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alectinib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
tyrosine kinase inhibitors	4937	1256580-46-7

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: alectinib alectinib hydrochloride alecensa CH5424802 alectinib HCl RO5424802 RO-5424802	Alectinib is a tyrosine kinase inhibitor that targets ALK and RET. In nonclinical studies, alectinib inhibited ALK phosphorylation and ALK-mediated activation of the downstream signaling proteins STAT3 and AKT, and decreased tumor cell viability in multiple cell lines harboring ALK fusions, amplifications, or activating mutations. The major active metabolite of alectinib, M4, showed similar in vitro potency and activity. Molecular weight: 482.63 Formula: C30H34N4O2 CLOGP: 5.66 LIPINSKI: 1 HAC: 6 HDO: 1 TPSA: 72.36 ALOGS: -4.66 ROTB: 3 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

alectinib
alectinib hydrochloride
alecensa
CH5424802
alectinib HCl
RO5424802
RO-5424802

Alectinib is a tyrosine kinase inhibitor that targets ALK and RET. In nonclinical studies, alectinib inhibited ALK phosphorylation and ALK-mediated activation of the downstream signaling proteins STAT3 and AKT, and decreased tumor cell viability in multiple cell lines harboring ALK fusions, amplifications, or activating mutations. The major active metabolite of alectinib, M4, showed similar in vitro potency and activity.

Molecular weight: 482.63
Formula: C30H34N4O2
CLOGP: 5.66
LIPINSKI: 1
HAC: 6
HDO: 1
TPSA: 72.36
ALOGS: -4.66
ROTB: 3

Status: ONP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
1.20	g	O

ADMET properties:

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Property	Value	Reference
CL (Clearance)	7.69 mL/min/kg	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	6.35 L/kg	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Bocci G, Oprea TI, Benet LZ
t_half (Half-life)	11.70 hours	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.00 %	Lombardo F, Berellini G, Obach RS

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Approvals:

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Date	Agency	Company
Dec. 11, 2015	FDA	HOFFMAN-LA ROCHE
Feb. 16, 2017	EMA	Roche Registration Limited
July 4, 2014	PMDA	Chugai Pharmaceutical Co., Ltd

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FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Metastases to central nervous system	154.08	28.68	47	3178	13058	63472739
Neoplasm progression	147.63	28.68	59	3166	36369	63449428
Disease progression	146.90	28.68	86	3139	122672	63363125
Death	92.86	28.68	104	3121	374277	63111520
Constipation	76.28	28.68	74	3151	224869	63260928
Haemolysis	69.91	28.68	22	3203	6746	63479051
Blood creatine phosphokinase increased	63.63	28.68	31	3194	30399	63455398
Pleural effusion	59.06	28.68	44	3181	93166	63392631
Drug resistance	49.86	28.68	24	3201	22909	63462888
Pneumonitis	45.47	28.68	26	3199	35196	63450601

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Disease progression	116.04	33.55	75	2028	108002	34846826
Death	80.35	33.55	108	1995	397941	34556887
Metastases to central nervous system	73.76	33.55	25	2078	8180	34946648
Neoplasm progression	72.88	33.55	33	2070	23267	34931561
Interstitial lung disease	59.43	33.55	41	2062	65241	34889587
Pneumonitis	55.62	33.55	31	2072	33847	34920981
Haemolysis	54.89	33.55	20	2083	8074	34946754
Pericardial effusion	44.41	33.55	24	2079	24638	34930190

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Disease progression	218.02	27.48	131	4184	184231	79555842
Metastases to central nervous system	156.87	27.48	51	4264	16324	79723749
Neoplasm progression	142.74	27.48	65	4250	51617	79688456
Interstitial lung disease	102.58	27.48	68	4247	112532	79627541
Death	98.58	27.48	136	4179	566378	79173695
Blood creatine phosphokinase increased	85.71	27.48	50	4265	66040	79674033
Pneumonitis	76.16	27.48	45	4270	60815	79679258
Pleural effusion	70.13	27.48	60	4255	145202	79594871
Constipation	64.75	27.48	78	4237	282972	79457101
Pericardial effusion	59.97	27.48	35	4280	46202	79693871

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	L01ED03	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS Anaplastic lymphoma kinase (ALK) inhibitors
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:62434	ALK inhibitor
FDA EPC	N0000175605	Kinase Inhibitor
FDA MoA	N0000175082	Kinase Inhibitors

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
Non-small cell lung cancer	indication	254637007	DOID:3908
Anaplastic lymphoma kinase positive anaplastic large cell lymphoma	indication	738770003

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	11.42	acidic
pKa2	7.47	Basic
pKa3	4.89	Basic

Orange Book patent data (new drug applications)

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Orange Book exclusivity data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
EQ 150MG BASE	ALECENSA	HOFFMANN-LA ROCHE	N208434	Dec. 11, 2015	RX	CAPSULE	ORAL	Nov. 6, 2024	FOR TREATMENT OF PATIENTS WITH ANAPLASTIC LYMPHOMA KINASE (ALK) POSITIVE, METASTATIC NON-SMALL-CELL LUNG CANCER (NSCLC) AS DETECTED BY AN FDA APPROVED TEST, EXCLUDING PATIENTS WHO HAVE PROGRESSED ON OR ARE INTOLERANT TO CRIZOTINIB

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
ALK tyrosine kinase receptor	Kinase	Q9UM73	ALK_HUMAN	INHIBITOR	IC50	8.72	SCIENTIFIC LITERATURE	DRUG LABEL
Proto-oncogene tyrosine-protein kinase receptor Ret	Kinase	P07949	RET_HUMAN	INHIBITOR	IC50	8.32	SCIENTIFIC LITERATURE	DRUG LABEL
Phosphorylase b kinase gamma catalytic chain, liver/testis isoform	Kinase	P15735	PHKG2_HUMAN		Kd	5.77	CHEMBL
Tyrosine-protein kinase Fer	Kinase	P16591	FER_HUMAN		Kd	5.42	CHEMBL
Dual specificity protein kinase CLK1	Kinase	P49759	CLK1_HUMAN		Kd	4.53	CHEMBL
Dual specificity protein kinase CLK2	Kinase	P49760	CLK2_HUMAN		Kd	5.63	CHEMBL
Dual specificity protein kinase CLK3	Kinase	P49761	CLK3_HUMAN		Kd	5.86	CHEMBL
Cyclin-G-associated kinase	Kinase	O14976	GAK_HUMAN		Kd	6.59	CHEMBL
ATP-binding cassette sub-family G member 2	Transporter	Q9UNQ0	ABCG2_HUMAN		IC50	5.82	CHEMBL
Casein kinase I isoform gamma-2	Kinase	P78368	KC1G2_HUMAN		Kd	6.29	CHEMBL

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External reference:

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ID	Source
016628	NDDF
016629	NDDF
1256589-74-8	SECONDARY_CAS_RN
1727454	RXNORM
237548	MMSL
31372	MMSL
4035251	VANDF
49806720	PUBCHEM_CID
716039000	SNOMEDCT_US
716040003	SNOMEDCT_US

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
ALECENSA	HUMAN PRESCRIPTION DRUG LABEL	1	50242-130	CAPSULE	150 mg	ORAL	NDA	29 sections
ALECENSA	HUMAN PRESCRIPTION DRUG LABEL	1	50242-130	CAPSULE	150 mg	ORAL	NDA	29 sections

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