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FLT3 in AML


Crenolanib

A next-gen tyrosine kinase inhibitor for use in FLT3-mutated AML

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FLT3 in AML


Crenolanib

A next-gen tyrosine kinase inhibitor for use in FLT3-mutated AML


THE ROLE OF FLT3 MUTATIONS IN AML

Roughly one-third of AML patients harbor an internal tandem duplication (ITD) in FLT3, a receptor tyrosine kinase. Mutations of FLT3 at D835, a point mutation in the tyrosine kinase domain (TKD), have also been observed in AML patients. Both ITD and TKD mutations lead to constitutive activation of the tyrosine kinase function, making FLT3 an attractive drug target in AML patients. Both ITD and TKD mutations render FLT3 resistant to currently approved inhibitors. Moreover, novel activating FLT3 mutations are being identified in patients with AML. As the clinical development of FLT3 inhibitors proceeds into advanced phase trials, FLT3 mutations will represent a new obstacle in the care of FLT3-mutated AML patients.


CRENOLANIB IS A SELECTIVE TYPE I PAN-FLT3 INHIBITOR

Crenolanib, a type I TKI, is a potent inhibitor of FLT3-ITD and secondary KD mutants. Crenolanib represents the first TKI to exhibit both kinase selectivity and invulnerability to resistance-conferring KD mutations. Crenolanib , which spares cKIT, represents a promising therapy for achieving deep and durable responses in FLT3-mutant AML.
 


Crenolanib


Crenolanib



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THERE ARE SEVERAL ATTRIBUTES THAT SET CRENOLANIB APART FROM OTHER THERAPEUTIC OPTIONS

  1. Crenolanib, whether delivered by itself or as part of a drug combination, has shown benefit in FLT3 mutant AML.

  2. Patients who progress after treatment with prior TKIs may still remain sensitive to crenolanib.

  3. Crenolanib has favorable pharmacokinetics and does not accumulate with repeated dosing.

  4. Crenolanib is a selective type I TKI that does not inhibit wild-type cKIT.


Recent Peer-Reviewed Publications


Recent Peer-Reviewed Publications


RECENT PEER-REVIEWED PUBLICATIONS



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For More Information


For more information visit clinicaltrials.gov or contact us directly.

5420 LBJ Freeway, Suite 410
Dallas, TX 75240
Email: info@arogpharma.com

For More Information


For more information visit clinicaltrials.gov or contact us directly.

5420 LBJ Freeway, Suite 410
Dallas, TX 75240
Email: info@arogpharma.com