Question

Dr. Clement shared the bad news with his patient. “I’m sorry, Oliver, but it appears that the Gleevec you have been taking is no longer working against your cancer, and your white blood cells are growing out of control again. We’ll do some genetic testing to confirm, but the most likely cause of this relapse is that the BCR-ABL gene has mutated once again, and that mutation has rendered the protein resistant to the Gleevec you have been taking.” Dr. Clement sat in his office reviewing the most recent genetic testing results with Oliver. “As I expected,” he said, “you have acquired a resistance mutation in BCR-ABL that is preventing Gleevec from doing its job. But the good news is, we have another drug, dasatinib, that should be able to counteract this mutation. I am going to call in a prescription for dasatinib that you should start right away.”

Oliver was skeptical. If Gleevec wasn’t working against his cancer, what was so magical about this new drug, dasatinib?

What class of inhibitor is dasatinib?

Compare and contrast the function of dasatinib and the function of imatinib/Gleevec.

Dasatinib, at nanomolar concentrations, inhibits the following kinases: BCR-ABL, SRC family (SRC, LCK, YES, FYN), c-KIT, EPHA2, and PDGFRβ. Imatinib, at nanomolar concentrations, inhibits primarily BCR-ABL. How may these properties may affect Oliver’s new treatment?

Answer 1

Here i am going to explain your question in 4 answers

1) Imatinib/Gleevec and Dasatinib/Sprycel

●Dasatinib is a second generation BCR-ABL Kinase inhibitor

●Its is highly potent BCR-ABL Kinase inhibitor than Imatinib

●Dasatinib show high rate cytogenetic response and progression free survival among 50% patient who fails to respond Imatinib

2)DASATINIB is a pyrimidine and thiazole derived antineoplastic agent and protein kinase inhibitor of BCR-ABL KINASE

3)● As compare the administeration of daily once Dasatinib has significantly higher and faster rates of complete cytogenetic response

●Dasatinib has major molecula4 response also

●Dasatinib may improve the long term outcomes among patients with newly diagnosed chronic phase disease

● Dasatinib has lower drug resistance

●Dasatinib has faster action with low dose

4)DASATINIB is a multidrug kinase inhibitor that potently inhibits BCR-ABL and tue SRC family kinase (SRC,LCK,HCK,YES,FYN,FGR,BLK,FRK) as well as C-KIT , PDGFR-a and b and ephrin receptor kinase

Mechanism behind Dasatinib is still unknown and there are many theories

•It may cause immunological modification that can display more diverse Tcell population compared with Imatinib