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Lecture one

Anticancer drug

TermDefinition
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
Created by: wind1980