Rociletinib: Difference between revisions

Rociletinib
Clinical data
Trade names	Xegafri
Other names	CO-1686, AVL-301
Routes of; administration	By mouth
ATC code	L01XE37 (WHO) ;
Legal status
Legal status	Investigational;
Identifiers
	IUPAC name N-(3-{[2-{[4-(4-Acetyl-1-piperazinyl)-2-methoxyphenyl]amino}-5-(trifluoromethyl)-4-pyrimidinyl]amino}phenyl)acrylamide;
CAS Number	1374640-70-6;
PubChem CID	57335384;
DrugBank	DB11907;
ChemSpider	30646712;
UNII	72AH61702G;
KEGG	D10858;
CompTox Dashboard (EPA)	DTXSID801025958 ;
Chemical and physical data
Formula	C27H28F3N7O3
Molar mass	555.562 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CC(=O)N1CCN(CC1)c2ccc(c(c2)OC)Nc3ncc(c(n3)Nc4cccc(c4)NC(=O)C=C)C(F)(F)F;
	InChI InChI=1S/C27H28F3N7O3/c1-4-24(39)32-18-6-5-7-19(14-18)33-25-21(27(28,29)30)16-31-26(35-25)34-22-9-8-20(15-23(22)40-3)37-12-10-36(11-13-37)17(2)38/h4-9,14-16H,1,10-13H2,2-3H3,(H,32,39)(H2,31,33,34,35); Key:HUFOZJXAKZVRNJ-UHFFFAOYSA-N;

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Revision as of 15:39, 15 March 2018

Rociletinib is a medication developed to treat non-small cell lung carcinomas with a specific mutation. It is a third-generation epidermal growth factor receptor tyrosine kinase inhibitor.^[1] It was being developed by Clovis Oncology.^[2] In May 2016, development of rociletinib was halted, along with its associated clinical trials, and Clovis Oncology withdrew its marketing authorisation application from the European Medicines Agency. Clovis Oncology will continue to supply the drug to people whose physicians had recommended continued treatment.^[3]

Medical uses

Rociletinib was used to treat locally advanced or metastatic non-small-cell lung cancer (NSCLC), if the cancer cells were positive for the T790M mutation in the gene coding for EGFR.^[4] The T790M mutation is usually acquired following first-line treatment with other tyrosine kinase inhibitors, such as gefitinib and afatinib.

References

^ Van Der Steen, Nele; Caparello, Chiara; Rolfo, Christian; Pauwels, Patrick; Peters, Godefridus; Giovannetti, Elisa (2016). "New developments in the management of non-small-cell lung cancer, focus on rociletinib: What went wrong?". OncoTargets and Therapy. 9: 6065. doi:10.2147/OTT.S97644. PMC 5063481. PMID 27785053.{{cite journal}}: CS1 maint: unflagged free DOI (link)
^ "FDA Requests Additional Data for Rociletinib in EGFR T790M-Mutant NSCLC". OncLive. 2015-11-16. Retrieved 2016-01-04.
^ "About Clovis". Retrieved 18 November 2016.
^ "Study to Evaluate Safety, Pharmacokinetics, and Efficacy of Rociletinib (CO-1686) in Previously Treated Mutant Epidermal Growth Factor Receptor (EGFR) in Non-Small Cell Lung Cancer (NSCLC) Patients - Full Text View - ClinicalTrials.gov". Retrieved 2018-03-15.

This antineoplastic or immunomodulatory drug article is a stub. You can help Wikipedia by expanding it.

[1] Van Der Steen, Nele; Caparello, Chiara; Rolfo, Christian; Pauwels, Patrick; Peters, Godefridus; Giovannetti, Elisa (2016). "New developments in the management of non-small-cell lung cancer, focus on rociletinib: What went wrong?". OncoTargets and Therapy. 9: 6065. doi:10.2147/OTT.S97644. PMC 5063481. PMID 27785053.{{cite journal}}: CS1 maint: unflagged free DOI (link)

[OncLive_2015-2] "FDA Requests Additional Data for Rociletinib in EGFR T790M-Mutant NSCLC". OncLive. 2015-11-16. Retrieved 2016-01-04.

[3] "About Clovis". Retrieved 18 November 2016.

[4] "Study to Evaluate Safety, Pharmacokinetics, and Efficacy of Rociletinib (CO-1686) in Previously Treated Mutant Epidermal Growth Factor Receptor (EGFR) in Non-Small Cell Lung Cancer (NSCLC) Patients - Full Text View - ClinicalTrials.gov". Retrieved 2018-03-15.

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-'''Rociletinib''' ([[International Nonproprietary Name|INN]]) is a drug for the treatment of [[non-small cell lung cancer]], acting as an inhibitor of the [[epidermal growth factor receptor]] (EGFR).<ref>{{cite journal|doi=10.2147/OTT.S97644|pmc=5063481|title=New developments in the management of non-small-cell lung cancer, focus on rociletinib: What went wrong?|journal=OncoTargets and Therapy|pages=6065|year=2016|last1=Van Der Steen|first1=Nele|last2=Caparello|first2=Chiara|last3=Rolfo|first3=Christian|last4=Pauwels|first4=Patrick|last5=Peters|first5=Godefridus|last6=Giovannetti|first6=Elisa|pmid=27785053|volume=9}}</ref> It was being developed by [[Clovis Oncology]].<ref name="OncLive 2015">{{cite web | title=FDA Requests Additional Data for Rociletinib in EGFR T790M-Mutant NSCLC | website=OncLive | date=2015-11-16 | url=http://www.onclive.com/web-exclusives/fda-requests-additional-data-for-rociletinib-in-egfr-t790m-mutant-nsclc | accessdate=2016-01-04}}</ref> According to the company web site as of November 2016, development was halted and studies on the drug are no longer accepting new patients, but Clovis will continue to supply the drug to patients whose physicians had recommended continued treatment.<ref>{{cite web |url=http://clovisoncology.com/about-clovis/ |title=About Clovis |access-date=18 November 2016}}</ref>
+'''Rociletinib''' is a medication developed to treat [[non-small cell lung carcinoma]]s with a specific mutation. It is a third-generation [[epidermal growth factor receptor]] [[tyrosine kinase inhibitor]].<ref>{{cite journal|doi=10.2147/OTT.S97644|pmc=5063481|title=New developments in the management of non-small-cell lung cancer, focus on rociletinib: What went wrong?|journal=OncoTargets and Therapy|pages=6065|year=2016|last1=Van Der Steen|first1=Nele|last2=Caparello|first2=Chiara|last3=Rolfo|first3=Christian|last4=Pauwels|first4=Patrick|last5=Peters|first5=Godefridus|last6=Giovannetti|first6=Elisa|pmid=27785053|volume=9}}</ref> It was being developed by [[Clovis Oncology]].<ref name="OncLive 2015">{{cite web | title=FDA Requests Additional Data for Rociletinib in EGFR T790M-Mutant NSCLC | website=OncLive | date=2015-11-16 | url=http://www.onclive.com/web-exclusives/fda-requests-additional-data-for-rociletinib-in-egfr-t790m-mutant-nsclc | accessdate=2016-01-04}}</ref> In May 2016, development of rociletinib was halted, along with its associated clinical trials, and Clovis Oncology withdrew its [[marketing authorisation application]] from the [[European Medicines Agency]]. Clovis Oncology will continue to supply the drug to people whose physicians had recommended continued treatment.<ref>{{cite web |url=http://clovisoncology.com/about-clovis/ |title=About Clovis |access-date=18 November 2016}}</ref>
+==Medical uses==
+Rociletinib was used to treat locally advanced or metastatic [[non-small-cell lung cancer]] (NSCLC), if the cancer cells were positive for the [[T790M]] mutation in the gene coding for [[epidermal growth factor receptor|EGFR]].<ref>{{Cite news|url=https://clinicaltrials.gov/ct2/show/study/NCT01526928|title=Study to Evaluate Safety, Pharmacokinetics, and Efficacy of Rociletinib (CO-1686) in Previously Treated Mutant Epidermal Growth Factor Receptor (EGFR) in Non-Small Cell Lung Cancer (NSCLC) Patients - Full Text View - ClinicalTrials.gov|access-date=2018-03-15|language=en}}</ref> The T790M mutation is usually acquired following first-line treatment with other tyrosine kinase inhibitors, such as [[gefitinib]] and [[afatinib]].
 ==References==