DGIdb - ALECTINIB Drug Record

ALECTINIB chembl:CHEMBL1738797 ApprovedAntineoplastic

Alternate Names:

CH-5424802
ALECENSA
AF-802
RO-5424802
RO5424802
ALECTINIB
AF802
CH5424802
CH 5424802
AF 802
9-ETHYL-6,6-DIMETHYL-8-[4-(MORPHOLIN-4-YL)PIPERIDIN-1-YL]-11-OXO-6,11-DIHYDRO-5H-BENZO[B]CARBAZOLE-3-CARBONITRILE
ALECENSA®
pubchem.compound:49806720
rxcui:1727455
chemidplus:1256580-46-7
chembl:CHEMBL1738797
drugbank:11363

Drug Info:

Drug Class	Kinase Inhibitors
FDA Approval	Non-small cell lung cancer (with ALK fusion)
Drug Groups	investigational
Drug Categories	antineoplastic agents
Drug Categories	antineoplastic and immunomodulating agents
Drug Categories	cytochrome p-450 cyp3a substrates
Drug Categories	cytochrome p-450 cyp3a4 substrates
Drug Categories	cytochrome p-450 cyp3a4 substrates with a narrow therapeutic index
Drug Categories	cytochrome p-450 substrates
Drug Categories	heterocyclic compounds, fused-ring
Drug Categories	kinase inhibitor
Drug Categories	p-glycoprotein inhibitors
Drug Categories	p-glycoprotein substrates
Drug Categories	tyrosine kinase inhibitors

(10 More Sources)

Publications:

Amin et al., 2016, TKI sensitivity patterns of novel kinase-domain mutations suggest therapeutic opportunities for patients with resistant ALK+ tumors., Oncotarget
Mologni et al., 2015, NPM/ALK mutants resistant to ASP3026 display variable sensitivity to alternative ALK inhibitors but succumb to the novel compound PF-06463922., Oncotarget
Paik J et al., 2018, Alectinib: A Review in Advanced, ALK-Positive NSCLC., Drugs
Katayama et al., 2012, Mechanisms of acquired crizotinib resistance in ALK-rearranged lung Cancers., Sci Transl Med
Johung et al., 2016, Extended Survival and Prognostic Factors for Patients With ALK-Rearranged Non-Small-Cell Lung Cancer and Brain Metastasis., J. Clin. Oncol.
Yoshida et al., 2016, Rapid and dramatic response to alectinib in an anaplastic lymphoma kinase rearranged non-small-cell lung cancer patient who is critically ill., Anticancer Drugs
Johnson et al., 2016, Identification of I1171N resistance mutation in ALK-positive non-small-cell lung cancer tumor sample and circulating tumor DNA., Lung Cancer
Ou et al., 2014, Identification of a novel HIP1-ALK fusion variant in Non-Small-Cell Lung Cancer (NSCLC) and discovery of ALK I1171 (I1171N/S) mutations in two ALK-rearranged NSCLC patients with resistance to Alectinib., J Thorac Oncol
Hida T et al., 2017, Alectinib versus crizotinib in patients with ALK-positive non-small-cell lung cancer (J-ALEX): an open-label, randomised phase 3 trial., Lancet
Shaw et al., 2016, Alectinib in ALK-positive, crizotinib-resistant, non-small-cell lung cancer: a single-group, multicentre, phase 2 trial., Lancet Oncol.
Peters et al., 2017, Alectinib versus Crizotinib in Untreated ALK-Positive Non-Small-Cell Lung Cancer., N. Engl. J. Med.
Yoshimura et al., 2016, Antitumor activity of alectinib, a selective ALK inhibitor, in an ALK-positive NSCLC cell line harboring G1269A mutation: Efficacy of alectinib against ALK G1269A mutated cells., Cancer Chemother. Pharmacol.
Ceccon et al., 2015, Treatment Efficacy and Resistance Mechanisms Using the Second-Generation ALK Inhibitor AP26113 in Human NPM-ALK-Positive Anaplastic Large Cell Lymphoma., Mol. Cancer Res.
Pall G, 2015, The next-generation ALK inhibitors., Curr Opin Oncol
Morán et al., 2013, Targeting EML4-ALK driven non-small cell lung cancer (NSCLC)., Transl Lung Cancer Res
Gainor et al., 2016, Molecular Mechanisms of Resistance to First- and Second-Generation ALK Inhibitors in ALK-Rearranged Lung Cancer., Cancer Discov
Ou et al., 2016, Alectinib in Crizotinib-Refractory ALK-Rearranged Non-Small-Cell Lung Cancer: A Phase II Global Study., J. Clin. Oncol.
Katayama et al., 2014, Two novel ALK mutations mediate acquired resistance to the next-generation ALK inhibitor alectinib., Clin. Cancer Res.
Sakamoto et al., 2011, CH5424802, a selective ALK inhibitor capable of blocking the resistant gatekeeper mutant., Cancer Cell
Seto et al., 2013, CH5424802 (RO5424802) for patients with ALK-rearranged advanced non-small-cell lung cancer (AF-001JP study): a single-arm, open-label, phase 1-2 study., Lancet Oncol.
Shaw et al., 2016, Resensitization to Crizotinib by the Lorlatinib ALK Resistance Mutation L1198F., N. Engl. J. Med.
Yoda S et al., 2018, Sequential ALK Inhibitors Can Select for Lorlatinib-Resistant Compound <i>ALK</i> Mutations in ALK-Positive Lung Cancer., Cancer Discov
Ou et al., 2017, Dual occurrence of ALK G1202R solvent front mutation and small cell lung cancer transformation as resistance mechanisms to second generation ALK inhibitors without prior exposure to crizotinib. Pitfall of solely relying on liquid re-biopsy?, Lung Cancer
Kim et al., 2013, Heterogeneity of genetic changes associated with acquired crizotinib resistance in ALK-rearranged lung cancer., J Thorac Oncol
Gadgeel et al., 2014, Safety and activity of alectinib against systemic disease and brain metastases in patients with crizotinib-resistant ALK-rearranged non-small-cell lung cancer (AF-002JG): results from the dose-finding portion of a phase 1/2 study., Lancet Oncol.
Fontana et al., 2015, Activity of second-generation ALK inhibitors against crizotinib-resistant mutants in an NPM-ALK model compared to EML4-ALK., Cancer Med
Lu et al., 2017, The second-generation ALK inhibitor alectinib effectively induces apoptosis in human neuroblastoma cells and inhibits tumor growth in a TH-MYCN transgenic neuroblastoma mouse model., Cancer Lett.
Singhi et al., 2017, Identification of Targetable ALK Rearrangements in Pancreatic Ductal Adenocarcinoma., J Natl Compr Canc Netw
Tani et al., 2016, Activation of EGFR Bypass Signaling by TGFα Overexpression Induces Acquired Resistance to Alectinib in ALK-Translocated Lung Cancer Cells., Mol. Cancer Ther.
Lin et al., 2016, Clinical Activity of Alectinib in Advanced RET-Rearranged Non-Small Cell Lung Cancer., J Thorac Oncol

ALECTINIB EML4

Interaction Score: 7.81

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type Advanced Solid Tumor

Response Type resistant

Approval Status Preclinical

PMIDs:
27009859 28476735 25393796 26849637 27432227 26682573 25228534 21575866 26698910 23344087

Sources:
JAX-CKB
ALECTINIB ALK

Interaction Score: 4.69

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Alteration ALK:I1171T

Drug family ALK inhibitor

Alteration ALK__.

PMIDs:
27009859 25749034 30030733 22277784 26438117 26938871 27565911 25393796 28501140 26708155 28586279 26849637 25421750 25588040 25806224 27432227 26598747 25228534 21575866 23639470 26698910 29650534 28285684 23344087 25153538 25727400 28455243

Sources:
OncoKB FDA PharmGKB JAX-CKB CIViC TTD DrugBank COSMIC TALC MyCancerGenome GuideToPharmacology CGI
ALECTINIB NPM1

Interaction Score: 1.78

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type anaplastic large cell lymphoma

Response Type decreased response

Approval Status Preclinical

PMIDs:
27009859 25749034 25421750

Sources:
JAX-CKB
ALECTINIB SMAD4

Interaction Score: 1.18

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type pancreatic ductal adenocarcinoma

Response Type predicted – sensitive

Approval Status Clinical Study

PMIDs:
28476735

Sources:
JAX-CKB
ALECTINIB CDKN2A

Interaction Score: 0.65

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type pancreatic ductal adenocarcinoma

Response Type predicted – sensitive

Approval Status Clinical Study

PMIDs:
28476735

Sources:
JAX-CKB
ALECTINIB RET

Interaction Score: 0.3

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type non-small cell lung carcinoma

Response Type predicted – sensitive

Approval Status Clinical Study

PMIDs:
27544060

Sources:
JAX-CKB CIViC
ALECTINIB FGFR1

Interaction Score: 0.15

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type pancreatic ductal adenocarcinoma

Response Type predicted – sensitive

Approval Status Clinical Study

PMIDs:
28476735

Sources:
JAX-CKB
ALECTINIB MET

Interaction Score: 0.06

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

MyCancerGenome: CH5424802
- Version: 20-Jun-2017
Alternate Names:

CH5424802 Development Name

AF802 Development Name

Drug Info:

Drug Class Kinase Inhibitors

Publications:
MyCancerGenome: ALECTINIB
- Version: 20-Jun-2017
Alternate Names:

ALECENSA Trade Name

Drug Info:

Drug Class Kinase Inhibitors

FDA Approval Non-small cell lung cancer (with ALK fusion)

Publications:
DrugBank: DB11363
- Version: 5.1.7
Alternate Names:

ALECTINIB DrugBank Drug Name

1256580-46-7 CAS Number

Alecensa Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Groups investigational

Publications:

JAX-CKB: Alectinib

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Amin et al., 2016, TKI sensitivity patterns of novel kinase-domain mutations suggest therapeutic opportunities for patients with resistant ALK+ tumors., Oncotarget

Mologni et al., 2015, NPM/ALK mutants resistant to ASP3026 display variable sensitivity to alternative ALK inhibitors but succumb to the novel compound PF-06463922., Oncotarget

Ceccon et al., 2015, Treatment Efficacy and Resistance Mechanisms Using the Second-Generation ALK Inhibitor AP26113 in Human NPM-ALK-Positive Anaplastic Large Cell Lymphoma., Mol. Cancer Res.

PharmGKB: alectinib
- Version: 18-August-2020
Alternate Names:

Drug Info:

Publications:

Pall G, 2015, The next-generation ALK inhibitors., Curr Opin Oncol

CIViC: ALECTINIB

Version: 14-September-2020

Alternate Names:

Drug Info:

Publications:

Paik J et al., 2018, Alectinib: A Review in Advanced, ALK-Positive NSCLC., Drugs

Katayama et al., 2012, Mechanisms of acquired crizotinib resistance in ALK-rearranged lung Cancers., Sci Transl Med

Yoshida et al., 2016, Rapid and dramatic response to alectinib in an anaplastic lymphoma kinase rearranged non-small-cell lung cancer patient who is critically ill., Anticancer Drugs

GuideToPharmacology: 223366072
- Version: 29-September-2020
Alternate Names:

ALECTINIB GuideToPharmacology Ligand Name

Drug Info:

Publications:
TTD: Alectinib
- Version: 2020.06.01
Alternate Names:

D0U3SY TTD Drug ID

Drug Info:

Publications:
TALC: CHS424802
- Version: 12-May-2016
Alternate Names:

CHS424802 Primary Drug Name

CHS424802 Drug Synonym

AF802 Drug Synonym

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL1738797
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
CGI: Alectinib
- Version: 27-September-2017
Alternate Names:

Drug Info:

Publications:
OncoKB: Alectinib
- Version: 23-July-2020
Alternate Names:

Drug Info:

Publications:
FDA: Alectinib
- Version: 04-September-2020
Alternate Names:

Drug Info:

Publications:
COSMIC: Alectinib
- Version: 4-Sep-2020
Alternate Names:

Drug Info:

Publications:

Indication/Tumor Type	Advanced Solid Tumor
Response Type	resistant
Approval Status	Preclinical

Alteration	ALK:I1171T
Drug family	ALK inhibitor
Alteration	ALK__.

Indication/Tumor Type	anaplastic large cell lymphoma
Response Type	decreased response
Approval Status	Preclinical

Indication/Tumor Type	pancreatic ductal adenocarcinoma
Response Type	predicted – sensitive
Approval Status	Clinical Study

Indication/Tumor Type	non-small cell lung carcinoma
Response Type	predicted – sensitive
Approval Status	Clinical Study

Direct Interaction?	False
Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

ALECTINIB	DrugBank Drug Name
1256580-46-7	CAS Number
Alecensa	Drug Brand

Drug Type	small molecule
Drug Groups	approved
Drug Groups	investigational

CHS424802	Primary Drug Name
CHS424802	Drug Synonym
AF802	Drug Synonym

ALECTINIB Drug Record

ALECTINIB chembl:CHEMBL1738797 ApprovedAntineoplastic

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type Advanced Solid Tumor Response Type resistant Approval Status Preclinical

PMIDs: 27009859 28476735 25393796 26849637 27432227 26682573 25228534 21575866 26698910 23344087

Sources: JAX-CKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Alteration ALK:I1171T Drug family ALK inhibitor Alteration ALK__.

PMIDs: 27009859 25749034 30030733 22277784 26438117 26938871 27565911 25393796 28501140 26708155 28586279 26849637 25421750 25588040 25806224 27432227 26598747 25228534 21575866 23639470 26698910 29650534 28285684 23344087 25153538 25727400 28455243

Sources: OncoKB FDA PharmGKB JAX-CKB CIViC TTD DrugBank COSMIC TALC MyCancerGenome GuideToPharmacology CGI

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type anaplastic large cell lymphoma Response Type decreased response Approval Status Preclinical

PMIDs: 27009859 25749034 25421750

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type pancreatic ductal adenocarcinoma Response Type predicted – sensitive Approval Status Clinical Study

PMIDs: 28476735

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type pancreatic ductal adenocarcinoma Response Type predicted – sensitive Approval Status Clinical Study

PMIDs: 28476735

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type non-small cell lung carcinoma Response Type predicted – sensitive Approval Status Clinical Study

PMIDs: 27544060

Sources: JAX-CKB CIViC

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type pancreatic ductal adenocarcinoma Response Type predicted – sensitive Approval Status Clinical Study

PMIDs: 28476735

Sources: JAX-CKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction? False Specific Action of the Ligand Inhibition Endogenous Drug? False

PMIDs: None found

Sources: GuideToPharmacology

MyCancerGenome: CH5424802

Alternate Names: CH5424802 Development Name AF802 Development Name

Drug Info: Drug Class Kinase Inhibitors

Publications:

MyCancerGenome: ALECTINIB

Alternate Names: ALECENSA Trade Name

Drug Info: Drug Class Kinase Inhibitors FDA Approval Non-small cell lung cancer (with ALK fusion)

Publications:

DrugBank: DB11363

Alternate Names: ALECTINIB DrugBank Drug Name 1256580-46-7 CAS Number Alecensa Drug Brand

Drug Info: Drug Type small molecule Drug Groups approved Drug Groups investigational

Publications:

JAX-CKB: Alectinib

Alternate Names:

Drug Info:

PharmGKB: alectinib

Alternate Names:

Drug Info:

Publications: Pall G, 2015, The next-generation ALK inhibitors., Curr Opin Oncol

CIViC: ALECTINIB

Alternate Names:

Drug Info:

GuideToPharmacology: 223366072

Alternate Names: ALECTINIB GuideToPharmacology Ligand Name

Drug Info:

Publications:

TTD: Alectinib

Alternate Names: D0U3SY TTD Drug ID

Drug Info:

Publications:

TALC: CHS424802

Alternate Names: CHS424802 Primary Drug Name CHS424802 Drug Synonym AF802 Drug Synonym

Drug Info:

Publications:

ChemblDrugs: chembl:CHEMBL1738797

Alternate Names:

Drug Info:

Publications:

CGI: Alectinib

Alternate Names:

Drug Info:

Publications:

OncoKB: Alectinib

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type Advanced Solid Tumor

Response Type resistant

Approval Status Preclinical

PMIDs:
27009859 28476735 25393796 26849637 27432227 26682573 25228534 21575866 26698910 23344087

Sources:
JAX-CKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Alteration ALK:I1171T

Drug family ALK inhibitor

Alteration ALK__.

PMIDs:
27009859 25749034 30030733 22277784 26438117 26938871 27565911 25393796 28501140 26708155 28586279 26849637 25421750 25588040 25806224 27432227 26598747 25228534 21575866 23639470 26698910 29650534 28285684 23344087 25153538 25727400 28455243

Sources:
OncoKB FDA PharmGKB JAX-CKB CIViC TTD DrugBank COSMIC TALC MyCancerGenome GuideToPharmacology CGI

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type anaplastic large cell lymphoma

Response Type decreased response

Approval Status Preclinical

PMIDs:
27009859 25749034 25421750

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type pancreatic ductal adenocarcinoma

Response Type predicted – sensitive

Approval Status Clinical Study

PMIDs:
28476735

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type pancreatic ductal adenocarcinoma

Response Type predicted – sensitive

Approval Status Clinical Study

PMIDs:
28476735

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type non-small cell lung carcinoma

Response Type predicted – sensitive

Approval Status Clinical Study

PMIDs:
27544060

Sources:
JAX-CKB CIViC

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type pancreatic ductal adenocarcinoma

Response Type predicted – sensitive

Approval Status Clinical Study

PMIDs:
28476735

Sources:
JAX-CKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

Alternate Names:

CH5424802 Development Name

AF802 Development Name

Drug Info:

Drug Class Kinase Inhibitors

Alternate Names:

ALECENSA Trade Name

Drug Info:

Drug Class Kinase Inhibitors

FDA Approval Non-small cell lung cancer (with ALK fusion)

Alternate Names:

ALECTINIB DrugBank Drug Name

1256580-46-7 CAS Number

Alecensa Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Groups investigational

Publications:

Pall G, 2015, The next-generation ALK inhibitors., Curr Opin Oncol

Alternate Names:

ALECTINIB GuideToPharmacology Ligand Name

Alternate Names:

D0U3SY TTD Drug ID

Alternate Names:

CHS424802 Primary Drug Name

CHS424802 Drug Synonym

AF802 Drug Synonym