growth renal cel carcinoma |
| Trastuzumab (Herceptin) | breast cancer |
| apatilnib ditosylate, GW572016) | breast and lung cancer |
| Dasatinib (Sprycel) | chronic phase (CP) accelerated phase (AP) myeloid blast (MB) lymphoid blast (LB) Philadelphia chromosome positive (Ph+) chronic myelogenous leukemia (CML) |
| Nilotinib (Tasigna) | drug resistant chronic myelogenous leukemia (CML) |
| Everolimus (Afinitor) | Kidney cancer |
| Bevacizumab (Avastin) | colon cancer; NSCLC; breast cancer |
| Crizotinib (Xalkori, Pfizer) | NSCLC |
| Vemurafenib (Zelboraf) | melanoma |
| Nanoparticle albumin-bound (nab)-paclitaxel (Abraxane, Celgene) | metastatic pancreatic cancer |
| Bevacizumab (Avastin) | last stage cervical cancer |
| Nivolumab | melanoma |
| Pembrolizumab | melanoma |
| Beleodaq (belinostat) | peripheral T-cell lymphoma MOA: Histone deacetylase (HDAC) inhibitor |
| Vectibix (panitumumab) | metastatic colorectal cancer |
| Imbruvica (ibrutinib) | chronic lymphocytic leukemia |
| Zydelig (idelalisib) | chronic lymphocytic leukemia (CLL) and non-Hodgkin lymphoma (NHL) MOA: phosphoinositide 3-kinase (PI3K) delta inhibitor |
| Velcade (bortezomib) | multiple myeloma |
| Avastin (bevacizumab) | cervical cancer |