Alectinib

Kinase Inhibitor — ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Key facts

Alectinib is an onp drug in the Kinase Inhibitor class catalogued in DrugCentral. It was first approved by the PMDA in 2014. Its mechanism of action is classified as Kinase Inhibitors. DrugCentral lists 18 molecular targets, including ALK, RET and SRPK2. Recorded indications include Anaplastic lymphoma kinase positive anaplastic large cell lymphoma and Non-small cell lung cancer.

• Approval status: onp (first approved 2014 by the PMDA).
• Drug class: Kinase Inhibitor.
• Mechanism of action: Kinase Inhibitors.
• Molecular targets: ALK, RET, SRPK2 and SRPK1 (18 listed in DrugCentral).
• Indications: Anaplastic lymphoma kinase positive anaplastic large cell lymphoma and Non-small cell lung cancer.
• ATC code: L01ED03 (Anaplastic lymphoma kinase (ALK) inhibitors).
• Molecular formula: C30H34N4O2; molecular weight 482.63 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (2)

• Anaplastic lymphoma kinase positive anaplastic large cell lymphoma
• Non-small cell lung cancer

Mechanism & targets

• Mechanism of action (MoA): Kinase Inhibitors
• Established pharmacologic class: Kinase Inhibitor

Molecular targets (18)

Target	Gene	Action	Activity
ALK tyrosine kinase receptor	ALK	inhibitor	IC50 8.72
Proto-oncogene tyrosine-protein kinase receptor Ret	RET	inhibitor	IC50 8.32
SRSF protein kinase 2	SRPK2	unknown	IC50 7.55
SRSF protein kinase 1	SRPK1	unknown	IC50 6.71
Ephrin type-A receptor 1	EPHA1	unknown	Kd 6.71
Cyclin-G-associated kinase	GAK	unknown	Kd 6.59
Peroxisomal acyl-coenzyme A oxidase 1	ACOX1	unknown	Kd 6.57
Casein kinase I isoform gamma-2	CSNK1G2	unknown	Kd 6.29
Dual specificity protein kinase CLK3	CLK3	unknown	Kd 5.86
Vascular endothelial growth factor receptor 2	KDR	unknown	IC50 5.85
ATP-binding cassette sub-family G member 2	ABCG2	unknown	IC50 5.82
Phosphorylase b kinase gamma catalytic chain, liver/testis isoform	PHKG2	unknown	Kd 5.77
Proto-oncogene tyrosine-protein kinase ROS	ROS1	unknown	Ki 5.70
Dual specificity protein kinase CLK2	CLK2	unknown	Kd 5.63
Peroxisomal acyl-coenzyme A oxidase 3	ACOX3	unknown	Kd 5.58
Tyrosine-protein kinase Fer	FER	unknown	Kd 5.42
Dual specificity protein kinase CLK1	CLK1	unknown	Kd 4.53
Calcium/calmodulin-dependent protein kinase kinase 2	CAMKK2	unknown	Kd 4.45

Regulatory approvals (3)

Date	Agency	Marketed as	Applicant	Orphan
2017-02-16	EMA	—	Roche Registration Limited
2015-12-11	FDA	—	HOFFMAN-LA ROCHE
2014-07-04	PMDA	—	Chugai Pharmaceutical Co., Ltd	Yes

ATC classification

ATC code	Therapeutic hierarchy
L01ED03	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › PROTEIN KINASE INHIBITORS › Anaplastic lymphoma kinase (ALK) inhibitors

Pharmacogenomics

Drug-label and guideline annotations from PharmGKB and CPIC.

• EMA label: ALK · Testing Required
• FDA label: ALK · Testing Required
• HCSC label: ALK · Testing Required

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
No adverse event	610.6
Disease progression	542.6
Metastases to central nervous system	399.5
Blood bilirubin increased	317.0
Blood creatine phosphokinase increased	247.9
Neoplasm progression	240.3
Constipation	195.4
Death	194.9
Anaemia	172.8
Haemolytic anaemia	163.1
Pneumonitis	145.8
Aspartate aminotransferase increased	144.6

Chemical structure

• Molecular formula: C₃₀H₃₄N₄O₂
• Molecular weight: 482.63 g/mol
• CAS number: —
• InChIKey: KDGFLJKFZUIJMX-UHFFFAOYSA-N
• PubChem CID: 49806720

CCC1=CC2=C(C=C1N1CCC(CC1)N1CCOCC1)C(C)(C)C1=C(C3=CC=C(C=C3N1)C#N)C2=O

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Alectinib used for?

DrugCentral lists the following indications for Alectinib: Anaplastic lymphoma kinase positive anaplastic large cell lymphoma and Non-small cell lung cancer.

How does Alectinib work?

Alectinib is classified as Kinase Inhibitors; its molecular targets in DrugCentral include ALK (inhibitor), RET (inhibitor), SRPK2 and SRPK1.

When was Alectinib first approved?

Alectinib was first approved by the PMDA in 2014.

What drug class does Alectinib belong to?

Alectinib is in the Kinase Inhibitor class.

What is the chemical formula of Alectinib?

Alectinib has the molecular formula C30H34N4O2 and a molecular weight of 482.63 g/mol.

Sources

• DrugCentral drug card 4937 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1738797 — compound record and bioactivity
• PubChem CID 49806720 — chemical identifiers
• DrugBank DB11363 — drug record
• FDA UNII LIJ4CT1Z3Y — substance identity
• DailyMed: FDA labels for Alectinib — current prescribing information (label search)
• UniProt Q9UM73 (ALK) — target protein
• UniProt P07949 (RET) — target protein
• UniProt P78362 (SRPK2) — target protein
• UniProt Q96SB4 (SRPK1) — target protein
• UniProt P21709 (EPHA1) — target protein
• UniProt O14976 (GAK) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral
• PharmGKB / CPIC — pharmacogenomic label annotations

How this page is built: methodology · editorial policy & corrections.