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Tyrosine kinase inh & monoclonal ab

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medmaestro's version from 2016-01-21 10:39

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TYROSINE KINASE INHIBITORS
DRUGINHIBIT -TYROSINE KINASE ACTIVATED BYINDICATION
AxitinibVEGFR-1,2,3advanced renal cell carcinoma
Bosutinibabl-bcr,srcCML
Cirzotinibc-MET,ALKNon small cell lung carcinoma
Carbozantinibc-MET,VEGFR-2Medullary carcinoma thyroid
Dasatinibabl-bcr,src family,c-kit,EPHA-2,PDGFRβCML,Philadelphia +ve ALL
ErlotinibEGFRNon small cell lung carcinoma,Pancreatic ca
GeftinibEGFRNon small cell lung carcinoma
Imatinibabl-bcr , c-KIT,PDGFCML,GIST
Lapatinibher-2/Neu,erb-B2,EGFRBreast carcinoma
Nilotinibabl-bcrCML
PazopanibVEGFR-1,2,3 ; PDGFRα,β;c-KITAdvanced renal cell carcinoma
Ponatinibabl-bcrCML Philadelphia positive,ALL
RegorafenibVDGFR2,TIE2Colorectal carcinoma,GIST
RuxolitinibJAK 1,2Myelofibrosis
SorafenibVEGFR,PDGFR,RAF,c-KITRenal cell carcinoma,Hepatocellular carcinoma
Sunitinib(SECOND GENERATION RECEPTOR TYROSINE KINASE INHIBITORS)VEGFR,PDGFR,c-KIT,FLT-3,RETRenal cell carcinoma,pancreatic neuroendocrine tumours,GIST
TofacitinibJAKRheumatoid arthritis
TemsirolimusmTORRCC
VandetanibVEGFR,EGFRMedullary carcinoma thyroid
VemurafenibBRAFMalignant melanoma
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MONOCLONAL ANTIBODIES:

MONOCLONAL ANTIBODIESTARGETED AGAINSTINDICATIONCOMMENTS
RituximabCD 20CLL,Hemolytic anemia(Autoimmune,AIHA),Idiopathic Thrombocytopenic purpura,Non hodgkin lymphoma,Arthritis--------
AlemtuzumabCD52Low grade lymphomas,B-Cell CLL -------
TranstuzumabHer 2 /neuBreast carcinoma,Recently approved for cancer of stomach or gastro-oesophageal junctioncan cause cardiotoxicity
CetuximabEGFRColon cancer (with Irinotecan);Head and neck cancer (with radiation therapy)(ADR-Cause hypersensitivity reactions)cause rash,hypersensitivity reactions,hypomagnesemia,interstitial lung disease
PanitumumabEGFREGFR positive metastatic colorectal carcinomaFully human monoclonal Ab ,so no hypersensitivity
BevacizumabVEGFMetastatic colorectal carcinoma,Breast ca,Glioblastoma,metastatic renal cell ca,non small cell lung cacombined with 5 FU
Gemtizumab ,OzogamicinCD33CD 33 Positive AMLLinked to calicheamicin
I131-Tositumomab , Y 90-Ibritumomab tiuxetanCD20Relapsed lymphomaconjugated with radioisotopes
Denileukin diftitox---recurrent cutaneous T cell lymphomaRecombinant IL-2 + Diphtheria toxin
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FDA APPROVED MONOCLONAL ANTIBODIES-APPENDIX 34
Clues-
Question Answer
-ximabchimeric
-mumabhuman
-zumabhumanized
-momabmurine
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CHIMERIC MONOCLONAL ANTIBODIES(-ximab)

ANTIBODYTARGETINDICATION
Abciximabinhibition of glycoprotein IIb/IIIacardiovascular disease
BasiliximabIL-2 Rα Receptor (CD 25)Transplant rejection
Cetuximabepidermal growth factor receptorcolorectal cancer , head and neck cancer
Infliximabinhibition of TNF-α signallingseveral autoimmune disorders
RituximabCD 20Non-Hodgkin lymphoma
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HUMAN MONOCLONAL ANTIBODIES(-mumab)

ANTIBODYTARGETINDICATION
Adalimumabinhibition of TNF-α signallingseveral autoimmune disorders
PanitumumabEpidermal Growth Factor Receptor (EGFR)Colorectal cancer
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HUMANIZED MONOCLONAL ANTIBODIES(-zumab)

Question Answer Column 3
AlemtuzumabCD52 chronic lymphocytic leukemia
Bevacizumabvascular endothelial growth factor (VEGF)Colorectal cancer,Age related macular degeneration
Certolizumab pegolinhibition of TNF-α signallingCrohn’s disease
DaclizumabIL-2 R α Receptor (CD25)Transplant rejection
EculizumabComplement system protein C5Paroxysmal Nocturnal Hemoglobinuria(PNH)
EfalizumabCD 11aPsoriasis
GemtuzumabCD 33Acute myelogenous leukemia(with calicheamicin)
Natalizumabα – 4 IntegrinMultiple sclerosis,Crohn’s disease
OmalizumabIg EMainly allergy related asthma
Palivizumaban epitope of RSV F ProteinRespiratory synctial virus
RanibizumabVascular endothelial growth factor A(VEGF-A)Macular degeneration
TranstuzumabErbB2Breast cancer
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MURINE MONOCLONAL ANTIBODIES(-momab)

Question Answer Column 3
Ibritumomab tiuxetanCD20Non-Hodgkin lymphoma (with Yttrium-90 or Indium-111)
Muromonab-CD3Tcell CD 3 ReceptorTransplant rejection
TositumomabCD 20Non Hodgkin lymphoma
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DRUGS USED TO PREVENT TOXICITY OF ANTI CANCER DRUGS
DRUGMECHANISMINDICATIONS
Allopurinolinhibit Xanthine oxidaseprevent hyperuricemia from tumour lysis syndrome
Rasburicaserecombinant urate oxidaseprevent hyperuricemia from tumour lysis
Mesnaneutralizuing agentprevent hemorrhagic cystitis due to Ifosfamide and high dose cyclophosphamide
Leucovorin(Folinic acid (INN) or leucovorin (USAN), generally administered as calcium or sodium folinate (or leucovorin calcium/sodium), is an adjuvant used in cancer chemotherapy involving the drug methotrexate. It is also used in synergistic combination with the chemotherapy agent 5-fluorouracil. Leucovorin is a folic acid derivative. Methotrexate and the folic acid antagonists block the body's production of folate. Leucovorin works by replacing folate in the body)replete tetrahydrofolic acidrescue after high dose Methotrexate
AmifostineWR-2721=prodrug,Active=free thiol=WR-1065,Activation @ normal tissue; CYTOPROTECTION OF NORMAL TISSUEprevent radiation induced xerostomia and cisplatin induced nephrotoxicity
Dexrazoxaneiron chelatorprevent cardiotoxicity due to anthracyclines
Paliferminkeratinocyte growth factorprevent mucositis following chemotherapy
Pilocarpinecholinergic agonistradiation induced xerostomia
Pamidronate & Zolendronatebisphosphonateshypercalcemia of pregnancy
Epoetin –alpha & Darbopoetin alphaerythropoietinanaemia
Filgrastim ,Peg-FilgrastimG-CSFFebrile neutropenia prophylaxis
SargramostimGM-CSFFebrile neutropenia prophylaxis
OprelvekinIL-11Thrombocytopenia
Ondansetron5HT3 antagonistnausea and vomiting
Granisetron5HT3 antagonistnausea and vomiting
Palonosetron5HT3 antagonistnausea and vomiting
AprepitantNK-1 antagonistCisplatin induced delayed vomiting
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