Lestaurtinib: Difference between revisions

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{{Short description|A tyrosine kinase inhibitor used in cancer treatment}}


'''Lestaurtinib''' ([[International Nonproprietary Name|rINN]], codenamed CEP-701) is a [[tyrosine kinase]] inhibitor structurally related to [[staurosporine]], and is being developed by [[Cephalon]].
'''Lestaurtinib''' is a small molecule [[tyrosine kinase inhibitor]] that has been investigated for its potential use in the treatment of various types of [[cancer]]. It is particularly noted for its activity against the [[FLT3]] receptor, which is often mutated in certain types of [[leukemia]].


It is an inhibitor of [[FLT3]],<ref name="pmid16857985">{{cite journal |author=Knapper S, Burnett AK, Littlewood T, ''et al.'' |title=A phase 2 trial of the FLT3 inhibitor lestaurtinib (CEP701) as first-line treatment for older patients with acute myeloid leukemia not considered fit for intensive chemotherapy |journal=Blood |volume=108 |issue=10 |pages=3262–70 |date=November 2006 |pmid=16857985 |doi=10.1182/blood-2006-04-015560 |url=http://www.bloodjournal.org/cgi/pmidlookup?view=long&pmid=16857985}}</ref> [[JAK2]],<ref name="pmid17984313">{{cite journal |author=Hexner EO, Serdikoff C, Jan M, ''et al.'' |title=Lestaurtinib (CEP701) is a JAK2 inhibitor that suppresses JAK2/STAT5 signaling and the proliferation of primary erythroid cells from patients with myeloproliferative disorders |journal=Blood |volume=111 |issue=12 |pages=5663–71 |date=June 2008 |pmid=17984313 |doi=10.1182/blood-2007-04-083402 |url=http://www.bloodjournal.org/cgi/pmidlookup?view=long&pmid=17984313 |pmc=2424161}}</ref> [[TrkA]], [[TrkB]] and [[TrkC]].<ref>{{cite journal |author=Revill, P., Serradell, N., Bolos, J., Rosa, E.|title=Lestaurtinib |journal=Drugs of the Future |volume=32 |issue=3 |pages=215|year=2007|doi=10.1358/dof.2007.032.03.1084137}}</ref>
==Mechanism of Action==
Lestaurtinib functions by inhibiting the activity of [[tyrosine kinases]], which are enzymes that play a critical role in the signaling pathways that regulate cell division and survival. By blocking these enzymes, lestaurtinib can interfere with the growth and proliferation of cancer cells. The drug is particularly effective against the [[FLT3]] receptor, a common mutation in [[acute myeloid leukemia]] (AML) that leads to uncontrolled cell growth.


==Uses==
==Clinical Applications==
It is undergoing research for the treatment of [[acute myelogenous leukemia]] (AML) and [[myeloproliferative]] disorders.  
Lestaurtinib has been studied in clinical trials for its efficacy in treating [[acute myeloid leukemia]] (AML), especially in patients with FLT3 mutations. It has also been explored for use in other malignancies, including [[acute lymphoblastic leukemia]] (ALL) and certain solid tumors. However, its development has faced challenges, and it is not currently approved for general clinical use.


{{As of| 2009}}, it is in Phase II clinical trials for AML and Phase II clinical trials for myeloproliferative disorders.<ref>{{cite web |url=http://www.cephalon.com/fileadmin/media/downloads/Cephalon_Oncology_Pipeline_Fact_Sheet_FINAL_10_2009.pdf |title=Oncology pipeline Oct 2009 }}</ref><ref>{{cite web |url=http://clinicaltrials.gov/ct2/results?term=Lestaurtinib |title=Trials of Lestaurinib }}</ref>
==Pharmacokinetics==
The pharmacokinetic profile of lestaurtinib involves its absorption, distribution, metabolism, and excretion. It is administered orally and undergoes hepatic metabolism. The drug's half-life and bioavailability are important considerations in its dosing regimen.


==See also==
==Side Effects==
*[[Janus kinase inhibitor]]
As with many cancer therapies, lestaurtinib can cause a range of side effects. Common adverse effects include gastrointestinal disturbances, fatigue, and hematological abnormalities such as neutropenia and thrombocytopenia. Monitoring and managing these side effects is crucial in patients undergoing treatment.
==References==
 
{{Reflist}}
==Research and Development==
{{Extracellular chemotherapeutic agents}}
Lestaurtinib has been the subject of numerous clinical trials aimed at assessing its safety and efficacy. While initial results have shown promise, further research is needed to fully understand its potential and to optimize its use in combination with other therapies.
[[Category:Receptor tyrosine kinase inhibitors]]
 
[[Category:Lactams]]
==Related Pages==
[[Category:Non-receptor tyrosine kinase inhibitors]]
* [[Tyrosine kinase inhibitor]]
[[Category:Indolocarbazoles]]
* [[FLT3]]
{{pharma-stub}}
* [[Acute myeloid leukemia]]
* [[Cancer treatment]]
 
[[Category:Tyrosine kinase inhibitors]]
[[Category:Experimental cancer drugs]]

Latest revision as of 19:06, 22 March 2025

A tyrosine kinase inhibitor used in cancer treatment


Lestaurtinib is a small molecule tyrosine kinase inhibitor that has been investigated for its potential use in the treatment of various types of cancer. It is particularly noted for its activity against the FLT3 receptor, which is often mutated in certain types of leukemia.

Mechanism of Action[edit]

Lestaurtinib functions by inhibiting the activity of tyrosine kinases, which are enzymes that play a critical role in the signaling pathways that regulate cell division and survival. By blocking these enzymes, lestaurtinib can interfere with the growth and proliferation of cancer cells. The drug is particularly effective against the FLT3 receptor, a common mutation in acute myeloid leukemia (AML) that leads to uncontrolled cell growth.

Clinical Applications[edit]

Lestaurtinib has been studied in clinical trials for its efficacy in treating acute myeloid leukemia (AML), especially in patients with FLT3 mutations. It has also been explored for use in other malignancies, including acute lymphoblastic leukemia (ALL) and certain solid tumors. However, its development has faced challenges, and it is not currently approved for general clinical use.

Pharmacokinetics[edit]

The pharmacokinetic profile of lestaurtinib involves its absorption, distribution, metabolism, and excretion. It is administered orally and undergoes hepatic metabolism. The drug's half-life and bioavailability are important considerations in its dosing regimen.

Side Effects[edit]

As with many cancer therapies, lestaurtinib can cause a range of side effects. Common adverse effects include gastrointestinal disturbances, fatigue, and hematological abnormalities such as neutropenia and thrombocytopenia. Monitoring and managing these side effects is crucial in patients undergoing treatment.

Research and Development[edit]

Lestaurtinib has been the subject of numerous clinical trials aimed at assessing its safety and efficacy. While initial results have shown promise, further research is needed to fully understand its potential and to optimize its use in combination with other therapies.

Related Pages[edit]