AASraw tsim NMN thiab NRC hmoov hauv qhov ntau!

Ceritinib (LDK378)

Ceritinib yog siv los kho cov neeg mob metastatic tsis mob me me ntawm cov ntsws ntsws mob qog nqaij hlav (NSCLC) uas muaj qhov zoo rau cov mob qog nqaij hlav tsis txaus (ALK) thiab nws cov qog ua haujlwm nce lossis tsis tuaj yeem tiv taus Crotinib (crizotinib).

Hauj lwm yam khoom

Cov yam ntxwv yooj yim

khoom npe Ceritinib (LDK378)
CAS Number 1032900-25-6
molecular Formula C28H36CIN5O3S
Mis Lub Cev 558.135
Synonyms LDK-378;

NVP-LDK378;

NVP-LDK378-NX;

5-Chloro-N2-[5-methyl-4-(piperidin-4-yl)-2-(propan-2-yloxy)phenyl]-N4-[2-(propan-2-ylsulfonyl)phenyl]pyrimidine-2,4-diamine.

tsos Dawb rau hmoov zoo dawb
Cia thiab Ua Haujlwm Khaws nws ntawm chav sov thiab deb ntawm qhov kub thiab noo noo.

 

Ceritinib (LDK378)Hauj lwm

Ceritinib yog siv rau kev kho mob ntawm cov neeg mob qog nqaij hlav ntshav tsis zoo (ALK +) metastatic tsis yog mob qog nqaij hlav hauv lub ntsws loj (NSCLC) uas tau ua tsis zoo lossis tsis mob siab rau crizotinib tom qab kho nrog crizotinib.

Cov chromosomal kho rov qab sib koom nrog lub anaplastic lymphoma kinase (ALK) raws li tus neeg tsav tsheb oncogenic tau hloov kho cov kev kho mob uas tsis yog-me-hlwb mob ntsws. Nyob rau kaum xyoo dhau los, cov tshuaj tau tshwm sim muaj txiaj ntsig zoo ntawm tus kheej rau ALK-rov ua haujlwm tsis yog-me me-cov ntsws mob ntsws. Kev tso cai sai ntawm cov muaj zog ALK inhibitors, xws li crizotinib thiab ntau dua tsis ntev los no ceritinib (LDK378), raws li cov qauv tsim theem I / II muaj kev sim ua rau muaj kev vam meej hauv kev tshawb nrhiav kab mob qog nqaij hlav thiab pab txhawb rau lub sijhawm tshiab ntawm oncogenic tsom kev kho tshwj xeeb los ntawm kev ntxim nyiam soj ntsuam kev tsim qauv. ceritinib los ua qhov muaj hwj chim rau crizotinib rau ALK-rov ua haujlwm tsis yog-me me ntawm cov ntsws ntsws qog nqaij hlav tseem tau nthuav tawm.

 

Ceritinib (LDK378)Mechanism of Action

Ceritinib yog siv los kho cov neeg mob metastatic tsis mob me me ntawm cov ntsws ntsws mob qog nqaij hlav (NSCLC) uas muaj qhov zoo rau cov mob qog nqaij hlav tsis txaus (ALK) thiab nws cov qog ua haujlwm nce lossis tsis tuaj yeem tiv taus Crotinib (crizotinib).

Ceritinib yog qhov xaiv thiab muaj zog inhibitor ntawm anaplastic lymphoma kinase (ALK). Hauv lub cev physiology li qub, ALK ua haujlwm los ua cov kauj ruam tseem ceeb hauv kev txhim kho thiab kev ua haujlwm ntawm cov hlab ntsha. Txawm li cas los xij, chromosomal hloov chaw thiab fusion muab nce mus rau ib daim ntawv oncogenic ntawm ALK uas tau cuam tshuam nyob rau hauv kev ua tiav ntawm NSCLC. Ceritinib yog li ua rau inhibit qhov enzyme mutated thiab tso tseg kev loj hlob ntawm tes, thaum kawg tso tseg kev mob qog noj ntshav. Vim tias ceritinib suav tias yog kev kho mob qog noj ntshav, kev tshuaj pom zoo los ntawm FDA yuav tsum txiav txim siab seb cov neeg mob yog neeg sib tw ua ceritinib. Qhov kev ntsuam xyuas no, tsim los ntawm Roche, yog VENTANA ALK (D5F3) CDx Assay thiab yog siv los txheeb xyuas ALK-zoo NSCLC cov neeg mob uas yuav tau txais txiaj ntsig los ntawm kev kho mob ceritinib.

 

Ceritinib (LDK378)Daim ntawv thov

Ceritinib yog ib qho anaplastic lymphoma kinase (ALK) -positive inhibitor feem ntau siv rau kev kho mob ntawm metastatic NSCLC.Preothing, nws tsuas yog qhia rau cov neeg mob uas tau tsim tawm tiv thaiv crizotinib, lwm qhov tshuaj tiv thaiv ALK-zoo, tab sis tau txij li thaum nws txoj kev siv nthuav dav rau ua qhov kev xaiv thib ib rau metastatic NSCLC.

 

Ceritinib (LDK378)Sab sij huam & Lus Ceeb Toom

Cov kev mob tshwm sim hnyav ntxiv xws li mob plab hnyuv, ua kom mob rau cov ntshav, mob siab, mob ntsws, ua haujlwm QT mob ntev, hyperglycemia, bradycardia, thiab pancreatitis.

Feem ntau cov kev mob tshwm sim feem ntau yog zawv plab, xeev siab, nce ntshav siab daim siab, ntuav, mob plab, qaug zog, tsis qab los, thiab cem quav. Vim tias qhov kev pheej hmoo ntawm kev nce siab daim siab ua siab ntev, kev tshuaj ntsuam lub siab ua haujlwm yuav tsum ua txhua ob lub lis piam rau thawj 9 lub lim tiam ntawm kev kho mob.

Thaum kawg, ceritinib yog ob qho tib si substrate thiab muaj zog inhibitor ntawm enzyme CYP3A4, yog li cov tshuaj yuav tsum tau saib xyuas kom zoo uas yuav cuam tshuam nrog ceritinib.

 

Hu rau koj tus kws kho mob ib zaug yog tias koj muaj:

Diarrhea mob raws plab heev;

▪ mob taub hau, tsis meej pem, hloov pauv ntawm lub hlwb, tsis pom kev, pom qhov chua leeg (nriaj);

Tso zis me me lossis tsis tso zis;

Bleeding los ntshav txawv (ntshav ntswg, los ntshav coj los ntshav), lossis lwm yam los ntshav uas yuav tsis nres;

▪ pom ntawm lub plab bleeding ua ntshav lossis tso quav, hnoos txog ntshav lossis ntuav uas zoo li thaj chaw kas fes;

▪ mob plawv – mob hauv siab, mob hauv koj lub puab tsaig lossis pwg, o, nce qhov nrawm nrawm, ua tsis taus pa;

▪ cov cim ntawm ntshav txhaws num cia li hnov ​​ib ce lossis tsis muaj zog, muaj teeb meem tsis pom kev lossis hais lus;

Problems teeb meem mob siab urine cov zis tsaus nti, cov quav pleev xim av daj, tawv nqaij daj (daj tawv nqaij lossis qhov muag);

Calcium Qes calcium tsis tshua muaj sp nqaij leeg txhaws lossis mob pob, txham lossis hnov ​​zoo siab (nyob ib ncig ntawm koj lub qhov ncauj, lossis hauv koj cov ntiv tes thiab ntiv taw);

▪ nce ntshav siab – mob taub hau heev, plooj tsis pom kev, tawm hauv koj lub caj dab lossis pob ntseg, ntxhov siab, qhov ntswg.

Koj cov kev kho mob cancer tej zaum yuav qeeb lossis tsis tu ncua yog tias koj muaj qee yam tshwm sim.

 

reference

[1] “Zykadia (ceritinib) Capsules, rau Kev Siv Ncauj Lus. Cov Ntawv Qhia Txhua Yam ”(PDF). Novartis Kev lag luam tshuaj Corporation. Txais 14 Lub Ob Hlis 2017.

[2] “Cov npe tsis yog thoob ntiaj teb rau Cov Npe Tshuaj (INN). Pom zoo Cov Npe Tsis Muaj Lag Luam Hauv Npe: Sau 71 ”(PDF). Koom Haum Saib Xyuas Kev Noj Qab Haus Huv Thoob Ntiaj Teb. 2014. p. 79. Nqa Tau 14 Lub Ob Hlis 2017

[3] “FDA pom zoo Ceritinib rau Kab Mob Kuaj Mob HLOB CUB ALK”. Medscape. Plaub Hlis 29, 2014.

[4] “Kev muab cov ntaub ntawv sau cia” (PDF). www.pharma.us.novartis.com. Tawm Tsiab 2019-06-12.

[5] “FDA nthuav dav pom zoo Ceritinib rau mob ntsws”. Koom haum Cancer National. 27 Lub Rau Hli 2017.