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Product Indentification

Name:   Carfilzomib
Synonyms:   (S)-4-methyl-N-((S)-1-((S)-4-methyl-1-((R)-2-methyloxiran-2-yl)-1-oxopentan-2-ylamino)-1-oxo-3-phenylpropan-2-yl)-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamide
CAS Registry Number:   868540-17-4
Molecular Formula:   C40H57N5O7
Molecular Weight:    719.91
Molecular Structure:    




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Related info:


       Carfilzomib (CFZ) is a tetrapeptide epoxyketone and a selective proteasome inhibitor. It is an analog of epoxomicin.



Clinical trials:


        A phase 2 trial for multiple myeloma showed promising results.

       A single-arm, phase 2 trial of carfilzomib in patients with relapsed and refractory multiple myeloma showed that single-agent   carfilzomib had durable responses in 36 percent of the 257 patients evaluated.

       In another phase 2 trial of patients with relapsed and/or refractory multiple myeloma, carfilzomib in combination with lenalidomide and dexamethasone demonstrated an overall response rate of 78 percent. Researchers found carfilzomib could be administered over a period of 14-23 months with no new or overlapping toxicities.

       In a phase 2 trial, carfilzomib had a 53 percent overall response rate among patients with relapsed and/or refractory multiple myeloma who had not previously received bortezomib. This study also found prolonged carfilzomib treatment is well-tolerated with approximately 22 percent of patients continuing treatment beyond one year.

       In phase 2 trials of carfilzomib, the most common grade 3 or higher treatment-emergent adverse events were thrombocytopenia, anemia, lymphoenia, neutropenia, pneumonia, fatigue and hyponatremia.

       A phase 3 trial comparing carfilzomib, lenalidomide and dexamethasone versus lenalidomide and dexamethasone in patients with relapsed multiple myeloma is ongoing.

       In a frontline phase 1/2 study, the combination of carfilzomib, lenalidomide, and low-dose dexamethasone was highly active and well-tolerated, permitting the use of full doses for an extended time in newly-diagnosed multiple myeloma patients, with limited need for dose modification. Responses were rapid and improved over time, reaching 100% very good partial response.




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