CCR FOCUS
... transporters of the ATP-binding cassette (ABC) transporter family, which include the multidrug resistance gene product P-glycoprotein (P-gp; ABCB1), and the breast cancer resistance protein (ABCG2), may have a significant effect on restricting drug uptake from tumor cells through active efflux (24). ...
... transporters of the ATP-binding cassette (ABC) transporter family, which include the multidrug resistance gene product P-glycoprotein (P-gp; ABCB1), and the breast cancer resistance protein (ABCG2), may have a significant effect on restricting drug uptake from tumor cells through active efflux (24). ...
Word 25KB
... Tyrosine kinase inhibitors for non-small cell lung cancer This report compared the predicted and actual use of the tyrosine kinase inhibitors (TKIs), erlotinib and gefitinib, for the treatment of Stage IIIB (locally advanced) or Stage IV (metastatic) non-small cell lung cancer (NSCLC). The number of ...
... Tyrosine kinase inhibitors for non-small cell lung cancer This report compared the predicted and actual use of the tyrosine kinase inhibitors (TKIs), erlotinib and gefitinib, for the treatment of Stage IIIB (locally advanced) or Stage IV (metastatic) non-small cell lung cancer (NSCLC). The number of ...
PowerPoint プレゼンテーション
... tyrosine kinases (RTKs), which are autophosphorylated (illustrated by Y-P) to trigger downstream signalling pathways, including the pathway involving RAS, RAF, extracellular signal-regulated kinase (ERK) and mitogen-activated protein kinase (MAPK)/ERK kinase (MEK). RAF kinase activity initiates a ki ...
... tyrosine kinases (RTKs), which are autophosphorylated (illustrated by Y-P) to trigger downstream signalling pathways, including the pathway involving RAS, RAF, extracellular signal-regulated kinase (ERK) and mitogen-activated protein kinase (MAPK)/ERK kinase (MEK). RAF kinase activity initiates a ki ...
Selective mutation in ATP-binding site reduces affinity of drug to the
... Mutation in protein kinases is very common in cancer and causes constitutive activation of protein kinases resulting in hyper activation of survival pathways. Recent studies suggest that mutation in ATP binding site of kinases confers resistance to the chemotherapy [1]. Thus, understanding how muta ...
... Mutation in protein kinases is very common in cancer and causes constitutive activation of protein kinases resulting in hyper activation of survival pathways. Recent studies suggest that mutation in ATP binding site of kinases confers resistance to the chemotherapy [1]. Thus, understanding how muta ...
Data Sheet Sorafenib Tosylate
... Description: Sorafenib Tosylate, also known as Bay 43-9006, is a novel bi-aryl urea compound that inhibits cell proliferation by targeting receptor tyrosine kinases, including VEGFR-2 and PDGFR--β and their associated signaling cascades of the ERK pathway and angiogenesis. It was originally develope ...
... Description: Sorafenib Tosylate, also known as Bay 43-9006, is a novel bi-aryl urea compound that inhibits cell proliferation by targeting receptor tyrosine kinases, including VEGFR-2 and PDGFR--β and their associated signaling cascades of the ERK pathway and angiogenesis. It was originally develope ...
CML
... FISH showing the BCR (green), ABL (orange), and BCR-ABL fusion signals (arrow): A=positive (contains a residual ABL signal), B=normal ...
... FISH showing the BCR (green), ABL (orange), and BCR-ABL fusion signals (arrow): A=positive (contains a residual ABL signal), B=normal ...
CYP3A4 Inhibitors
... 3. P-glycoprotein up regulation: i.e. over expression of multidrug resistance P-gp (efflux pump). 4. Alpha acid glycoprotein binding of imatinib: the plasma protein alpha 1 acid glycoprotein (AGP) has been proposed to bind to imatinib & prevent imatinib from reaching its target. ...
... 3. P-glycoprotein up regulation: i.e. over expression of multidrug resistance P-gp (efflux pump). 4. Alpha acid glycoprotein binding of imatinib: the plasma protein alpha 1 acid glycoprotein (AGP) has been proposed to bind to imatinib & prevent imatinib from reaching its target. ...
Tuberculosis complicating imatinib treatment for chronic myeloid leukaemia CASE STUDY
... suggesting that imatinib might impair the immune system, leading to a variety of infections, including varicella zoster and hepatitis B [7–9]. In vitro studies show inhibition of the development of CD34+ progenitor cell-derived dendritic cells with a reduced capacity to induce a cytotoxic T-cell res ...
... suggesting that imatinib might impair the immune system, leading to a variety of infections, including varicella zoster and hepatitis B [7–9]. In vitro studies show inhibition of the development of CD34+ progenitor cell-derived dendritic cells with a reduced capacity to induce a cytotoxic T-cell res ...
PDF
... Imatinib is an ATP-mimicking inhibitor targeting the tyrosine kinase activity of BCR-ABL-associated human leukaemias. Despite the success of imatinib in chronic myeloid leukaemia (CML) first line treatment, response rates of patients in accelerated or blastic phase are significantly decreased. Thus, ...
... Imatinib is an ATP-mimicking inhibitor targeting the tyrosine kinase activity of BCR-ABL-associated human leukaemias. Despite the success of imatinib in chronic myeloid leukaemia (CML) first line treatment, response rates of patients in accelerated or blastic phase are significantly decreased. Thus, ...
Chronic myeloid leukemia - Katedra i Klinika Hematologii
... Inhibits activity of mutant tyrosine kinase by blocking ATP binding Imatinib has less toxicity, is easier to administer, and induces higher hematologic (90 percent vs. 75percent), cytogenetic (40 percent vs. 10 percent) and molecular (7% vs. 2 %) types of remission ...
... Inhibits activity of mutant tyrosine kinase by blocking ATP binding Imatinib has less toxicity, is easier to administer, and induces higher hematologic (90 percent vs. 75percent), cytogenetic (40 percent vs. 10 percent) and molecular (7% vs. 2 %) types of remission ...
Managing Treatment Related Side Effects - CML
... Imatinib: CP=Gr 3/4 newly diagnosed and chronic phase Ifn (interferon) failure; Gleevec Prescribing Information Nov 2007. Sprycel Prescribing Information, Nov 2007; Tasigna, Prescribing Information, Oct 2007 ...
... Imatinib: CP=Gr 3/4 newly diagnosed and chronic phase Ifn (interferon) failure; Gleevec Prescribing Information Nov 2007. Sprycel Prescribing Information, Nov 2007; Tasigna, Prescribing Information, Oct 2007 ...
The Philadelphia chromosome
... targets BCR/abl, the constitutively activated tyrosine kinase fusion protein caused by the Philadelphia chromosome translocation. ...
... targets BCR/abl, the constitutively activated tyrosine kinase fusion protein caused by the Philadelphia chromosome translocation. ...
Slides
... Interferon alfa-2a approved for treatment of Philadelphia chromosome-positive CML patients who are minimally pretreated (within 1 year of diagnosis) ...
... Interferon alfa-2a approved for treatment of Philadelphia chromosome-positive CML patients who are minimally pretreated (within 1 year of diagnosis) ...
Binding Studies of Type I, II, and III Kinase Inhibitors against Bcr
... Figure 1. A model showing where various inhibitors bind Bcr-Abl kinase is shown. Note the large distance between the ATP binding pocket and site in which GNF-2/ GNF-5 binds. Resistance to imatinib results from the emergence of point mutations within the kinase domain of the Bcr-Abl protein that redu ...
... Figure 1. A model showing where various inhibitors bind Bcr-Abl kinase is shown. Note the large distance between the ATP binding pocket and site in which GNF-2/ GNF-5 binds. Resistance to imatinib results from the emergence of point mutations within the kinase domain of the Bcr-Abl protein that redu ...
Chronic Myeloid Leukemia: The Poster Child of
... 30%) of the patients in CP who failed IM despite median follow up of only 3 months. A potential advantage of a narrower kinase inhibitor is the potential to decrease toxicity attributed to off-targeted effects. No drug related pleural effusions and myelosuppression has been minimal 3/4 thrombocytope ...
... 30%) of the patients in CP who failed IM despite median follow up of only 3 months. A potential advantage of a narrower kinase inhibitor is the potential to decrease toxicity attributed to off-targeted effects. No drug related pleural effusions and myelosuppression has been minimal 3/4 thrombocytope ...
Presentation - Chronice Myeloid Leukemia
... • Patients are instructed not to take nilotinib with food since food can affect levels of nilotinib resulting in side effects such as the potential to affect heart rhythym • They should avoid taking grapefruit with nilotinib • They should take nilotinib at least 2 hours after eating food and then wa ...
... • Patients are instructed not to take nilotinib with food since food can affect levels of nilotinib resulting in side effects such as the potential to affect heart rhythym • They should avoid taking grapefruit with nilotinib • They should take nilotinib at least 2 hours after eating food and then wa ...
a case report: imatinib induced hepatotoxicity in chronic
... abnormalities are found and other translocation are also found. Accelerated Phase: various criteria have been develop to identity this phase. World health organization and MD Anderson cancer center has also provided various criteria for the diagnosis of the accelerated phase: Myeloblast (10 – 19 % ...
... abnormalities are found and other translocation are also found. Accelerated Phase: various criteria have been develop to identity this phase. World health organization and MD Anderson cancer center has also provided various criteria for the diagnosis of the accelerated phase: Myeloblast (10 – 19 % ...
203469Orig1s000 RISK ASSESSMENT and RISK MITIGATION REVIEW(S)
... Ponatinib appears to inhibit multiple tyrosine kinases including Bcr-Abl TKI and VEGFreceptor kinases inhibitors. The safety profile of ponatinib is similar to that observed with other Bcr-Abl TKI used to treat CML (Appendix A). Arterial thromboembolic events, gastrointestinal perforations, proteinu ...
... Ponatinib appears to inhibit multiple tyrosine kinases including Bcr-Abl TKI and VEGFreceptor kinases inhibitors. The safety profile of ponatinib is similar to that observed with other Bcr-Abl TKI used to treat CML (Appendix A). Arterial thromboembolic events, gastrointestinal perforations, proteinu ...
CHANGES AND CHALLENGES: GIST, MUTATED c-KIT AND IMATINIB RESISTANCE Sabrina Pricl
... A series of patients surgically treated at Istituto Nazionale per lo Studio e la Cura dei Tumori in Milan, Italy showed evidence of progressing GIST disease despite of Imatinib treatment. Accordingly, they were investigated for the presence of KIT and PDGFRA gene mutations. All patients showed the p ...
... A series of patients surgically treated at Istituto Nazionale per lo Studio e la Cura dei Tumori in Milan, Italy showed evidence of progressing GIST disease despite of Imatinib treatment. Accordingly, they were investigated for the presence of KIT and PDGFRA gene mutations. All patients showed the p ...
Presentation - Chronice Myeloid Leukemia
... Abnormal BCR-ABL fusion gene abnormal fusion protein This protein – “enzyme” - Tyrosine Kinase (TK) TKs control cell growth BCR-ABL protein has abnormal tyrosine kinase (TK) activity. Produces unregulated growth of white blood cells which is typical for CML. • Treatment targeted to block (inhibit) ...
... Abnormal BCR-ABL fusion gene abnormal fusion protein This protein – “enzyme” - Tyrosine Kinase (TK) TKs control cell growth BCR-ABL protein has abnormal tyrosine kinase (TK) activity. Produces unregulated growth of white blood cells which is typical for CML. • Treatment targeted to block (inhibit) ...
New TKI toward highly targeted therapies
... Avantages • Solve nearly all the mutationsrelated resistance problems • Faster response rates • Deeper responses + lower rate of progression compared to imatinib ...
... Avantages • Solve nearly all the mutationsrelated resistance problems • Faster response rates • Deeper responses + lower rate of progression compared to imatinib ...
CHRONIC MYELOGENOUS LEUKEMIA - 2012
... occlusive disease, chronic effects on pancreas or bone metabolism (??) - nilotinib Activity vs. other kinases differ T/NK lymphocytosis with dasatinib (good or ...
... occlusive disease, chronic effects on pancreas or bone metabolism (??) - nilotinib Activity vs. other kinases differ T/NK lymphocytosis with dasatinib (good or ...
Imatinib
... phase CML and 600 mg/day for patients in accelerated phase or blast crisis. Dose increases from 400 mg to 600 mg or 800 mg in patients with chronic phase disease, or from 600 mg to a maximum of 800 mg (given as 400 mg twice daily) in patients with accelerated phase or blast crisis may be considered ...
... phase CML and 600 mg/day for patients in accelerated phase or blast crisis. Dose increases from 400 mg to 600 mg or 800 mg in patients with chronic phase disease, or from 600 mg to a maximum of 800 mg (given as 400 mg twice daily) in patients with accelerated phase or blast crisis may be considered ...
IJBCP International Journal of Basic & Clinical
... Chronic myeloid leukemia (CML), the most common myeloproliferative disorder, occurring due to balanced reciprocal translocation between chromosome 9 and 22 and resulting in a chimeric oncogene called breakpoint cluster region-abelson (BCR-ABL) whose protein product has tyrosine kinase activity, caus ...
... Chronic myeloid leukemia (CML), the most common myeloproliferative disorder, occurring due to balanced reciprocal translocation between chromosome 9 and 22 and resulting in a chimeric oncogene called breakpoint cluster region-abelson (BCR-ABL) whose protein product has tyrosine kinase activity, caus ...
Titel voorbeeld titel
... which compete with ATP for binding at the tyrosine kinase receptor. Erlotinib and gefitinib are selective inhibitors of the epidermal growth factor receptor (EGFR), which is often overactive in tumors cells. Erlotinib and gefitinib are common used for treatment of non-small cell lung cancer. Imatini ...
... which compete with ATP for binding at the tyrosine kinase receptor. Erlotinib and gefitinib are selective inhibitors of the epidermal growth factor receptor (EGFR), which is often overactive in tumors cells. Erlotinib and gefitinib are common used for treatment of non-small cell lung cancer. Imatini ...